Drug intelligence / Profile preview

colchicine + cyclosporine

Development stage
Unknown
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral
01

Overview

This combination refers to the **coadministration of colchicine and cyclosporine**, most frequently encountered in patients with solid organ transplants where colchicine is used for gout prophylaxis or treatment and cyclosporine as an immunosuppressant. Colchicine is a small molecule that acts as an anti-inflammatory by inhibiting microtubule polymerization, primarily affecting neutrophil function and cell division. Cyclosporine is a calcineurin inhibitor immunosuppressant that inhibits T-cell activation. Cyclosporine is a strong inhibitor of both cytochrome P450 3A4 (CYP3A4) and P-glycoprotein (P-gp), leading to significantly increased plasma concentrations and toxicity risk of colchicine when used concurrently. Serious adverse effects including myoneuropathy, multiorgan dysfunction, and fatal toxicity have been reported with this combination. Dose adjustment and vigilant monitoring are required when both are prescribed together[1][3][5].

Other names
cyclosporine and colchicinecolchicine and cyclosporine
02

Targets

CYP3A4 (Cytochrome P450 3A4)ABCB1 (P-glycoprotein)

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