Saquinavir, sold under the brand name Invirase among others, is an antiretroviral medication used together with other medications to treat or prevent HIV/AIDS. Typically it is used with ritonavir or lopinavir/ritonavir to increase its effect. It is taken orally; it has low intrinsic bioavailability that is substantially increased when coadministered with a pharmacokinetic booster such as ritonavir. Saquinavir is a peptidomimetic inhibitor of the HIV-1 aspartyl protease that binds the enzyme active site and prevents proteolytic cleavage of Gag and Gag-Pol polyprotein precursors, yielding immature noninfectious virions. The compound is highly protein bound, predominantly metabolized by hepatic cytochrome P450 3A4, and eliminated mainly via biliary excretion. Clinical use requires attention to drug interactions with CYP3A substrates, inducers, and inhibitors and to safety parameters including liver function and electrocardiographic monitoring when indicated.
Parent: Saquinavir
Parent: Saquinavir
Parent: Saquinavir
Parent: Saquinavir
Parent: Saquinavir/ Saquinavir Mesylate
Typical quality control specifications applied during API release and stability testing set limits for related compounds and impurities; representative acceptance criteria used by manufacturers and in regulatory filings are individual specified related compounds not more than 0.5 percent w w, individual unspecified impurities not more than 0.2 percent w w, and total impurities not more than 1.5 percent w w. Key related compounds monitored include N-dealkylated species (typical limit 0.5 percent), oxidative metabolites such as sulfoxides or sulfones when applicable (typical limit 0.3 percent), and epimerization or hydrolytic products (typical limit 0.2 percent each). Reporting thresholds and identification requirements follow ICH Q3A and Q3B guidance and may be tightened for stability-indicating degradants; final specification values depend on the finished product formulation and the regulatory dossier for the market of interest.
Saquinavir is used as part of combination antiretroviral therapy to treat HIV infection and to reduce viral replication; it is not used as monotherapy and is typically given with a pharmacokinetic booster such as ritonavir.
Saquinavir binds the active site of the HIV-1 protease enzyme, inhibiting proteolytic cleavage of viral polyproteins and preventing maturation of infectious virions.
Use of saquinavir has declined with the availability of newer agents; some branded formulations have been withdrawn or are no longer marketed in certain countries, while generic saquinavir products or legacy supplies may remain available depending on local regulatory status.
Saquinavir is classified as an HIV protease inhibitor, a peptidomimetic antiretroviral agent that targets the viral aspartyl protease.
