Drug intelligence / Profile preview

ezetimibe + sirolimus

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

Overview

Ezetimibe + sirolimus is a combination of two small molecule drugs, ezetimibe and sirolimus. Ezetimibe is a cholesterol absorption inhibitor that selectively blocks the Niemann-Pick C1-Like 1 (NPC1L1) protein in the small intestine, reducing intestinal absorption of cholesterol and phytosterols. Sirolimus (also known as rapamycin) is an immunosuppressant that inhibits the mechanistic target of rapamycin (mTOR), thereby suppressing T-cell activation and proliferation. This combination has been studied primarily in organ transplant recipients who develop hyperlipidemia as a side effect of sirolimus-based immunosuppression; ezetimibe may be used to manage elevated cholesterol levels in these patients[1][2][4]. Clinical studies have evaluated potential pharmacokinetic interactions between these agents, but no major clinically relevant interactions have been observed[2][4][6]. The combination does not represent a marketed fixed-dose product but rather co-administration for specific clinical scenarios.

02

Targets

FKBP1AMechanistic target of rapamycin complex 1NPC1L1 (Niemann-pick C1-Like 1 transporter)

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