Peptide Schedule
Leuprolide (Lupron)9 residuesHWSYGLRPGEach bubble = one amino acid. Size = residue mass. Color = chemical class.Leuprolide (Lupron) Dosage Calculator
Leuprolide acetate is a synthetic nonapeptide analog of naturally occurring gonadotropin-releasing hormone (GnRH/LHRH).
1mcg · Daily
Summary: Add 0mL BAC water to your 5mg vial. Draw to < 0.1 units on a U-100 syringe for a 1mcg dose. This vial will last 0 doses.
Cycle Planner
Leuprolide (Lupron) Pharmacokinetics
Pharmacokinetics — Active Dose Over Time
t½ = ~3 hours (terminal elimination after SC/IV; depot formulations sustain release over 1-6 months)Disclaimer: This curve is a simplified first-order exponential decay model. Actual pharmacokinetics vary based on injection site, individual metabolism, body composition, and other factors. Half-life values are approximate and based on available preclinical and clinical literature. Many research peptides lack formal human pharmacokinetic studies. This is for educational purposes only — not medical advice.
Leuprolide (Lupron) Dosing Protocol
| Level | Dose / Injection | Frequency |
|---|---|---|
| Beginner | 1mg | Daily |
| Moderate | 7.5mg | Monthly |
| Aggressive | 22.5mg | Monthly |
Note: Leuprolide is available in multiple formulations with very different dosing schedules. The DAILY subcutaneous injection (Lupron Injection) is 1 mg/day SC. The DEPOT formulations (Lupron Depot, Eligard) are intramuscular or subcutaneous injections given on fixed schedules: 7.5 mg monthly, 22.5 mg every 3 months, 30 mg every 4 months, or 45 mg every 6 months. The "Weekly" frequency selected above is the closest valid option but does NOT reflect actual clinical dosing — depot injections are given monthly to every 6 months depending on formulation. Dosing varies by indication: prostate cancer uses 7.5-45 mg depot, endometriosis and fibroids use 3.75 mg monthly or 11.25 mg every 3 months for up to 6 months, and central precocious puberty uses weight-based dosing starting at 7.5-15 mg monthly. IMPORTANT: The first 1-2 weeks of therapy cause a "flare" — a transient surge in testosterone (males) or estrogen (females) that can temporarily worsen symptoms. In prostate cancer, anti-androgen cover (e.g., bicalutamide) is often co-prescribed for the first 2-4 weeks to block flare effects.
About Leuprolide (Lupron)
Leuprolide acetate is a synthetic nonapeptide analog of naturally occurring gonadotropin-releasing hormone (GnRH/LHRH). First approved by the FDA in 1985, it is one of the most widely prescribed peptide drugs in the world, marketed under brand names including Lupron, Lupron Depot, and Eligard. Leuprolide is approximately 15-20 times more potent than native GnRH due to a D-leucine substitution at position 6 and an ethylamide group replacing the C-terminal glycine, which confer resistance to enzymatic degradation. The defining pharmacological feature of leuprolide is its biphasic effect on the hypothalamic-pituitary-gonadal (HPG) axis. Initial administration acts as a strong GnRH agonist, stimulating the pituitary to release LH and FSH, which in turn drives a transient increase in sex steroid production — testosterone in males, estrogen and progesterone in females. This "flare" phase lasts approximately 1-2 weeks. With continued administration, sustained receptor stimulation causes downregulation and desensitization of pituitary GnRH receptors through beta-arrestin-mediated internalization. The result is a profound suppression of LH and FSH secretion, leading to castrate levels of testosterone (<50 ng/dL in males) or postmenopausal levels of estradiol in females. This mechanism makes leuprolide effective across a wide range of hormone-dependent conditions. In advanced prostate cancer, it provides androgen deprivation therapy comparable to surgical castration. In endometriosis and uterine fibroids, the induced hypoestrogenic state shrinks lesions and reduces pain. In central precocious puberty, it halts premature sexual development until an appropriate age. Leuprolide is also used as part of transgender hormone therapy and in assisted reproduction protocols. The peptide is primarily degraded by peptidases rather than cytochrome P-450 enzymes, with approximately 46% plasma protein binding. Following subcutaneous injection, the terminal elimination half-life is about 3 hours. Depot formulations use microsphere or polymer matrix technology to sustain drug release over 1-6 months from a single injection, maintaining therapeutic suppression without daily dosing.