Drug intelligence / Profile preview

Epidiolex + tacrolimus

Development stage
Phase 1
Lead developer
Jazz Pharmaceuticals
Modality
Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Epidiolex + tacrolimus is a combination of two pharmaceutical drugs used together, typically in patients who require both seizure management and immunosuppression. Epidiolex is the brand name for purified cannabidiol (CBD), a non-psychoactive cannabinoid approved for the treatment of seizures associated with Lennox-Gastaut syndrome, Dravet syndrome, and tuberous sclerosis complex. Its precise mechanism of action in epilepsy is not fully understood but may involve modulation of neuronal excitability through multiple pathways. Tacrolimus is an immunosuppressant calcineurin inhibitor primarily used to prevent organ transplant rejection by inhibiting T-cell activation via calcineurin inhibition. When co-administered, there is a clinically significant drug-drug interaction due to CBD’s inhibition of cytochrome P450 enzymes (notably CYP3A4 and CYP2C19), which are involved in the metabolism of tacrolimus. This can lead to increased blood levels of tacrolimus and heightened risk for toxicity; dose adjustments and therapeutic drug monitoring are recommended when these drugs are combined[1][5][7][8].

02

Targets

HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))CNR1 (Cannabinoid receptor 1)CN (Calcineurin)FKBP1AGPR55 (G protein-coupled receptor 55)TRPV1 (Transient receptor potential cation channel subfamily V member 1)

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