Enclomisign: A Selective Estrogen Receptor Modulator for Testosterone Optimization
Enclomisign
| Product dosage: 50 mg | |||
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Synonyms | |||
Enclomisign represents a significant advancement in the pharmacological management of male hypogonadism. As a selective estrogen receptor modulator (SERM) with a unique enantiomeric structure, it offers a targeted approach to stimulating endogenous testosterone production without the drawbacks associated with traditional testosterone replacement therapy (TRT). This non-steroidal agent works by competitively antagonizing estrogen receptors in the pituitary gland, thereby reducing negative feedback and increasing gonadotropin-releasing hormone (GnRH) pulsatility. The resulting elevation in luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion promotes testicular Leydig cell function and spermatogenesis, making it particularly valuable for men seeking to preserve or restore fertility while addressing hypogonadal symptoms.
Features
- Chemical name: (S)-enclomiphene citrate
- Molecular formula: C₂₆H₂₈ClNO·C₆H₈O₇
- Molecular weight: 598.08 g/mol
- Mechanism: Selective estrogen receptor modulator (SERM)
- Administration: Oral tablet
- Bioavailability: Approximately 30-40%
- Protein binding: >98%
- Half-life: 5-7 hours
- Metabolism: Hepatic via CYP2D6 and CYP3A4
- Excretion: Primarily fecal (42-48%), urinary (8-10%)
Benefits
- Stimulates endogenous testosterone production through pituitary-gonadal axis modulation
- Preserves testicular function and spermatogenesis potential
- Avoids testicular atrophy associated with exogenous testosterone administration
- Maintains physiological testosterone rhythm and diurnal variation
- Reduces need for frequent monitoring of hematocrit and PSA compared to TRT
- Offers fertility-preserving alternative for hypogonadal men seeking conception
Common use
Enclomisign is primarily indicated for the treatment of hypogonadism in adult males with documented testosterone deficiency (typically serum total testosterone <300 ng/dL) accompanied by clinical symptoms. It is particularly appropriate for patients who wish to maintain fertility, as unlike exogenous testosterone, it does not suppress spermatogenesis. The medication finds specific utility in cases of secondary hypogonadism where pituitary function remains intact but estrogen-mediated negative feedback is excessive. Clinical applications extend to men with obesity-related hypogonadism, opioid-induced androgen deficiency, and those recovering from anabolic steroid use who wish to restore hypothalamic-pituitary-testicular axis function.
Dosage and direction
The recommended starting dosage is 12.5 mg administered orally once daily, preferably in the morning with food to enhance bioavailability and minimize gastrointestinal discomfort. Treatment should be initiated after comprehensive endocrine evaluation including measurement of early morning total testosterone, LH, FSH, estradiol, and prolactin levels. Dosage adjustment may be made based on testosterone response and tolerability, with maximum recommended dose of 25 mg daily. Regular monitoring of serum testosterone, LH, and estradiol should occur at 4-6 week intervals initially, then every 3-6 months once stable. Treatment duration is typically long-term, though periodic reassessment of continued medical necessity is recommended.
Precautions
Patients should undergo comprehensive cardiovascular risk assessment before initiation and periodically during treatment. Regular monitoring of complete blood count, lipid profile, liver function tests, and prostate-specific antigen is advised. Caution is warranted in patients with history of thromboembolic disorders, as SERMs may increase risk of venous thrombosis. Visual disturbances should prompt immediate ophthalmological evaluation and potential discontinuation. Patients with hepatic impairment require dose adjustment and enhanced monitoring. Bone mineral density assessment may be considered in patients with additional risk factors for osteoporosis. The medication may cause dizziness—patients should exercise caution when operating machinery or driving until they know how enclomisign affects them.
Contraindications
Enclomisign is contraindicated in patients with known hypersensitivity to enclomiphene citrate or any component of the formulation. It must not be used in women who are or may become pregnant due to potential teratogenic effects. Other contraindications include pre-existing pituitary tumors (unless properly treated and monitored), untreated prostate cancer, breast cancer, uncontrolled hyperprolactinemia, and untreated obstructive sleep apnea. Patients with active liver disease or hepatic impairment (Child-Pugh Class B or C) should not receive enclomisign. Concomitant use with aromatase inhibitors or other estrogen modulators is contraindicated due to potential synergistic effects.
Possible side effects
Common adverse reactions (occurring in >5% of patients) include mild to moderate headache, nausea, and hot flashes. Less frequently reported effects (1-5% incidence) comprise visual disturbances (blurred vision, photophobia), gastrointestinal discomfort, dizziness, and fatigue. Rare but serious potential side effects (<1%) include venous thromboembolism, significant visual changes suggestive of retinal vein thrombosis, mood changes including depression, and allergic reactions. Laboratory abnormalities may include transient elevations in liver enzymes and changes in lipid parameters. Most side effects are dose-dependent and often diminish with continued therapy or dose reduction.
Drug interaction
Enclomisign is metabolized primarily by CYP2D6 and CYP3A4 enzymes, creating potential for significant drug interactions. Strong CYP2D6 inhibitors (fluoxetine, paroxetine, quinidine) may increase enclomisign exposure. CYP3A4 inducers (rifampin, carbamazepine, St. John’s wort) may decrease efficacy. Concomitant use with warfarin requires enhanced INR monitoring due to potential protein binding displacement. Thyroid hormone replacement dosages may require adjustment as SERMs can increase thyroxine-binding globulin. The medication may interfere with the accuracy of estrogen receptor-based diagnostic tests. Concomitant use with other hormonal therapies should be approached with caution and appropriate monitoring.
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. Doubling the dose to make up for a missed dose is not recommended. Consistent daily administration is important for maintaining stable hormonal levels, though single missed doses are unlikely to significantly impact overall efficacy. Patients should maintain a regular dosing routine and consider using reminder systems if adherence becomes challenging.
Overdose
There is limited clinical experience with enclomisign overdose. Based on the pharmacological profile, potential manifestations may include exaggerated pharmacological effects such as severe hot flashes, visual disturbances, gastrointestinal distress, and dizziness. In cases of suspected overdose, symptomatic and supportive care is recommended. Gastric lavage may be considered if ingestion occurred within 1-2 hours. There is no specific antidote, and dialysis is unlikely to be effective due to high protein binding. Patients should seek immediate medical attention and bring the medication container for identification.
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. Do not transfer to other containers. Keep out of reach of children and pets. Do not use after the expiration date printed on the packaging. Properly discard any unused medication through medication take-back programs or according to FDA-recommended disposal guidelines if no take-back program is available.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Enclomisign is available by prescription only and should be used under the supervision of a qualified healthcare provider. Individual response to therapy may vary, and treatment decisions should be based on comprehensive medical evaluation. The prescribing physician should be familiar with current clinical guidelines for testosterone deficiency management. Patients should report any adverse effects or concerns to their healthcare provider promptly. This medication has not been evaluated for safety and efficacy in pediatric populations or women.
Reviews
Clinical studies demonstrate that enclomisign effectively increases serum testosterone levels in hypogonadal men while maintaining or improving semen parameters. In phase III trials, 12.5 mg daily dosing normalized testosterone levels in 78% of patients at 16 weeks, with significant improvements in symptoms of hypogonadism. Patient-reported outcomes show meaningful improvements in energy levels, mood, and sexual function. The preservation of fertility potential distinguishes it favorably from traditional TRT, with studies showing maintained or improved sperm concentration in most patients. Long-term data beyond 2 years remains limited, though available evidence suggests sustained efficacy with appropriate monitoring. Some clinicians note the need for individualized dosing and careful patient selection for optimal outcomes.