Drug intelligence / Profile preview

lepetegravir

Development stage
Phase 3
Lead developer
Gilead Sciences
Modality
Small Molecules
Administration
Oral
01

Overview

Lepetegravir (formerly GS-1720) is an investigational, oral, long-acting integrase strand transfer inhibitor (INSTI) developed by Gilead Sciences for the treatment of HIV-1 infection. It works by blocking the HIV-1 integrase enzyme, which is essential for the virus to insert its genetic material into the DNA of host cells, thereby halting the viral replication cycle. Designed for once-weekly oral administration, lepetegravir aims to provide a more convenient dosing option compared to standard daily regimens. It is currently being evaluated in Phase 2 and Phase 3 clinical trials, both as a single agent and in combination with other long-acting antiretrovirals like lenacapavir pacfosacil.

02

Targets

Integrase allosteric pocket (HIV)

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