Sauinavir-d9 is intended for use as an internal standard for the quantification of saquinavir by GC- or LC-MS. Saquinavir is an HIV protease inhibitor (Kis = 0.12 and <0.1 nM for HIV-1 and HIV-2 protease, respectively) that exhibits antiviral activity with low cytotoxicity.1,2 When co-administered with ritonavir , the bioavailability of saquinavir (20 mg/kg) has been shown to increase 325-fold in mice through a mechanism that inhibits its metabolism by CYP3A.3
|1. Roberts, N.A., Martin, J.A., Kinchington, D., et al. Rational design of peptide-based HIV proteinase inhibitors. Science 248(4953), 358-361 (1990).|2. Tucker, T.J., Lumma, W.C., Jr., Payne, L.S., et al. A series of potent HIV-1 protease inhibitors containing a hydroxyethyl secondary amine transition state isostere: Synthesis, enzyme inhibition, and antiviral activity. J. Med. Chem. 35(14), 2525-2533 (1992).|3. Tomaru, A., Takeda-Morishita, M., Banba, H., et al. Analysis of the pharmacokinetic boosting effects of ritonavir on oral bioavailability of drugs in mice. Drug Metab. Pharmacokinet. 28(2), 144-152 (2013).