Abiraterone Acetate and Impurities
853-23-6
853-23-6
115375-60-5
115375-60-5
2174-13-2
2174-13-2
979-02-2
979-02-2
154229-18-2
Abiraterone Acetate
154229-18-2
154229-26-2
154229-26-2
154229-19-3
Abiraterone
154229-19-3
B0038-007226
B0038-007225
Anhydro abiraterone
154229-20-6
B0038-007224
B0038-007223

Background


Introduction

Abiraterone acetate inhibits androgen in testis, prostate and adrenal gland. Abiraterone acetate is a CYP17 (cytochrome P450, family 17) inhibitor that may also cause the adrenal gland to increase mineralocorticoid production. CYP17A (cytochrome P450, family 17, subfamily A) is the rate-limiting enzyme in androgen biosynthesis, not only in the testis, but also in adrenal and prostate cancer cells. Therefore, abiraterone acetate can block the synthesis of androgen in the testes, adrenal glands, and prostate, and does not cause adrenal insufficiency.

TARGET:  Cytochrome P450

Synthesis

Abiraterone Acetate

References:
1. WO9320097A1.
2. US5604213A.
3. WO2014207762A1.
4. WO2015015246A1.
5. WO2015014686A1.
6. CN104109185A.
7. CN103965282A.
8. WO2014102833A2.
9. CN103864878A.
10. CN103665084A.
11. WO2014075978A1.
12. WO2014071983A1 / WO2014071984A1.
13. WO2006021777A1 / US8389714B2.
14. WO2006021776A1 / US7700766B2.
15. WO2013123878A1 / CN103254265A.
16. CN103059090A.
17. CN102731605A.
18. CN102030798A.
19. CN103193849A.


Abiraterone Acetate

References:
1. WO9509178A1.
2. WO2014188445A1.
3. WO2014083512A1.
4. CN103665085A.
5. CN103172690A.
6. CN102816200A.
7. CN103570791A.
8. CN103864877A.
9. CN103242410A.
10. CN103804457A.
11. Chinese J. Synthetic Chem. 2013, 21, 245-247.


Abiraterone Acetate

References:
1. WO2014207567A2 / US2015005489A1.
2. WO2013053691A1 / US2014256932A1.


Abiraterone Acetate

References:
1. WO2013030410A2 / US2014011992A1.
2. CN103387597A.


Abiraterone Acetate

References:
1. WO2014016830A1.
2. WO2013159225A1.
3. CN102898495A.
4. CN103059091A.
5. CN103450313A.


Abiraterone Acetate

References:
1. CN102627681A.
2. CN102838649A.
3. CN104370991A.

Clinical Trial Information

NCT Number Phase Status Date Conditions Sponsor/Collaborators
NCT02268175 2 Active, not recruiting 2019-05-24 Prostate AdenocarcinomaProstate CancerHigh Risk Prostate Cancer Dana-Farber Cancer Institute
NCT02903368 2 Active, not recruiting 2019-05-24 Prostate Cancer Dana-Farber Cancer Institute
NCT02123758 1 Active, not recruiting 2019-05-23 Prostatic NeoplasmsMetastatic Castration-Resistant Prostate Cancer Aragon Pharmaceuticals, Inc.
NCT02924766 1 Active, not recruiting 2019-05-23 Prostatic Neoplasms Janssen Research & Development, LLC
NCT03706365 2 Recruiting 2019-05-21 Prostate Cancer Eli Lilly and Company

Literatures

Publication Date Title Journal
2014-03-01 Differential response to abiraterone acetate and di-n-butyl phthalate in an androgen-sensitive human fetal testis xenograft bioassay. Toxicological sciences: an official journal of the Society of Toxicology
2014-01-01 Changing paradigms in management of metastatic Castration Resistant Prostate Cancer (mCRPC). BMC urology
2012-08-01 Urologists and oncologists: adapting to a new treatment paradigm in castration-resistant prostate cancer (CRPC). BJU international
2012-08-01 Effect of abiraterone acetate plus prednisone on the QT interval in patients with metastatic castration-resistant prostate cancer. Cancer chemotherapy and pharmacology
2012-07-01 Abiraterone inhibits 3β-hydroxysteroid dehydrogenase: a rationale for increasing drug exposure in castration-resistant prostate cancer. Clinical cancer research : an official journal of the American Association for Cancer Research