Indinavir
From Proteopedia
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Revision as of 07:17, 2 December 2010
|
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 | Amprenavir | Fosamprenavir | Lopinavir | Ritonavir | Darunavir | Atazanavir | Nelfinavir |
| Cmax (ng/ml) | 13120 | 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) | 4.78 | 4.2 | 1.8 | 7-12 | Amprenavir | Fosamprenavir | Lopinavir | Ritonavir | Darunavir | Atazanavir | Nelfinavir |
| AUC (ng/ml/hr) | 128100 | 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) | 600 | 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
- ↑ 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
- ↑ Ferry et al, United States Patent US6147095, Pharmacia & Upjohn Company.
