Saquinavir as Fortovase: Why Does It Matter?

Saquinavir, the first HIV protease inhibitor approved for treating HIV infection, was initially available as Invirase, which was the mesylate salt of the drug in a hard gelatin capsule (saquinavir-HGC). This formulation was limited by extremely low bioavailability (averaging 4% of the administered dose1), owing to the very low water solubility of saquinavir-HGC and high rate of first-pass metabolism by cytochrome P450 3A in both the gut and the liver.

In November 1997 Roche received approval for a new formulation of saquinavir, Fortovase, consisting of the free base of saquinavir dissolved in liquid and then packaged in a soft gelatin capsule (saquinavir-SGC). This formulation has been shown to be significantly more bioavailable in both heal…