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Adipotide
Weight Management
AOD-9604
Weight Management
BPC-157
Healing & Recovery
Cagrilintide
Weight Management
CJC-1295
Growth Hormone
DSIP
Sleep & Recovery
Epithalon
Anti-Aging
GHK-Cu
Anti-Aging
GHRP-2
Growth Hormone
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Hormone Support
Hexarelin
Growth Hormone
HGH
Growth Hormone
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Growth Hormone
Kisspeptin
Hormone Support
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Cosmetic
MOTS-C
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NAD+
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Hormone Support
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Weight Management
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Sermorelin
Growth Hormone
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SS-31
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TB-500
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Tesamorelin
Growth Hormone
Thymosin Alpha-1
Immune
Tirzepatide
Weight Management
Total Peptides: 32
Back to Home
Eagle LogoPEPTIDE INITIATIVE

Peptide Database

Goals
Peptides
Adipotide
Weight Management
AOD-9604
Weight Management
BPC-157
Healing & Recovery
Cagrilintide
Weight Management
CJC-1295
Growth Hormone
DSIP
Sleep & Recovery
Epithalon
Anti-Aging
GHK-Cu
Anti-Aging
GHRP-2
Growth Hormone
HCG
Hormone Support
Hexarelin
Growth Hormone
HGH
Growth Hormone
IGF-1 LR3
Growth Hormone
Kisspeptin
Hormone Support
Melanotan-2
Cosmetic
MOTS-C
Metabolic
NAD+
Anti-Aging
Oxytocin Acetate
Hormone Support
PEG-MGF
Recovery
PNC-27
Cancer Research
PT-141
Sexual Health
Retatrutide
Weight Management
Selank
Cognitive
Semaglutide
Weight Management
Semax
Cognitive
Sermorelin
Growth Hormone
Snap-8
Cosmetic
SS-31
Mitochondrial
TB-500
Healing & Recovery
Tesamorelin
Growth Hormone
Thymosin Alpha-1
Immune
Tirzepatide
Weight Management
Total Peptides: 32
Back to Home

Peptide History

Cetrorelix
Acetate

The game-changing antagonist that stops the hormone surge instantly instead of causing a dangerous flare

Cetrorelix is a revolutionary peptide drug that blocks GnRH, a master control hormone. Unlike older agonist drugs, cetrorelix works immediately without an initial hormone surge. Developed by Asta Medica and approved by the FDA in 2000, it changed how doctors manage IVF cycles worldwide. It works like a blocker on a door, preventing hormone signals from passing through, rather than overstimulating the system first.

Scroll to Discover

Quick Facts

Cetrorelix at a Glance

FDA-approved and standard in IVF clinics globally

1995

Discovery Year

When this peptide was first identified

Peptide

Type

Compound classification

FDA-approved and standard in IVF clinics globally

Status

Current regulatory status

Research compound

Primary Use

Main area of investigation

Injection

Administration

How this peptide is typically given

Peptide chain

Size

Molecular structure type

The Visionaries

Pioneers Who Dared
to Challenge the Impossible

Asta Medica AG (now Baxter), Dresden, Germany

Asta Medica

Original developer

Created cetrorelix and pioneered GnRH antagonist development in the 1990s

""

Zentaris GmbH (now Æterna Zentaris), Frankfurt, Germany

Zentaris

Developer and researcher

Conducted extensive clinical trials to prove cetrorelix safety and effectiveness

""

Merck Serono (EMD Serono), Geneva, Switzerland

Merck Serono

Current manufacturer

Acquired Zentaris and continues marketing Cetrotide globally

""

U.S. Food and Drug Administration, Silver Spring, MD

FDA Review Panel

Regulatory approval body

Approved cetrorelix in 2000 based on strong clinical evidence

""

The Journey

A Story of
Persistence & Triumph

The Discovery

Chapter 1

By the 1990s, IVF doctors used GnRH agonists to control egg release timing.

Key Moment

By the 1990s, IVF doctors used GnRH agonists to control egg release timing.

By the 1990s, IVF doctors used GnRH agonists to control egg release timing. It worked but had a dangerous problem. The initial hormone surge could cause ovarian hyperstimulation. Women developed severe pain, nausea, and fluid buildup. Some cases were life-threatening. Doctors needed something safer. They needed a drug that would block GnRH signals immediately, without the dangerous flare. Scientists knew theoretically it should be possible. But could they build it?

The Breakthrough

Chapter 2

While agonists like buserelin over-stimulated the system, antagonists worked like locks.

Key Moment

While agonists like buserelin over-stimulated the system, antagonists worked like locks.

While agonists like buserelin over-stimulated the system, antagonists worked like locks. Instead of pressing a button over and over, antagonists blocked the button from working at all. This was the opposite approach. Asta Medica scientists in Germany realized they could create an antagonist that was strong enough to block GnRH instantly. It would be like turning off a light switch instead of flipping it on and on until the system breaks.

The Trials

Chapter 3

Asta Medica and Zentaris partnered to develop and test cetrorelix.

Key Moment

Asta Medica and Zentaris partnered to develop and test cetrorelix.

Asta Medica and Zentaris partnered to develop and test cetrorelix. They ran Phase 1, 2, and 3 clinical trials with hundreds of women undergoing IVF. The results were striking. Cetrorelix prevented the dangerous LH surge. Women did not have dangerous hormone flares. Pregnancy rates were excellent. The side effect profile was much better than agonists. By the late 1990s, the evidence was undeniable.

The Crisis

Chapter 4

In 2000, the FDA approved cetrorelix as Cetrotide.

Key Moment

In 2000, the FDA approved cetrorelix as Cetrotide.

In 2000, the FDA approved cetrorelix as Cetrotide. This approval was a turning point. IVF clinics across the United States immediately began using it. The drug worked as marketed: immediate action, no flare, perfect control of the egg-release timing. Doctors reported fewer emergency visits from patients with ovarian hyperstimulation. Success rates improved. Cetrorelix became standard of care for IVF protocols worldwide.

The Legacy

Chapter 5

Today, cetrorelix and other GnRH antagonists are used more often than agonists in IVF clinics.

Key Moment

The antagonist revolution continues to help patients have healthier, safer fertility treatment.

Today, cetrorelix and other GnRH antagonists are used more often than agonists in IVF clinics. The drug showed that sometimes the best answer is to block signals instead of over-stimulate them. This philosophy changed not just IVF but how doctors approach hormone control across many treatments. Thousands of couples every year achieve their dream of parenthood thanks to safer protocols built around cetrorelix. The antagonist revolution continues to help patients have healthier, safer fertility treatment.

Years of Progress

Timeline of
Breakthroughs

1992

Asta Medica begins GnRH antagonist research program

Asta Medica begins GnRH antagonist research program

1993

Early-stage research shows antagonist concept can work in humans

Early-stage research shows antagonist concept can work in humans

1995

Cetrorelix enters first clinical trials (Phase 1)

Cetrorelix enters first clinical trials (Phase 1)

1996

Phase 2 trials show strong efficacy and safety data

Phase 2 trials show strong efficacy and safety data

1998

Phase 3 trials involving hundreds of IVF patients completed

Phase 3 trials involving hundreds of IVF patients completed

1999

FDA receives official approval application

FDA receives official approval application

2000

FDA approves cetrorelix (Cetrotide) for IVF use

FDA approves cetrorelix (Cetrotide) for IVF use

2001

US IVF centers rapidly adopt cetrorelix protocols

US IVF centers rapidly adopt cetrorelix protocols

2005

Cetrorelix becomes preferred agent over agonists in most IVF clinics

Cetrorelix becomes preferred agent over agonists in most IVF clinics

2010

Over one million cycles completed with cetrorelix worldwide

Over one million cycles completed with cetrorelix worldwide

2015

Established as gold standard for antagonist protocols in fertility

Established as gold standard for antagonist protocols in fertility

2020

Cetrorelix used in over 50 percent of IVF cycles globally

Cetrorelix used in over 50 percent of IVF cycles globally

2023

Continues as first-line antagonist choice in major fertility centers

Continues as first-line antagonist choice in major fertility centers

2024

Research explores cetrorelix use in additional reproductive conditions

Research explores cetrorelix use in additional reproductive conditions

2025

Cetrorelix remains revolutionary standard in modern fertility medicine

Cetrorelix remains revolutionary standard in modern fertility medicine

The Science

Understanding
the Mechanism

Cetrorelix works like a security guard at a locked door. GnRH is a hormone signal trying to open the door. The guard is cetrorelix. It stands in front of the door and says no. GnRH cannot pass through. The pituitary gland cannot receive the signal. Without the signal, it stops releasing LH and FSH. These hormones are what tell the ovaries to release eggs. By blocking them at exactly the right time, doctors can prevent the dangerous LH surge. This is different from agonists. Agonists force the door open so hard that the lock breaks. Cetrorelix just keeps the door closed until the doctor decides to open it.

Molecular Structure

Cetrorelix is a ten-amino-acid peptide (longer than buserelin's nine amino acids)

Chemical Type

1431.0 grams per mole (heavier than buserelin)

Molecular Weight

Cetrorelix attaches strongly to the GnRH door on pituitary cells, preventing natural GnRH from attaching

How It Blocks GnRH

C70H92ClN17O14 (contains chlorine atom making it unique among GnRH antagonists)

Chemical Formula

Global Impact

Transforming Lives
Across the World

2000

Year cetrorelix was FDA-approved

Year cetrorelix was FDA-approved, revolutionizing IVF worldwide

25+ years

Safe use in over

Safe use in over ten million IVF cycles across the globe

50-70%

Share of modern IVF

Share of modern IVF programs now using antagonist protocols like cetrorelix

70-80%

Reduction in dangerous ovarian

Reduction in dangerous ovarian hyperstimulation cases after cetrorelix adoption

Real Stories, Real Lives

Rachel

""

Robert

""

The Future of Cetrorelix

Research Stage

Extended applications - researchers are testing cetrorelix for additional reproductive conditions beyond basic IVF

Research Stage

Combination strategies - scientists are developing new protocols combining cetrorelix with other medications for even better results

Research Stage

Personalized dosing - doctors are learning to predict exactly how much cetrorelix each patient needs based on individual factors

Research Stage

Mechanism studies - ongoing research to understand exactly how cetrorelix could help in other hormone-related conditions

Be Inspired

The story of Cetrorelix is ultimately about the relentless pursuit of better medicine for humanity.

Continue the legacy. The next breakthrough could be yours.

Cetrorelix Chronicles

Part of the Peptide History series — honoring the science that shapes our future.

© 2026 Peptide History. Educational content for research purposes.

This content is for educational purposes only and should not be considered medical advice.