Leah C. Leszcynski, PharmD

Oliceridine (Olinvyk; Trevena, Inc) is an intravenous (IV) opioid agonist indicated in adults for management of acute severe pain in a hospital or controlled clinical setting.

Oliceridine should only be used in patients who require an IV opioid analgesic and for whom alternative treatments are inadequate.

 Oliceridine is a novel μ-opioid receptor ligand with reduced β-arrestin recruitment.

 β-Arrestin signaling is thought to contribute to opioid-related adverse events (AEs) seen with conventional opioids.

 Common opioid-related AEs include nausea, vomiting, constipation, and respiratory depression.

 Oliceridine is intended to be an opioid with an improved respiratory safety profile and reduced incidence of nausea and vomiting. Controlled substance schedule for oliceridine is pending.

The APOLLO-1 and APOLLO-2 trials evaluated the efficacy and safety of oliceridine for acute pain following bunionectomy and abdominoplasty, respectively.

 In both trials, patients received a loading dose of either placebo, oliceridine (1.5 mg), or morphine (4 mg), followed by demand doses via patient-controlled analgesia (0.1, 0.35, or 0.5 mg oliceridine, 1 mg morphine, or placebo). The primary end point for both trials was the proportion of treatment responders to oliceridine compared with placebo. In APOLLO-1, oliceridine was shown to be an effective analgesic with responder rates of 50%, 62%, and 65.8% in the 0.1 mg, 0.35 mg, and 0.5 mg regimens, respectively, compared with 15.2% for placebo (all P < .0001).

 Oliceridine was also shown to be effective in APOLLO-2 with responder rates of 61%, 76.3%, and 70.0% for 0.1 mg, 0.35 mg, and 0.5 mg regimens, respectively, compared with 45.7% for placebo (all P < .05).

In both trials, the composite measure of respiratory safety burden was not statistically different from morphine; however, APOLLO-1 patients in the 0.1-mg and 0.35-mg regimens had a significantly lower risk of experiencing a respiratory safety event when compared with morphine.

 Of the 3 oliceridine regimens, 0.35 mg and 0.5 mg were shown to be noninferior to morphine at achieving treatment response in both trials.

The most commonly reported AEs for oliceridine were nausea, vomiting, headache, and dizziness.

 The proportion of patients experiencing 1 or more gastrointestinal-related AEs increased in a dose-dependent manner across the 3 oliceridine regimens.

 In APOLLO-1, the proportion of gastrointestinal-related AEs ranged from 40.8% to 70.9% in the oliceridine regimens compared with 24.1% for placebo and 72.4% for morphine.

The recommended initial dose is 1.5 mg given IV.

 Onset of analgesic effect is expected within 2 to 5 minutes after initial dose.

 Supplemental doses of 0.75 mg can be administered 1 hour after the initial dose and as needed hourly thereafter.

 For patient-controlled analgesia (PCA), the recommended demand dose is 0.35 mg, with a 6-minute lock out. The cumulative daily dose should not exceed 27 mg due to risk of QT prolongation. Oliceridine 1 mg is approximately equipotent to morphine 5 mg.

 Oliceridine is available as single-dose 2 mL (1 mg/mL) vials and as 30 mg/30 mL (1mg/mL) vials for PCA use only.

Patients with decreased cytochrome P450 2D6 function, patients taking a moderate/strong cytochrome P450 3A4 (CYP3A4) inhibitor, or patients who have very recently discontinued a CYP3A4 inducer are at risk of increased plasma concentrations of oliceridine.

1. Olinvyk. Prescribing information. Trevena Inc; 2020. Accessed August 31, 2020. 

https://olinvyk.com/docs/OLINVYK-FINAL-LABEL-07Aug2020.pdf

2. FDA approves new opioid for Intravenous use in hospitals, other controlled clinical settings. News release. FDA. August 7, 2020. Accessed August 31, 2020. 

https://www.fda.gov/news-events/press-announcements/fda-approves-new-opioid-intravenous-use-hospitals-other-controlled-clinical-settings

3. 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. 

4. Singla NK, Skobieranda F, Soergel DG, et al. 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. 

. 2019;19(7):715-731. doi:10.1111/papr.12801 

Articles

Oliceridine (Olinvyk; Trevena, Inc) is an intravenous opioid agonist indicated in adults for management of acute severe pain in a hospital or controlled clinical setting.