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Ritonavir

Catalog No. DB00503 Name DrugBank
CAS Number 155213-67-5 Website http://www.ualberta.ca/
M. F. C37H48N6O5S2 Telephone (780) 492-3111
M. W. 720.94422 Fax (780) 492-1071
Purity Email david.wishart@ualberta.ca
Storage Chembase ID: 386

SYNONYMS

IUPAC name
1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[(2S)-3-methyl-2-{[methyl({[2-(propan-2-yl)-1,3-thiazol-4-yl]methyl})carbamoyl]amino}butanamido]-1,6-diphenylhexan-2-yl]carbamate
IUPAC Traditional name
ritonavir
Brand Name
Norvir
Norvir Sec
Synonyms
ritonavir
Abbott 84538

DATABASE IDS

CAS Number 155213-67-5
PubChem CID 392622
PubChem SID 46505050

PROPERTIES

Hydrophobicity(logP) 3.9
Solubility Practically insoluble

DETAILS

Description (English)
Item Information
Drug Groups approved; investigational
Description An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. [PubChem]
Indication Indicated in combination with other antiretroviral agents for the treatment of HIV-infection.
Pharmacology Ritonavir is a protease inhibitor with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Protease inhibitors block the part of HIV called protease. HIV-1 protease is an enzyme required for the proteolytic cleavage of the viral polyprotein precursors into the individual functional proteins found in infectious HIV-1. Ritonavir binds to the protease active site and inhibits the activity of the enzyme. This inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature non-infectious viral particles. Protease inhibitors are almost always used in combination with at least two other anti-HIV drugs.
Toxicity Human experience of acute overdose with ritonavir is limited. One patient in clinical trials took ritonavir 1500 mg/day for two days. The patient reported paresthesias which resolved after the dose was decreased. A post-marketing case of renal failure with eosinophilia has been reported with ritonavir overdose. The approximate lethal dose was found to be greater than 20 times the related human dose in rats and 10 times the related human dose in mice.
Affected Organisms
Human Immunodeficiency Virus
Biotransformation Hepatic. Five metabolites have been identified. The isopropylthiazole oxidation metabolite (M-2) is the major metabolite and has antiviral activity similar to that of ritonavir, however, plasma concentrations are low. The cytochrome P450 enzymes CYP3A and CYP2D6 are primarily involved in the metabolism of ritonavir.
Absorption The absolute bioavailability of ritonavir has not been determined.
Half Life 3-5 hours
Protein Binding 98-99%
External Links
Wikipedia
RxList
Drugs.com

REFERENCES