Drug intelligence / Profile preview

cannabidiol + cannabigerol + tetrahydrocannabinol + cannabidivarin

Development stage
Preclinical
Lead developer
Jazz Pharmaceuticals
Modality
Small Molecules
Administration
Oral, Buccal, Topical, Inhalation
01

Overview

This is an unbranded combination formulation containing four naturally occurring phytocannabinoids from Cannabis sativa: **cannabidiol (CBD)**, **cannabigerol (CBG)**, **tetrahydrocannabinol (THC)**, and **cannabidivarin (CBDV)**. Each component acts through modulation of the endocannabinoid system but with differing mechanisms: - **Cannabidiol (CBD)** is a non-psychoactive cannabinoid acting primarily as a negative allosteric modulator of the Cannabinoid-1 (CB1) receptor and as an agonist or modulator at other non-cannabinoid receptor targets. It has demonstrated anticonvulsant, anxiolytic, analgesic, muscle relaxant, antipsychotic, anti-inflammatory, and neuroprotective effects[4][6][8]. - **Cannabigerol (CBG)** is a non-psychoactive cannabinoid shown to act as a partial agonist at CB1 and CB2 receptors, as well as modulating α2-adrenoceptors and possibly transient receptor potential (TRP) channels. It exhibits anti-inflammatory, neuroprotective, metabolic, and some appetite-modulating effects[3][7]. - **Tetrahydrocannabinol (THC)** is the principal psychoactive component of cannabis and acts as a weak partial agonist of CB1 and CB2 receptors, causing analgesia, changes in appetite and cognition, and muscle relaxation. In combination with CBD, adverse psychoactive effects are lessened while analgesia is enhanced[1][4]. - **Cannabidivarin (CBDV)** is analogous to CBD and modulates certain ion channels and receptors, with early research showing potential as an anticonvulsant and anti-inflammatory agent. It makes nerve cells less active, reducing inflammation, seizures, and pain, but clinical evidence is limited[2]. Combination formulations with similar ingredients have been tested for chronic pain (especially neuropathic pain), spasticity (notably in multiple sclerosis), epilepsy, anxiety, insomnia, inflammatory bowel disease, metabolic syndrome, and neuroprotection. The mechanism of action primarily involves modulation of cannabinoid receptors and related pathways, leading to reduced inflammation, altered neurotransmitter release, and symptomatic benefit in select conditions[1][4][7]. Safety is generally favorable with dose titration, though psychoactive effects are a risk due to THC[1].

02

Targets

PPARG (Peroxisome proliferator-activated receptor gamma)TRPV2 (Transient receptor potential cation channel subfamily V member 2)ADRA2A (α2A)TRPV1 (Transient receptor potential cation channel subfamily V member 1)CNR1 (Cannabinoid receptor 1)CNR2 (Cannabinoid receptor type 2)TRPA1 (Transient receptor potential cation channel subfamily A member 1)PPARA (Peroxisome proliferator-activated receptor alpha)

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