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Source Abiraterone acetate (154229-18-2) from LEAPChem

Nov. 2018/12/5 14:41:37 By LEAP Chem


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Basic Information of Abiraterone acetate

Chemical Name: Abiraterone acetate

Cas No.: 154229-18-2

Molecular Formula: C26H33NO2

Chemical Structure:

 154229-18-2.png

 

Abiraterone acetate, sold under the brand name Zytiga among others, is an antiandrogen medication which is used in the treatment of prostate cancer. It is specifically indicated for use in conjunction with castration and prednisone for the treatment of metastatic castration-resistant prostate cancer (mCRPC) and in the treatment of metastatic high-risk castration-sensitive prostate cancer (mCSPC). It is taken by mouth once per day on an empty stomache.

Side effects of abiraterone acetate include fatigue, arthralgia, hypertension, nausea, edema, hypokalemia, hot flashes, diarrhea, vomiting, cough, headache, glucocorticoid deficiency, mineralocorticoid excess, and hepatotoxicity among others. The drug is an androgen synthesis inhibitor – specifically, a CYP17A1 inhibitor – and thereby inhibits the production of androgens like testosterone and dihydrotestosterone in the body. In doing so, it prevents the effects of these hormones in the prostate gland and elsewhere in the body. Abiraterone acetate is a prodrug of abiraterone.

Abiraterone acetate is indicated for use in combination with prednisone, a corticosteroid, as a treatment for mCRPC (previously called hormone-resistant or hormone-refractory prostate cancer). This is a form of prostate cancer that is not responding to first-line androgen deprivation therapy or treatment with androgen receptor antagonists. Abiraterone acetate has received FDA (28 April 2011), EMA (23 September 2011), MHRA (5 September 2011) and TGA (1 March 2012) approval for this indication. In Australia it is covered by the Pharmaceutical Benefits Scheme when being used to treat castration-resistant prostate cancer and given in combination with prednisone/prednisolone (subject to the conditions that the patient is not currently receiving chemotherapy, is either resistant or intolerant of docetaxel, has a WHO performance status of <2, and his disease has not since become progressive since treatment with PBS-subsidised abiraterone acetate has commenced).

Abiraterone may be useful for prevention of the testosterone flare at the initiation of GnRH agonist therapy in men with prostate cancer.

A phase III study in subjects previously treated with docetaxel started in 2008. In September 2010, an independent panel found that the interim results in patients previously treated with docetaxel were so much better compared to those treated with placebo that it was unethical to keep half the study participants on placebo, and all patients began receiving the drug. Overall survival was increased by 3.9 months in to this study (14.8 months versus 10.9 months for placebo).

Contraindications include hypersensitivity to abiraterone acetate. Although documents state that it should not be taken by women who are or who may become pregnant, there is no medical reason that any woman should take it. Women who are pregnant should not even touch the pills unless they are wearing gloves. Other cautions include severe baseline hepatic impairment, mineralocorticoid excess, cardiovascular disease including heart failure and hypertension, uncorrected hypokalemia, and adrenocorticoid insufficiency.

 

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References:

https://en.wikipedia.org/wiki/Abiraterone_acetate

https://www.ncbi.nlm.nih.gov/pubmed/28819727

https://www.ncbi.nlm.nih.gov/pubmed/29494958

 

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