Indinavir

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Revision as of 07:45, 2 December 2010

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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][2][3][4]
Parameter	Ritonavir	Tipranavir	Indinavir	Saquinavir	Amprenavir	Fosamprenavir	Lopinavir	Darunavir	Atazanavir	Nelfinavir
Tmax (hr)	4.4	~3	Indinavir	Saquinavir	.98	Fosamprenavir	Lopinavir	Darunavir	Atazanavir	Nelfinavir
Cmax (ng/ml)	13120	14600	Indinavir	1540	4901	Fosamprenavir	Lopinavir	Darunavir	Atazanavir	4381
Bioavailability (%)	Ritonavir	Tipranavir	65	Saquinavir	Amprenavir	Fosamprenavir	Lopinavir	Darunavir	Atazanavir	Nelfinavir
Protein Binding (%)	99	>99	61	98	Amprenavir	Fosamprenavir	Lopinavir	Darunavir	Atazanavir	Nelfinavir
T1/2 (hr)	4.78	4.2	1.8	4.5	5.56	Fosamprenavir	Lopinavir	Darunavir	Atazanavir	3.3
AUC (ng/ml/hr)	128100	46500	Indinavir	16200	11999	Fosamprenavir	Lopinavir	Darunavir	Atazanavir	27000
IC50 (nM)	Ritonavir	Tipranavir	Indinavir	Saquinavir	Amprenavir	Fosamprenavir	Lopinavir	Darunavir	Atazanavir	Nelfinavir
Clearance (L/h)	Ritonavir	32.4	Indinavir	Saquinavir	56.76	Fosamprenavir	Lopinavir	Darunavir	Atazanavir	Nelfinavir
Dosage (mg)	600	600	Indinavir	Saquinavir	600	Fosamprenavir	Lopinavir	Darunavir	Atazanavir	750
Metabolism	Hepatic (CYP3A4)	Hepatic (CYP3A4)	Hepatic (CYP3A4)	Hepatic (CYP3A4)	Amprenavir	Hepatic (CYP3A4)	Lopinavir	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
2. ↑ Ferry et al, United States Patent US6147095, Pharmacia & Upjohn Company.
3. ↑ L. Veronese et al. Single-Dose Pharmacokinetics of Amprenavir, a Human Immunodeficiency Virus Type 1 Protease Inhibitor, in Subjects with Normal or Impaired Hepatic Function. Antimicrob Agents Chemother. 2000 April; 44(4): 821–826.
4. ↑ J. Ford, et al. Intracellular and Plasma Pharmacokinetics of Saquinavir-Ritonavir, Administered at 1,600/100 Milligrams Once Daily in Human Immunodeficiency Virus-Infected Patients. Antimicrob Agents Chemother. 2004 July; 48(7): 2388–2393.