Abiraterone

Structural formula
General
Non-proprietary name	Abiraterone
other names	(3 S , 8 R , 9 S , 10 R , 13 S , 14 S ) -10,13-dimethyl-17- (pyridin-3-yl) -2,3,4,7,8,9,10, 11,12,13,14,15-dodecahydro-1 H -cyclopenta [ a ] phenanthren-3-ol ( IUPAC ) 17- (3-pyridyl) androsta-5,16-dien-3 β -ol
Molecular formula	C 24 H 31 NO
External identifiers / databases
CAS number 154229-19-3 EC number 810-941-6 ECHA InfoCard 100.241.170 PubChem 132971 DrugBank DB05812 Wikidata Q321431
Drug information
ATC code	L02 BX03
Mechanism of action	Cyp17A1 inhibitor
properties
Molar mass	349.51 g · mol -1
safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed GHS labeling of hazardous substances Caution H and P phrases H: 361fd-373 P: 201-202-260-280-308 + 313-405
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Abiraterone is a chemical compound from the group of steroids that is approved in the EU as a drug for hormone therapy and for the treatment of castration-resistant prostate cancer .

Abiraterone Acetate (Prodrug) CAS No. 154229-18-2

Abiraterone is the active form of the prodrug abiraterone acetate and has good oral bioavailability. Abiraterone acetate has been commercially available in Germany since October 2011 under the trade name Zytiga . Abiraterone was developed by Cougar Biotechnology Inc. The company was bought by Johnson & Johnson (J&J) in 2009 . In Germany, the drug is marketed by the J&J subsidiary Janssen-Cilag .

Mechanism of action

Abiraterone is a selective inhibitor of the enzyme steroid-17 α -hydroxylase (CYP17A1) which steps in the androgen ( testosterone ) - and estrogen catalyzes biosynthesis. By doing this, it lowers the production of hormones in the testicles , adrenal gland, and prostate .

Early benefit assessment

Since 2011, newly approved drugs with new active ingredients have to undergo an " early benefit assessment " by the Federal Joint Committee (G-BA) based on Section 35a SGB ​​V ( AMNOG ) if the pharmaceutical manufacturer wants to achieve a higher sales price than just the fixed amount . Only if there is an additional benefit can the pharmaceutical manufacturer negotiate a price with the umbrella association of statutory health insurance companies. The Institute for Quality and Efficiency in Health Care (IQWiG) prepares the dossier assessments on the basis of which the G-BA makes its decision .

Due to expanded indications, the active ingredient underwent several early benefit assessments with different appropriate comparator therapies: For patients with prostate cancer and progression during or after docetaxel-containing chemotherapy, abiraterone in combination with prednisone or prednisolone was compared with best supportive care . According to the G-BA, there was an indication of a considerable added benefit. For patients with prostate cancer in whom there is no indication for chemotherapy after androgen withdrawal therapy, abiraterone was compared to a wait-and-see approach while maintaining the existing conventional androgen withdrawal. According to the G-BA, there was again an indication of a considerable added benefit. For high-risk patients, a combination of abiraterone with androgen deprivation therapy was compared with conventional androgen deprivation. According to the G-BA, there was also an indication of a considerable added benefit here.

Finished medicinal products

Zytiga (D, A, CH, I, USA, CND)

literature

• JE Ang, D. Olmos, JS de Bono: CYP17 blockade by abiraterone: further evidence for frequent continued hormone-dependence in castration-resistant prostate cancer. In: British Journal of Cancer . Volume 100, No. 5, March 2009, pp. 671-675, doi: 10.1038 / sj.bjc.6604904 .
• Neeraj Agarwal, Thomas E. Hutson, Nicholas J. Vogelzang, Guru Sonpavde: Abiraterone acetate: a promising drug for the treatment of castration-resistant prostate cancer. In: Future Oncology . Volume 6, No. 5, May 2010, pp. 665-679, doi: 10.2217 / fon.10.48 .
• Charles J. Ryan, Matthew R. Smith, Lawrence Fong, Jonathan E. Rosenberg, Philip Kantoff, Florence Raynaud, Vanessa Martins, Gloria Lee, Thian Kheoh, Jennifer Kim, Arturo Molina, Eric J. Small: Phase I Clinical Trial of the CYP17 Inhibitor Abiraterone Acetate Demonstrating Clinical Activity in Patients With Castration-Resistant Prostate Cancer Who Received Prior Ketoconazole Therapy. In: Journal of Clinical Oncology . Volume 28, No. 9, 2010, pp. 1481–1488, doi: 10.1200 / JCO.2009.24.1281 .
• Daniel C. Danila, Michael J. Morris, Johann S. de Bono, Charles J. Ryan, Samuel R. Denmeade, Matthew R. Smith, Mary-Ellen Taplin, Glenn J. Bubley, Thian Kheoh, Christopher Haqq, Arturo Molina, Aseem Anand, Michael Koscuiszka, Steve M. Larson, Lawrence H. Schwartz, Martin Fleisher Howard I. Scher: Phase II Multicenter Study of Abiraterone Acetate Plus Prednisone Therapy in Patients With Docetaxel-Treated Castration-Resistant Prostate Cancer. In: Journal of Clinical Oncology. Volume 28, No. 9, 2010, pp. 1496-1501, doi: 10.1200 / JCO.2009.25.9259 .

Web links

• Zytiga ^® (Abirateron) - newly approved indication (PDF; 127 kB) Information from the Drugs Commission of the German Medical Association (AkdÄ) , as of April 15, 2013

Individual evidence

1. ↑ ^{a b} Entry on Abiraterone at TCI Europe, accessed on November 5, 2019.
2. ^ European Medicines Agency (EMA): Zytiga: EPAR - Summary for the public . Retrieved December 1, 2011.
3. ↑ "New Medicines" Zytiga (Abirateron) For the treatment of metastatic castration-resistant prostate cancer (CRPC) in adult men . (PDF; 296 kB) Drugs Commission of the German Medical Association (AkdÄ); Retrieved December 1, 2011.
4. ↑ External identifiers or database links for abiraterone acetate : CAS number: 154229-18-2, EC number: 620-314-7, ECHA InfoCard: 100.149.063 , PubChem : 9821849 , ChemSpider : 7997598 , Wikidata : Q27888393 .
5. ↑ Red List 2017 . Verlag Rote Liste Service, Frankfurt am Main, ISBN 978-3-946057-10-9 , p. 157.
6. ↑ Johnson & Johnson (JNJ) Completes Acquisition of Cougar Biotechnology. In: streetinsider.com. Retrieved July 28, 2016 . 
7. ↑ WebSite for specialist groups: Janssen-Cilag.de accessed on December 1, 2011.
8. ↑ A11-20 Abiraterone acetate - benefit assessment according to Section 35a Social Code Book V (dossier assessment). accessed on March 23, 2020.
9. ↑ Benefit assessment procedure for the active ingredient abiraterone acetate (prostate cancer, progression during or after docetaxel-containing chemotherapy, combination with prednisone or prednisolone). accessed on March 23, 2020.
10. ↑ A13-06 Abiraterone acetate (new area of ​​application) - Benefit assessment according to Section 35a SGB V (dossier assessment). accessed on March 23, 2020.
11. ↑ Benefit assessment procedure for the active ingredient abiraterone acetate (new area of ​​application: prostate carcinoma, after androgen deprivation therapy, no indication for chemotherapy). accessed on March 23, 2020.
12. ↑ A18-26 Abiraterone acetate (prostate carcinoma) - Addendum to Commission A17-64. accessed on March 23, 2020.
13. ↑ Benefit assessment procedure for the active ingredient abiraterone acetate (new area of ​​application: prostate cancer, high risk, combination with androgen deprivation therapy). accessed on March 23, 2020.

This article is about a health issue. It is not used for self-diagnosis and does not replace a diagnosis by a doctor. Please note the information on health issues !