Abiraterone Acetate - CAS 154229-18-2
Catalog number: B0084-461965
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
Cytochrome P450
The acetate form of abiraterone, which blocks the synthesis of androgens by inhibiting CYP17A1.
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B0084-461965 10 g $298 In stock
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Brife Description:
CYP17A1 inhibitor, metastatic, castration-resistant prostate cancer
CB7630; Zytiga; CB-7630; CB7630; Abiraterone (acetate)
the treatment of metastatic, castration-resistant prostate cancer
Canonical SMILES:
1.Value of treatment in clinical trials versus the real world: the case of abiraterone acetate (Zytiga) for postchemotherapy metastatic castration-resistant prostate cancer patients in Sweden.
Svensson J1, Andersson E1, Persson U1, Edekling T2, Ovanfors A3, Ahlgren G4. Scand J Urol. 2016 Apr 25:1-6. [Epub ahead of print]
OBJECTIVE: In a randomized clinical trial (COU-AA-301), abiraterone acetate (Zytiga®) was shown to be superior to prednisone in the treatment of metastatic castration-resistant prostate cancer (mCRPC). However, the value of abiraterone treatment for patients with mCRPC in clinical practice in Sweden is not known. The aim of this study was to compare the outcomes and treatment patterns of abiraterone treatment in a Swedish observational study to those of the pivotal clinical trial, thereby discussing the external validity of the postchemotherapy clinical trial from a Swedish perspective.
2.Development and Validation of a Novel LC-MS/MS Method for Simultaneous Determination of Abiraterone and Its Seven Metabolites in Human Serum: Innovation in Separation of Diastereoisomers Without Use of a Chiral Column.
Alyamani M1, Li Z2, Upadhyay SK3, Anderson D4, Auchus RJ3, Sharifi N5. J Steroid Biochem Mol Biol. 2016 Apr 7. pii: S0960-0760(16)30098-X. doi: 10.1016/j.jsbmb.2016.04.002. [Epub ahead of print]
Abiraterone acetate (AA), the prodrug of abiraterone, is FDA-approved for the treatment of castration-resistant prostate cancer. Abiraterone is metabolized in patients to a more potent analogue, D4A. However, we have recently reported that this analogue is further metabolized to additional metabolites in patients treated with AA. Here, we present a liquid chromatography-tandem mass spectrometry method developed to resolve and detect abiraterone and its seven metabolites in human serum using an AB Sciex Qtrap 5500 mass analyzer coupled with a Shimadzu Nexera UPLC station. Analytes and the internal standard (abiraterone-d4) were extracted from human serum using the liquid-liquid extraction procedure. The analytes were separated using a Zorbax Eclipse Plus C18 150×2.1mm, 3.5μm column at 40°C and an isocratic mobile phase 35% A (0.1% formic acid in water), 65% B (0.1% formic acid in methanol:acetonitrile; 60:40). Electrospray ionization in positive mode was applied with multiple reaction monitoring in a total run time of 13minutes.
3.The Effect of Food on the Intraluminal Behavior of Abiraterone Acetate in Man.
Geboers S1, Stappaerts J1, Mols R1, Snoeys J2, Tack J3, Annaert P1, Augustijns P4. J Pharm Sci. 2016 Apr 6. pii: S0022-3549(16)00436-6. doi: 10.1016/j.xphs.2016.03.008. [Epub ahead of print]
To relate the reported positive effect of food on the oral bioavailability of abiraterone to the intraluminal behavior of abiraterone acetate, an in vivo experiment was performed, in which duodenal fluids and plasma samples were collected from healthy volunteers after the administration of abiraterone acetate in fasted and postprandial conditions. The plasma concentration-time profiles confirmed the positive food effect. Nevertheless, intraduodenal concentrations of abiraterone acetate and abiraterone did not fully reflect this observation. This apparent discrepancy was explored by performing several in vitro experiments including solubility, dissolution, and transfer studies. Gastrointestinal transfer studies illustrated a positive impact of gastric processing of the abiraterone acetate formulation on the duodenal concentrations in the fasted state, which could not be observed in the postprandial condition. As the influence of gastric dissolution on the intraluminal concentrations in the small intestine declines aborally, it is most likely the superior solubility of abiraterone acetate and abiraterone in intestinal fluids of the fed state which dictates the food effect.
4.A phase II trial of abiraterone acetate plus prednisone in patients with triple-negative androgen receptor positive locally advanced or metastatic breast cancer (UCBG 12-1).
Bonnefoi H1, Grellety T2, Tredan O3, Saghatchian M4, Dalenc F5, Mailliez A6, L'Haridon T7, Cottu P8, Abadie-Lacourtoisie S9, You B10, Mousseau M11, Dauba J12, Del Piano F13, Desmoulins I14, Coussy F15, Madranges N2, Grenier J16, Bidard FC8, Proudhon C8, M Ann Oncol. 2016 May;27(5):812-8. doi: 10.1093/annonc/mdw067. Epub 2016 Feb 18.
BACKGROUND: Several expression array studies identified molecular apocrine breast cancer (BC) as a subtype that expresses androgen receptor (AR) but not estrogen receptor α. We carried out a multicentre single-arm phase II trial in women with AR-positive, estrogen, progesterone receptor and HER2-negative (triple-negative) metastatic or inoperable locally advanced BC to assess the efficacy and safety of abiraterone acetate (AA) plus prednisone.
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CAS 154229-18-2 Abiraterone Acetate

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