Atazanavir

Atazanavir Struktur
198904-31-3
CAS-Nr.
198904-31-3
Englisch Name:
Atazanavir
Synonyma:
Atv;Atazanavir iMpurity;CS-534;CS-2210;atazanvir;EOS-60363;Atazanavir;Aids057755;Aids-057755;Latazanavir
CBNumber:
CB0500863
Summenformel:
C38H52N6O7
Molgewicht:
704.86
MOL-Datei:
198904-31-3.mol

Atazanavir Eigenschaften

Schmelzpunkt:
207-2090C
alpha 
D -47° (c = 1 in ethanol)
Dichte
1.178±0.06 g/cm3(Predicted)
storage temp. 
-20°C
Löslichkeit
Ethanol (Slightly), Methanol (Slightly)
pka
11.11±0.46(Predicted)
Aggregatzustand
powder
Farbe
white to beige
CAS Datenbank
198904-31-3
Sicherheit
  • Risiko- und Sicherheitserklärung
  • Gefahreninformationscode (GHS)
Bildanzeige (GHS) GHS hazard pictograms
Alarmwort Warnung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H319 Verursacht schwere Augenreizung. Schwere Augenreizung Kategorie 2 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P280, P305+P351+P338,P337+P313P
Sicherheit
P305+P351+P338 BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach Möglichkeit entfernen. Weiter spülen.

Atazanavir Chemische Eigenschaften,Einsatz,Produktion Methoden

Chemische Eigenschaften

Crystalline Solid

Verwenden

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.

Allgemeine Beschreibung

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.

Pharmazeutische Anwendungen

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.

Pharmakokinetik

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)

Nebenwirkungen

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 Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Atazanavir Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global( 329)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Hebei Mojin Biotechnology Co., Ltd
+8613288715578
sales@hbmojin.com China 12468 58
Henan Fengda Chemical Co., Ltd
+86-371-86557731 +86-13613820652
info@fdachem.com China 18222 58
Alpha Biopharmaceuticals Co., Ltd
+86-411-39042497 +8613921981412
sales@alphabiopharm.com China 886 58
Capot Chemical Co.,Ltd.
571-85586718 +8613336195806
sales@capotchem.com China 29797 60
Shanghai Daken Advanced Materials Co.,Ltd
+86-371-66670886
info@dakenam.com China 15956 58
Henan Tianfu Chemical Co.,Ltd.
+86-0371-55170693 +86-19937530512
info@tianfuchem.com China 21689 55
career henan chemical co
+86-0371-86658258
sales@coreychem.com China 29914 58
Casorganics US Corp
+17326109938
sales@casorganics.com CHINA 174 58
BOC Sciences
+1-631-485-4226
inquiry@bocsci.com United States 19553 58
Chongqing Chemdad Co., Ltd
+86-023-61398051 +8613650506873
sales@chemdad.com China 39916 58

198904-31-3()Verwandte Suche:


  • atazanvir
  • Atazanavir, >=99%
  • Atazanavir Enantiomer
  • Atazanavir Isomer Impurity
  • Atazanavir Isomer Impurity 1
  • Atazanavir Isomer Impurity 2
  • Atazanavir Isomer Impurity 3
  • Atazanavir Intermediate Impurity 1
  • Atazanavir Intermediate Impurity 2
  • Atazanavir Intermediate Impurity 4
  • methyl((5S,10S,11S,14S)-11-benzyl-5-(tert-butyl)-10-hydroxy-15,15-dimethyl-3,6,13-trioxo-8-(4-(pyridin-2-yl)benzyl)-2-oxa-4,7,8,12-tetraazahexadecan-14-yl)carbamate
  • Methyl N-[(2S)-1-[[(2S,3S)-3-hydroxy-4-[[[(2S)-2-(methoxycarbonylamino)-3,3-dimethylbutanoyl]a
  • Atazanavir Intermediate Impurity 3
  • Atazanavir
  • (3S,8S, 9S, 12S)-2,5,6,13-Pentaazatetradecanedioic Acid
  • 3,12-Bis(1,1-dimethylethyl)-8-hydroxy-4,11-dioxo-9-(phenylmethyl)-6-[[4-(2-pyridinyl)phenyl]methyl]-dimethyl Ester
  • Methyl N-[(2S)-1-[[(2S,3S)-3-hydroxy-4-[[[(2S)-2-(methoxycarbonylamino)-3,3-dimethylbutanoyl]amino]-[(4-pyridin-2-ylphenyl)methyl]amino]-1-phenylbutan-2-yl]amino]-3,3-dimethyl-1-oxobutan-2-yl]carbamate
  • (2S)-N-(3-{[(2S)-2-(Methoxycarbonylamino)-3,3-dimethylbutanoylamino][(4-(2-pyridyl)phenyl)methyl]amino}(1S,2S)-2-hydroxy-1-benzylpropyl)-2-(methoxycarbonylamino)-3,3-dimethylbutanamide
  • 229975-97-7 (Sulfate 1:1)
  • Aids057755
  • Aids-057755
  • Atazanavir & Atazanavir Sulfate
  • BMS-232632(Atazanavir)
  • Atazanavir(BMS-232632)
  • Methyl N-[(2S)-1-[[(2S,3S)-3-hydroxy-4-[[[(2S)-2-(MethoxycarbonylaMino)-
  • ATAZANAVIR, BISULFATE SALT
  • Atazanavir free base
  • 2,5,6,10,13-Pentaazatetradecanedioicacid,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)-
  • CS-534
  • BMS-232632-05; REYATAZ;BMS23263205
  • CS-2210
  • BMS 232632 - Atazanavir | CGP 73547
  • EOS-60363
  • Atazanavir Base
  • Latazanavir
  • Dimethyl (3S,8S,9S,12S)-9-benzyl-3,12,di-tert-butyl-8-hydroxy-4,11-dioxo-6-(p-2-pyridylbenzyl)-2,5,6,10,13-pentaazatetradecanedioate
  • 1,14-Dimethyl (3S,8S,9S,12S)-3,12-bis(1,1-dimethylethyl)-8-hydroxy-4,11-dioxo-9-(phenylmethyl)-6-[[4-(2-pyridinyl)phenyl]methyl]-2,5,6,10,13-pentaazatetradecanedioate
  • Atazanavir USP/EP/BP
  • Atazanavir (10mM in DMSO)
  • Atazanavir iMpurity
  • Atv
  • 198904-31-3
  • Atazanavir API
  • 198904-31-3
  • C38H52N6O7
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