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Prevents mast cells from degranulating — stopping the release of histamine, leukotrienes, and other inflammatory mediators before they trigger symptoms.
Blocks histamine H1 receptors directly at target tissues — a second line of action that manages symptoms even when some mediator release occurs.
Important: Mesterolone (Proviron) is not currently available through Compounding Finder. Very few U.S. compounding pharmacies can source mesterolone API, and it is not FDA-approved in the United States. Quote requests for Mesterolone cannot be fulfilled at this time.
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Mesterolone is a DHT-derived oral androgen that binds strongly to SHBG (sex hormone-binding globulin), freeing up circulating testosterone. It does not aromatize to estrogen and has no estrogenic or progestogenic activity, making it useful for androgen replacement without estrogen-related side effects.
⚠️ Mesterolone (Proviron) is not currently available through U.S. compounding pharmacies. While not explicitly restricted by the FDA for compounding, the active pharmaceutical ingredient is extremely difficult to source from FDA-registered suppliers in the United States. Compounding Finder is unable to process quote requests for this medication at this time.
Mesterolone is a synthetic DHT (dihydrotestosterone) derivative marketed as Proviron by Bayer in countries outside the United States. It has been used since the 1960s primarily for male hypogonadism, infertility, and libido support.
Unlike testosterone, mesterolone does not convert to estrogen via aromatase, making it attractive for patients who experience gynecomastia or fluid retention on testosterone therapy. It also has one of the highest binding affinities for SHBG of any androgen, which can increase free testosterone levels when used alongside TRT.
However, Proviron has never been FDA-approved in the United States, and the raw mesterolone API is extremely difficult to source domestically from FDA-registered suppliers — making compounding functionally unavailable in most cases.
DHT-Derivative Activity
Mesterolone is already 5-alpha reduced, so it does not undergo further conversion by 5-alpha reductase. It acts directly on androgen receptors with moderate androgenic activity.
SHBG Binding
Mesterolone has exceptionally high affinity for SHBG — displacing bound testosterone and increasing free testosterone availability. This is one of its primary clinical advantages when used alongside TRT.
No Aromatization
Because mesterolone cannot be converted to estrogen by aromatase, it produces no estrogenic side effects such as gynecomastia, water retention, or mood changes associated with estrogen elevation.
Male Hypogonadism: Androgen deficiency where DHT-based therapy is preferred over testosterone
Male Infertility: Oligozoospermia — may improve sperm count and quality
Libido Support: Potency disturbances due to androgen deficiency
Adjunct to TRT: Used alongside testosterone to reduce SHBG and increase free testosterone
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⚠️ Dosing should be determined by your prescriber. The information below is general guidance only.
Androgen replacement: 25–50mg 2–3 times daily
Infertility: 25mg 2–3 times daily for several months
Maintenance: 25mg 1–2 times daily once improvement is achieved
Common:
Serious (rare):
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Prevents mast cells from degranulating — stopping the release of histamine, leukotrienes, and other inflammatory mediators before they trigger symptoms.
