Enclomiphene Citrate 100x12.5mg
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NOT FOR HUMAN CONSUMPTIO
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.)
| 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. |
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.
| 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 |
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.
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.
| 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 |
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 |
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.
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.
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.
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