Fosamprenavir

spinqualitylabelsall models Fosamprenavir, better known as Lexiva, (3nu4) Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Better Known as: Lexiva or Telzir Marketed By: Viiv Healthcare (Joint venture of Pfizer & GlaxoSmithKline) Major Indication: Human Immunodeficiency Virus Infection Drug Class: HIV Protease Inhibitor Date of FDA Approval (Discontinued): 2003 (2017) 2007 Sales: $240 Million Importance: As a prodrug, It is rapidly metabolized by the liver into its active form, also known as Amprenavir. As a prodrug, it is a slow release form of Amprenavir, thus requiring less frequent dosing. It was one of the first instances of a successful drug stemming from joint ventures of major pharmaceutical companies. See Pharmaceutical Drugs for more information about other drugs and diseases. Mechanism of Action Fosamprenavir is a potent HIV Protease inhibitor. As a prodrug form of Amprenavir, it has an identical mechanism of action as Amprenavir. Drug Resistance The biggest difficulty with treating HIV is the rapidity at which it mutates and becomes resistant to treatments. To view a comprehensive and interactive analysis of the mutations which confer drug resistance to HIV Protease, See: HIV Protease Inhibitor Resistance Profile

Pharmacokinetics

HIV Protease Inhibitor Human Immunodeficiency Virus Parameter HIV Protease Amprenavir Pharmaceutical Drugs HIV Protease Amprenavir Fosamprenavir HIV HIV Protease HIV Protease Inhibitor Resistance Profile Nelfinavir Tmax (hr) 4.4 ~3 1.5 3.7 .98 1.5-4 2 .5 2-4 3.1 Cmax (ng/ml) 13120 14600 8100 2297 4901 4820 11.9 2730 ~4393 4701 Bioavailability (%) -- -- 65 4 -- -- -- -- 68 20-80 Protein Binding (%) 99 >99 61 98 90 90 99 95 86 98 T1/2 (hr) 4.8 4.2 1.2 4.5 5.5 7.7 6.1 29.4 5.3 3.3 AUC (ng/ml/hr) 128100 46500 20900 13467 11999 35000 117600 4746 ~26045 31906 Clearance (L/h) ~8.4 32.4 49.5 36.7 56.8 84.4 1.7 32.8 13.6 37.3 Dosage (mg) 600 600 800 1000 600 1400 280 400 400 1250 Metabolism Hepatic (CYP3A4 & CYP2C19) Hepatic (CYP3A4) Hepatic (CYP3A4) Hepatic (CYP3A4 & CYP3A5) Hepatic (CYP3A4) Hepatic (CYP3A4) Hepatic (CYP3A4) Hepatic (CYP3A4) Hepatic (CYP3A4) Hepatic (CYP3A4) For Pharmacokinetic Data References, See: References

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