BioCentury
ARTICLE | Distillery Therapeutics

Infectious disease

June 13, 2018 6:19 PM UTC

In vitro and cell culture studies identified an allophenylnorstatine-tetrahydrofuranylglycine conjugate-based inhibitor of HIV protease that could help treat protease inhibitor-resistant HIV infection. Chemical synthesis and in vitro activity assays of allophenylnorstatine-tetrahydrofuranylglycine conjugate analogs yielded a compound that inhibited 97% of HIV protease activity at a concentration of 1 nM. In a human T cell line infected with wild-type, Kaletra lopinavir/ritonavir-resistant, or two Prezista darunavir-resistant HIV strains, the compound inhibited cell death with EC50 values of 1.71, 25, 0.3 and 1.21 nM, respectively. Next steps could include testing the compound in animal models of HIV infection.

AbbVie Inc. markets Kaletra, a combination of the generic HIV protease inhibitors lopinavir and ritonavir, which inhibits the cytochrome P450 3A4 (CYP3A4)-mediated metabolism of lopinavir, to treat HIV infection and has the product in Phase III testing for malaria...

BCIQ Target Profiles

HIV protease