Drug intelligence / Profile preview

Sativex + ketoconazole

Development stage
Unknown
Lead developer
Jazz Pharmaceuticals
Modality
Small Molecules
Administration
Oromucosal, Oral
01

Overview

Sativex + ketoconazole refers to the co-administration of Sativex (nabiximols) and ketoconazole. Sativex is an oromucosal spray containing two main active ingredients, delta-9-tetrahydrocannabinol (THC) and cannabidiol (CBD), both derived from *Cannabis sativa* extracts. It is primarily used for symptomatic relief of moderate to severe spasticity in multiple sclerosis patients who have not responded adequately to other treatments[3][4][5]. The mechanism of action involves THC acting as a partial agonist at cannabinoid CB1 and CB2 receptors, modulating pain pathways and immune function, while CBD acts as an agonist at the TRPV-1 receptor and inhibits adenosine uptake[6]. Ketoconazole is a broad-spectrum antifungal agent that acts by inhibiting fungal ergosterol synthesis via inhibition of cytochrome P450 enzymes[1]. When administered together, ketoconazole—a potent CYP3A4 inhibitor—increases the plasma concentrations (Cmax and AUC) of both THC and CBD due to reduced metabolic clearance; this may necessitate dose adjustment of Sativex when starting or stopping ketoconazole therapy[5].

02

Targets

CYP3A4 (Cytochrome P450 3A4)TRPV1 (Transient receptor potential cation channel subfamily V member 1)CNR2 (Cannabinoid receptor type 2)

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