Drug intelligence / Profile preview

colchicine + diltiazem ER

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

Overview

Colchicine + diltiazem ER refers to the *co-administration* of colchicine (commonly used to treat and prevent gout and certain autoinflammatory conditions) and extended-release diltiazem (a calcium channel blocker primarily used for hypertension, angina, and some arrhythmias). There is no unique branded combination product; this regimen describes the concurrent use of these two agents. Colchicine is a microtubule polymerization inhibitor that acts by binding to tubulin, thus disrupting cellular functions such as neutrophil migration and activity, leading to its anti-inflammatory effects. Diltiazem ER inhibits L-type calcium channels in the heart and blood vessels, producing anti-anginal and antihypertensive effects. Diltiazem ER is also a potent inhibitor of both cytochrome P450 3A4 (CYP3A4) and P-glycoprotein (P-gp), enzymes and transporters responsible for colchicine metabolism and transport. Their co-administration results in decreased clearance and increased plasma levels of colchicine, necessitating careful dose adjustment and/or increased monitoring due to the elevated risk of colchicine toxicity, including life-threatening outcomes such as pancytopenia, multiorgan failure, and cardiac arrhythmias[1][2][4][7].

Other names
colchicine and diltiazem extended-releasecolchicine + diltiazem extended-release
02

Targets

ABCB1 (P-glycoprotein)TUBB (Tubulin (alpha and beta subunits))LTCC (Voltage-gated calcium channel (L-type))CYP3A4 (Cytochrome P450 3A4)

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