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Atazanavir sulfate

Atazanavir sulfate structure

CAS No:
229975-97-7
Formula:
C38H52N6O7.H2O4S
Chemical Name:
Atazanavir sulfate
Synonyms:
2,5,6,10,13-Pentaazatetradecanedioic acid,3,12-bis(1,1-dimethylethyl)-8-hydroxy-4,11-dioxo-9-(phenylmethyl)-6-[[4-(2-pyridinyl)phenyl]methyl]-,1,14-dimethyl ester,(3S,8S,9S,12S)-,sulfate (1:1);2,5,6,10,13-Pentaazatetradecanedioic acid,3,12-bis(1,1-dimethylethyl)-8-hydroxy-4,11-dioxo-9-(phenylmethyl)-6-[[4-(2-pyridinyl)phenyl]methyl]-,dimethyl ester,(3S,8S,9S,12S)-,sulfate (1:1) (salt);Atazanavir sulfate;Atazor;Reyataz
Categories:
Active Pharmaceutical Ingredients > Antibiotics

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) pro

Atazanavir Sulfate is a sulfate salt form of atazanavir, an aza-dipeptide analogue with a bis-aryl substituent on the (hydroxethyl)hydrazine moiety with activity against both wild type and mutant forms of HIV protease. Atazanavir does not elevate serum lipids, a common problem with other protease inhibitors.|An azapeptide and HIV-PROTEASE INHIBITOR that is used in the treatment of HIV INFECTIONS and AIDS in combination with other ANTI-HIV AGENTS.

Atazanavir sulfate Basic Attributes

Molecular Weight：

802.93

Exact Mass：

802.357117

EC Number：

1312995-182-4

UNII：

4MT4VIE29P

NCI Thesaurus Code：

C28835

ATC Code：

J05AR|J05AE08

HScode：

29333990

Characteristics

PSA：

254

XLogP3：

6.20320

Density：

1.164g/cm3

Melting Point：

195.0°, or acetone; mp 198-199° (dec)

Boiling Point：

995.5ºC at 760 mmHg

Flash Point：

555.8ºC

Specific rotation：

D22 -46.1° (c = 1 in 1:1 CH3OH/H2O, pH = 2.6)

Safety Information

Transport codes：

NONH for all modes of transport

safety instructions：

24/25

Precautionary statement(s)：

P260-P280-P305 + P351 + P338 + P310

Hazard Statements：

H318-H372

GHS Classification：

|Danger|H302 (14.29%): Harmful if swallowed [Warning Acute toxicity, oral]|P260, P261, P264, P270, P271, P273, P280, P301+P312, P302+P352, P304+P340, P305+P351+P338, P310, P312, P314, P321, P330, P332+P313, P337+P313, P362, P391, P403+P233, P405, and P501|Aggregated GHS information provided by 7 companies from 6 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

Drug Indication：

Evotaz is indicated in combination with other antiretroviral medicinal products for the treatment of HIV-1 infected adults without known mutations associated with resistance to atazanavir.|Reyataz capsules, co-administered with low dose ritonavir, are indicated for the treatment of HIV-1 infected adults and paediatric patients 6 years of age and older in combination with other antiretroviral medicinal products (see section 4.2).Based on available virological and clinical data from adult patients, no benefit is expected in patients with strains resistant to multiple protease inhibitors (≥ 4 PI mutations).The choice of Reyataz in treatment experienced adult and paediatric patients should be based on individual viral resistance testing and the patient's treatment history (see sections 4.4 and 5.1).Reyataz oral powder, co-administered with low dose ritonavir, is indicated in combination with other antiretroviral medicinal products for the treatment of HIV-1 infected paediatric patients at least 3 months of age and weighing at least 5 kg (see section 4.2).Based on available virological and clinical data from adult patients, no benefit is expected in patients with strains resistant to multiple protease inhibitors ( 4 PI mutations). The choice of Reyataz in treatment experienced adult and paediatric patients should be based on individual viral resistance testing and the patient's treatment history (see sections 4.4 and 5.1).|Treatment of human immunodeficiency virus (HIV-1) infection

MeSH：

Inhibitors of HIV PROTEASE, an enzyme required for production of proteins needed for viral assembly. (See all compounds classified as HIV Protease Inhibitors.)

MeSH Entry Terms：

232632, BMS

Atazanavir sulfate Use and Manufacturing

Uses

Atazanavir is a HIV protease inhibitor with Ki of 2.66 nM

Use Classification：

Human drugs -> Evotaz -> EMA Drug Category|Antivirals for systemic use -> Human pharmacotherapeutic group|Human drugs -> Reyataz -> EMA Drug Category|Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:802.9
Hydrogen Bond Donor Count:7
Hydrogen Bond Acceptor Count:13
Rotatable Bond Count:18
Exact Mass:802.35712773
Monoisotopic Mass:802.35712773
Topological Polar Surface Area:254
Heavy Atom Count:56
Complexity:1190
Defined Atom Stereocenter Count:4
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

Atazanavir is an azapeptide HIV-1 protease inhibitor that selectively inhibits specific processing of viral Gag and Gag-Pol polyproteins in HIV-1 infected cells, thereby blocking the formation of mature virions. In the absence of human serum, the average 50% effective concentration (EC50) of atazanavir is 2-5 nM for a large number of laboratory and clinically isolated HIV-1 virus strains colonized in peripheral blood monocytes, macrophages, CEM-SS cells and MT2 cells. Atazanavir is active against HIV-1M subtype A, B, C, D, AE, AG, F, G, and J isolates in cell lines. However, it has different activity against HIV-2 isolates (1.9-32 nM), and the EC50 value is higher than the EC50 value of the virus strain that failed to inhibit.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Atazanavir Sulfate Capsules
Ingredients	The main ingredient of this product is atazanavir sulfate.
Indication	1. This product is a moderate CYP3A inhibitor with an inhibition constant of 2.2-2.7 nmol/L. When used in combination with ritonavir, a powerful CYP3A inhibitor, the blood concentration of this product increased several times. 2. When used in combination with the CYP3A inducer efavirenz, the Cmax, AUC and Cmin of this product decreased by 59%, 74% and 99%, respectively. 3. Healthy volunteers took this product 1 hour before giving stavudine and didanosine, and there was no obvious interaction. However, when the three drugs were taken at the same time, the Cmax and AUC of this product decreased by 89.3% and 87%, respectively. The reason may be due to the formation of an acid-resistant buffering effect caused by didanosine. 4. The dose of this product does not need to be adjusted when used in combination with lamivudine and zidovudine. 5. This product is 400 mg, once a day, with stavudine
Specifications	0.1 g (calculated as C38H52N6O7)

Atazanavir Sulfate Capsules
Ingredients	The main ingredient of this product is atazanavir sulfate.
Indication	1. This product is a moderate CYP3A inhibitor with an inhibition constant of 2.2-2.7 nmol/L. When used in combination with ritonavir, a powerful CYP3A inhibitor, the blood concentration of this product increased several times. 2. When used in combination with the CYP3A inducer efavirenz, the Cmax, AUC and Cmin of this product decreased by 59%, 74% and 99%, respectively. 3. Healthy volunteers took this product 1 hour before giving stavudine and didanosine, and there was no obvious interaction. However, when the three drugs were taken at the same time, the Cmax and AUC of this product decreased by 89.3% and 87%, respectively. The reason may be due to the formation of an acid-resistant buffering effect caused by didanosine. 4. The dose of this product does not need to be adjusted when used in combination with lamivudine and zidovudine. 5. This product is 400 mg, once a day, with stavudine
Specifications	0.15 g (calculated as C38H52N6O7)

Atazanavir Sulfate Capsules
Ingredients	The main ingredient of this product is atazanavir sulfate.
Indication	1. This product is a moderate CYP3A inhibitor with an inhibition constant of 2.2-2.7 nmol/L. When used in combination with ritonavir, a powerful CYP3A inhibitor, the blood concentration of this product increased several times. 2. When used in combination with the CYP3A inducer efavirenz, the Cmax, AUC and Cmin of this product decreased by 59%, 74% and 99%, respectively. 3. Healthy volunteers took this product 1 hour before giving stavudine and didanosine, and there was no obvious interaction. However, when the three drugs were taken at the same time, the Cmax and AUC of this product decreased by 89.3% and 87%, respectively. The reason may be due to the formation of an acid-resistant buffering effect caused by didanosine. 4. The dose of this product does not need to be adjusted when used in combination with lamivudine and zidovudine. 5. This product is 400 mg, once a day, with stavudine
Specifications	0.2g (calculated as C38H52N6O7)

Registered Holders

CDYMAX (INDIA) PHARMA PRIVATE LTD

United States
Active
LAURUS LABS LTD

United States
Active
RAKS PHARMA PVT LTD

United States
Active

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