Drug intelligence / Profile preview

GW873140 + lopinavir + ritonavir

Development stage
Discontinued
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

GW873140 + lopinavir + ritonavir is a triple antiretroviral drug regimen investigated for the treatment of HIV infection. GW873140 (also known as aplaviroc) is a small molecule antagonist of CC chemokine receptor 5 (CCR5), blocking HIV entry by inhibiting virus interaction with the host cell receptor[2]. Lopinavir and ritonavir are both HIV-1 protease inhibitors; ritonavir 'boosts' lopinavir levels by inhibiting its metabolism[1][5][7]. This combination acts via two mechanisms: blocking viral entry (CCR5 antagonism) and inhibiting viral protease, disrupting HIV replication. GW873140 development was discontinued because of hepatotoxicity[6], but drug–drug interaction studies showed that combination with lopinavir/ritonavir boosts GW873140 plasma levels and was well tolerated short-term[3]. Lopinavir/ritonavir (marketed as Kaletra) is approved as part of combination therapy for HIV/AIDS[1][5][7].

Brand names
Kaletra
Other names
aplaviroc + lopinavir + ritonavirlopinavir/ritonavir
02

Targets

PR (Progesterone receptor)CCR5 (C-C chemokine receptor type 5)

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