Drug intelligence / Profile preview

MK-2048A

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

Overview

MK-2048A is an investigational combination intravaginal ring (IVR) designed for the prevention of HIV-1 infection (pre-exposure prophylaxis, PrEP) in women. It is a drug-device combination product engineered to provide sustained local release of two antiretroviral agents over a 28-day period: vicriviroc (MK-4176), a CCR5 co-receptor antagonist that blocks HIV entry into host cells, and MK-2048, a second-generation HIV-1 integrase strand transfer inhibitor (INSTI) that prevents the integration of viral DNA into the host genome. Developed by Merck & Co. in collaboration with the National Institute of Allergy and Infectious Diseases (NIAID) and the Microbicide Trials Network (MTN), MK-2048A has been evaluated in Phase 1 clinical trials (e.g., MTN-027, MTN-028) to assess its safety, tolerability, and pharmacokinetics. These studies demonstrated that the ring achieves high concentrations of both drugs in vaginal tissues and fluids with minimal systemic absorption, potentially reducing the risk of systemic side effects while providing effective protection at the site of exposure.

Other names
vicriviroc + MK-2048 intravaginal ringVCV/MK-2048 IVR
02

Targets

Integrase allosteric pocket (HIV)

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