Drug intelligence / Profile preview

nabiximols

Development stage
Phase 3
Lead developer
Jazz Pharmaceuticals
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Buccal, Sublingual
01

Overview

Nabiximols is a prescription **cannabinoid botanical drug** and fixed-composition combination product derived from *Cannabis sativa*, formulated as an **oromucosal spray** containing approximately **2.7 mg delta-9-tetrahydrocannabinol and 2.5 mg cannabidiol per 100 microliter actuation**, along with minor cannabinoid and non-cannabinoid constituents. It was originally developed by **GW Pharmaceuticals** and is now owned by **Jazz Pharmaceuticals** following Jazz's acquisition of GW. Nabiximols is marketed outside the United States as **Sativex** for improvement of **moderate to severe multiple sclerosis-related spasticity** in adults who have had inadequate response to other antispasticity medicines and who show clinically meaningful benefit during an initial trial of therapy. Mechanistically, its therapeutic effect is only partly understood, but it is generally attributed to combined cannabinoid signaling mediated primarily through **cannabinoid receptor 1 and cannabinoid receptor 2**, with THC providing partial agonist activity and CBD modulating cannabinoid signaling and the overall neuropharmacologic profile. Publicly reported development has also included U.S. Phase 3 studies in MS spasticity and exploratory or negative studies in pediatric spasticity, ADHD, cannabis withdrawal, pain, and other symptom domains; the pediatric cerebral palsy or traumatic CNS injury spasticity trial did not show efficacy and raised neuropsychiatric tolerability concerns including hallucinations.

Brand names
Sativex
Other names
THC/CBD oromucosal spraydelta-9-tetrahydrocannabinol/cannabidiol oromucosal spraycannabis extractnabiximols oromucosal spray
02

Targets

CNR2 (Cannabinoid receptor type 2)

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