Leuprolide acetate is an injectable medicine that lowers sex hormone levels (testosterone in men, estrogen in women) by acting on the brain's hormone control centre. It belongs to a class of medicines called GnRH agonists, used for advanced prostate cancer, endometriosis, uterine fibroids, and central precocious puberty in children. It is a prescription-only medicine, given as periodic depot injections.

• Therapeutic Class: Hormonal therapy (oncology use in men; gynecologic and pediatric endocrine use in women/children).

• Pharmacological Class: Gonadotropin-releasing hormone (GnRH) agonist.

• Drug Family: Synthetic decapeptide analogs of natural GnRH.

• ATC Classification: L02AE02 (Leuprorelin).

• Approved: Advanced prostate cancer (palliative treatment); endometriosis, including management of pain; anaemia associated with uterine fibroids (as preoperative treatment, often combined with iron therapy); and central precocious puberty (CPP) in children.

• Commonly used for: Men with advanced prostate cancer needing testosterone suppression, women with endometriosis or fibroid-related heavy bleeding, and children with early-onset puberty needing hormone suppression.

• Off-label use (only under medical guidance): Sometimes used in other hormone-dependent conditions, including certain fertility treatment protocols, under specialist guidance.

• Injection (depot suspension, intramuscular or subcutaneous, prefilled dual-chamber syringe or vial): available in multiple depot strengths for 1-month (e.g., 7.5 mg), 3-month (e.g., 22.5 mg), 4-month (e.g., 30 mg), and 6-month (e.g., 45 mg) administration, depending on the specific product and indication.

Note: The 1-month, 3-month, 4-month, and 6-month depot formulations are not interchangeable, and fractional dosing of any depot formulation should not be attempted.

Leuprolide acetate initially stimulates the pituitary gland to briefly increase hormone release (a temporary 'flare' effect), but with continued use, it desensitises the pituitary's GnRH receptors, ultimately suppressing the release of LH and FSH. This shuts down testosterone production in men or estrogen production in women, achieving a reversible, medically induced state of very low sex hormone levels.

• Standard dose (advanced prostate cancer): 7.5 mg every 4 weeks (1-month), 22.5 mg every 12 weeks (3-month), 30 mg every 16 weeks (4-month), or 45 mg every 24 weeks (6-month), depending on the specific depot formulation chosen.

• Condition-wise dose (endometriosis): 3.75 mg once monthly, or 11.25 mg every 3 months, typically for up to 6 months; sometimes combined with norethindrone acetate add-back therapy to reduce low-estrogen side effects.

• Condition-wise dose (central precocious puberty, pediatric): Dose individualised on a mg/kg basis for each child; younger children generally require relatively higher doses.

• Route: Intramuscular or subcutaneous depot injection (depending on product), administered by a healthcare professional; injection sites should be varied periodically.

• Missed dose: Rescheduled by the treating clinical team as close to the intended interval as possible; not self-timed by the patient.

• Overdose: Not well characterised in clinical trials; managed with supportive care and monitoring by the treating team.

• Common: Hot flashes, injection-site reactions, headache, and (in men) an initial testosterone 'flare' with possible temporary worsening of prostate cancer symptoms in the first weeks.

• Serious: Bone density loss (osteoporosis) with longer-term use, increased blood sugar/diabetes risk, elevated blood lipids, non-alcoholic fatty liver changes, and, rarely, interstitial lung disease. In men with prostate cancer that has spread to the spine, the initial testosterone flare can rarely cause spinal cord compression and, in severe cases, paralysis.

• Emergency symptoms: New or worsening bone pain, urinary blockage, numbness/weakness or paralysis symptoms (particularly in men with spinal metastases, especially during the first weeks), or new breathing symptoms.

• Recovery advice: The initial hormone 'flare' is expected and typically managed proactively by the treating team, especially in men with more advanced prostate cancer; hot flashes usually ease over time as the body adjusts to low hormone levels.

• Pregnancy: Contraindicated in women who are or may become pregnant; non-hormonal contraception is recommended during treatment for women of reproductive potential.

• Breastfeeding: A decision should be made to discontinue breastfeeding or discontinue the medicine, weighing the importance of treatment to the mother.

• Liver disease: Used with routine monitoring; no formal major dose adjustment established.

• Kidney disease: Used with routine monitoring; no formal major dose adjustment established.

• Elderly: Commonly used in this age group for prostate cancer, as this is the primary population studied for that indication.

• Children: Approved for central precocious puberty, with dosing carefully individualised by a pediatric endocrinologist; certain formulations (e.g., 3.75 mg 1-month, 11.25 mg 3-month) are not indicated in postmenopausal women or, per specific product labelling, in women over 65.

● Other hormone therapies: not typically combined with other GnRH agonists or antagonists.

● Norethindrone acetate (add-back therapy): specifically used together in endometriosis treatment to reduce low-estrogen side effects, rather than as an interaction to avoid.

● Medicines affecting heart rhythm (QT-prolonging drugs): used with added caution, given that hormone suppression itself can be associated with cardiovascular risk factors over time.

● Diabetes medicines: leuprolide can affect blood sugar control, so dose adjustment of diabetes medicines may be needed.

● Testosterone or estradiol levels periodically, to confirm adequate hormone suppression.

● Bone mineral density assessment with longer-term use.

● Blood glucose and HbA1c periodically, along with blood lipid monitoring.

● In children, growth, height, weight, and bone age monitored every 6 to 12 months during treatment for central precocious puberty.

Goserelin, Triptorelin (other GnRH agonists); Relugolix, Degarelix (GnRH antagonists, which avoid the initial testosterone/estrogen flare effect).

In endometriosis, often combined with norethindrone acetate add-back therapy to offset low-estrogen side effects; in prostate cancer, an anti-androgen medicine is sometimes given briefly at the start of treatment to reduce the effects of the initial testosterone flare.

● Prostate Cancer Medicines

● Endometriosis & Uterine Fibroid Treatments

● GnRH Agonists

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1. https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/019732s045,020517s043lbl.pdf

2. https://www.ncbi.nlm.nih.gov/books/NBK551662/

The information on this page is for educational purposes only and is not a substitute for medical advice. Please consult your doctor to know if this treatment is appropriate for your condition.