Atazanavir
- CAS No.
- 198904-31-3
- Chemical Name:
- Atazanavir
- Synonyms
- Atv;Atazanavir iMpurity;CS-534;CS-2210;atazanvir;EOS-60363;Atazanavir;Aids057755;Aids-057755;Latazanavir
- CBNumber:
- CB0500863
- Molecular Formula:
- C38H52N6O7
- Molecular Weight:
- 704.86
- MOL File:
- 198904-31-3.mol
- Modify Date:
- 2024/4/16 16:23:18
| Melting point | 207-2090C |
|---|---|
| alpha | D -47° (c = 1 in ethanol) |
| Density | 1.178±0.06 g/cm3(Predicted) |
| storage temp. | -20°C |
| solubility | Ethanol (Slightly), Methanol (Slightly) |
| pka | 11.11±0.46(Predicted) |
| form | powder |
| color | white to beige |
| CAS DataBase Reference | 198904-31-3 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H319 | |||||||||
| Precautionary statements | P305+P351+P338 | |||||||||
| NFPA 704 |
|
Atazanavir price More Price(2)
Atazanavir Chemical Properties,Uses,Production
Chemical Properties
Crystalline Solid
Uses
Atazanavir is a novel azapeptide protease inhibitor (PI)
Definition
ChEBI: A heavily substituted carbohydrazide that is an antiretroviral drug of the protease inhibitor (PI) class used to treat infection of human immunodeficiency virus (HIV).
Acquired resistance
Mutations at positions 50 (I50L), 84 (I84V) and 88 (N88S) of the protease gene are associated with resistance.
General Description
Atazanavir is an antiretroviral agent that has been approvedby the FDA for use in combination with other anti-RTagents for the treatment of HIV infections. The drug is alwaysused in combination with RT inhibitors.
Pharmaceutical Applications
An azapeptide formulated as the sulfate for oral use.
Mechanism of action
Atazanavir is dosed orally once daily, thus reducing "pill burden," and it appears to have minimal impact on lipid parameters but does increase total bilirubin. The drug is well absorbed when administered orally with food (bioavailability, ~68%). The drug is highly bound to plasma protein (86%) and is metabolized by CYP3A isoenzyme. Atazanavir is a moderate inhibitor of CYP3A, and potential drug–drug interactions are possible with CYP3A inhibitors and inducers.
Pharmacokinetics
Oral absorption: c. 68%
Cmax 400 mg once daily: c. 3.15 μg/L
300 mg + ritonavir 100 mg once daily: c. 4.47 μg/L
Cmin 400 mg once daily: c. 0.27 μg/L
300 mg + ritonavir 100 mg once daily: c. 0.65 μg/L
Plasma half-life: c. 8.6 h (300 mg+ ritonavir
100 mg)
Volume of distribution: c. Not known/available
Plasma protein binding: c. 86%
Absorption
Administration with food enhances bioavailability and reduces pharmacokinetic variability. Absorption is dependent on gastric pH. It should be given separately from proton-pump inhibitors or H2-receptor antagonists. Buffered or entericcoated formulations should be given (with food) 2 h before or 1 h after co-administration of didanosine.
Distribution
It penetrates moderately well into the CNS. The semen:plasma ratio is 0.11–4.42. It is distributed into breast milk.
Metabolism
It is extensively metabolized by CYP3A4. Administration with ritonavir prevents metabolization and enhances the pharmacokinetic profile.
Excretion
Following a single 400 mg dose, 79% and 13% of the dose was recovered in the feces and urine, respectively. It should be used with caution in the presence of mild hepatic impairment and should not be used in patients with more severe hepatic impairment.
Clinical Use
Treatment of HIV infection (in combination with other antiretroviral drugs)
Side effects
The most common adverse reactions (≥2%) are nausea, jaundice/ scleral icterus, rash, headache, abdominal pain, vomiting, insomnia, peripheral neurological symptoms, dizziness, myalgia, diarrhea, depression and fever.
Atazanavir Preparation Products And Raw materials
Raw materials
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chevron_rightPreparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| AVD pharmaceuticals Pvt Ltd | +919860835260 | Pune, India | 102 | 58 | Inquiry |
| Anant Pharmaceuticals Pvt Ltd | +91-8550986868 +91-9485998001 | Haryana, India | 461 | 58 | Inquiry |
| J S LABS | +91-7330612784 +91-7330612784 | Tamil Nadu, India | 160 | 58 | Inquiry |
| GLP Pharma Standards | +91 9866074638 | Hyderabad, India | 1644 | 58 | Inquiry |
| Dodhia Group | +91-9619867345 +91-9619867345 | Mumbai, India | 129 | 58 | Inquiry |
| Aurobindo Pharma Limited | +914066725000 | Telangana, India | 112 | 58 | Inquiry |
| Macleods Pharmaceuticals Limited | +91-2266762800 +91-2266762800 | Maharashtra, India | 116 | 58 | Inquiry |
| HRV Global Life Sciences | +91-9820219686 +91-9820219686 | Telangana, India | 379 | 58 | Inquiry |
| Laurus Labs Ltd | +91-4066594333 +91-4039804333 | Telangana, India | 50 | 58 | Inquiry |
| Raising Sun Pharma | +91-9399941155 +91-9399941155 | Telangana, India | 127 | 58 | Inquiry |
| Supplier | Advantage |
|---|---|
| AVD pharmaceuticals Pvt Ltd | 58 |
| Anant Pharmaceuticals Pvt Ltd | 58 |
| J S LABS | 58 |
| GLP Pharma Standards | 58 |
| Dodhia Group | 58 |
| Aurobindo Pharma Limited | 58 |
| Macleods Pharmaceuticals Limited | 58 |
| HRV Global Life Sciences | 58 |
| Laurus Labs Ltd | 58 |
| Raising Sun Pharma | 58 |
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