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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="Ubrogepant" /><meta name="citation_publisher" content="National Institute of Diabetes and Digestive and Kidney Diseases" /><meta name="citation_date" content="2025/01/12" /><meta name="citation_pmid" content="34324284" /><meta name="citation_fulltext_html_url" content="https://www.ncbi.nlm.nih.gov/books/NBK572431/" /><link rel="schema.DC" href="http://purl.org/DC/elements/1.0/" /><meta name="DC.Title" content="Ubrogepant" /><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="2025/01/12" /><meta name="DC.Identifier" content="https://www.ncbi.nlm.nih.gov/books/NBK572431/" /><meta name="description" content="Ubrogepant is an orally available, small molecule inhibitor of the calcitonin gene-related peptide (CGRP) receptor that blocks the action of CGRP, a potent vasodilator believed to play a role in migraine headaches. Ubrogepant is approved for treatment of acute migraine attacks. In clinical trials, urbrogepant was generally well tolerated with only rare instances of transient serum aminotransferase elevations during therapy and with no reported instances of clinically apparent liver injury." /><meta name="og:title" content="Ubrogepant" /><meta name="og:type" content="book" /><meta name="og:description" content="Ubrogepant is an orally available, small molecule inhibitor of the calcitonin gene-related peptide (CGRP) receptor that blocks the action of CGRP, a potent vasodilator believed to play a role in migraine headaches. Ubrogepant is approved for treatment of acute migraine attacks. In clinical trials, urbrogepant was generally well tolerated with only rare instances of transient serum aminotransferase elevations during therapy and with no reported instances of clinically apparent liver injury." /><meta name="og:url" content="https://www.ncbi.nlm.nih.gov/books/NBK572431/" /><meta name="og:site_name" content="NCBI Bookshelf" /><meta name="og:image" content="https://www.ncbi.nlm.nih.gov/corehtml/pmc/pmcgifs/bookshelf/thumbs/th-livertox-lrg.png" /><meta name="twitter:card" content="summary" /><meta name="twitter:site" content="@ncbibooks" /><meta name="bk-non-canon-loc" content="/books/n/livertox/Ubrogepant/" /><link rel="canonical" href="https://www.ncbi.nlm.nih.gov/books/NBK572431/" /><link rel="stylesheet" href="/corehtml/pmc/css/figpopup.css" type="text/css" media="screen" /><link rel="stylesheet" href="/corehtml/pmc/css/bookshelf/2.26/css/books.min.css" type="text/css" /><link rel="stylesheet" href="/corehtml/pmc/css/bookshelf/2.26/css/books_print.min.css" type="text/css" /><style type="text/css">p a.figpopup{display:inline !important} .bk_tt {font-family: monospace} .first-line-outdent .bk_ref {display: inline} </style><script type="text/javascript" src="/corehtml/pmc/js/jquery.hoverIntent.min.js"> </script><script type="text/javascript" src="/corehtml/pmc/js/common.min.js?_=3.18"> </script><script type="text/javascript">window.name="mainwindow";</script><script type="text/javascript" src="/corehtml/pmc/js/bookshelf/2.26/book-toc.min.js"> </script><script type="text/javascript" src="/corehtml/pmc/js/bookshelf/2.26/books.min.js"> </script>
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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="_NBK572431_"><span class="title" itemprop="name">Ubrogepant</span></h1><p class="small">Last Update: <span itemprop="dateModified">January 12, 2025</span>.</p></div><div class="body-content whole_rhythm" itemprop="text"><div id="Ubrogepant.OVERVIEW"><h2 id="_Ubrogepant_OVERVIEW_">OVERVIEW</h2><div id="Ubrogepant.Introduction"><h3>Introduction</h3><p>Ubrogepant is an orally available, small molecule inhibitor of the calcitonin gene-related peptide (CGRP) receptor that blocks the action of CGRP, a potent vasodilator believed to play a role in migraine headaches. Ubrogepant is approved for treatment of acute migraine attacks. In clinical trials, urbrogepant was generally well tolerated with only rare instances of transient serum aminotransferase elevations during therapy and with no reported instances of clinically apparent liver injury.</p></div><div id="Ubrogepant.Background"><h3>Background</h3><p>Ubrogepant (ue broe’ je pant) is a small molecule inhibitor of the receptor for the calcitonin gene- related peptide (CGRP), which is believed to play a role in the pathogenesis of migraine headaches. CGRP is a potent vasodilator and pain-signaling neurotransmitter that is found throughout the central and peripheral nervous system but is particularly common in trigeminal ganglia. Levels of CGRP are elevated during episodes of migraine headache, and administration of the peptide can induce migraines in susceptible patients. For this reason, approaches to inhibition of CGRP signaling were developed as potential therapies for migraine, both as preventive therapies to decrease the rate of migraine as well as for treatment of acute attacks. Several small molecule inhibitors of the CGRP receptor (the “-gepants”) are available for treatment of acute migraine (remigepant, ubrogepant, and zavegepant) and two for prevention of acute attacks (alogepant and remigepant). In several randomized, placebo controlled trials, ubrogepant in oral doses of 50 or 100 mg was found to increase the rate of being free from headache pain 2 hours after dosing (19% to 26% compared to 9% to 11% with placebo). Ubrogepant was approved for treatment of acute migraine headaches in the United States in 2019 and is available in tablets of 50 and 100 mg under the brand name Ubrelvy. The recommended dose is 50 or 100 mg orally as soon as possible after onset of migraine with the option to repeat the dose after 2 hours but not to exceed 200 mg during any 24-hour period. Ubrogepant can be safely given in patients receiving preventive therapy with monoclonal antibodies to CGRP or its receptor. It is not approved for prevention of migraine attacks. Ubrogepant is generally well tolerated with side effects of nausea, dizziness, somnolence, and dry mouth that are generally uncommon (<5%), transient and mild-to-moderate in severity. Hypersensitivity reactions can also occur such as rash, urticaria, and pruritus and can be severe including anaphylaxis, dyspnea, and angioedema which can occur immediately or up to days after administration.</p></div><div id="Ubrogepant.Hepatotoxicity"><h3>Hepatotoxicity</h3><p>In preregistration controlled trials of ubrogepant in several thousand patients, mild-to-moderate serum aminotransferase elevations arose in a small percentage of patients (1% to 2%) and overall rates were not different from those in placebo recipients. In the controlled trials and subsequently with general use, there have been no reports of clinically apparent liver injury attributed to ubrogepant. In contrast, telcagepant, the initial oral CGRP receptor antagonist evaluated as therapy for migraine headaches, was abandoned during development because of several instances of clinically apparent liver injury in recipients that was characterized by marked elevations in serum aminotransferase levels and symptoms of fatigue, nausea and abdominal discomfort arising within 2 to 4 weeks of starting therapy which rapidly resolved with prompt stopping of therapy. Similar episodes have not been reported with ubrogepant.</p><p>Likelihood score: E (unlikely cause of clinically apparent acute liver injury).</p></div><div id="Ubrogepant.Mechanism_of_Injury"><h3>Mechanism of Injury</h3><p>Possible mechanisms of liver injury due to ubrogepant are not known. It is metabolized in the liver largely by CYP 3A4 and is susceptible to drug-drug interactions with agents that induced or inhibit this microsomal enzyme. Lower doses should be used in patients receiving CYP 3A4 inhibitors.</p></div><div id="Ubrogepant.Outcome_and_Management"><h3>Outcome and Management</h3><p>Drug Class: <a href="/books/n/livertox/MigraineHeadacheAgen/">Migraine Headache Agents</a></p><p>Other Small Molecule Inhibitors of CGRP Receptors: <u>Atogepant</u>, <a href="/books/n/livertox/Rimegepant/">Rimegepant</a>, Zavegepant</p></div></div><div id="Ubrogepant.PRODUCT_INFORMATION"><h2 id="_Ubrogepant_PRODUCT_INFORMATION_">PRODUCT INFORMATION</h2><p>
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<b>REPRESENTATIVE TRADE NAMES</b>
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</p><p>Ubrogepant – Ubrelvy®</p><p>
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<b>DRUG CLASS</b>
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</p><p>Migraine Headache Agents</p><p>
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<a href="https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=Ubrogepant" ref="pagearea=body&targetsite=external&targetcat=link&targettype=uri">COMPLETE LABELING</a>
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</p><p>Product labeling at DailyMed, National Library of Medicine, NIH</p></div><div id="Ubrogepant.CHEMICAL_FORMULA_AND_STRUCTUR"><h2 id="_Ubrogepant_CHEMICAL_FORMULA_AND_STRUCTUR_">CHEMICAL FORMULA AND STRUCTURE</h2><div id="Ubrogepant.Tc" class="table"><p class="large-table-link" style="display:none"><span class="right"><a href="/books/NBK572431/table/Ubrogepant.Tc/?report=objectonly" target="object">View in own window</a></span></p><div class="large_tbl" id="__Ubrogepant.Tc_lrgtbl__"><table><thead><tr><th id="hd_h_Ubrogepant.Tc_1_1_1_1" scope="col" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">DRUG</th><th id="hd_h_Ubrogepant.Tc_1_1_1_2" scope="col" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">CAS REGISTRY NO.</th><th id="hd_h_Ubrogepant.Tc_1_1_1_3" scope="col" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">MOLECULAR FORMULA</th><th id="hd_h_Ubrogepant.Tc_1_1_1_4" scope="col" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">STRUCTURE</th></tr></thead><tbody><tr><td headers="hd_h_Ubrogepant.Tc_1_1_1_1" scope="row" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">Ubrogepant</td><td headers="hd_h_Ubrogepant.Tc_1_1_1_2" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">
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||
<a href="https://pubchem.ncbi.nlm.nih.gov/substance/163370735" ref="pagearea=body&targetsite=entrez&targetcat=link&targettype=pubchem">1374248-77-7</a>
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||
</td><td headers="hd_h_Ubrogepant.Tc_1_1_1_3" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">C29-H26-F3-N5-O3</td><td headers="hd_h_Ubrogepant.Tc_1_1_1_4" rowspan="1" colspan="1" style="text-align:left;vertical-align:top;">
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||
<a href="https://pubchem.ncbi.nlm.nih.gov/substance/163370735" title="View this structure in PubChem" class="img_link" ref="pagearea=body&targetsite=entrez&targetcat=link&targettype=pubchem"><img src="https://pubchem.ncbi.nlm.nih.gov/image/imgsrv.fcgi?t=l&sid=163370735" alt="image 163370735 in the ncbi pubchem database" /></a>
|
||
</td></tr></tbody></table></div></div></div><div id="Ubrogepant.ANNOTATED_BIBLIOGRAPHY"><h2 id="_Ubrogepant_ANNOTATED_BIBLIOGRAPHY_">ANNOTATED BIBLIOGRAPHY</h2><p>References updated: 12 January 2025</p><p>Abbreviations: CGRP, calcitonin gene-related peptide.</p><ul class="first-line-outdent"><li><div class="bk_ref" id="Ubrogepant.REF.zimmerman.1999">Zimmerman HJ. Hepatotoxicity: the adverse effects of drugs and other chemicals on the liver. 2nd ed. Philadelphia: Lippincott, 1999.<div><i>(Review of hepatotoxicity published in 1999 before the availability of CGRP antagonists).</i></div></div></li><li><div class="bk_ref" id="Ubrogepant.REF2">FDA. Clinical Review. <a href="https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211765Orig1s000MedR.pdf" ref="pagearea=cite-ref&targetsite=external&targetcat=link&targettype=uri">https://www<wbr style="display:inline-block"></wbr>.accessdata<wbr style="display:inline-block"></wbr>.fda.gov/drugsatfda_docs<wbr style="display:inline-block"></wbr>/nda/2019/211765Orig1s000MedR.pdf</a><div><i>(FDA Drug Approvals website that has product labels [package inserts], letters of approval and full FDA multidisciplinary scientific review of the ubrogepant application including specific discussion of hepatic adverse events which consisted mainly of mild-to-moderate ALT or AST elevations which were similar in frequency in ubrogepant vs placebo recipients, and two patients with clinically apparent liver injury had evidence of a preexisting and unrelated diagnosis; cholecystitis and pancreatitis).</i></div></div></li><li><div class="bk_ref" id="Ubrogepant.REF.ho.2014.958">Ho
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TW, Connor
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KM, Zhang
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||
Y, Pearlman
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E, Koppenhaver
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J, Fan
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X, Lines
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||
C, et al.
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||
Randomized controlled trial of the CGRP receptor antagonist telcagepant for migraine prevention.
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||
Neurology
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||
2014; 83: 958-66.
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||
[<a href="https://pubmed.ncbi.nlm.nih.gov/25107879" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 25107879</span></a>]<div><i>(Among 660 patients with migraine enrolled in a controlled trial of telcagepant [140 or 280 mg] vs placebo twice daily for 12 weeks, 13 patients on telcagepant developed ALT elevations above 3 times ULN, generally between weeks 4 and 6 of treatment, and in two instances rising to 33 and 39 times ULN accompanied by symptoms but not jaundice leading to prompt discontinuation and to early termination of the trial because of the risk of significant hepatotoxicity).</i></div></div></li><li><div class="bk_ref" id="Ubrogepant.REF.voss.2016.887">Voss
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T, Lipton
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RB, Dodick
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DW, Dupre
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N, Ge
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JY, Bachman
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R, Assaid
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||
C, et al.
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||
A phase IIb randomized, double-blind, placebo-controlled trial of ubrogepant for the acute treatment of migraine.
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||
Cephalalgia
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||
2016; 36: 887-98.
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[<a href="https://pubmed.ncbi.nlm.nih.gov/27269043" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 27269043</span></a>]<div><i>(Among 834 patients treated with ubrogepant [1, 10, 25, 50 or 100 mg] or placebo for an acute attack of migraine, 26% of those receiving 100 mg were headache pain free at 2 hours compared to 9% on placebo, while adverse events more frequent with ubrogepant included low rates of nausea and dizziness and there were no ALT elevations above 3 times ULN).</i></div></div></li><li><div class="bk_ref" id="Ubrogepant.REF.tfelthansen.2019.113">Tfelt-Hansen
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P, Loder
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||
E.
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||
The Emperor's new gepants: are the effects of the new oral CGRP antagonists clinically meaningful?
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||
Headache
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||
2019; 59: 113-7.
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||
[<a href="https://pubmed.ncbi.nlm.nih.gov/30451300" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 30451300</span></a>]<div><i>(Commentary on the relative efficacy of two oral CGRP receptor antagonists, ubrogepant and rimegepant, which show only modest efficacy in acute migraine [therapeutic gain of 5-8%] and only when compared to placebo as compared to well known effective therapies such as aspirin and other nonsteroidal antiinflammatory agents [8-14%] and the triptans [16-32%]).</i></div></div></li><li><div class="bk_ref" id="Ubrogepant.REF.goadsby.2019.1753">Goadsby
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PJ, Tepper
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SJ, Watkins
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PB, Ayele
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G, Miceli
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R, Butler
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M, Severt
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L, et al.
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Safety and tolerability of ubrogepant following intermittent, high-frequency dosing: Randomized, placebo-controlled trial in healthy adults.
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||
Cephalalgia
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||
2019; 39: 1753-61.
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||
[<a href="/pmc/articles/PMC6900570/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC6900570</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/31537107" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 31537107</span></a>]<div><i>(Study of safety of ubrogepant given in intermittent doses [200 mg per day for 2 days] to healthy adults found the overall adverse event rates were the same as with placebo [44% vs 45%], including headache [11% vs 10%] and ALT elevations of 3 times ULN or more [in 5 on placebo and 2 on ubrogepant], which were transient and resolved even with drug continuation and without bilirubin elevations or symptoms).</i></div></div></li><li><div class="bk_ref" id="Ubrogepant.REF.lipton.2019.1887">Lipton
|
||
RB, Dodick
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DW, Ailani
|
||
J, Lu
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||
K, Finnegan
|
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M, Szegedi
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||
A, Trugman
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||
JM. Effect of ubrogepant vs placebo on pain and the most bothersome associated symptom in the acute treatment of migraine: the ACHIEVE II randomized clinical trial.
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||
JAMA
|
||
2019; 322: 1887-98.
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||
[<a href="/pmc/articles/PMC6865323/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC6865323</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/31742631" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 31742631</span></a>]<div><i>(Among 1465 adults with an acute migraine headache, freedom from pain at 2 hours was achieved by 21% and 22% of ubrogepant [25 or 50 mg] vs 14% of placebo recipients, while adverse events of nausea and dizziness were generally mild and uncommon [~ 2%] and ALT or AST elevations of at least 3 times ULN arose in only 4 of 966 [<1%] rimegepant treated patients, all of which were transient and without symptoms or jaundice).</i></div></div></li><li><div class="bk_ref" id="Ubrogepant.REF.dodick.2019.2230">Dodick
|
||
DW, Lipton
|
||
RB, Ailani
|
||
J, Lu
|
||
K, Finnegan
|
||
M, Trugman
|
||
JM, Szegedi
|
||
A. Ubrogepant for the treatment of migraine.
|
||
N Engl J Med
|
||
2019; 381: 2230-41.
|
||
[<a href="https://pubmed.ncbi.nlm.nih.gov/31800988" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 31800988</span></a>]<div><i>(Among 1672 adults with migraine headache, freedom from pain within 2 hours was achieved by 19% and 21% of ubrogepant recipients [50 or 100 mg] vs 12% of placebo recipients, and adverse events of dry mouth, somnolence and nausea were generally mild and uncommon [less than 5%], while ALT or AST elevations of 3 times ULN or greater arose in 0.4% and 0.6% vs 0.2% of patients on placebo).</i></div></div></li><li><div class="bk_ref" id="Ubrogepant.REF.ailani.2020.141">Ailani
|
||
J, Lipton
|
||
RB, Hutchinson
|
||
S, Knievel
|
||
K, Lu
|
||
K, Butler
|
||
M, Yu
|
||
SY, et al.
|
||
Long-term safety evaluation of ubrogepant for the acute treatment of migraine: phase 3,randomized, 52-week extension trial.
|
||
Headache
|
||
2020; 60: 141-52.
|
||
[<a href="/pmc/articles/PMC7004213/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC7004213</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/31913519" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 31913519</span></a>]<div><i>(Among 1230 adults randomized to ubrogepant [50 or 100 mg] or usual care to treat migraine attacks over a 52 week period, elevations in ALT arose in 31% and 32% on ubrogepant vs 31% on usual care and were above 3 times ULN in 1.3% and 2.7% vs 1%, but none of the elevations were associated with jaundice or symptoms).</i></div></div></li><li><div class="bk_ref" id="Ubrogepant.REF.ankrom.2020.462">Ankrom
|
||
W, Bondiskey
|
||
P, Li
|
||
CC, Palcza
|
||
J, Liu
|
||
W, Dockendorf
|
||
MF, Matthews
|
||
C, et al.
|
||
Ubrogepant is not associated with clinically meaningful elevations of alanine aminotransferase in healthy adult males.
|
||
Clin Transl Sci
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||
2020; 13: 462-72.
|
||
[<a href="/pmc/articles/PMC7214647/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC7214647</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/31899602" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 31899602</span></a>]<div><i>(In two pharmacokinetic and safety studies conducted in 72 healthy male adults, ubrogepant in single and multiple doses of 40 to 400 mg daily for up to 28 days was well tolerated with no serious adverse events or ALT elevations above 3 times ULN; overall rates of ALT abnormalities were similar to those with placebo).</i></div></div></li><li><div class="bk_ref" id="Ubrogepant.REF.scott.2020.323">Scott
|
||
LJ. Ubrogepant: First approval.
|
||
Drugs
|
||
2020; 80: 323-8.
|
||
[<a href="/pmc/articles/PMC7062659/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC7062659</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/32020557" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 32020557</span></a>]<div><i>(Review of the mechanism of action, history of development, pharmacology, clinical efficacy and safety of ubrogepant shortly after its approval for use in the US, mentions that ALT or AST elevations above 3 times ULN arose in 1-3% of patients, but none were associated with jaundice and rates were similar between ubrogepant and placebo recipients).</i></div></div></li><li><div class="bk_ref" id="Ubrogepant.REF12">Lasmiditan (Reyvow) and ubrogepant (Ubrelvy) for acute treatment of migraine.
|
||
Med Lett Drugs Ther
|
||
2020; 62: 35-9.
|
||
[<a href="https://pubmed.ncbi.nlm.nih.gov/32555120" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 32555120</span></a>]<div><i>(Concise review of the mechanism of action, clinical efficacy, safety and costs of ubrogepant and lasmiditan as therapy of acute migraine shortly after their approval for this indication in the US, mentions side effects of ubrogepant being nausea and somnolence but does not mention ALT elevations or hepatotoxicity).</i></div></div></li><li><div class="bk_ref" id="Ubrogepant.REF13">Rimegepant (Nurtec ODT) for acute treatment of migraine.
|
||
Med Lett Drugs Ther
|
||
2020; 62: 70-2.
|
||
[<a href="https://pubmed.ncbi.nlm.nih.gov/32555113" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 32555113</span></a>]<div><i>(Concise review of the mechanism of action, pharmacology, clinical efficacy, safety and cost of rimegepant shortly after its approval in the US as therapy of acute migraine in adults, mentions that it “was generally well tolerated in clinical trials; nausea was the most common adverse event [~2%]”).</i></div></div></li><li><div class="bk_ref" id="Ubrogepant.REF14">Drugs for migraine.
|
||
Med Lett Drugs Ther
|
||
2020; 62: 153-60.
|
||
[<a href="https://pubmed.ncbi.nlm.nih.gov/33434187" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 33434187</span></a>]<div><i>(Concise summary of the relative clinical efficacy, safety and costs of drugs to treat acute migraine headache [such as analgesics, opiates, triptans, ergots and oral CGRP receptor antagonists] and to prevent migraines [such as anticonvulsants, beta blockers, antidepressants and the monoclonal antibodies to CGRP and its receptor]).</i></div></div></li><li><div class="bk_ref" id="Ubrogepant.REF.hutchinson.2021.235">Hutchinson
|
||
S, Dodick
|
||
DW, Treppendahl
|
||
C, Bennett
|
||
NL, Yu
|
||
SY, Guo
|
||
H, Trugman
|
||
JM. Ubrogepant for the acute treatment of migraine: pooled efficacy, safety, and tolerability from the ACHIEVE I and ACHIEVE II phase 3 randomized trials.
|
||
Neurol Ther
|
||
2021; 10: 235-49.
|
||
[<a href="/pmc/articles/PMC8140011/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC8140011</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/33608814" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 33608814</span></a>]<div><i>(Post hoc analysis of efficacy and safety from two controlled trials in 2240 patients with migraine, found pain-free rates at 2 hours to be 20.5% with ubrogepant vs 13% with placebo, with similar overall rates of adverse events [11.5% vs 11.2%] and no serious adverse events requiring discontinuation).</i></div></div></li><li><div class="bk_ref" id="Ubrogepant.REF.jakate.2021.642">Jakate
|
||
A, Blumenfeld
|
||
AM, Boinpally
|
||
R, Butler
|
||
M, Borbridge
|
||
L, Contreras-De Lama
|
||
J, McGeeney
|
||
D, et al.
|
||
Pharmacokinetics and safety of ubrogepant when coadministered with calcitonin gene-related peptide-targeted monoclonal antibody migraine preventives in participants with migraine: A randomized phase 1b drug-drug interaction study.
|
||
Headache
|
||
2021; 61: 642-52.
|
||
[<a href="/pmc/articles/PMC8252052/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC8252052</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/33818780" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 33818780</span></a>]<div><i>(Among 40 patients enrolled in pharmacokinetic studies of ubrogepant with or without concurrent preventive therapy with erenumab or galcanezumab, pharmacokinetic parameters were similar with and without concurrent monoclonal antibodies to CGRP and adverse event rates appeared to be unaffected; there were “no clinically relevant changes in laboratory parameters”).</i></div></div></li><li><div class="bk_ref" id="Ubrogepant.REF.robbins.2021.1874">Robbins
|
||
MS. Diagnosis and management of headache: a review.
|
||
JAMA
|
||
2021; 325: 1874-85.
|
||
[<a href="https://pubmed.ncbi.nlm.nih.gov/33974014" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 33974014</span></a>]<div><i>(Review of the diagnosis and management of headache including use of calcitonin gene-related peptide antagonists for acute migraine attacks which has uncommon side effects of dry mouth and dizziness; no mention of ALT elevations or hepatotoxicity).</i></div></div></li><li><div class="bk_ref" id="Ubrogepant.REF.woodhead.2022.108">Woodhead
|
||
JL, Siler
|
||
SQ, Howell
|
||
BA, Watkins
|
||
PB, Conway
|
||
C. Comparing the liver safety profiles of 4 next-generation CGRP receptor antagonists to the hepatotoxic CGRP inhibitor telcagepant using quantitative systems toxicology modeling.
|
||
Toxicol Sci.
|
||
2022;188:108-116.
|
||
[<a href="/pmc/articles/PMC9237996/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC9237996</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/35556143" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 35556143</span></a>]<div><i>(Mechanistic simulation of hepatotoxicity indicated that telcagepant had multiple potential adverse effects on liver function compared to the more recently developed CGRP antagonists, rimegepant, ubrogepant, atogepant, and zavegepant).</i></div></div></li><li><div class="bk_ref" id="Ubrogepant.REF.battini.2023.1105">Battini
|
||
V, Carnovale
|
||
C, Clementi
|
||
E, Sessa
|
||
M.
|
||
Ubrogepant and rimegepant: signal detection using spontaneous reports of adverse events from the Food and Drug Administration Adverse Event Reporting System.
|
||
Expert Opin Drug Saf.
|
||
2023;22:1105-1112.
|
||
[<a href="https://pubmed.ncbi.nlm.nih.gov/37293948" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 37293948</span></a>]<div><i>(Extraction of adverse event reports made to the FDAs Adverse Event Reporting System for ubrogepant [n=2010] and rimegepant [3691] found no excess reports of hepatic reactions).</i></div></div></li><li><div class="bk_ref" id="Ubrogepant.REF.dodick.2023.2307">Dodick
|
||
DW, Goadsby
|
||
PJ, Schwedt
|
||
TJ, Lipton
|
||
RB, Liu
|
||
C, Lu
|
||
K, Yu
|
||
SY, et al.
|
||
Ubrogepant for the treatment of migraine attacks during the prodrome: a phase 3, multicentre, randomised, double-blind, placebo-controlled, crossover trial in the USA.
|
||
Lancet.
|
||
2023;402(10419):2307-2316.
|
||
[<a href="https://pubmed.ncbi.nlm.nih.gov/37979595" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 37979595</span></a>]<div><i>(Among 480 adults with episodic migraine treated with ubrogepant [100 mg] or placebo at onset of a prodromal event, subsequent absence of a headache occurred in 46% vs 29% while adverse events were more frequent with drug [17% vs 12%], they being mostly mild-to-moderate nausea [5% vs 3%], fatigue [3% vs 2%], and somnolence [2% vs 1%], with no deaths or serious adverse events [laboratory tests were not done]).</i></div></div></li><li><div class="bk_ref" id="Ubrogepant.REF21">Drugs for migraine.
|
||
Med Lett Drugs Ther.
|
||
2023;65:89-96.
|
||
[<a href="https://pubmed.ncbi.nlm.nih.gov/37266987" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 37266987</span></a>]<div><i>(Concise summary of the relative clinical efficacy, safety, and costs of drugs to treat and to prevent migraine headaches, states that systemic adverse effects are uncommon with use of oral CGRP receptor antagonists, but that nausea and somnolence can occur; no mention of ALT elevations or hepatotoxicity).</i></div></div></li><li><div class="bk_ref" id="Ubrogepant.REF.liang.2024.1431562">Liang
|
||
Q, Liao
|
||
X, Wu
|
||
H, Huang
|
||
Y, Liang
|
||
T, Li
|
||
H. Real-world study of adverse events associated with gepant use in migraine treatment based on the VigiAccess and U.S. Food and Drug Administration's adverse event reporting system databases.
|
||
Front Pharmacol.
|
||
2024;15:1431562.
|
||
[<a href="/pmc/articles/PMC11322337/" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pmc">PMC free article<span class="bk_prnt">: PMC11322337</span></a>] [<a href="https://pubmed.ncbi.nlm.nih.gov/39144633" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 39144633</span></a>]<div><i>(Search of two large registry databases on spontaneous reports of adverse events due to -gepants [rimegepant, ubrogepant, and atogepant] identified 23,542 reports, but only 0.09% to 0.27% were liver related, attesting to the lack of severe liver injury due to the currently available oral CGRP receptor antagonists).</i></div></div></li><li><div class="bk_ref" id="Ubrogepant.REF.cao.2024.297">Cao
|
||
B, Gu
|
||
S, Shen
|
||
Z, Zhang
|
||
Y, Shen
|
||
Y, Chen
|
||
H.
|
||
Evaluating Ubrogepant-related adverse events using the FDA adverse event reporting system.
|
||
Expert Opin Drug Saf.
|
||
2024;23:297-303.
|
||
[<a href="https://pubmed.ncbi.nlm.nih.gov/37608560" ref="pagearea=cite-ref&targetsite=entrez&targetcat=link&targettype=pubmed">PubMed<span class="bk_prnt">: 37608560</span></a>]<div><i>(Extraction of data from the FDA’s Adverse Event Reporting System identified 2067 reports attributed to ubrogepant, of which only one was hepatobiliary).</i></div></div></li></ul></div><div id="bk_toc_contnr"></div></div></div>
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