GSK706769 + Kaletra

GSK706769 + Kaletra refers to the co-administration of GSK706769, an experimental CCR5 antagonist, and Kaletra (a fixed-dose combination of lopinavir and ritonavir), a protease inhibitor-based antiretroviral therapy. GSK706769 was developed by GSK (and later ViiV Healthcare) as a small molecule entry inhibitor designed to block the CCR5 co-receptor on CD4+ T cells, thereby preventing R5-tropic HIV-1 from entering and infecting host cells. Kaletra is used to inhibit the HIV protease enzyme, with ritonavir acting as a pharmacokinetic enhancer (booster) for lopinavir by inhibiting the CYP3A4 enzyme. This specific combination was evaluated in Phase I clinical trials to determine the pharmacokinetic interactions between the two regimens, specifically how the CYP3A4 inhibition by ritonavir in Kaletra affected the plasma levels of GSK706769. Development of GSK706769 appears to have been discontinued following the formation of ViiV Healthcare.

Brand names

Kaletra

Other names

GSK706769 + lopinavir + ritonavir