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Epitestosterone: a potential new antiandrogen
The Journal of Investigative Dermatology
|August 1, 1987
Summary
Epitestosterone (EpiT) effectively acts as an antiandrogen, inhibiting testosterone and dihydrotestosterone effects on skin structures in hamsters. EpiT shows no intrinsic androgenic activity, likely acting as a receptor inhibitor and 5 alpha-reductase inhibitor.
Area of Science:
- Endocrinology
- Dermatology
- Pharmacology
Background:
- Epitestosterone (EpiT) is a testosterone (T) metabolite with known 5 alpha-reductase inhibitory properties.
- The antiandrogenic potential of EpiT has not been extensively studied in cutaneous models.
Purpose of the Study:
- To investigate the antiandrogenic effects of EpiT on androgen-dependent skin structures.
- To determine if EpiT possesses intrinsic androgenic activity.
Main Methods:
- Female Golden Syrian hamsters received subcutaneous implants of T or dihydrotestosterone (DHT) to induce androgenic stimulation.
- EpiT was co-administered at 5- and 10-fold excess doses with T or DHT.
- Measurements included pigmented spot size, sebaceous gland surface area, and hair follicle diameter.
Main Results:
- T and DHT significantly increased pigmented spot size, sebaceous gland SA, and hair follicle diameter.
- EpiT alone showed no androgenic effect.
- EpiT significantly inhibited T- and DHT-induced stimulation of all measured cutaneous structures, particularly pigment and sebaceous glands.
Conclusions:
- Epitestosterone functions as an effective antiandrogen in the hamster flank organ model.
- EpiT likely acts via competitive inhibition of the androgen receptor and 5 alpha-reductase inhibition.
- Cutaneous structures like pigment and sebaceous glands are more sensitive to EpiT's antiandrogenic effects than hair follicles.