Substance
ID:74030
Names and Identifiers
Synonyms
Deuterated Atazanivir-D3-1
IUPAC name
(2H3)methyl N-[(1S)-1-{N'-[(2S,3S)-2-hydroxy-3-[(2S)-2-{[(2H3)methoxycarbonyl]amino}-3,3-bis(2H3)methyl(4,4,4-2H3)butanamido]-4-phenylbutyl]-N'-{[4-(pyridin-2-yl)phenyl]methyl}hydrazinecarbonyl}-2,2-dimethylpropyl]carbamate
IUPAC Traditional name
(2H3)methyl N-[(1S)-1-{N'-[(2S,3S)-2-hydroxy-3-[(2S)-2-{[(2H3)methoxycarbonyl]amino}-3,3-bis(2H3)methyl(4,4,4-2H3)butanamido]-4-phenylbutyl]-N'-{[4-(pyridin-2-yl)phenyl]methyl}hydrazinecarbonyl}-2,2-dimethylpropyl]carbamate
Registration numbers
CAS Number
Properties
Pharmacology Properties
Target
Infection
Safety Information
Storage Condition
-20°C
Molecule Details
Biological Activity
Description
Atazanivir-D3-1 is a azapeptide derivative and inhibits HIV protease.
Targets
HIV protease
IC50
In Vitro
Atazanivir-D3-1 is an azapeptide derivative and is a HIV protease inhibitor. Atazanivir-D3-1 is the sulfate form of an azapeptide derivative.[1] Atazanivir-D3-1 is a deuterium-containing agent with ameliorated ADME properties. Atazanivir-D3-1 displays approximately 50% increase in half life compared with atazanavir. Atazanavir sulfate prevents the formation of mature HIV virions in HIV-1 infected cells by selectively inhibiting virus-specific processing of certain polyproteins (viral Gag and Gag-Pol).[1] Atazanavir sulfate is currently approved for the treatment of HIV infection. Atazanavir is contraindicated for co-administration with medicines that are highly dependent on CYP3A for clearance and for which elevated plasma concentrations are associated with serious and/or life-threatening events. Due to inhibitory effects of atazanavir on CYP3A, CYP2C8, and UGTIAl, caution is advised when prescribing. Common adverse events associated with atazanavir include hyperbilirubinemia, rash, nausea, headache, mid jaundice/sclcral icterus.[1]
In Vivo
Clinical Trials
Features
Molecular Spectra
No Data Available
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References
• Harbeson, S.L., et al. Eur. Pat. Appl. 2008, 59 pp. EP 2003120 A1 20081217.