What is the Origin of CYP17 Inhibitors?

The term is derived from the enzyme's name, CYP17, which stands for Cytochrome P450 family 17, and "inhibitors," which denotes a substance that impedes a chemical reaction. The development of these inhibitors stems from advancements in molecular endocrinology and pharmacology, targeting specific steps in the steroid hormone biosynthetic cascade. This therapeutic strategy represents a precise intervention point within the complex endocrine system.

What is the Mechanism of CYP17 Inhibitors?

The CYP17 enzyme is expressed in the adrenal glands and gonads, catalyzing two sequential reactions: 17α-hydroxylation and 17,20-lyase activity. Inhibitors, such as abiraterone acetate, bind directly to the active site of the enzyme, rendering it incapable of converting pregnenolone and progesterone into their 17α-hydroxy derivatives and subsequently into dehydroepiandrosterone (DHEA) and androstenedione. This blockade significantly reduces the systemic circulation of androgens, which are potent growth factors for certain hormone-dependent cells.

CYP17 Inhibitors ∞ Area

CYP17 Inhibitors

Meaning

CYP17 inhibitors are a class of pharmaceutical agents designed to selectively block the enzymatic activity of Cytochrome P450 17α-hydroxylase/17,20-lyase, an enzyme critical in the steroidogenesis pathway. These agents prevent the conversion of progestogens into androgens, specifically inhibiting the production of testosterone and other male sex hormones. Clinically, they are employed in the management of hormone-sensitive conditions, most notably in the treatment of prostate cancer to achieve maximal androgen deprivation.

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How Do Different Androgen Suppression Methods Affect Heart Health?

Different androgen suppression methods alter heart health via distinct metabolic and hormonal pathways, impacting lipids, insulin, and vascular function.

∞ Metabolic Syndrome
∞ GnRH Agonists
∞ Androgen Suppression

HRTioAugust 23, 2025

CYP17 Inhibitors

Meaning

Origin

Mechanism

How Do Different Androgen Suppression Methods Affect Heart Health?

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