Peptide profile
Leuprolide (Lupron)
Long-acting GnRH agonist for hormone therapy
Compare Leuprolide (Lupron) with other peptides →Summary
A long-lasting medicine that lowers certain body hormones.
- Typical dose
- 3.75-22.5mg (1-month depot) Every 1, 3, 4, or 6 months
- Route
- Subcutaneous, Intramuscular
- Cycle length
- Varies by condition (weeks to years)
- Evidence
- Limited human data
Mechanism
How it works
Leuprolide works like a key stuck in the lock — it briefly jiggles the door (stimulates), then jams the mechanism so no more keys work (suppression).
Leuprolide is a potent GnRH agonist that initially stimulates then downregulates pituitary GnRH receptors, suppressing LH/FSH and sex hormone production.
Reported in research
Benefits
- Lowers hormones to fight prostate cancer and help with endometriosis
- Only needs a shot once a month or even less often
- Hormone changes can go back to normal later
- Helps kids who start puberty too early
Context, not a prescription
Dosing
- Typical range
- 3.75-22.5mg (1-month depot) Every 1, 3, 4, or 6 months (Subcutaneous, Intramuscular)
- Cycle length
- Varies by condition (weeks to years)
Safety
Side effects & contraindications
Possible side effects
- Injection site pain
- Hot flashes
- Testicular atrophy
- Loss of libido
- Tumor flare (initial)
- Bone density loss (long-term)
- Cardiovascular events
Contraindications
- Pregnancy or breastfeeding
- Spinal cord compression risk
- Pituitary adenoma
Research information, not medical advice. Always consult a licensed clinician before considering any peptide.
In depth
Full profile
What it does
Lowers testosterone in men or estrogen in women. It treats cancers that grow with hormones.
How it works
Leuprolide is like a key stuck in a lock. It wiggles the door open at first, then jams it so no other keys work.
It grabs onto special spots in the brain. This makes hormones rise at first, then drop way down.
What to expect
Hormones rise for 2-4 weeks, then drop low after 4-6 weeks.
- Days 1-14: Hormones jump up at first.
- Weeks 3-4: Hormones slowly start dropping.
- Weeks 4-6: Hormones stay very low and steady.
Good to know
- Check how strong your bones are
- Add a little hormone back if used for a long time
- Take calcium and vitamin D
Staying safe
- Sore spot where you got the shot
- Feeling suddenly hot
- Testicles getting smaller
- Less interest in sex
Avoid if you have:
- If pregnant or breastfeeding
- If there is a risk of pressure on the spine
- If there is a growth on the brain's gland
Mechanism of action
Leuprolide is a potent GnRH agonist that initially stimulates then downregulates pituitary GnRH receptors, suppressing LH/FSH and sex hormone production.
Binds to GnRH receptors with high affinity, causing initial gonadotropin release followed by receptor desensitization and downregulation.
Pharmacodynamics
Initial flare (2-4 weeks) then suppression (4-6 weeks).
Suppressed testosterone (men) or estrogen (women); therapy for hormone-sensitive cancers.
Timeline
- Days 1-14: Initial hormone surge (flare).
- Weeks 3-4: Progressive hormone suppression.
- Weeks 4-6: Medical castration (steady state).
Comparisons
- Leuprolide — effectiveness High, safety Good, cost $$$$, Easy to use
- Degarelix — effectiveness High, safety Good, cost $$$$, Easy to use
Adverse effects
Common:
- Injection site pain
- Hot flashes
- Testicular atrophy
- Loss of libido
Rare:
- Tumor flare (initial)
- Bone density loss (long-term)
- Cardiovascular events
Contraindications & risk mitigation
Contraindicated in:
- Pregnancy or breastfeeding
- Spinal cord compression risk
- Pituitary adenoma
- Monitor bone density
- Add back low-dose hormones for long-term use
- Calcium/vitamin D supplementation
Qué hace
Reduce la testosterona en los hombres o el estrógeno en las mujeres. Trata cánceres que crecen con hormonas.
Cómo funciona
La leuprolida es como una llave atascada en una cerradura. Al principio mueve la puerta para abrirla, luego la traba para que ninguna otra llave funcione.
Se une a puntos especiales en el cerebro. Esto hace que las hormonas suban al principio y luego bajen mucho.
Qué esperar
Las hormonas suben durante 2-4 semanas y luego bajan mucho después de 4-6 semanas.
- Días 1-14: Las hormonas suben al principio.
- Semanas 3-4: Las hormonas comienzan a bajar lentamente.
- Semanas 4-6: Las hormonas se mantienen muy bajas y estables.
Bueno saber
- Revisar qué tan fuertes son los huesos
- Agregar un poco de hormona de nuevo si se usa por mucho tiempo
- Tomar calcio y vitamina D
Manteniéndose seguro
- Zona dolorosa donde se aplicó la inyección
- Sensación repentina de calor
- Encogimiento de los testículos
- Menos interés sexual
Evitar si tienes:
- Si está embarazada o en periodo de lactancia
- Si existe riesgo de presión sobre la columna vertebral
- Si hay un crecimiento en la glándula del cerebro
Mecanismo de acción
La leuprolida es un agonista potente de GnRH que inicialmente estimula y luego regula a la baja los receptores de GnRH hipofisarios, suprimiendo la producción de LH/FSH y hormonas sexuales.
Se une a los receptores de GnRH con alta afinidad, provocando una liberación inicial de gonadotropinas seguida de desensibilización y regulación a la baja de los receptores.
Farmacodinamia
Rebote inicial (2-4 semanas) seguido de supresión (4-6 semanas).
Testosterona suprimida (hombres) o estrógeno (mujeres); terapia para cánceres sensibles a hormonas.
Cronología
- Días 1-14: Pico hormonal inicial (rebote).
- Semanas 3-4: Supresión hormonal progresiva.
- Semanas 4-6: Castración médica (estado estable).
Comparaciones
- Leuprolida — efectividad Alta, seguridad Buena, costo $$$$, Fácil de usar
- Degarelix — efectividad Alta, seguridad Buena, costo $$$$, Fácil de usar
Efectos adversos
Comunes:
- Dolor en el sitio de inyección
- Sofoques
- Atrofia testicular
- Pérdida de libido
Raros:
- Rebote tumoral (inicial)
- Pérdida de densidad ósea (a largo plazo)
- Eventos cardiovasculares
Contraindicaciones y mitigación de riesgos
Contraindicado en:
- Embarazo o lactancia
- Riesgo de compresión de la médula espinal
- Adenoma hipofisario
- Monitorear la densidad ósea
- Reintroducir hormonas en dosis bajas para uso prolongado
- Suplementación con calcio/vitamina D
Reference data
Specifications
- Route
- Subcutaneous, Intramuscular
- Cycle length
- Varies by condition (weeks to years)
FAQ
Common questions
Does leuprolide cause permanent infertility?
Children treated for precocious puberty usually have normal fertility; adults may have reversible suppression.
Why is it used for prostate cancer?
Prostate cancer is androgen-sensitive; leuprolide lowers testosterone to starve cancer cells.
What is the evidence level?
This compound is classified as Limited human data. Some human data exists but trials are small, short-term, or not yet replicated.
Research
Research & sources
Current evidence for Leuprolide (Lupron) is rated as Limited human data. Limited human data is available.
- 1. Leuprolide for prostate cancer (1995) — DOI:10.1056/NEJM199505043321812
- 2. GnRH agonists review (2006) — DOI:10.1016/j.eururo.2006.02.015
- 3. Leuprolide for prostate cancer (1995)
- 4. GnRH agonists review (2006)