Drug intelligence / Profile preview

olorinab

Development stage
Phase 2
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Olorinab is a novel, oral, peripherally acting, highly selective small molecule agonist of the cannabinoid receptor 2 (CB2). It was originally developed by Arena Pharmaceuticals and later by Pfizer for the treatment of gastrointestinal pain associated with conditions such as irritable bowel syndrome (IBS) and Crohn's disease. Olorinab exhibits over 1000-fold selectivity for CB2 over CB1 receptors, minimizing central nervous system side effects like psychoactivity. Its mechanism involves activation of CB2 receptors on colonic nociceptors and immune cells, leading to reduced visceral hypersensitivity and antinociceptive effects in models of inflammatory bowel disease (IBD) and IBS. Clinical trials have shown that olorinab is well tolerated; while it did not meet primary efficacy endpoints in broad populations with IBS-related abdominal pain, it showed significant benefit in subgroups with moderate-to-severe baseline pain[2][3][5][6].

02

Targets

CB (Cannabinoid receptors)

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