Drug intelligence / Profile preview

MK-2048

Development stage
Phase 1
Lead developer
Merck
Modality
Small Molecules
Administration
Vaginal, Topical
01

Overview

MK-2048 is a second-generation HIV-1 integrase strand transfer inhibitor (INSTI) developed by Merck. As a member of the INSTI class, it binds to the active site of the HIV-1 integrase enzyme, specifically blocking the strand transfer step required to integrate viral DNA into the host cell's genome. MK-2048 has been primarily investigated as a long-acting topical agent for pre-exposure prophylaxis (PrEP) to prevent HIV-1 infection in women, with clinical evaluations focusing on delivery via intravaginal rings (IVRs) and extended-release vaginal films. Additionally, research has demonstrated its potential in treating Human T-cell leukemia virus type 1 (HTLV-1) infections; it appears to selectively induce apoptosis in HTLV-1-infected cells by activating the PERK-ATF4-CHOP endoplasmic reticulum (ER) stress pathway.

02

Targets

Integrase allosteric pocket (HIV)HTLV-1 IN (HTLV-1 integrase)EIF2AK3 (Pkr-like endoplasmic reticulum kinase)

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