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GSK2248761 + lopinavir + ritonavir

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

Overview

This entry refers to a combination of **GSK2248761** (formerly IDX899), a next-generation, once-daily non-nucleoside reverse transcriptase inhibitor (NNRTI), with **lopinavir** and **ritonavir**, both HIV-1 protease inhibitors. GSK2248761 displayed potent activity against wild-type and efavirenz-resistant HIV-1 strains, but development was discontinued due to safety concerns, specifically seizure events[2][4]. Lopinavir/ritonavir is a well-established fixed-dose antiretroviral regimen where ritonavir boosts plasma levels of lopinavir by inhibiting CYP3A4-mediated metabolism; this combination is marketed as Kaletra[3][7]. The triple combination was studied for drug-drug interactions in HIV-1 treatment, with data showing potential PK interactions but not marketed as a single product[1].

Brand names
Kaletra
Other names
lopinavir/ritonavir
02

Targets

Human immunodeficiency virus type 1 reverse transcriptaseCYP3A4 (Cytochrome P450 3A4)PR (Progesterone receptor)

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