Description
Mesterolone is a unique, orally active anabolic steroid derived from dihydrotestosterone (DHT). It possesses strong androgenic properties with very low anabolic activity and is non-aromatizable. Mesterolone is primarily valued not for building muscle, but for its ability to increase free testosterone levels, enhance androgenicity, improve libido, and act as an anti-estrogen by competitively binding to the aromatase enzyme and sex hormone-binding globulin (SHBG).
Mechanism of Action
The mechanism of action for Mesterolone is multifaceted. First, it binds with high affinity to SHBG, displacing bound testosterone and increasing the percentage of active, free testosterone in the bloodstream. Second, it can compete with androgens for binding to the aromatase enzyme, thereby exerting a mild anti-estrogenic effect by reducing the conversion of other steroids to estrogen. As a pure DHT-derivative, Mesterolone itself does not aromatize. Its strong androgenic binding also directly contributes to mood, libido, and a sense of well-being, without significant anabolic tissue-building effects.
Clinical Application and Dosage
Mesterolone has clinical approval in some countries for the treatment of male hypogonadism and low libido. In performance and physique enhancement, Mesterolone is used as an ancillary compound. It is employed during cycles to harden the physique, improve mental drive and libido (especially when other compounds cause suppression), and to mitigate estrogenic side effects by lowering circulating estrogen and increasing free testosterone.
Dosage of Mesterolone is typically moderate. For its ancillary benefits, common dosages range from 25 mg to 100 mg daily, often split into two doses (e.g., 25 mg twice daily). The 25 mg tablet strength of this Mesterolone formulation allows for precise titration. It is commonly used throughout a steroid cycle or during post-cycle therapy (PCT) to support libido. It is not typically used as a standalone muscle-building agent.
Treatment Protocol and Monitoring
Mesterolone can be used for extended periods, often throughout a cycle of 8-16 weeks or during a PCT phase. Its effects on libido and sense of well-being can be noticeable within days. Monitoring is generally less intensive than with hepatotoxic orals, but should include attention to androgenic side effects and, if used long-term, potential impacts on lipid profiles. Blood work to assess free testosterone and estrogen can demonstrate its biochemical effects.
Pharmacological Profile
Mesterolone is not 17-alpha-alkylated; instead, it is 1-methylated, which allows for oral bioavailability while presenting significantly less hepatotoxicity than common alkylated orals. It has a half-life of approximately 12-15 hours, supporting twice-daily dosing. It is not aromatizable and is metabolized in the liver, but its pathway is less stressful than that of c-17 alpha alkylated compounds.
Common Side Effects
The side effects of Mesterolone are primarily androgenic, given its strong binding to the androgen receptor and lack of anabolic/estrogenic activity. The most common include:
- Androgenic Effects: Acne, oily skin, accelerated male pattern hair loss, and increased body hair growth in genetically predisposed individuals.
- Prostate Effects: Potential exacerbation of benign prostatic hyperplasia (BPH) symptoms due to its DHT nature.
- Negative Lipid Impact: Can negatively affect cholesterol ratios, suppressing HDL (“good”) cholesterol.
- Suppression: While mild, it can contribute to the suppression of the HPTA, especially at higher doses.
- Aggression: Increased irritability or aggression in some users due to its strong androgenic nature.
Mesterolone does not cause estrogenic side effects like gynecomastia or water retention. It is contraindicated in men with existing prostate cancer or severe liver impairment.
You can buy Mesterolone made by Apoxar in bulk in Canada via our website. Navigate to the “Purchase” tab and fill the contact form with details of your wholesale order. Please note: we do not sell single packs or ship directly to consumers, Apoxar is a wholesale fitness medication manufacturer and we work exclusively with our approved distributors.

