Peptide Profile
Buserelin
A synthetic GnRH agonist that suppresses hormones to help treat prostate cancer, endometriosis, and infertility
Dose Range
200 mcg-1,500 mcgmcg
Frequency
Once daily
Route
Subcutaneous injection
Cycle Length
Ongoing/indefinite
Onset
Moderate (1-2 weeks)
Evidence
Strong
Compound Profile
Scientific & Efficacy Data
C60H86N16O13
Molecular Formula
1239.4 g/mol
Molecular Weight
2-4 hours (subcutaneous), 30-60 minutes (intranasal); longer for depot formulation (28-40 days)
Half-Life
~1% (oral); ~10-15% (intranasal); ~95% (subcutaneous)
Bioavailability
57773-65-6
CAS #
50225
PubChem ID ↗
Developed By · 1983
Hoechst AG Research Team
Hoechst AG (now Sanofi)
Primary Benefits
Reversible hormone suppression after treatment stops
Suppresses testosterone to near-castrate levels for prostate cancer management
Improves fertility outcomes when combined with IVF protocols
Amino Acid Sequence
pGlu-His-Trp-Ser-Tyr-D-Ser-Leu-Arg-Pro-NHEtDosing
How much
do I take?
Timing
Best time to take
Administer Buserelin at the same time each day (or on the same day each week for weekly injections). Many users prefer morning or evening administration. Pick a time you'll remember consistently.
With food?
Buserelin injections can be given regardless of meal timing. However, if GI effects occur, administering on an empty stomach or with a light meal may help reduce discomfort.
If stacking
Buserelin should be used as directed by your healthcare provider. If combining with other medications or supplements, discuss potential interactions with your provider. Avoid combining with compounds that have overlapping mechanisms unless specifically guided by a medical professional.
Adjusting Your Dose
Increase if
- +You've tolerated the current dose for the recommended period without significant side effects
- +Therapeutic goals haven't been met at the current dose level
- +Your healthcare provider recommends dose escalation based on your response
- +Lab work or clinical assessments support a higher dose
Decrease if
- -Side effects are bothersome or impacting daily life despite management strategies
- -You experience any signs of an adverse reaction
- -Lab results indicate the need for dose reduction
- -Your healthcare provider recommends a lower dose based on your response
Signs of right dose
- ✓Therapeutic goals being met with minimal side effects
- ✓Stable and consistent response to treatment
- ✓Lab values or clinical markers trending in the right direction
- ✓Good tolerance with manageable or absent side effects
Dosing Calculator
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Suitability
Is this
right for me?
Best For
Managing advanced prostate cancer
Buserelin is particularly well-suited for individuals focused on managing advanced prostate cancer. Research and clinical experience suggest meaningful benefits in this area when used as part of a comprehensive treatment approach.
Treating endometriosis and reducing associated pain
Buserelin is particularly well-suited for individuals focused on treating endometriosis and reducing associated pain. Research and clinical experience suggest meaningful benefits in this area when used as part of a comprehensive treatment approach.
Optimizing ovarian response during fertility treatments
Buserelin is particularly well-suited for individuals focused on optimizing ovarian response during fertility treatments. Research and clinical experience suggest meaningful benefits in this area when used as part of a comprehensive treatment approach.
Consider Alternatives If
Who Should Avoid
Do not use if
- ×Pregnancy or breastfeeding
- ×Hypersensitivity to GnRH agonists
- ×Certain bone diseases when long-term use is planned
Use with caution if
- !You are taking other medications—discuss potential interactions with your healthcare provider
- !You have a history of liver or kidney disease
- !You are elderly or have multiple medical conditions
- !You are planning surgery in the near future—inform your surgeon about Buserelin use
- !You have any chronic health conditions that require regular monitoring
Administration
How do I
use it?
Reconstitution
What you need
- •Buserelin vial (lyophilized powder or solution)
- •Bacteriostatic water or sterile sodium chloride for reconstitution
- •Alcohol swabs for cleaning vial tops and injection sites
- •Appropriately sized syringes with fine-gauge needles (27-30 gauge)
- •Sharps disposal container
Injection
Route
Subcutaneous injection (into the fatty tissue just under the skin)—allows for consistent absorption and can be self-administered at home after proper training
Best sites
- •Abdomen (stomach area)—at least 2 inches from the belly button, most popular choice for self-injection
- •Front of thighs—middle to upper portion of the outer leg
- •Back of upper arm—outer area (may need assistance from another person)
Technique
- 1.Wash your hands thoroughly with soap and water before handling supplies
- 2.Clean the injection site with an alcohol swab and let it air dry completely
- 3.Pinch a fold of skin at the chosen injection site
- 4.Insert the needle at a 45-90 degree angle (depending on needle length and body composition)
- 5.Inject the medication slowly and steadily over 5-10 seconds
- 6.Release the skin fold and remove the needle, applying gentle pressure with a clean swab
- 7.Rotate injection sites to prevent tissue irritation or lipodystrophy
- 8.Dispose of the needle safely in a sharps container—never recap or reuse needles
Storage
Signs of degradation
Sample Daily Schedule
Safety
Is it
safe?
Safety Profile
Buserelin is an FDA-approved GnRH agonist with safety data from Phase 3 trials and decades of clinical use, but carries well-documented risks from intentional testosterone/estrogen suppression. The initial testosterone flare (first 2-3 weeks) can worsen prostate cancer symptoms and cause tumor flare pain in 10-20% of patients. Long-term use causes bone density loss of 2-3% annually, with vertebral fractures in 10-20% of long-term users. Cardiovascular risks include increased MI and stroke in men over 65. Hot flashes affect 40-80%, erectile dysfunction is nearly universal, and liver enzyme elevations occur in 5%. Nasal spray formulation causes local irritation in 20-30% of users.
Buserelin was studied through Phase 3 clinical trials before FDA approval, with decades of post-market pharmacovigilance data. The flare phenomenon, bone loss, cardiovascular effects, and endocrine complications are well-characterized from long-term studies spanning over 30 years. Comparative safety data with GnRH antagonists demonstrates buserelin's disadvantage regarding initial flare effect but similar long-term side effect profiles.
Stop and Seek Help If
- ×Severe or worsening side effects that don't improve with dose adjustment or supportive care
- ×Signs of an allergic reaction—rash, hives, swelling, or difficulty breathing
- ×Your healthcare provider recommends discontinuation based on your clinical response
- ×Development of any new medical condition that may be contraindicated with Buserelin
- ×Pregnancy or planning to become pregnant (unless specifically approved for use during pregnancy)
- ×Abnormal lab results or clinical markers that suggest adverse effects
Buserelin should only be started, adjusted, or discontinued under medical supervision. This information is for educational purposes only and does not replace professional medical advice. Never stop a prescribed treatment without consulting your healthcare provider first, as abrupt discontinuation may have consequences.
Interactions
With other peptides
- ✓May be used together under medical guidance.
- ✓May be used together under medical guidance.
- ✓May be used together under medical guidance.
With medications
- !Other GnRH agonists—redundant and increases side effects - Use with caution—discuss with your healthcare provider.
- !Alcohol in excess—may worsen hot flashes and mood changes - Use with caution—discuss with your healthcare provider.
With supplements
- ✓Multivitamins - Generally safe to take alongside Buserelin. Space doses apart if taking oral formulations to ensure optimal absorption.
- ✓Electrolyte supplements - Helpful if experiencing any GI side effects that could lead to dehydration. Safe to combine.
Effectiveness
Does it
work?
Evidence Level
Strong human trials
Signs It's Working
Treatment Response
- ✓Improvement in the primary symptoms or condition being treated
- ✓Positive changes in relevant lab values or clinical markers
- ✓Consistent, stable response to Buserelin over time
- ✓Reduction in symptom frequency or severity
General Well-being
- ✓Improved energy levels and daily functioning
- ✓Better quality of life related to the treated condition
- ✓Manageable or absent side effects indicating good tolerance
- ✓Positive feedback from healthcare provider during check-ups
Not Seeing Results?
Common reasons
- •Not at therapeutic dose yet—initial doses are for building tolerance, not maximum effect
- •Insufficient time at target dose—most compounds need several weeks to show full benefits
- •Inconsistent dosing schedule—regular, consistent use is crucial for optimal results
- •Individual variation in response—genetics, metabolism, and other factors affect outcomes
- •Underlying conditions or medications interfering with absorption or effectiveness
- •Improper storage leading to degraded product—always verify proper storage conditions
Key Research
"An improved use of buserelin in ovarian stimulation for in-vitro fertilization"
PubMed Central, 1990
Finding: Buserelin effectively suppressed natural hormone surges during fertility treatment, allowing doctors to better control egg production timing. A simplified single daily 600 mcg injection proved as effective as more complex dosing schedules.
View Study"Gonadotropin-releasing hormone agonists in prostate cancer: A comparative review of efficacy and safety"
Raja T, Sud R, Addla S, 2022
Finding: Buserelin achieved testosterone suppression below 50 ng/dL within one month, with long-term survival rates of 42-84% depending on treatment approach. When combined with other therapies, survival improved further to 87% in some patient groups.
View Study"Cardiovascular adverse events-related to GnRH agonists and GnRH antagonists: analysis of real-life data from Eudra-Vigilance and FDA databases"
Cicione A, Nacchia A, Guercio A, 2023
Finding: Real-world data showed buserelin had higher cardiovascular complication rates (9%) compared to modern antagonists. Patients under 65 years experienced very low cardiovascular risk, while older populations showed significant complications requiring monitoring.
View Study"Adverse event profile differences among long-acting gonadotropin-releasing hormone analogs: A real-world, pharmacovigilance study"
Chen Y, Lu W, Liao R, 2025
Finding: Buserelin showed distinct adverse effect profiles compared to other GnRH agonists, with higher incidence of gastrointestinal disorders. Pediatric patients experienced lower serious adverse event rates than adults, requiring different safety monitoring strategies.
View StudyFrequently Asked Questions