Indinavir

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Better Known as: Crixivan

• Marketed By: Merck & Co.
  
• Major Indication: Human Immunodeficiency Virus Infection
  
• Drug Class: HIV Protease Inhibitor
• Date of FDA Approval (Patent Expiration): 1996 (2014)
  
• 2006 Sales:
• Importance:
• The following is a list of Pharmacokinetic Parameters. See: Pharmaceutical Drugs for more information

Mechanism of Action

Pharmacokinetics

HIV Protease Inhibitor Pharmacokinetics[1]
Parameter	Ritonavir	Tipranavir	Indinavir	Saquinavir	Amprenavir	Fosamprenavir	Lopinavir	Ritonavir	Darunavir	Atazanavir	Nelfinavir
Tmax (hr)	2.67	~3	Indinavir	Saquinavir	Amprenavir	Fosamprenavir	Lopinavir	Ritonavir	Darunavir	Atazanavir	Nelfinavir
Cmax (ng/ml)	5444	14600	Indinavir	Saquinavir	Amprenavir	Fosamprenavir	Lopinavir	Ritonavir	Darunavir	Atazanavir	Nelfinavir
Bioavailability (%)	Ritonavir	Tipranavir	65	Saquinavir	Amprenavir	Fosamprenavir	Lopinavir	Ritonavir	Darunavir	Atazanavir	Nelfinavir
Protein Binding (%)	99	>99	61	98	Amprenavir	Fosamprenavir	Lopinavir	Ritonavir	Darunavir	Atazanavir	Nelfinavir
T1/2 (hr)	4	4.2	1.8	7-12	Amprenavir	Fosamprenavir	Lopinavir	Ritonavir	Darunavir	Atazanavir	Nelfinavir
AUC (ng/ml/hr)	58000	46500	Indinavir	Saquinavir	Amprenavir	Fosamprenavir	Lopinavir	Ritonavir	Darunavir	Atazanavir	Nelfinavir
IC50 (nM)	Ritonavir	Tipranavir	Indinavir	Saquinavir	Amprenavir	Fosamprenavir	Lopinavir	Ritonavir	Darunavir	Atazanavir	Nelfinavir
Clearance (L/h)	Ritonavir	32.4	Indinavir	Saquinavir	Amprenavir	Fosamprenavir	Lopinavir	Ritonavir	Darunavir	Atazanavir	Nelfinavir
Dosage (mg)	Ritonavir	600	Indinavir	Saquinavir	Amprenavir	Fosamprenavir	Lopinavir	Ritonavir	Darunavir	Atazanavir	Nelfinavir
Metabolism	Hepatic (CYP3A4)	Hepatic (CYP3A4)	Hepatic (CYP3A4)	Hepatic (CYP3A4)	Amprenavir	Fosamprenavir	Lopinavir	Ritonavir	Darunavir	Atazanavir	Nelfinavir

References

1. ↑ Goebel FD, MacGregor TR, Sabo JP, Castles M, Johnson PA, Legg D, McCallister S. Pharmacokinetic characterization of three doses of tipranavir boosted with ritonavir on highly active antiretroviral therapy in treatment-experienced HIV-1 patients. HIV Clin Trials. 2010 Jan-Feb;11(1):28-38. PMID:20400409 doi:10.1310/hct1101-28