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XV638

Development stage
Preclinical
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
01

Overview

XV638 is an experimental small molecule HIV protease inhibitor belonging to the class of diazepanones and benzamides. It is a potent inhibitor of HIV‑1 protease and has demonstrated efficacy against both wild-type and drug-resistant variants of the enzyme. Structural studies show that its increased potency over earlier cyclic urea-based inhibitors is due to enhanced P2-S2 interactions within the protease active site. These interactions provide more van der Waals contacts and additional hydrogen bonds compared to first-generation inhibitors. As a result, XV638 can inhibit a broad panel of drug-resistant HIV‑1 proteases by compensating for resistance-associated mutations in the S1 subsite[2][5]. The compound has not been approved for clinical use.

Other names
183854-11-7(4R-(4alpha,5alpha,6beta,7beta))-3,3'-((Tetrahydro-5,6-dihydroxy-2-oxo-4,7-bis(phenylmethyl)-1H-1,3-diazepine-1,3(2H)-diyl)-bis(methylene))bis(N-2-thiazolylbenzamide)
02

Targets

PR (Progesterone receptor)

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