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US Approved Rx

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Primary Target

Cytochrome P450 17A1

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Approved

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Approval Year

2011

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Condition

Metastatic castration-resistant prostate cancer

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Primary

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Cancer Research UK

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Other hormone antagonists and related agents

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ABIRATERONE

G819A456D0

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Status:

US Approved Rx (2019)

First approved in 2011

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Cytochrome P450 17A1

Conditions:

Metastatic castration-resistant prostate cancer

Abiraterone acetate (trade name Zytiga) is a prodrug to the abiraterone, steroidal compound with antiandrogen activity and a 17 α-hydroxylase/C17,20-lyase (CYP17) inhibitor. It is indicated in combination with prednisone for the treatment of patients...

with metastatic castration-resistant prostate cancer. Abiraterone acetate is converted in vivo to abiraterone which inhibits CYP17, enzyme expressed in testicular, adrenal, and prostatic tumor tissues and required for androgen biosynthesis. Administration of this agent may suppress testosterone production by both the testes and the adrenals to castrate-range levels. Androgen sensitive prostatic carcinoma responds to treatment that decreases androgen levels. Androgen deprivation therapies, such as treatment with GnRH agonists or orchiectomy, decrease androgen production in the testes but do not affect androgen production by the adrenals or in the tumor.

ABIRATERONE ACETATE

EM5OCB9YJ6

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Status:

US Approved Rx (2019)

First approved in 2011

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Cytochrome P450 17A1

Conditions:

Metastatic castration-resistant prostate cancer

Abiraterone acetate (trade name Zytiga) is a prodrug to the abiraterone, steroidal compound with antiandrogen activity and a 17 α-hydroxylase/C17,20-lyase (CYP17) inhibitor. It is indicated in combination with prednisone for the treatment of patients...

with metastatic castration-resistant prostate cancer. Abiraterone acetate is converted in vivo to abiraterone which inhibits CYP17, enzyme expressed in testicular, adrenal, and prostatic tumor tissues and required for androgen biosynthesis. Administration of this agent may suppress testosterone production by both the testes and the adrenals to castrate-range levels. Androgen sensitive prostatic carcinoma responds to treatment that decreases androgen levels. Androgen deprivation therapies, such as treatment with GnRH agonists or orchiectomy, decrease androgen production in the testes but do not affect androgen production by the adrenals or in the tumor.

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