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Androgens: Their Roles In Males

Endogenous Androgen Receptor Agonists
• Biosynthesis

Endogenous Androgen Receptor Agonists
Pharmacodynamics & binding

Androgen Receptor Agonists
SAR

Androgen Receptor Agonists
SAR (cont.)

Androgen Receptor Agonists
SAR (cont.)

Androgen Receptor Agonists
SAR (cont.)

Androgen Receptor Agonists
SAR (cont.)

Androgen Receptor Agonists
SAR (cont.)

Androgen Receptor Agonists
SAR (cont.)
Ring D: 17-OH

Androgen Receptor Agonists
SAR (cont.)
Ring D (cont.)

Androgen Receptor Agonists
SAR (cont.)
• Ring D (cont.)

Androgen Receptor Agonists
SAR (cont.)
• Rings A, B, & C

Androgen Receptor Agonists
SAR (cont.)
• Clascoterone- A PREGNANE

Endogenous Androgen Receptor Agonists
Metabolic transformations
• Testosterone

Androgen Receptor Steroidal anti-androgens

Androgen Receptor Antagonists
Non-steroidal anti-androgens

Androgen Receptor Antagonists
Non-steroidal anti-androgens
Bicalutamide (Casodex®)

Androgen Receptor Antagonists
Non-steroidal anti-androgens
Flutamide

Androgen Receptor Antagonists
Non-steroidal anti-androgens
Nilutamide (Nilandron®)

Androgen Receptor Antagonists
Non-steroidal anti-androgens
Apalutamide (Erleda® Feb., 2018)

Androgen Receptor Antagonists
Non-steroidal anti-androgens
Enzalutamide (Xtandi® July, 2018)

Androgen Receptor Non-steroidal anti-androgens antagonists (Newest addition…)
• Darolutamide (Nubega®)

5a-Reductase Inhibitors

5a-Reductase Inhibitors
SAR

5a-Reductase Inhibitor Mechanism

5a-Reductase Inhibitors
Finasteride (Proscar®, Propecia®)

5a-Reductase Inhibitors
Dutasteride (Avodart®)

5a-Reductase Inhibitors
Dutasteride (Avodart®)
• Metabolism

Effects/Risks of Anabolic Androgen Use/Abuse
(FYI)
