Amprenavir

Amprenavir (original brand name Agenerase, GlaxoSmithKline) is a protease inhibitor used to treat HIV infection.

It was approved by the Food and Drug Administration on April 15, 1999, for twice-a-day dosing instead of needing to be taken every eight hours.

Research aimed at development of renin inhibitors as potential antihypertensive agents had led to the discovery of compounds that blocked the action of this peptide cleaving enzyme.

The amino acid sequence cleaved by renin was found to be fortuitously the same as that required to produce the HIV peptide coat.

This unit is closely related to the one found in the statine, an unusual amino acid that forms part of the pepstatin, a fermentation product that inhibits protease enzymes.

HIV-1 protease dimer with amprenavir (sticks) bound in the active site. PDB entry 3nu3 [ 3 ]