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<meta name="robots" content="INDEX,FOLLOW,NOARCHIVE" /><meta name="citation_inbook_title" content="LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]" /><meta name="citation_title" content="Protein Kinase Inhibitors" /><meta name="citation_publisher" content="National Institute of Diabetes and Digestive and Kidney Diseases" /><meta name="citation_date" content="2024/11/13" /><meta name="citation_pmid" content="31643906" /><meta name="citation_fulltext_html_url" content="https://www.ncbi.nlm.nih.gov/books/NBK548591/" /><link rel="schema.DC" href="http://purl.org/DC/elements/1.0/" /><meta name="DC.Title" content="Protein Kinase Inhibitors" /><meta name="DC.Type" content="Text" /><meta name="DC.Publisher" content="National Institute of Diabetes and Digestive and Kidney Diseases" /><meta name="DC.Date" content="2024/11/13" /><meta name="DC.Identifier" content="https://www.ncbi.nlm.nih.gov/books/NBK548591/" /><meta name="description" content="The kinase inhibitors are a large group of unique and potent antineoplastic agents which specifically target protein kinases that are altered in cancer cells and that account for some of their abnormal growth. 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Many protein kinases are cell surface receptors and act to initiate an intracellular pathway of activation, after the receptor is engaged by its ligand, typically a cytokine or growth factor. Inhibitors of these kinases are called protein kinase receptor inhibitors. Other kinases are intracellular and take part in cell signaling. These kinases can be targeted by "non-receptor" protein kinases. 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<div class="pre-content"><div><div class="bk_prnt"><p class="small">NCBI Bookshelf. A service of the National Library of Medicine, National Institutes of Health.</p><p>LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. </p></div></div></div>
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<div class="main-content lit-style" itemscope="itemscope" itemtype="http://schema.org/CreativeWork"><div class="meta-content fm-sec"><h1 id="_NBK548591_"><span class="title" itemprop="name">Protein Kinase Inhibitors</span></h1><p class="small">Last Update: <span itemprop="dateModified">November 13, 2024</span>.</p></div><div class="body-content whole_rhythm" itemprop="text"><div id="ProteinKinaseInhibit.OVERVIEW"><h2 id="_ProteinKinaseInhibit_OVERVIEW_">OVERVIEW</h2><p>The kinase inhibitors are a large group of unique and potent antineoplastic agents which specifically target protein kinases that are altered in cancer cells and that account for some of their abnormal growth. Protein kinases are ubiquitous intracellular and cell surface proteins that play critical roles in cell signaling pathways involved in metabolism, injury responses, adaption, growth and differentiation. They act by adding a phosphate group to a protein (phosphorylation), usually on a specific amino acid which often makes the protein or enzyme "active". The human genome has more than 500 protein kinases and they can be classified as (1) tyrosine, (2) serine-theonine or (3) nonspecific (both), based upon their amino acid specificity. Many protein kinases are cell surface receptors and act to initiate an intracellular pathway of activation, after the receptor is engaged by its ligand, typically a cytokine or growth factor. Inhibitors of these kinases are called protein kinase receptor inhibitors. Other kinases are intracellular and take part in cell signaling. These kinases can be targeted by "non-receptor" protein kinases. Finally, some kinase inhibitors have specificity for multiple kinases and are called "multi-kinase inhibitors."</p><p>Protein kinases can be specifically involved in cell growth, proliferation and differentiation and mutations may lead to unregulated growth and proliferation that is typical of cancerous cells. These mutated protein kinases represent an attractive target for anticancer agents. The potent activity and lack of generalized toxicity of the kinase inhibitors relate to the specificity of antagonist for the mutated protein. In like manner, their toxicity often relates to off-target activity, either to the unmutated kinase or to closely related, normal kinases.</p><p>The protein kinases can be categorized based upon the amino acid that they phosphorylate: either serine, threonine or tyrosine. The tyrosine kinase receptor inhibitors were the initial and are perhaps the best characterized kinase inhibitors. The protein kinase inhibitors are relatively recently developed agents, all having been introduced since 2001. They are unique and represent a major advance in cancer chemotherapy, away from broadly cytotoxic agents and towards drugs that specifically target the molecular abnormalities of cancer cells. The initial tyrosine kinase inhibitor approved for use in the United States was imatinib (Gleevec: 2001) which is used to treat Philadelphia chromosome positive chronic lymphocytic leukemia, which has a mutated kinase receptor (BCR-ABL) that is created by the specific translocation that creates the Philadelphia chromosome. Imatinib is a specific inhibitor of the BCR-ABL kinase. The introduction of this first protein kinase inhibitor was followed by more than a dozen others within the next 10 years.</p><p>While most kinase inhibitors are antineoplastic agents, a few are also used for benign conditions including macular degeneration (pegaptanib), rheumatoid arthritis (tofacitinib) and idiopathic pulmonary fibrosis (nintedanib). Generally, however, the side effect profile of kinase inhibitors are such that they are reserved for severe, progressive, debilitating or potentially fatal conditions.</p><p>The protein kinase inhibitors all have some degree of hepatotoxicity and many have been linked to cases of clinically apparent liver injury which can be severe and even fatal. Interestingly, some of the cases of liver injury attributed to the protein kinase antagonists had features of autoimmunity, so that the liver injury may be caused by an immunologic reaction to metabolic products of the agent itself, rather than off-target activity of the inhibitor. In addition, at least two protein kinase inhibitors (imatinib and nilotinib) have been linked to instances of reactivation of hepatitis B. It is not clear whether this relates to a specific activity of the kinase inhibitor on hepatitis B virus replication or whether it is due to immunosuppression. Other kinase inhibitors have been linked to cases of rare and idiosyncratic liver injury, which can be hepatocellular or cholestatic and is typically self-limited but may be fatal.</p><p>The Table below lists the protein kinase inhibitors discussed in LiverTox, their brand name, predominant protein kinase (PK) specificity, year of approval in the United States, likelihood score, and major clinical uses.</p><div id="ProteinKinaseInhibit.PROTEIN_KINASE_INHI"><h3>
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<u>PROTEIN KINASE INHIBITORS</u>
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</h3><p>
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<i>Underlined Generic Names link to a LiverTox record.</i>
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</p><div id="ProteinKinaseInhibit.Tc" class="table"><p class="large-table-link" style="display:none"><span class="right"><a href="/books/NBK548591/table/ProteinKinaseInhibit.Tc/?report=objectonly" target="object">View in own window</a></span></p><div class="large_tbl" id="__ProteinKinaseInhibit.Tc_lrgtbl__"><table><tbody><tr><td colspan="5" scope="col" rowspan="1" style="text-align:left;vertical-align:top;">
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<b>CANCER</b>
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</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">
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<b>Generic Name</b>
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<br />
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<b>Brand Name</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">
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<b>Kinase Target</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">
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<b>Approval</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">
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<b>Likelihood<br />Score†</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">
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<b>Major Uses††</b>
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</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Abemaciclib/">Abemaciclib</a><br />Verzenio</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Cyclin dependent kinase 4/6</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2017</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Breast cancer</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Acalabrutinib/">Acalabrutinib</a><br />Calquence</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Bruton kinase</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2017</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">D</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Mantel cell lymphoma</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Adagrasib/">Adagrasib</a><br />Krazati</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">KRAS</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2022</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">D</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">NSCLC</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Afatinib/">Afatinib</a><br />Gilotrif</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">EGFR, HER2</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2013</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">D</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">NSCLC</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Alectinib/">Alectinib</a><br />Alecensa</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">ALK</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2015</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">D</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">NSCLC</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Alpelisib/">Alpelisib</a><br />Piqray</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">PIK3</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2019</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Breast cancer, HR positive, HER2 negative</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Asciminib/">Asciminib</a><br />Scemblix</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">ABL1 Myristoyl</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2021</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">CML</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Avapritinib/">Avapritinib</a><br />Ayvakit</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">PDGFRA, KIT</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2020</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Gastrointestinal stromal tumors</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Axitinib/">Axitinib</a><br />Inlyta</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">VEGFR 1-3</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2012</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Renal cell cancer</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/EncorafenibBinimetin/">Binimetinib</a><br />Mektovi</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">BRAF</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2018</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Melanoma</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Bortezomib/">Bortezomib</a><br />Velcade</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Proteasome</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2003</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">C</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Multiple myeloma, Mantle cell lymphoma</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Bosutinib/">Bosutinib</a><br />Bosulif</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">BCR-ABL, scr</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2012</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">D</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">CML, resistant</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Brigatinib/">Brigatinib</a><br />Alunbrig</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">ALK</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2017</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">NSCLC</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Cabozantinib/">Cabozantinib</a><br />Cometriq, Cabometyx</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">MET, VEGFR-2</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2012</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Medullary thyroid cancer, Renal cell cancer</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Capmatinib/">Capmatinib</a><br />Tabrecta</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">MET</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2020</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">NSCLC</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Carfilzomib/">Carfilzomib</a><br />Kyprolis</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Proteasome</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2012</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">D</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Multiple myeloma, resistant</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Ceritinib/">Ceritinib</a><br />Zykadia</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">ALK</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2014</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">D</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">NSCLC</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Cobimetinib/">Cobimetinib</a><br />Cotellic</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">MEK</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2015</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">D</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Melanoma</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Copanlisib/">Copanlisib</a><br />Aliqopa</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">PI3Kα/δ</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2017</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Follicular lymphoma</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Crizotinib/">Crizotinib</a><br />Xalkori</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">ALK</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2011</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">C</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">NSCLC</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Dabrafenib/">Dabrafenib</a><br />Tafinlar</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">BRAF</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2013</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Melanoma</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Dacomitinib/">Dacomitinib</a><br />Vizimpro</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">HER1,2,3</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2018</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">NSCLC</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Dasatinib/">Dasatinib</a><br />Sprycel</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">BCR-ABL, src</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2006</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">D</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">CML, resistant</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Duvelisib/">Duvelisib</a><br />Copiktra</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">PI3K</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2018</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">CLL, Small cell lymphoma</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Enasidenib/">Enasidenib</a><br />IDHIFA</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Mutant IDH-2</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2017</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">AML</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/EncorafenibBinimetin/">Encorafenib</a><br />Braftovi</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">BRAF</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2018</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Melanoma</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Entrectinib/">Entrectinib</a><br />Rozlytrek</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">NTRK, ROS1</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2019</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">NSCLC</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Erdafitinib/">Erdafitinib</a><br />Balversa</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">FGFR</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2019</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Urothelial cancer</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Erlotinib/">Erlotinib</a><br />Tarceva</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">EGFR, HER1</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2004</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">B</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">NSCLC, Pancreatic cancer</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Fedratinib/">Fedratinib</a><br />Inrebic</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">JAK-2</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2019</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">D</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Myelofibrosis</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Futibatinib/">Futibatinib</a>
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<br />Lytgobi</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">FGFR</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2022</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Cholangiocarcinoma</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Gefitinib/">Gefitinib</a><br />Iressa</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">EGFR</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2009</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">B</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">NSCLC</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Gilteritinib/">Gilteritinib</a><br />Xospata</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">FLT3</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2018</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">AML</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Glasdegib/">Glasdegib</a><br />Daurismo</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Hedgehog</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2018</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">AML</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Ibrutinib/">Ibrutinib</a><br />Imbruvica</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Bruton kinase</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2013</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">D</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Mantle cell lymphoma, CLL</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Idelalisib/">Idelalisib</a><br />Zydelig</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">PI3Kδ</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2014</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">D</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">CLL, Non-Hodgkin lymphoma</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Imatinib/">Imatinib</a><br />Gleevec</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">BCR-ABL, c-Kit</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2001</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">B</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">CML, GIST</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Infigratinib/">Infigratinib</a>
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<br />Truseltiq</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">FGFR</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2021</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Cholangiocarcinoma</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Ivosidenib/">Ivosidenib</a><br />Tibsovo</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Mutant IDH-1</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2018</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">AML</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Ixazomib/">Ixazomib</a><br />Ninlaro</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">26S Proteasome</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2015</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Multiple myeloma</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Lapatinib/">Lapatinib</a><br />Tykerb</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">EGFR, HER2</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2007</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">B</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Breast cancer, HER2 positive</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Larotrectinib/">Larotrectinib</a><br />Vitrakvi</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">NTRK</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2018</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Solid tumors</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Lenvatinib/">Lenvatinib</a><br />Lenvima</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">VEGFR 1-3, FGF 1-4, PDGF, c-Kit, RET</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2015<br />2016<br />2018</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">D</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Thyroid cancer<br />Renal cell cancer<br />Hepatocellular cancer</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Lorlatinib/">Lorlatinib</a><br />Lorbrena</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">ALK</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2018</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">NSCLC</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Midostaurin/">Midostaurin</a><br />Rydapt</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">FLT3</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2018</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">AML</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Mobocertinib/">Mobocertinib</a><br />Exkivity</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">EGFR exon 20</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2021</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">NSCLC</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Momelotinib/">Momelotinib</a><br />Ojjaara</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">JAK-1/2</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2023</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">D</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Myelofibrosis</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Neratinib/">Neratinib</a><br />Nerlynx</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">HER2</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2017</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Breast cancer</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Nilotinib/">Nilotinib</a><br />Tasigna</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">BCR-ABL</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2007</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">D</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">CML, resistant</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Niraparib/">Niraparib</a><br />Zejula</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">PARP</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2017</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Ovarian cancer</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Olaparib/">Olaparib</a><br />Lynparza</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">PARP</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2014<br />2018</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Ovarian cancer<br />Advanced breast cancer</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Olutasidenib/">Olutasidenib</a><br />Rezlidhia</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Mutant IDH-1</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2022</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">D</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">AML</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Osimertinib/">Osimertinib</a><br />Tagrisso</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">EGFR</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2015</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">NSCLC, refractory</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Pacritinib/">Pacritinib</a><br />Vonjo</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">JAK2, FLT3</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2023</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Myelofibrosis</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Palbociclib/">Palbociclib</a><br />Ibrance</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">ER+, HER2</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2015</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">C</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Breast cancer, HER2 negative</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Pazopanib/">Pazopanib</a><br />Votrient</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">VEGFR 1-3</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2009</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">C</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Renal cell cancer</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Pemigatinib/">Pemigatinib</a>
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<br />Pemazyre</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">FGFR</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2020</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Cholangiocarcinoma<br />Myeloid or lymphoid neoplasms</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Pexidartinib/">Pexidartinib</a><br />Turalio</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">CSF1, FLT3</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2019</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">B</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Tenosynovial giant cell tumor</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Pirtobrutinib/">Pirtobrutinib</a><br />Jaypirca</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Bruton kinase</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2023</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Mantel cell lymphoma<br />CLL, Small cell lymphoma</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Ponatinib/">Ponatinib</a><br />Iclusig</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">BCR-ABL</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2013</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">CML, ALL</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Pralsetinib/">Pralsetinib</a><br />Gavreto</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">RET</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2020 –<br />Accel.<br /><p>2023</p></td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">NSCLC, Thyroid cancer</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Quizartinib/">Quizartinib</a><br />Vanflyta</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">FLT3</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2023</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">AML</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Regorafenib/">Regorafenib</a><br />Stivarga</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">VEGFR 1-3, PDGF</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2012</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">B</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Colorectal cancer, GIST</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Ribociclib/">Ribociclib</a><br />Kisqali</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Cyclin dependent kinase 4/6</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2017</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">C</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Breast cancer</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Ripretinib/">Ripretinib</a><br />Qinlock</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">PDGFRA, KIT</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2020</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Gastrointestinal stromal tumors</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Rucaparib/">Rucaparib</a><br />Rubraca</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">PARP</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2016</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Ovarian cancer, advanced</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Ruxolitinib/">Ruxolitinib</a><br />Jakafi</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">JAK-1/2</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2011<br /><p>2014</p>
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<p>2019</p></td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">C</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Myelofibrosis<br /><p>Polycythemia vera</p>
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<p>Acute graft-vs-host disease, steroid-resistant</p></td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Selpercatinib/">Selpercatinib</a><br />Retevmo</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">RET</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2020 –<br />2022</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">NSCLC, Thyroid Cancer<br />[2020 Accel., 2022 NSCLC Approval]<br /><p>Solid Tumors</p>
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<p>[2022 Accel.]</p></td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Selumetinib/">Selumetinib</a><br />Koselugo</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">MEK 1/2</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2020</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Neurofibromatosis type 1</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Sonidegib/">Sonidegib</a><br />Odomzo</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Hedgehog</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2015</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Basal cell skin cancer</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Sorafenib/">Sorafenib</a><br />Nexavar</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">VEGFR 1-3</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2005<br />2007<br />2013</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">B</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Renal cell cancer<br />Hepatocellular cancer<br />Thyroid cancer</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><br /><a href="/books/n/livertox/Sotorasib/">Sotorasib</a><br />Lumakras</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">KRAS</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2019</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">D</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">NSCLC</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><br /><a href="/books/n/livertox/Sunitinib/">Sunitinib</a><br />Sutent</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">PDGF, c-Kit</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2006</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">B</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">CML, resistant; GIST, renal cell cancer</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Talazoparib/">Talazoparib</a><br />Talzenna</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">PARP</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2018</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Breast cancer</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Tepotinib/">Tepotinib</a><br />Tepmetko</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">MET</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2021</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">NSCLC</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Tivozanib/">Tivozanib</a><br />Fotivda</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">VEGFR-1,2,3, c-kit,<br />PDGFR-β</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2021</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Renal cell cancer</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Trametinib/">Trametinib</a><br />Mekinist</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">MEK 1/2</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2013</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Melanoma</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Trilaciclib/">Trilaciblib</a><br />Cosela</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Cyclin dependent kinase 4/6</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2021</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Prevention of chemotherapy-induced myelosuppression in SCLC</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Tucatinib/">Tucatinib</a><br />Tukysa</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">HER2</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2020<br />2023</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Breast cancer<br />Colorectal cancer</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Umbralisib/">Umbralisib</a><br />Ukoniq</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">PI3Kδ</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2021</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Follicular lymphoma</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Vandetanib/">Vandetanib</a><br />Caprelsa</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">VEGFR 2</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2011</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Medullary thyroid cancer</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Vemurafenib/">Vemurafenib</a><br />Zelboraf</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">BRAF</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2011</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Melanoma</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Vismodegib/">Vismodegib</a><br />Erivedge</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Hedgehog</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2012</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">C</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Basal cell skin cancer</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Zanubrutinib/">Zanubrutinib</a><br />Brukinsa</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">BTK</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2019</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Mantel cell lymphoma</td></tr><tr><td colspan="5" scope="col" rowspan="1" style="text-align:left;vertical-align:top;">
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<b>MISCELLANEOUS</b>
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</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">
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<b>Generic Name</b>
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<br />
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<b>Brand Name</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">
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<b>Kinase Target</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">
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<b>Approval</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">
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<b>Likelihood<br />Score†</b>
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</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">
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<b>Major Uses††</b>
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</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Abrocitinib/">Abrocitinib</a><br />Cibinqo</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Janus kinase 1</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2022</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Atopic dermatitis</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Baricitinib/">Baricitinib</a><br />Olumiant</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Janus kinase</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2018<br /><p>2022</p></td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Rheumatoid arthritis<br /><p>Alopecia areata</p></td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Belumosudil/">Belumosudil</a><br />Rezurock</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">ROCK</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2021</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Graft-versus-host disease</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Deucravacitinib/">Deucravacitinib</a><br />Sotyktu</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Tyrosine kinase 2</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2023</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Plaque psoriasis</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Deuruxolitinib/">Deuruxolitinib</a><br />Leqselvi</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Janus kinase</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2024</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Alopecia areata</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Fostamatinib/">Fostamatinib</a><br />Tavalisse</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Spleen tyrosine kinase</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2017</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Immune thrombocytopenia</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Leniolisib/">Leniolisib</a><br />Joenja</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">PI3Kδ</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2023</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Activated PI3K-delta Syndrome</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Lonafarnib/">Lonafarnib</a><br />Zokinvy</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">FTase</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2020</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Progeria syndrome</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Nintedanib/">Nintedanib</a><br />Ofev</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">VEGFR, FGFR, PDGFR</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2014</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Pulmonary fibrosis</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/MacularDegenerAgents/">Pegaptanib</a><br />Macugen</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">VEGFR 1-3</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2004</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Macular degeneration</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Ritlecitinib/">Ritlecitinib</a><br />Litfulo</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Janus kinase 3</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2023</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Alopecia areata</td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Tofacitinib/">Tofacitinib</a><br />Xeljanz</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Janus kinase</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2012<br /><p>2017</p>
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<p>2018</p></td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">E*</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Rheumatoid arthritis<br /><p>Psoriatic arthritis</p>
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<p>Ulcerative colitis</p></td></tr><tr><td scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;"><a href="/books/n/livertox/Upadacitinib/">Upadacitinib</a><br />Rinvoq</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Janus kinase</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">2019</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">D</td><td rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Rheumatoid arthritis</td></tr></tbody></table></div></div><p><b>†</b> Likelihood Score indicates the likelihood of association with drug induced liver injury, based upon the known potential of the drug to cause such injury.</p><p><b>††</b> Abbreviations: ALL, acute lymphocytic leukemia; AML, acute myeloid leukemia; CLL, chronic lymphocytic leukemia; CML, chronic myelogenous leukemia; GIST, gastrointestinal stromal tumor; NSCLC, non-small cell lung cancer.</p></div></div><div id="bk_toc_contnr"></div></div></div>
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