Drug intelligence / Profile preview

L-697661

Development stage
Phase 1
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

**L‑697661** is a small molecule non-nucleoside reverse transcriptase inhibitor (NNRTI) developed for the treatment of HIV‑1 infection. It acts by directly inhibiting the activity of HIV‑1 reverse transcriptase without being incorporated into viral DNA. Clinical studies demonstrated that it was orally active and well tolerated in patients with HIV‑1 infection, showing significant dose-related antiviral activity as measured by reductions in plasma p24 antigen levels and transient increases in CD4 counts. However, its effectiveness was limited by the rapid emergence of resistant viral strains due to mutations at positions 103 and 181 in the reverse transcriptase gene. Combination therapy with zidovudine (AZT) showed some benefit but did not prevent resistance or virologic rebound after discontinuation. The drug’s clinical development was ultimately halted due to these limitations[1][5][7].

Other names
3-(((4,7-dichloro-1,3-benzoxazol-2-yl)methyl)amino)-5-ethyl-6-methylpyridin-2(1H)-one3-[[(4,7-dichlorobenzoxazol-2-yl)methyl]amino]-5-ethyl-6-methylpyridin-2(1H)-oneCAS 135525–78–9
02

Targets

Human immunodeficiency virus type 1 reverse transcriptase

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