What are the considerations for Leuprolide (Leuprolide acetate) injection?

From the Guidelines

Leuprolide injection should be considered as a luteinizing hormone-releasing hormone (LHRH) agonist for the management of metastatic hormone-sensitive prostate cancer (mHSPC), with careful consideration of dosing, administration, and monitoring. Here are the key points:

• Dosing: Typically, leuprolide is administered as a depot injection every 1,3,4, or 6 months, depending on the formulation, with common doses ranging from 3.75 mg to 45 mg 1.
• Administration: It should be given intramuscularly or subcutaneously, depending on the specific product, and injection sites should be rotated to minimize local reactions.
• Timing: For prostate cancer, the first dose is often given with an antiandrogen (e.g., bicalutamide 50 mg daily for 2 weeks) to prevent tumor flare, as recommended by the AUA/ASTRO/SUO guideline 1.
• Monitoring: Regular PSA tests and testosterone levels should be performed to assess treatment efficacy in prostate cancer patients, with baseline PSA and serial PSAs at three- to six-month intervals after initiation of ADT 1.
• Side effects: Patients should be informed about potential side effects, including hot flashes, sexual dysfunction, and bone loss, and consider calcium and vitamin D supplementation.
• Duration: Treatment duration depends on the indication, with long-term treatment often necessary for prostate cancer.
• Contraception: Women of childbearing potential should use non-hormonal contraception during treatment and for some time after discontinuation. Leuprolide works by suppressing the production of sex hormones, which is why it's effective in hormone-sensitive conditions but also causes systemic effects, and clinicians should offer ADT with either LHRH agonists or antagonists or surgical castration in patients with mHSPC 1.

From the FDA Drug Label

Leuprolide acetate injection is indicated in the palliative treatment of advanced prostatic cancer. The considerations for Leuprolide (Leuprolide acetate) injection are for the palliative treatment of advanced prostatic cancer 2.

• The main consideration is the use of Leuprolide acetate injection for advanced prostatic cancer.
• No other considerations are directly mentioned in the provided drug labels.

From the Research

Considerations for Leuprolide (Leuprolide acetate) Injection

• Leuprolide acetate is a gonadotrophin-releasing hormone (GnRH) analogue used to treat sex hormone-related disorders, including advanced prostatic cancer, endometriosis, and precocious puberty 3
• The choice between leuprolide and orchiectomy may be made on the basis of the patient's treatment preference, along with specific patient characteristics and cost implications 3
• Leuprolide causes pituitary desensitisation and/or down-regulation, leading to suppressed circulating levels of gonadotrophins and sex hormones 3
• Monthly intramuscular or subcutaneous administration of depot leuprorelin 3.75 mg was superior to placebo, and comparable to oral danazol 800 mg/day or intranasal buserelin 900 micrograms/day, in achieving objective and subjective responses in women with endometriosis 3
• The recommended duration of leuprolide use in women with endometriosis is limited to 6 months because it reduces bone mineral density 3

Administration and Efficacy

• A 30-mg depot formulation of leuprolide, injected intramuscularly every 16 weeks, is effective in lowering serum testosterone to castrate levels in all patients and demonstrates a favorable response in 80% of patients with advanced prostate cancer 4
• The most common adverse events associated with leuprolide acetate depot injection are hot flashes, back pain, and arthralgia 4
• Leuprolide acetate has principal clinical applications for prostate cancer, and its use has become a concrete clinical reality thanks to recent advances in biotechnology 5

Patient Considerations

• Hormone therapy, including leuprolide acetate, is well established for treating patients with prostate cancer and remains the mainstay of the treatment of metastatic and locally advanced disease 6
• The depot formula of leuprolide has gained wide acceptance from both patients and physicians, and the 6-month formula has the potential to become a standard of care for patients eligible for androgen deprivation therapy 6
• Anaphylactic reactions to leuprolide acetate depots have been described as exceedingly rare, but can occur, as reported in a case of a 66-year-old man with clinically localized prostate cancer who experienced anaphylaxis immediately after his first injection of a leuprolide acetate depot 7