Oliceridine is a synthetic opioid analgesic and a relatively selective μ-opioid receptor agonist. It was developed as a novel opioid designed to preferentially activate G-protein signaling at the μ-opioid receptor. Oliceridine is the active ingredient of OLINVYK and is administered intravenously for the management of acute pain severe enough to require an intravenous opioid analgesic when alternative treatments are inadequate.
The pharmaceutical active substance is generally handled as oliceridine fumarate. FDA identifies oliceridine fumarate as a white to lightly colored solid that is sparingly soluble in water. The fumarate salt has a theoretical average molecular mass of 502.62 g/mol, while the free base has a molecular mass of 386.55 g/mol.
Oliceridine is a full opioid agonist with relative selectivity for the μ-opioid receptor. Its analgesic activity results from activation of opioid receptors in the central nervous system. FDA describes oliceridine as having preferential G-protein signaling with reduced β-arrestin2 recruitment relative to conventional opioid agonists, although this pharmacological property does not eliminate the risks associated with opioid therapy.
Oliceridine is the active pharmaceutical ingredient in OLINVYK, an intravenous opioid analgesic. FDA labeling states that it is indicated in adults for the management of acute pain severe enough to require an intravenous opioid analgesic when alternative treatments are inadequate.
Because oliceridine is an opioid controlled substance, its manufacture, handling, storage and distribution are subject to applicable controlled-substance regulations.
Oliceridine fumarate can be characterized using:
FDA's chemistry review identifies oliceridine fumarate as the drug substance and reports its solid-state and physicochemical characteristics.
For your CMS, it is important not to mix oliceridine free base and oliceridine fumarate specifications.
FDA reports:
The marketed finished product contains 1.0 mg/mL oliceridine free base, equivalent to 1.3 mg/mL oliceridine fumarate, and has a finished-product pH of 6.4–7.4. These are finished-product values and should not be entered as API specifications.
| Parameter | Specification |
|---|---|
| Appearance | White crystalline powder or crystals |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.2% |
| pH (1% Solution) | 5.0 – 7.0 |
| Individual Impurity | NMT 0.5% |
| Water Content | NMT 1.0% |
| Melting Point | 179–181°C |