Androgen Receptor Antagonists Structure-Activity Relationships

February 2000 in “ Current Medicinal Chemistry ”

Shankar Singh, Sylvain Gauthier, Fernand Labrie

androgen receptor antagonists antiandrogens androgenic alopecia flutamide non-steroidal antiandrogens hirsutism seborrhea acne hair loss androgen receptor blockers antiandrogens male pattern baldness flutamide non-steroidal antiandrogens excessive hair growth oily skin acne hair loss

TLDR Antiandrogens like flutamide are effective in treating conditions like prostate cancer and hair loss, but there's a need for more potent versions. Understanding their structure can help develop better treatments.

The 23-year-old study "Androgen Receptor Antagonists (Antiandrogens) Structure-Activity Relationships" explored the role and effectiveness of antiandrogens in treating conditions like prostate cancer, acne, seborrhea, hirsutism, and androgenic alopecia. The study found that non-steroidal antiandrogens, such as flutamide and its derivatives, displayed pure antiandrogenic activity and were highly effective in treating prostate cancer. However, all antiandrogens developed at that time showed only moderate affinity for the androgen receptor, suggesting a need for more potent antiandrogens. The study also found that certain structural features were associated with high affinity and high activity. For example, flutamide caused an 80% decrease in hirsutism, acne, seborrhea, and hair loss scores. The study concluded that understanding the structure-activity relationships of antiandrogens could aid in the development of more effective treatments for conditions such as hair loss and acne.

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research Androgen Receptor Antagonists Structure-Activity Relationships

204 citations, February 2000 in “Current Medicinal Chemistry”

Antiandrogens like flutamide are effective in treating conditions like prostate cancer and hair loss, but there's a need for more potent versions. Understanding their structure can help develop better treatments.

research Combination of an Antiandrogen and a 5α-Reductase Inhibitor: A Further Step Towards Total Androgen Blockade?

9 citations, March 1991 in “Endocrinology”

Using two drugs together, Flutamide and 4-MA, is more effective for blocking male hormones than using each one alone.