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Enclomiphene 1g resealable white pouch – Batch No.004, dated 16-10-2025, pharmaceutical-grade packaging for research or lab use, displayed on a neutral background.
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Enclomiphene Citrate 1g

Enclomiphene Citrate 1g

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                                        NOT FOR HUMAN CONSUMPTION

Enclomiphene is the trans (E) isomer of clomiphene citrate and acts as a selective estrogen-receptor modulator (SERM). In men, it blocks estradiol’s negative feedback at the hypothalamus/pituitary, raising GnRH → LH/FSH, which in turn stimulates endogenous testosterone production by Leydig cells while maintaining spermatogenesis (via FSH/Sertoli). Unlike exogenous testosterone, enclomiphene does not suppress the HPG axis and is commonly used off-label for men with functional/secondary hypogonadism who desire fertility preservation. (Not FDA/EMA-approved as a branded drug.)

Additional Benefits of Enclomiphene Now Under Investigation

Benefit Key take-aways
1 Restores physiologic testosterone with fertility preserved In men with secondary hypogonadism, enclomiphene increases TT/FT to mid-normal while maintaining or improving sperm counts, unlike TRT which often induces azoospermia.
2 Normalizes LH/FSH pulsatility Improves pituitary responsiveness and diurnal T dynamics (morning peak), supporting libido/energy improvements without exogenous androgen peaks.
3 Metabolic profile neutrality vs TRT Generally weight-neutral with modest improvements in insulin sensitivity/lipids in some cohorts; far less erythrocytosis than TRT.
4 Symptom relief (sexual & vitality) Reported gains in sexual desire, erectile function, mood, and fatigue parallel biochemical T normalization.
5 Estradiol balance Often yields physiologic E2 via aromatization of endogenous T; avoids extreme E2 suppression seen with AIs. Aromatase inhibitor can be added if E2 becomes high.
6 Testicular volume maintenance By stimulating intratesticular T, enclomiphene helps preserve testicular size vs the shrinking frequently seen with TRT.
7 Transition off AAS/TRT Used in post-cycle or TRT cessation plans to re-start the axis (with or without hCG); evidence is mainly observational.
8 Sleep apnea/BP neutrality (relative) Less fluid retention and hematocrit rise than TRT → lower risk of OSA or BP worsening; still monitor in predisposed patients.
9 Female applications (exploratory) In women, clomiphene is established for ovulation induction; enclomiphene-specificprograms explored ovulation induction with a shorter tissue persistence vs zuclomiphene, but it is not standard of care.

2. Molecular Mechanism of Action

2.1 Receptor pharmacodynamics

  • SERM activity (ERα/ERβ): Antagonist at hypothalamus/pituitary → ↑ GnRH → ↑ LH/FSH.

  • Testis: LH → Leydig → testosterone; FSH → Sertoli → spermatogenesis.

  • Enclomiphene vs zuclomiphene: Enclomiphene has shorter half-life, less estrogenic persistence, and a cleaner antiestrogenic profile centrally.

2.2 Down-stream biology

Pathway Functional outcome Context
GnRH–LH/FSH axis up-regulation Endogenous T ↑, sperm production preserved Male hypogonadism
Aromatization of T → E2 Physiologic estradiol for bone/libido Systemic
SHBG modulation Mild ↑/↔ depending on baseline Liver

3. Pharmacokinetics

  • Route: Oral tablet (usually compounded).

  • Onset: T rises within weeks; sperm parameters respond over 2–3+ months.

  • Half-life: Shorter than zuclomiphene (days vs weeks), reducing long tail accumulation typical of clomiphene mixes.

  • Dosing used clinically (off-label): 6.25–25 mg daily (common: 12.5–25 mg QD), or 25 mg QOD, titrated to mid-normal TT/FT and symptom control.

4. Clinical Evidence (high-level)

  • Secondary hypogonadism (men): RCTs and open-label studies show TT/FT increases comparable to low-dose TRT, with LH/FSH maintained and sperm counts preserved or improved.

  • Symptoms/QoL: Improvements in sexual function and vitality correlate with biochemical response.

  • Metabolic labs: Neutral to mildly favorable effects on lipids/insulin sensitivity; far lower rates of erythrocytosisthan TRT.

  • Female fertility: Clomiphene citrate remains standard; enclomiphene monotherapy is investigational.

Evidence quality note: Solid male endocrine data for biochemical efficacy; fewer large, long-term outcome trials than for TRT. Regulatory approval attempts in the US previously received complete response letters; enclomiphene remains unapproved as a branded product.

5. Emerging Clinical Interests

Field Rationale Status
Functional hypogonadism (obesity, opioids, OSA treated) Restore axis while preserving fertility Real-world/off-label
Adjunct with hCG hCG for intratesticular T + enclomiphene for pituitary tone Practice-based
Post-TRT/AAS recovery Re-engage axis with SERM ± hCG Observational
Male infertility with low-normal T Improve T and spermatogenesis before ART Ongoing practice research

6. Safety and Tolerability

  • Common: Headache, hot flashes, mood lability/irritability, GI upset, transient visual disturbances (rare; caution with night driving).

  • Endocrine: Possible E2 increase → breast tenderness/gynecomastia in sensitive men; consider dose adjustment or low-dose AI if symptomatic.

  • Hematologic: Erythrocytosis uncommon vs TRT, but check CBC.

  • Thromboembolic risk: SERMs carry a theoretical VTE risk (low in men but screen for history/family risk).

  • Hepatic: Rare transaminase elevations—obtain baseline and periodic LFTs.

  • Psych: Anxiety/irritability in a minority—monitor.

  • Ocular: Very rare optic events have been described with clomiphene-class SERMs—stop if visual symptomsoccur.

  • Contraindications: Active liver disease, prior VTE, uncontrolled polycythemia, hypersensitivity to SERM class.

  • Pregnancy: Contraindicated (SERM class).

  • Anti-doping: SERMs are prohibited by WADA (S4).

Comparative safety/efficacy matrix

Feature Enclomiphene Clomiphene citrate (mix) TRT (exogenous T) hCG
Axis effect Stimulates LH/FSH Stimulates (isomer mix; longer tail) SuppressesLH/FSH Stimulates Leydig (LH-mimic)
Fertility Preserved Preserved Often suppressed Preserved; supports spermatogenesis (±FSH)
Erythrocytosis Low Low–mod Higher Low
Gynecomastia risk E2-related (dose-dependent) Similar Aromatization of exogenous T Aromatization from ↑T
Visual/neurologic AEs Rare SERM-class Slightly more (zuclo tail) Uncommon Uncommon
Regulatory status Unapproved; off-label via compounding Approved (female), off-label (male) Approved Approved

7. Regulatory Landscape

  • Not FDA/EMA-approved as a branded product for male hypogonadism (prior NDA efforts were not approved).

  • Male hypogonadism treatment guidelines typically endorse TRT for confirmed organic deficiency; SERMs (clomiphene/enclomiphene) are discussed off-label for secondary hypogonadism with fertility intent.

8. Practical Use (clinic playbook)

  • Who’s a good candidate? Men with secondary/functional hypogonadism (low morning TT/FT with low/normal LH/FSH), desiring fertility preservation, without major SERM contraindications.

  • Baseline work-up: TT/FT (2 mornings), LH/FSH, E2, SHBG, prolactin, TSH, CBC, LFTs, semen analysis if fertility relevant; assess OSA, meds (opioids), obesity.

  • Dosing: Start 12.5 mg QD (range 6.25–25 mg). Recheck labs at 4–6 weeks; titrate to mid-normal TT/FT and symptom relief.

  • Follow-up (q8–12 wks early, then q3–6 mo): TT/FT, E2, LH/FSH, CBC, LFTs, BP/weight, symptoms; semen parameters every 3–6 months if fertility is an endpoint.

  • Adjuncts: If E2 climbs with symptoms, consider dose reduction, EOD dosing, or low-dose AI; if T response is blunted, consider add-on hCG.

  • Stop/hold if: Visual symptoms, VTE signs, persistent mood instability, significant LFT rise, or absent biochemical/clinical response after adequate trial.

Selected References

  • Journal of Clinical Endocrinology & Metabolism — SERM therapy for male secondary hypogonadism; enclomiphene vs clomiphene pharmacology.

  • Fertility and Sterility; Andrology — Effects on spermatogenesis, semen parameters, and fertility outcomes.

  • Endocrine Reviews; Clinical Endocrinology — Algorithms for diagnosing functional hypogonadism and fertility-preserving strategies.

  • Urology; BJU International — Comparative data: enclomiphene vs TRT on TT/FT, LH/FSH, hematologic and metabolic outcomes.

  • Drug Testing & Analysis; WADA Code — SERM prohibition in sport.