Abiraterone acetate
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| - | <StructureSection load='' size='340' side='right' caption=' | + | <StructureSection load='' size='340' side='right' caption='Abiraterone acetate' scene='97/978895/Cv/1'> |
Abiraterone acetate, sold under the brand name Zytiga among others, is a medication used to treat prostate cancer.<ref name="a9">[https://www.drugs.com/monograph/abiraterone.html|"Abiraterone Acetate Monograph for Professionals"]. Drugs.com. Archived from the original on 6 May 2012. Retrieved 15 November 2019.</ref> Specifically it is used together with a [[corticosteroid]] for metastatic castration-resistant prostate cancer (mCRPC) and metastatic high-risk castration-sensitive prostate cancer (mCSPC).<ref name="a2">[https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=4e338e89-3cf2-48eb-b6e2-a06c608c6513|"Zytiga- abiraterone acetate tablet, film coated"]. DailyMed. 13 June 2019. Archived from the original on 13 November 2014. Retrieved 15 November 2019.</ref><ref name="a3">[https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=b8967e10-f768-47ce-ac9e-2324c8390132|"Yonsa- abiraterone acetate tablet"]. DailyMed. 5 June 2018. Archived from the original on 13 August 2020. Retrieved 15 November 2019.</ref> See also [https://en.wikipedia.org/wiki/Abiraterone_acetate| Abiraterone acetate]. | Abiraterone acetate, sold under the brand name Zytiga among others, is a medication used to treat prostate cancer.<ref name="a9">[https://www.drugs.com/monograph/abiraterone.html|"Abiraterone Acetate Monograph for Professionals"]. Drugs.com. Archived from the original on 6 May 2012. Retrieved 15 November 2019.</ref> Specifically it is used together with a [[corticosteroid]] for metastatic castration-resistant prostate cancer (mCRPC) and metastatic high-risk castration-sensitive prostate cancer (mCSPC).<ref name="a2">[https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=4e338e89-3cf2-48eb-b6e2-a06c608c6513|"Zytiga- abiraterone acetate tablet, film coated"]. DailyMed. 13 June 2019. Archived from the original on 13 November 2014. Retrieved 15 November 2019.</ref><ref name="a3">[https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=b8967e10-f768-47ce-ac9e-2324c8390132|"Yonsa- abiraterone acetate tablet"]. DailyMed. 5 June 2018. Archived from the original on 13 August 2020. Retrieved 15 November 2019.</ref> See also [https://en.wikipedia.org/wiki/Abiraterone_acetate| Abiraterone acetate]. | ||
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<scene name='97/978895/Binding_site/1'>Abiraterone binding site</scene>. Water molecules are shown as red spheres. | <scene name='97/978895/Binding_site/1'>Abiraterone binding site</scene>. Water molecules are shown as red spheres. | ||
| - | CYP17A1 catalyzes two sequential reactions: (a) the conversion of <scene name='97/978895/Pregnenolone/1'>pregnenolone</scene> and <scene name='89/895670/Cv/7'>progesterone</scene> (see also [[progesterone]]) to their 17α-hydroxy derivatives by its 17α-hydroxylase activity, and (b) the subsequent formation of <scene name='97/978895/Dehydroepiandrosterone/1'>dehydroepiandrosterone</scene> (DHEA) and androstenedione, respectively, by its 17,20-lyase activity.<ref name="a25">PMID:16287438</ref> DHEA and androstenedione are androgens and precursors of testosterone. Inhibition of CYP17A1 activity by abiraterone acetate thus decreases circulating levels of androgens such as DHEA, testosterone, and dihydrotestosterone (DHT). Abiraterone acetate, via abiraterone, has the capacity to lower circulating testosterone levels to less than 1 ng/dL (''i.e.'', undetectable) when added to castration.<ref name="a23">Neidle S (30 September 2013). Cancer Drug Design and Discovery. Academic Press. pp. 341–342. ISBN 978-0-12-397228-6.</ref><ref name="a26">PMID:25311216</ref> | + | CYP17A1 catalyzes two sequential reactions: (a) the conversion of <scene name='97/978895/Pregnenolone/1'>pregnenolone</scene> and <scene name='89/895670/Cv/7'>progesterone</scene> (see also [[progesterone]]) to their 17α-hydroxy derivatives by its 17α-hydroxylase activity, and (b) the subsequent formation of <scene name='97/978895/Dehydroepiandrosterone/1'>dehydroepiandrosterone</scene> (DHEA) and <scene name='97/978895/Androstenedione/1'>androstenedione</scene>, respectively, by its 17,20-lyase activity.<ref name="a25">PMID:16287438</ref> DHEA and androstenedione are androgens and precursors of testosterone. Inhibition of CYP17A1 activity by abiraterone acetate thus decreases circulating levels of androgens such as DHEA, testosterone, and dihydrotestosterone (DHT). Abiraterone acetate, via abiraterone, has the capacity to lower circulating testosterone levels to less than 1 ng/dL (''i.e.'', undetectable) when added to castration.<ref name="a23">Neidle S (30 September 2013). Cancer Drug Design and Discovery. Academic Press. pp. 341–342. ISBN 978-0-12-397228-6.</ref><ref name="a26">PMID:25311216</ref> |
</StructureSection> | </StructureSection> | ||
== References == | == References == | ||
<references/> | <references/> | ||
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References
- ↑ "Abiraterone Acetate Monograph for Professionals". Drugs.com. Archived from the original on 6 May 2012. Retrieved 15 November 2019.
- ↑ "Zytiga- abiraterone acetate tablet, film coated". DailyMed. 13 June 2019. Archived from the original on 13 November 2014. Retrieved 15 November 2019.
- ↑ "Yonsa- abiraterone acetate tablet". DailyMed. 5 June 2018. Archived from the original on 13 August 2020. Retrieved 15 November 2019.
- ↑ 4.0 4.1 Neidle S (30 September 2013). Cancer Drug Design and Discovery. Academic Press. pp. 341–342. ISBN 978-0-12-397228-6.
- ↑ Fernández-Cancio M, Camats N, Flück CE, Zalewski A, Dick B, Frey BM, Monné R, Torán N, Audí L, Pandey AV. Mechanism of the Dual Activities of Human CYP17A1 and Binding to Anti-Prostate Cancer Drug Abiraterone Revealed by a Novel V366M Mutation Causing 17,20 Lyase Deficiency. Pharmaceuticals (Basel). 2018 Apr 29;11(2):37. PMID:29710837 doi:10.3390/ph11020037
- ↑ Attard G, Belldegrun AS, de Bono JS. Selective blockade of androgenic steroid synthesis by novel lyase inhibitors as a therapeutic strategy for treating metastatic prostate cancer. BJU Int. 2005 Dec;96(9):1241-6. PMID:16287438 doi:10.1111/j.1464-410X.2005.05821.x
- ↑ Small EJ. Can targeting the androgen receptor in localized prostate cancer provide insights into why men with metastatic castration-resistant prostate cancer die? J Clin Oncol. 2014 Nov 20;32(33):3689-91. PMID:25311216 doi:10.1200/JCO.2014.57.8534
