Approved & therapeutic
Clomiphene citrate
Clomid, Serophene
Clomiphene citrate is an oral selective estrogen receptor modulator, FDA-approved for ovulation induction in women. Its widespread use in men for secondary hypogonadism and for restarting the axis after androgen use is entirely off-label — there is no approved male indication and therefore no labeled male regimen.
Also known as: Clomid, Serophene, clomifene, clomiphene
- Status
- Clomiphene citrate is approved by the U.S. FDA and has official prescribing information.
- Evidence
- Approved labeling. Official prescribing information exists, based on clinical trials in people.
- Half-life
- Around 5 to 7 days for the mixture overall, but the isomers differ sharply: enclomiphene clears within days while zuclomiphene persists for weeks and accumulates on repeated dosing.
- How it's taken
- Oral tablet
- Mechanism
- Reproductive axis (GnRH / kisspeptin / oxytocin)
- Pathways
- Estrogen, Androgen, GnRH
How Clomiphene citrate works
Clomiphene blocks estrogen receptors at the hypothalamus and pituitary. Because circulating estradiol normally exerts negative feedback there, blocking that signal makes the brain read estrogen as low and increase GnRH pulse frequency, raising LH and FSH. In women that recruits a follicle and induces ovulation; in men the same LH rise stimulates testicular Leydig cells to produce testosterone endogenously — which is why it is used off-label as an alternative to exogenous testosterone that preserves fertility. Marketed clomiphene is a mixture of two isomers with different properties: enclomiphene is the antagonist responsible for the intended effect, while zuclomiphene is a longer-acting partial agonist that accumulates with repeated dosing.
What research has looked at
- FDA-approved for ovulation induction in anovulatory women who wish to become pregnant, with a long clinical record.
- In its off-label male use it raises testosterone by stimulating endogenous production, so unlike exogenous testosterone it does not suppress the axis or impair spermatogenesis — the principal reason it is chosen by men who want to preserve fertility.
- It is oral and inexpensive, with no injections and no transfer risk to household contacts.
- The same mechanism underlies its use in post-cycle protocols to restart a suppressed axis, though this application has no controlled trial support.
Evidence level: Approved labeling. Official prescribing information exists, based on clinical trials in people. These are areas studied or reported, not promised effects.
Reported side effects and risks
- There is no FDA-approved male indication. Any use in men is off-label, which means no labeled dose, no labeled duration and no labeled monitoring schedule exists for that use — the approved regimen in this entry is the female ovulation-induction one and must not be read across.
- Zuclomiphene, the partial-agonist isomer, has a half-life of days to weeks and accumulates with repeated dosing. Its estrogenic activity is thought to drive the mood changes and visual symptoms, and is the specific problem enclomiphene was developed to avoid.
- Visual disturbances — blurring, scotomata, floaters, light sensitivity — are a recognised effect and the label directs discontinuation if they occur. Cases persisting after stopping have been reported.
- Mood changes, irritability and depressive symptoms are reported and are a common reason for discontinuation in off-label male use.
- In the approved female indication: ovarian hyperstimulation, ovarian enlargement, and a substantially increased rate of multiple pregnancy.
- Hot flashes, nausea, breast tenderness and headache.
- It is on the WADA Prohibited List at all times as a hormone and metabolic modulator.
- Long-term safety data for continuous use in men — which is how it is often taken off-label — do not exist. The approved female use is short, cyclical and time-limited by design.
Sources
- FDA approved-drug listing for clomiphene citrate · U.S. Food & Drug Administration
- DailyMed prescribing information for clomiphene citrate · NIH · DailyMed
- PubMed research on clomiphene men secondary hypogonadism off-label zuclomiphene · NIH · National Library of Medicine
- DrugBank record for clomiphene · DrugBank
Track Clomiphene citrate in Peptide Vault
Log every dose, set reminders on your own schedule, rotate injection sites and keep your vials organized. Peptide Vault records what you enter. It doesn't recommend compounds or doses. iPhone, on-device.
Related compounds
Clomiphene citrate FAQ
What is Clomiphene citrate?
Clomiphene citrate is an oral selective estrogen receptor modulator, FDA-approved for ovulation induction in women. Its widespread use in men for secondary hypogonadism and for restarting the axis after androgen use is entirely off-label — there is no approved male indication and therefore no labeled male regimen.
How does Clomiphene citrate work?
Clomiphene blocks estrogen receptors at the hypothalamus and pituitary. Because circulating estradiol normally exerts negative feedback there, blocking that signal makes the brain read estrogen as low and increase GnRH pulse frequency, raising LH and FSH. In women that recruits a follicle and induces ovulation; in men the same LH rise stimulates testicular Leydig cells to produce testosterone endogenously — which is why it is used off-label as an alternative to exogenous testosterone that preserves fertility. Marketed clomiphene is a mixture of two isomers with different properties: enclomiphene is the antagonist responsible for the intended effect, while zuclomiphene is a longer-acting partial agonist that accumulates with repeated dosing.
Is Clomiphene citrate FDA approved?
Yes. Clomiphene citrate is approved by the U.S. FDA and has official prescribing information. Evidence level: approved labeling. Official prescribing information exists, based on clinical trials in people.
What is the half-life of Clomiphene citrate?
Reported half-life: Around 5 to 7 days for the mixture overall, but the isomers differ sharply: enclomiphene clears within days while zuclomiphene persists for weeks and accumulates on repeated dosing.
How is Clomiphene citrate taken?
Oral tablet.
What side effects have been reported with Clomiphene citrate?
Reported in the sources: There is no FDA-approved male indication. Any use in men is off-label, which means no labeled dose, no labeled duration and no labeled monitoring schedule exists for that use — the approved regimen in this entry is the female ovulation-induction one and must not be read across; Zuclomiphene, the partial-agonist isomer, has a half-life of days to weeks and accumulates with repeated dosing. Its estrogenic activity is thought to drive the mood changes and visual symptoms, and is the specific problem enclomiphene was developed to avoid; Visual disturbances — blurring, scotomata, floaters, light sensitivity — are a recognised effect and the label directs discontinuation if they occur. Cases persisting after stopping have been reported; Mood changes, irritability and depressive symptoms are reported and are a common reason for discontinuation in off-label male use; In the approved female indication: ovarian hyperstimulation, ovarian enlargement, and a substantially increased rate of multiple pregnancy; Hot flashes, nausea, breast tenderness and headache; It is on the WADA Prohibited List at all times as a hormone and metabolic modulator; Long-term safety data for continuous use in men — which is how it is often taken off-label — do not exist. The approved female use is short, cyclical and time-limited by design.
Educational summary compiled from the sources listed above. Not medical advice. Peptide Vault does not sell, source or recommend any compound. Talk to a qualified clinician before starting or changing anything.