Drug intelligence / Profile preview

colesevelam + ciclosporin

Development stage
Unknown
Lead developer
Daiichi Sankyo
Modality
Small Molecules
Administration
Oral
01

Overview

**Colesevelam + ciclosporin** is a non-fixed combination regimen involving the co-administration of colesevelam, a bile acid sequestrant, and ciclosporin, an immunosuppressant agent.\n- **Colesevelam** acts by binding bile acids in the intestine, reducing their reabsorption, leading to increased conversion of cholesterol to bile acids and promoting upregulation of LDL receptors in the liver, thereby lowering serum LDL-cholesterol[3].\n- **Ciclosporin** is a calcineurin inhibitor, which suppresses immune responses by inhibiting T-lymphocyte activation.\n- Concomitant administration significantly decreases the oral bioavailability of ciclosporin by up to 34% AUC and 44% Cmax due to reduced absorption by colesevelam, which can impact ciclosporin therapeutic levels[1][2]. Clinical use of both drugs together requires careful dose adjustment and therapeutic drug monitoring of ciclosporin[1][2]. No specific indication exists for their joint use; rather, their interaction is an important clinical consideration when both are prescribed for a patient.

02

Targets

PPIA (Peptidyl-prolyl cis-trans isomerase A)CN (Calcineurin)

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