Drug intelligence / Profile preview

sirolimus + maraviroc

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Sirolimus + maraviroc is a drug combination that has been studied for potential synergistic effects in HIV treatment and other conditions. Sirolimus (rapamycin) is an mTOR inhibitor that works by binding to the cytoplasmic receptor FK506-binding protein-12 (FKBP12) to form an immunosuppressive complex. This complex inhibits the activation of the mammalian target of rapamycin (mTOR), a serine/threonine-specific protein kinase that regulates cell growth, proliferation, and survival[6]. Sirolimus is primarily used to prevent organ transplant rejections. Maraviroc is a CCR5 co-receptor antagonist that blocks the entry of HIV into host cells by preventing the interaction between HIV gp120 and the CCR5 co-receptor[1][2]. It is used in combination with other antiretroviral medications to treat CCR5-tropic HIV-1 infection. Studies have shown that low doses of rapamycin (sirolimus) can reduce CCR5 density on cells and enhance the antiviral activity of CCR5 antagonists against HIV[3][4]. This combination has been investigated for potential synergistic effects in treating HIV infection and other conditions like atherosclerosis and inflammation.

Other names
rapamycin + maravirocRAPA + MVC
02

Targets

CCR5 (C-C chemokine receptor type 5)Mechanistic target of rapamycin complex 1

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