Indinavir

From Proteopedia

proteopedia linkproteopedia link

Revision as of 07:17, 2 December 2010 (edit) David Canner (Talk | contribs) ← Previous diff		Revision as of 07:20, 2 December 2010 (edit) (undo) David Canner (Talk | contribs) Next diff →
Line 33:		Line 33:
	! Indinavir		! Indinavir
	! Saquinavir		! Saquinavir
-	! Amprenavir	+	! .98
	! Fosamprenavir		! Fosamprenavir
	! Lopinavir		! Lopinavir
Line 46:		Line 46:
	! Indinavir		! Indinavir
	! Saquinavir		! Saquinavir
-	! Amprenavir	+	! 4901
	! Fosamprenavir		! Fosamprenavir
	! Lopinavir		! Lopinavir
Line 85:		Line 85:
	! 1.8		! 1.8
	! 7-12		! 7-12
-	! Amprenavir	+	! 5.56
	! Fosamprenavir		! Fosamprenavir
	! Lopinavir		! Lopinavir
Line 98:		Line 98:
	! Indinavir		! Indinavir
	! Saquinavir		! Saquinavir
-	! Amprenavir	+	! 11999
	! Fosamprenavir		! Fosamprenavir
	! Lopinavir		! Lopinavir
Line 124:		Line 124:
	! Indinavir		! Indinavir
	! Saquinavir		! Saquinavir
-	! Amprenavir	+	! 56.76
	! Fosamprenavir		! Fosamprenavir
	! Lopinavir		! Lopinavir
Line 137:		Line 137:
	! Indinavir		! Indinavir
	! Saquinavir		! Saquinavir
-	! Amprenavir	+	! 600
	! Fosamprenavir		! Fosamprenavir
	! Lopinavir		! Lopinavir

---

Revision as of 07:20, 2 December 2010

spinqualitylabelsall models Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image

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]
Parameter	Ritonavir	Tipranavir	Indinavir	Saquinavir	Amprenavir	Fosamprenavir	Lopinavir	Ritonavir	Darunavir	Atazanavir	Nelfinavir
Tmax (hr)	4.4	~3	Indinavir	Saquinavir	.98	Fosamprenavir	Lopinavir	Ritonavir	Darunavir	Atazanavir	Nelfinavir
Cmax (ng/ml)	13120	14600	Indinavir	Saquinavir	4901	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)	4.78	4.2	1.8	7-12	5.56	Fosamprenavir	Lopinavir	Ritonavir	Darunavir	Atazanavir	Nelfinavir
AUC (ng/ml/hr)	128100	46500	Indinavir	Saquinavir	11999	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	56.76	Fosamprenavir	Lopinavir	Ritonavir	Darunavir	Atazanavir	Nelfinavir
Dosage (mg)	600	600	Indinavir	Saquinavir	600	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
2. ↑ Ferry et al, United States Patent US6147095, Pharmacia & Upjohn Company.