OVERVIEW

PRODUCT INFORMATION

REPRESENTATIVE TRADE NAMES

Oliceridine – Olinvyk®

DRUG CLASS

Opioids

COMPLETE LABELING

Product labeling at DailyMed, National Library of Medicine, NIH

CHEMICAL FORMULA AND STRUCTURE

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DRUG	CAS REGISTRY NUMBER	MOLECULAR FORMULA	STRUCTURE
Oliceridine	1401028-24-7	C22-H30-N2-O2-S

BIBLIOGRAPHY

References updated: 05 July 2024

Abbreviations: ULN, upper limit of normal range.

• FDA. Integrated Review. 2020.
• https://www​.accessdata​.fda.gov/drugsatfda_docs​/nda/2020/210730Orig1s000MultidisciplineR.pdf

  (FDA Integrated review of the data on oliceridine safety and efficacy submitted in support of its application for approval as therapy of acute moderate-to-severe pain in adults mentions that ALT elevations occurred at similar rates with oliceridine as morphine, were not associated with jaundice, and were judged to be unrelated to therapy).
• Chen XT, Pitis P, Liu G, Yuan C, Gotchev D, Cowan CL, Rominger DH, et al. Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophe n-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. J Med Chem. 2013;56:8019-31. [PubMed: 24063433]

  (History of development of oliceridine based upon structure activity relationships to G protein biased μ opioid receptor agonism).
• Wadman M. 'Biased' opioids could yield safer pain relief. Science. 2017;358(6365):847-848. [PubMed: 29146784]

  (Commentary on the concept that biased opioids might be found with similar potency and analgesic effect but with less adverse events such as gastrointestinal symptoms and respiratory depression).
• Viscusi ER, Skobieranda F, Soergel DG, Cook E, Burt DA, Singla N. APOLLO-1: a randomized placebo and active-controlled phase III study investigating oliceridine (TRV130), a G protein-biased ligand at the µ-opioid receptor, for management of moderate-to-severe acute pain following bunionectomy. J Pain Res. 2019;12:927-943. [PMC free article: PMC6417853] [PubMed: 30881102]

  (Among 389 patients with moderate-to-severe pain after bunionectomy treated with a loading dose followed by patient-controlled analgesia, response rates were 50-66% with 3 doses of oliceridine, vs 71% with morphine, and 15% with placebo with no clinically meaning differences between the active treatment regimens in…clinical chemistry parameters”).
• Singla NK, Skobieranda F, Soergel DG, Salamea M, Burt DA, Demitrack MA, Viscusi ER. APOLLO-2: A randomized, placebo and active-controlled phase III study investigating oliceridine (TRV130), a G protein-biased ligand at the μ-opioid receptor, for management of moderate to severe acute pain following abdominoplasty. Pain Pract. 2019;19:715-731. [PMC free article: PMC6851842] [PubMed: 31162798]

  (Among 401 patients undergoing abdominoplasty who received oliceridine vs morphine or placebo for management of postoperative pain, response rates were 62-76% with 3 doses of oliceridine, vs 78% with morphine, and 46% with placebo, while respiratory depression and headache were similar with the two opioids, gastrointestinal adverse events of nausea and vomiting were somewhat less with oliceridine; transient ALT elevations arose in 3% vs 2.4% but there were no hepatic severe adverse events).
• Bergese SD, Brzezinski M, Hammer GB, Beard TL, Pan PH, Mace SE, Berkowitz RD, et al. ATHENA: A phase 3, open-label study of the safety and effectiveness of oliceridine (TRV130), a G-protein selective agonist at the µ-opioid receptor, in patients with moderate to severe acute pain requiring parenteral opioid therapy. J Pain Res. 2019;12:3113-3126. [PMC free article: PMC6861532] [PubMed: 31814753]

  (Among 768 patients with moderate-to-severe pain of varying causes [94% surgery related] treated with oliceridine with an initial 1-2 mg bolus followed by patient-controlled analgesia, there was a rapid reduction in pain that was maintained with continued therapy and adverse events were mostly mild-to-moderate, 20 had at least one elevation in liver test results, but none were jaundiced, all resolved, and all were considered unrelated to therapy).
• Markham A. Oliceridine: first approval. Drugs. 2020;80:1739-1744. [PubMed: 33025536]

  (Review of the structure and mechanism of action, history of development, pharmacology, clinical efficacy, and safety of oliceridine; no mention of ALT elevations or hepatotoxicity).
• Oliceridine (Olinvyk) - a new opioid for severe pain. Med Lett Drugs Ther. 2021;63:37-39. [PubMed: 33755654]

  (Concise review of the mechanism of action, clinical efficacy, safety, and costs of oliceridine shortly after its approval for use in the US, mentions that it has a side effect profile similar to that of other opiates but may have fewer gastrointestinal side effects than morphine, but also had a lower rate of response than morphine and higher average cost; no mention of ALT elevations or hepatotoxicity).
• Opioids for pain. Med Lett Drugs Ther. 2022;64:193-200. [PubMed: 36541938]

  (Concise review of the mechanism of action, clinical efficacy, safety, and costs of opioids in use for treatment of moderate-to-severe acute pain mentions that “oliceridine appears to cause less GI toxicity than morphine, but its maximum daily dose is limited by a risk of QT-interval prolongation, and it is expensive”).