Atazanavir sulfate

Modify Date: 2024-01-06 21:00:38

Atazanavir sulfate structure	Common Name	Atazanavir sulfate
	CAS Number	229975-97-7	Molecular Weight	802.934
	Density	1.164g/cm3	Boiling Point	995.5ºC at 760 mmHg
	Molecular Formula	C₃₈H₅₄N₆O₁₁S	Melting Point	195.0°, or acetone; mp 198-199° (dec)
	MSDS	N/A	Flash Point	555.8ºC
	Symbol	GHS05, GHS08	Signal Word	Danger

Use of Atazanavir sulfate

Atazanavir sulfate is a sulfate salt form of atazanavir that is an highly potent HIV-1 protease inhibitor.Target: HIV-1 protease inhibitorAtazanavir sulfate is a sulfate salt form of atazanavir that is an highly potent HIV-1 protease inhibitor. It has a pharmacokinetic profile that supports once-daily dosing and has demonstrated a unique resistance profile and superior virologic potency compared with other antiretrovirals in vitro. In subjects with HIV, atazanavir (400 mg once daily) produced rapid and sustained improvements in viral load and CD4 counts in both antiretroviral-naive as well as previously treated patients when used in combination with dual nucleoside reverse transcriptase inhibitor (NRTI) treatment [1].After intravenous (iv), oral (po) and intraportal (ip) administration of ATV at a dosage of 7 mg/kg, AUCs in HL rats were 12.41, 5.24 and 8.89 microg/mLh, respectively, and were significantly higher than those in control rats (4.09, 1.70 and 3.38 microg/mLh). Despite the decrease of distribution volume (Vd(ss)), the terminal half-life (t(1/2)) in HL tended to be shorter than in control, and hepatic distribution of ATV in HL rats was 4.8-fold increases. These results suggested that the uptake of ATV into liver might counteract the decrease of Vd(ss). On the other hand, there was no significant difference in bioavailability, and the lymphatic transport to AUC showed no statistical change. In conclusion, although the protein binding rate and AUC were significantly increased, the pharmacokinetics of ATV might be tolerated in HL [2].Clinical indications: HIV-1 infection Toxicity: torsades de pointes

Name	atazanavir sulfate
Synonym	More Synonyms

Description	Atazanavir sulfate is a sulfate salt form of atazanavir that is an highly potent HIV-1 protease inhibitor.Target: HIV-1 protease inhibitorAtazanavir sulfate is a sulfate salt form of atazanavir that is an highly potent HIV-1 protease inhibitor. It has a pharmacokinetic profile that supports once-daily dosing and has demonstrated a unique resistance profile and superior virologic potency compared with other antiretrovirals in vitro. In subjects with HIV, atazanavir (400 mg once daily) produced rapid and sustained improvements in viral load and CD4 counts in both antiretroviral-naive as well as previously treated patients when used in combination with dual nucleoside reverse transcriptase inhibitor (NRTI) treatment [1].After intravenous (iv), oral (po) and intraportal (ip) administration of ATV at a dosage of 7 mg/kg, AUCs in HL rats were 12.41, 5.24 and 8.89 microg/mLh, respectively, and were significantly higher than those in control rats (4.09, 1.70 and 3.38 microg/mLh). Despite the decrease of distribution volume (Vd(ss)), the terminal half-life (t(1/2)) in HL tended to be shorter than in control, and hepatic distribution of ATV in HL rats was 4.8-fold increases. These results suggested that the uptake of ATV into liver might counteract the decrease of Vd(ss). On the other hand, there was no significant difference in bioavailability, and the lymphatic transport to AUC showed no statistical change. In conclusion, although the protein binding rate and AUC were significantly increased, the pharmacokinetics of ATV might be tolerated in HL [2].Clinical indications: HIV-1 infection Toxicity: torsades de pointes
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> HIV Protease Signaling Pathways >> Anti-infection >> HIV Research Areas >> Infection
References	[1]. Piliero PJ. Atazanavir: A novel once-daily protease inhibitor. Drugs Today (Barc). 2004 Nov;40(11):901-12. [2]. Fukushima K, et al. Effect of serum lipids on the pharmacokinetics of atazanavir in hyperlipidemic rats. Biomed Pharmacother. 2009 Nov;63(9):635-42.

Description

Related Catalog

Signaling Pathways >> Metabolic Enzyme/Protease >> HIV Protease

Signaling Pathways >> Anti-infection >> HIV

Research Areas >> Infection

References

[1]. Piliero PJ. Atazanavir: A novel once-daily protease inhibitor. Drugs Today (Barc). 2004 Nov;40(11):901-12.

[2]. Fukushima K, et al. Effect of serum lipids on the pharmacokinetics of atazanavir in hyperlipidemic rats. Biomed Pharmacother. 2009 Nov;63(9):635-42.

Density	1.164g/cm3
Boiling Point	995.5ºC at 760 mmHg
Melting Point	195.0°, or acetone; mp 198-199° (dec)
Molecular Formula	C₃₈H₅₄N₆O₁₁S
Molecular Weight	802.934
Flash Point	555.8ºC
Exact Mass	802.357117
PSA	254.20000
LogP	6.20320
Vapour Pressure	0mmHg at 25°C

Symbol	GHS05, GHS08
Signal Word	Danger
Hazard Statements	H318-H372
Precautionary Statements	P260-P280-P305 + P351 + P338 + P310
Target Organs	Heart, Liver
Hazard Codes	Xi
Safety Phrases	24/25
RIDADR	NONH for all modes of transport

Zrivada {Sulfate}

methyl [(1S,4S,5S,10S)-4-benzyl-1,10-di-tert-butyl-5-hydroxy-2,9,12-trioxo-7-(4-pyridin-2-ylbenzyl)-13-oxa-3,7,8,11-tetraazatetradec-1-yl]carbamate sulfate (salt)

BMS-232632-05 {Sulfate}

Methyl {(5S,10S,11S,14S)-11-benzyl-10-hydroxy-15,15-dimethyl-5-(2-methyl-2-propanyl)-3,6,13-trioxo-8-[4-(2-pyridinyl)benzyl]-2-oxa-4,7,8,12-tetraazahexadecan-14-yl}carbamate sulfate (1:1) (non-preferred name)

Butanoic acid, 2-[(methoxycarbonyl)amino]-3,3-dimethyl-, 2-[(2S,3S)-2-hydroxy-3-[[(2S)-2-[(methoxycarbonyl)amino]-3,3-dimethyl-1-oxobutyl]amino]-4-phenylbutyl]-2-[[4-(2-pyridinyl)phenyl]methyl]hydrazide, (2S)-, sulfate (1:1) (salt)

BMS-232632-05

Atazanavir Bisulfate Salt

Atazanavir sulfate

[(1S,4S,5S,10S)-4-benzyl-1,10-bis(1,1-diméthyléthyl)-5-hydroxy-2,9,12-trioxo-7-(4-pyridin-2-ylbenzyl)-13-oxa-3,7,8,11-tétraazatétradéc-1-yl]carbamate de méthyle sulfate (salt)

Reyataz {Sulfate}

butanoic acid, 2-[(methoxycarbonyl)amino]-3,3-dimethyl-, 2-[(2S,3S)-2-hydroxy-3-[[(2S)-2-[(methoxycarbonyl)amino]-3,3-dimethyl-1-oxobutyl]amino]-4-phenylbutyl]-2-[[4-(2-pyridinyl)phenyl]methyl]hydrazi

de, (2S)-, sulfate (1:1) (salt)

Methyl-[(1S,4S,5S,10S)-4-benzyl-1,10-di-tert-butyl-5-hydroxy-2,9,12-trioxo-7-(4-pyridin-2-ylbenzyl)-13-oxa-3,7,8,11-tetraazatetradec-1-yl]carbamatsulfat(salt)

Atazanavir (sulfate)