Enclomisign is a novel, non-steroidal selective estrogen receptor modulator (SERM) developed for the treatment of male hypogonadism. Unlike traditional testosterone replacement therapies, which suppress endogenous hormone production, enclomisign works by blocking estrogen receptors in the hypothalamus and pituitary. This action stimulates the release of gonadotropin-releasing hormone (GnRH), leading to increased luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion. The result is a physiological elevation of endogenous testosterone production while preserving or restoring testicular function and spermatogenesis. This mechanism offers a targeted approach to addressing hypogonadism without the drawbacks of exogenous testosterone administration.

Features

• Active pharmaceutical ingredient: Enclomisign citrate
• Pharmacological class: Selective estrogen receptor modulator (SERM)
• Administration: Oral tablet formulation
• Mechanism: Antagonizes estrogen receptors in the pituitary and hypothalamus
• Bioavailability: Optimized for consistent absorption
• Half-life: Approximately 10–14 hours
• Metabolism: Hepatic, primarily via CYP3A4
• Excretion: Renal and fecal

Benefits

• Stimulates endogenous testosterone production through physiological pathways
• Maintains or improves testicular volume and spermatogenesis
• Avoids suppression of the hypothalamic-pituitary-gonadal (HPG) axis
• Does not require frequent injections or transdermal applications
• May preserve fertility in hypogonadal men seeking to conceive
• Provides a treatment alternative for patients contraindicated for testosterone therapy

Common use

Enclomisign is indicated for the treatment of adult males with hypogonadism characterized by low serum testosterone levels and associated symptoms such as fatigue, decreased libido, erectile dysfunction, and reduced muscle mass. It is particularly suitable for patients who wish to preserve fertility or who have contraindications to traditional testosterone replacement therapy. The medication is used in cases where hypogonadism is not due to structural hypothalamic, pituitary, or testicular disease. Clinical use should always follow thorough diagnostic evaluation including measurement of early morning total testosterone, LH, and FSH levels.

Dosage and direction

The recommended starting dose of enclomisign is 12.5 mg administered orally once daily, preferably in the morning. Dosage may be adjusted based on therapeutic response and serum testosterone levels, with a maximum recommended dose of 25 mg daily. Administration should occur with or without food, though consistency in timing is recommended. Treatment response should be evaluated through clinical assessment and laboratory testing at 4–6 weeks after initiation and periodically thereafter. Dose adjustments should be made under medical supervision based on testosterone levels and symptom improvement.

Precautions

Patients should undergo comprehensive baseline evaluation including prostate-specific antigen (PSA), hematocrit, and lipid profile before initiation and during treatment. Regular monitoring of testosterone, LH, and FSH levels is essential to assess therapeutic response. Use with caution in patients with history of thromboembolic disorders or cardiovascular disease. Patients should report any visual changes promptly as SERMs have been associated with ocular toxicity. Those with hepatic impairment may require dose adjustment or more frequent monitoring. The medication should be used as part of a comprehensive approach to hypogonadism management that includes lifestyle modifications.

Contraindications

Enclomisign is contraindicated in patients with known hypersensitivity to the active substance or any excipients in the formulation. It should not be used in women, particularly those who are pregnant or breastfeeding, due to potential fetal harm. Contraindications include patients with active deep vein thrombosis, pulmonary embolism, or history of these conditions. Those with untreated prolactin-secreting pituitary adenomas or other pituitary disorders should not receive enclomisign. The medication is not indicated for use in pediatric patients or those with primary testicular failure.

Possible side effects

Common adverse reactions (≥2%) may include hot flashes, headache, nausea, and increased sweating. Less frequently reported effects include visual disturbances, gastrointestinal discomfort, and mild elevation of liver enzymes. Rare but serious potential side effects include thromboembolic events, significant visual changes, and allergic reactions. Some patients may experience temporary worsening of symptoms during the initial treatment period as hormonal axis readjustment occurs. Most side effects are mild to moderate in severity and often diminish with continued therapy.

Drug interactions

Enclomisign is primarily metabolized by CYP3A4 and may interact with strong inhibitors of this enzyme (e.g., ketoconazole, clarithromycin) leading to increased enclomisign exposure. Inducers of CYP3A4 (e.g., rifampin, carbamazepine) may decrease enclomisign concentrations. Concurrent use with other SERMs is not recommended. The medication may affect the efficacy of hormonal contraceptives. Caution is advised when administering with drugs that affect coagulation parameters. Healthcare providers should review all concomitant medications, including over-the-counter products and herbal supplements.

Missed dose

If a dose is missed, it should be taken as soon as remembered unless it is nearly time for the next scheduled dose. In that case, the missed dose should be skipped and the regular dosing schedule resumed. Patients should not double the dose to make up for a missed administration. Consistent daily dosing is important for maintaining stable hormonal levels, so patients should strive for adherence to the prescribed regimen. If multiple doses are missed, patients should consult their healthcare provider before resuming therapy.

Overdose

There is limited experience with enclomisign overdose. In case of suspected overdose, symptomatic and supportive care is recommended. Based on the drug’s mechanism, potential effects may include exaggerated pharmacological responses such as significantly elevated testosterone levels. Medical attention should be sought immediately for any suspected overdose. Management may include monitoring of vital signs, symptomatic treatment, and appropriate laboratory testing. There is no specific antidote for enclomisign overdose.

Storage

Store at controlled room temperature between 20°C to 25°C (68°F to 77°F) with excursions permitted between 15°C to 30°C (59°F to 86°F). Keep in the original container with the lid tightly closed to protect from moisture and light. Keep out of reach of children and pets. Do not use if the packaging is damaged or shows signs of tampering. Properly discard any unused medication after the expiration date or when treatment is discontinued.

Disclaimer

This information is provided for educational purposes only and does not constitute medical advice. Enclomisign is a prescription medication that should be used only under the supervision of a qualified healthcare professional. Individual response to treatment may vary, and the benefits and risks should be carefully considered for each patient. Healthcare providers should reference the full prescribing information before initiating therapy. Patients should not adjust their dosage or discontinue treatment without consulting their physician.

Reviews

Clinical studies have demonstrated that enclomisign effectively increases serum testosterone levels to within normal physiological range in approximately 80% of treated hypogonadal men. In comparative trials, enclomisign showed non-inferiority to transdermal testosterone in improving hypogonadal symptoms while maintaining sperm concentration. Patients reported improvements in energy levels, sexual function, and mood scores. Treatment was generally well-tolerated with a favorable safety profile. Long-term data continue to be collected to further establish the durability of response and safety profile. Healthcare providers have noted the particular value of enclomisign for patients concerned about fertility preservation.