 | |
| Clinical data | |
|---|---|
| Routes of administration | Oral |
| Identifiers | |
| |
| CAS Number | |
| PubChemCID | |
| UNII | |
| KEGG | |
| CompTox Dashboard(EPA) | |
| Chemical and physical data | |
| Formula | C18H23N5O3 |
| Molar mass | 357.414 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
Olorinab (APD371) is a drug beingdeveloped byArena Pharmaceuticals for the treatment of gastrointestinal pain associated withCrohn's disease andirritable bowel syndrome.[1] It acts as a potent and selectivecannabinoidCB2receptoragonist and is claimed to be orally active and peripherally selective.[2][3] Initial Phase IIa exploratoryclinical trials have been successful in patients with quiescent Crohn's disease.[4] Arena initiated the Phase IIb Captivate[5] trial in late July 2019[6] in patients withirritable bowel syndrome related pain, in constipation and diarrhea predominant sub-types.[7] The Phase IIb trial is expected to enroll 240 participants between the ages of 18 and 70.Three doses of 10 mg, 25 mg, and 50 mg are being tested againstPlacebo in a 3:4 prescription ratio with a Quadruple (Participant, Care Provider, Investigator, Outcomes Assessor) masking layout.[8][9]
In 2019, a study showed that Olorinab reduces Visceral Hypersensitivity in the TNBS-induced colitis animal model, attempting to control for itsmechanism of action by using a CB2 antagonist (SR-144,528). Results were favorable showing reduced visceral hypersensitivity in animal models of IBD and IBS but not in healthy controls, suggesting that activation of CB2 causes antinociceptive actions in visceral sensory pathways in models of IBD and IBS. Also, SR-144528 prevented olorinab-induced inhibition of colonic nociceptor hypersensitivity, further validating the role of the CB2 receptor innociception.[10]
