Evidence Grade A — Regulatory approved. 2331 published studies. 384 registered clinical trials.
Medically reviewed by a licensed medical professional
Loading...
Leuprolide (sold as Lupron Depot, Eligard, and Fensolvi) is one of the most widely used hormone-suppressing medications in the world. Given as a depot injection lasting one to six months, it dramatically reduces testosterone or oestrogen levels and is prescribed across multiple medical specialities — for prostate cancer, endometriosis, uterine fibroids, central precocious puberty in children, and as part of fertility treatment.
Leuprolide is also known by these brand and alternate names:
2,331 published studies: 1714 human, 280 animal, 342 in-vitro, 203 reviews
Leuprolide is marketed as Lupron Depot, Eligard, and Fensolvi, and was first approved in 1985. It is available in depot formulations lasting one, three, four, or six months. Its clinical applications span multiple specialities: oncology (advanced prostate cancer), gynaecology (endometriosis, uterine fibroids), paediatric endocrinology (central precocious puberty), and reproductive medicine.
Leuprolide's long clinical history provides extensive safety data. The initial hormone surge in the first one to two weeks can temporarily worsen symptoms — a well-known effect called 'flare' that is managed by co-prescribing an anti-androgen in prostate cancer patients. Long-term use carries risks including bone density loss, cardiovascular effects, and metabolic changes. Despite the availability of newer GnRH antagonists that avoid the initial flare, leuprolide remains the dominant treatment in this category due to its proven track record and range of formulations.
Your brain's pituitary gland releases sex hormones in a pulsed pattern. Leuprolide mimics the natural signalling hormone (GnRH) that controls this process, but instead of pulsing, it provides a constant signal. After an initial brief surge in hormone levels lasting one to two weeks, this continuous stimulation causes the pituitary gland to shut down its hormone production entirely. The result is a dramatic and sustained drop in testosterone or oestrogen levels. This is used therapeutically in conditions that are driven or worsened by sex hormones, such as prostate cancer (testosterone-dependent) and endometriosis (oestrogen-dependent).
Leuprolide has been in clinical use since 1985 with four decades of safety data. Its long track record and wide range of depot formulations (one-month, three-month, four-month, and six-month options) make it the dominant GnRH agonist despite the availability of newer alternatives. The well-known limitation is the initial hormone flare in the first one to two weeks — testosterone or oestrogen levels rise temporarily before the suppressive effect takes hold. In prostate cancer, this flare can worsen symptoms like bone pain, requiring co-administration of an anti-androgen. GnRH antagonists (degarelix, relugolix) avoid this flare entirely, and oral relugolix in particular has emerged as a convenient alternative. Long-term hormone suppression carries risks including bone density loss, hot flashes, cardiovascular effects, and metabolic changes. Generic versions exist, though the complexity of depot formulation technology limits straightforward substitution.
PeptideTrace tracks 384 registered clinical trials for Leuprolide sourced from ClinicalTrials.gov.
Antineoplaston Therapy in Treating Patients With Stage III or Stage IV Prostate Cancer
GnRH Agonist and Antagonists in an Oocyte Donation Program
The JET Study: a Phase I Trial of Cabazitaxel, Radiotherapy and Long-term Androgen Deprivation
Impact of Formulation Change on Ovarian Suppression in Young Breast Cancer Patients.
BRE-06: Study to Increase Tolerance to Aromatase Inhibitors for Patients With Early-Stage Hormone Receptor Positive Breast Cancer Who Developed Hypoactive Sexual Desire Disorder
FDA ORIG 1
FDA SUPPL 2
FDA SUPPL 3
FDA ORIG 1
FDA SUPPL 1
FDA SUPPL 3
FDA SUPPL 7
FDA SUPPL 6
FDA SUPPL 4
FDA SUPPL 8
FDA SUPPL 5
FDA SUPPL 8
FDA SUPPL 11
FDA SUPPL 7
FDA SUPPL 10
FDA SUPPL 6
FDA SUPPL 9
FDA SUPPL 9
FDA SUPPL 10
FDA SUPPL 13
FDA SUPPL 12
FDA SUPPL 11
FDA SUPPL 14
FDA ORIG 1
FDA SUPPL 1
FDA SUPPL 12
FDA SUPPL 16
FDA SUPPL 15
FDA SUPPL 13
FDA SUPPL 17
FDA SUPPL 14
FDA SUPPL 18
FDA SUPPL 19
FDA SUPPL 15
FDA SUPPL 20
FDA SUPPL 2
FDA SUPPL 17
FDA ORIG 1
FDA SUPPL 21
FDA SUPPL 18
FDA SUPPL 1
FDA SUPPL 19
FDA SUPPL 22
FDA SUPPL 24
FDA SUPPL 20
FDA SUPPL 2
FDA SUPPL 23
FDA SUPPL 22
Health Canada Market Authorisation
FDA SUPPL 23
FDA SUPPL 26
FDA SUPPL 4
FDA SUPPL 24
FDA SUPPL 29
FDA SUPPL 27
FDA SUPPL 26
FDA SUPPL 28
FDA SUPPL 6
FDA SUPPL 15
FDA SUPPL 7
FDA SUPPL 30
FDA ORIG 1
FDA SUPPL 33
FDA SUPPL 36
FDA SUPPL 35
FDA SUPPL 31
FDA SUPPL 35
FDA SUPPL 18
FDA SUPPL 37
FDA SUPPL 19
FDA SUPPL 10
FDA SUPPL 3
FDA SUPPL 20
FDA SUPPL 5
FDA SUPPL 36
FDA SUPPL 11
FDA SUPPL 37
FDA SUPPL 38
FDA SUPPL 27
FDA SUPPL 26
FDA SUPPL 39
FDA SUPPL 40
FDA SUPPL 29
FDA SUPPL 41
FDA SUPPL 28
FDA SUPPL 30
FDA SUPPL 31
FDA SUPPL 12
FDA SUPPL 32
FDA SUPPL 14
FDA SUPPL 33
FDA SUPPL 42
FDA SUPPL 34
FDA SUPPL 17
FDA SUPPL 18
FDA SUPPL 14
FDA SUPPL 15
FDA SUPPL 42
FDA ORIG 1
FDA SUPPL 43
FDA SUPPL 39
FDA SUPPL 44
FDA SUPPL 46
FDA ORIG 1
FDA SUPPL 22
FDA SUPPL 20
FDA SUPPL 44
FDA SUPPL 47
FDA ORIG 1
FDA SUPPL 48
FDA SUPPL 45
FDA SUPPL 2
FDA SUPPL 50
EMA Marketing Authorisation
FDA ORIG 1
FDA SUPPL 3
FDA SUPPL 4
FDA SUPPL 53
FDA SUPPL 47
FDA SUPPL 48
FDA SUPPL 5
FDA SUPPL 54
FDA SUPPL 48
FDA SUPPL 51
FDA SUPPL 4
FDA SUPPL 49
FDA SUPPL 52
FDA SUPPL 6
FDA SUPPL 4
FDA ORIG 1
FDA SUPPL 7
FDA SUPPL 55
FDA SUPPL 6
FDA SUPPL 56
FDA SUPPL 7
FDA SUPPL 56
FDA SUPPL 50
FDA SUPPL 32
FDA SUPPL 11
FDA SUPPL 34
FDA SUPPL 39
FDA SUPPL 58
FDA SUPPL 9
FDA SUPPL 10
FDA SUPPL 2
FDA SUPPL 57
FDA SUPPL 11
Leuprolide is a synthetic nonapeptide (9 amino acids) GnRH agonist with D-Leu6 and N-ethyl-prolinamide9 substitutions that increase receptor affinity and resistance to enzymatic degradation relative to native GnRH. It is available in multiple long-acting depot formulations.
Continuous, non-pulsatile GnRH receptor stimulation by leuprolide causes an initial transient surge in LH, FSH, and downstream sex steroids (the 'flare' effect, lasting ~1–2 weeks), followed by GnRH receptor downregulation and desensitization. This leads to sustained suppression of the hypothalamic-pituitary-gonadal axis, reducing testosterone and estrogen to castrate/postmenopausal levels after 2–4 weeks of treatment. The effect is reversible upon discontinuation.
Leuprolide is marketed as Lupron Depot, Eligard, and Fensolvi. First approved April 9, 1985, it is available in depot formulations spanning 1-month (7.5 mg), 3-month (22.5 mg), 4-month (30 mg), and 6-month (45 mg) durations. Indications include advanced prostate cancer, endometriosis, uterine fibroids (with iron therapy), and central precocious puberty (CPP). It is the most widely prescribed GnRH agonist globally.
Carbetocin has not been approved by the FDA. It is registered in over 80 countries for prevention of uterine atony and excessive bleeding after caesarean delivery. A heat-stable formulation was added to the WHO Essential Medicines List in 2019. The CHAMPION trial (WHO, 2018; over 29,000 women) compared a heat-stable carbetocin formulation to oxytocin for preventing postpartum haemorrhage after vaginal delivery, and found it to be non-inferior. The heat-stable formulation addresses a significant limitation of oxytocin, which degrades in warm climates without refrigeration — a major concern in low-resource settings where postpartum haemorrhage causes the most deaths. Its regulatory status varies by jurisdiction.
Kisspeptin-54 has no marketing authorisation. Phase II trials conducted primarily at Imperial College London have investigated its use as an IVF oocyte maturation trigger. One trial (60 patients) reported 95% oocyte maturation with zero cases of ovarian hyperstimulation syndrome. Kisspeptin-54 has a more advanced clinical evidence base than kisspeptin-10, with multiple Phase II studies in reproductive medicine. Its potential advantage over conventional IVF triggers relates to a lower risk of the serious complication of ovarian hyperstimulation. Clinical development is ongoing in academic settings. No Phase III trials have been completed.
Goserelin is marketed as Zoladex by AstraZeneca, available as 3.6 mg monthly and 10.8 mg three-monthly subcutaneous implants. First approved in 1989, it is used in advanced prostate cancer, premenopausal breast cancer, endometriosis, and for thinning the uterine lining before surgical procedures. Goserelin achieves castrate-level testosterone suppression (below 50 ng/dL) within two to four weeks. Its unique implant delivery system means there is no liquid injection, reconstitution, or refrigeration required — a practical advantage in some clinical settings. Like all GnRH agonists, it causes an initial hormone flare before suppression takes effect. Goserelin holds an important niche in breast cancer treatment, where it is used to suppress ovarian function in premenopausal women with hormone-receptor-positive disease, often in combination with aromatase inhibitors.
Evidence Reviews
Timelines
Regulatory Status
Deep Dives
This content is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional before making decisions about your health.
