Pharmacokinetic and pharmacodynamic modeling of cetrorelix, an LH-RH antagonist, after subcutaneous administration in healthy premenopausal women.

Nagaraja NV, Pechstein B, Erb K, Klipping C, Hermann R, Niebch G, Derendorf H

Clinical pharmacology and therapeutics1 Dec 2000Cited by 13 (Europe PMC)

PMID11180022DOI10.1067/mcp.2000.111481PepBankPUB-11180022

Publisher page PubMedAsk about this study

Summary

The text of this summary is not shown here, because the article license does not allow reuse. Read it at the source (opens in a new tab)

Text rights: Publisher copyright. Results still quote short attributed sentences.

Results from this study7

7 results from studies that gave the peptide. 7 results from people.

01HumanNon-randomized trialPharmacokinetics
In healthy premenopausal women, cetrorelix had a terminal half-life of 56.9 +/- 27.1 hours in a two-compartment model.
In plain wordsIn healthy premenopausal women, the terminal half-life of cetrorelix was 56.9 +/- 27.1 hours.
Peptide
Cetrorelix
Outcome
Not applicableTerminal half-life
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
1, 3, and 5 mg · subcutaneous · single doseAs given in this study (human).
Measurements
Terminal half-life
56.9 hours
mean
Terminal half-life variability
27.1 hours
+/-
Source sentences
Summary
Cetrorelix pharmacokinetics were described by a 2-compartment model with a terminal half-life of 56.9 +/- 27.1 hours.
1 context sentence(design, population, supporting numbers)
Summary · context
In a placebo-controlled study, single subcutaneous doses of 1, 3, and 5 mg of cetrorelix were given to 36 subjects on day 8 of the natural menstrual cycle.
Report a problemFND-1118002201
02HumanNon-randomized trialEfficacy outcome
In healthy premenopausal women, cetrorelix at 1 mg shifted the LH surge by a mean of 4.1 days.
In plain wordsIn healthy premenopausal women, cetrorelix at 1 mg shifted the LH surge by a mean of 4.1 days.
Peptide
Cetrorelix
Outcome
Direction not reportedLH surge shift at 1 mg
Study
n: not reported in source
Outcome group
Sex hormones and fertility · Endocrine and hormones
Studied dose
1 mg · subcutaneous · single doseAs given in this study (human).
Measurements
LH surge shift
4.1 days
1 mg
Source sentences
Summary
Mean shift in LH surge was by 4.1, 7.5, and 9.3 days with the 1-, 3-, and 5-mg doses, respectively.
1 context sentence(design, population, supporting numbers)
Summary · context
In a placebo-controlled study, single subcutaneous doses of 1, 3, and 5 mg of cetrorelix were given to 36 subjects on day 8 of the natural menstrual cycle.
Report a problemFND-1118002202
03HumanNon-randomized trialEfficacy outcome
In healthy premenopausal women, cetrorelix at 3 mg shifted the LH surge by a mean of 7.5 days.
In plain wordsIn healthy premenopausal women, cetrorelix at 3 mg shifted the LH surge by a mean of 7.5 days.
Peptide
Cetrorelix
Outcome
Direction not reportedLH surge shift at 3 mg
Study
n: not reported in source
Outcome group
Sex hormones and fertility · Endocrine and hormones
Studied dose
3 mg · subcutaneous · single doseAs given in this study (human).
Measurements
LH surge shift
7.5 days
3 mg
Source sentences
Summary
Mean shift in LH surge was by 4.1, 7.5, and 9.3 days with the 1-, 3-, and 5-mg doses, respectively.
1 context sentence(design, population, supporting numbers)
Summary · context
In a placebo-controlled study, single subcutaneous doses of 1, 3, and 5 mg of cetrorelix were given to 36 subjects on day 8 of the natural menstrual cycle.
Report a problemFND-1118002203
04HumanNon-randomized trialEfficacy outcome
In healthy premenopausal women, cetrorelix at 5 mg shifted the LH surge by a mean of 9.3 days.
In plain wordsIn healthy premenopausal women, cetrorelix at 5 mg shifted the LH surge by a mean of 9.3 days.
Peptide
Cetrorelix
Outcome
Direction not reportedLH surge shift at 5 mg
Study
n: not reported in source
Outcome group
Sex hormones and fertility · Endocrine and hormones
Studied dose
5 mg · subcutaneous · single doseAs given in this study (human).
Measurements
LH surge shift
9.3 days
5 mg
Source sentences
Summary
Mean shift in LH surge was by 4.1, 7.5, and 9.3 days with the 1-, 3-, and 5-mg doses, respectively.
1 context sentence(design, population, supporting numbers)
Summary · context
In a placebo-controlled study, single subcutaneous doses of 1, 3, and 5 mg of cetrorelix were given to 36 subjects on day 8 of the natural menstrual cycle.
Report a problemFND-1118002204
05HumanNon-randomized trialActivity measurement
In women, the estimated cetrorelix concentration for half-maximal LH suppression was 3.6 ng/mL.
In plain wordsIn women, the estimated cetrorelix concentration for half-maximal LH suppression was 3.6 ng/mL.
Peptide
Cetrorelix
Outcome
Not applicableLH suppression IC50
Study
n: not reported in source
Outcome group
Receptor activity and mechanism · Pharmacology
Studied dose
1, 3, and 5 mg · subcutaneous · single doseAs given in this study (human).
Measurements
IC50
3.6 ng/mL
LH suppression
Source sentences
Summary
The inhibitory concentration of 50% (for LH suppression) and median effective concentration (for surge shift) estimates were 3.6 ng/mL and 1.6 ng/mL, respectively.
1 context sentence(design, population, supporting numbers)
Summary · context
In a placebo-controlled study, single subcutaneous doses of 1, 3, and 5 mg of cetrorelix were given to 36 subjects on day 8 of the natural menstrual cycle.
Report a problemFND-1118002205
06HumanNon-randomized trialActivity measurement
In women, the estimated median effective cetrorelix concentration for LH surge shift was 1.6 ng/mL.
In plain wordsIn women, the estimated median effective cetrorelix concentration for LH surge shift was 1.6 ng/mL.
Peptide
Cetrorelix
Outcome
Not applicableLH surge shift EC50
Study
n: not reported in source
Outcome group
Receptor activity and mechanism · Pharmacology
Studied dose
1, 3, and 5 mg · subcutaneous · single doseAs given in this study (human).
Measurements
EC50
1.6 ng/mL
surge shift
Source sentences
Summary
The inhibitory concentration of 50% (for LH suppression) and median effective concentration (for surge shift) estimates were 3.6 ng/mL and 1.6 ng/mL, respectively.
1 context sentence(design, population, supporting numbers)
Summary · context
In a placebo-controlled study, single subcutaneous doses of 1, 3, and 5 mg of cetrorelix were given to 36 subjects on day 8 of the natural menstrual cycle.
Report a problemFND-1118002206
07HumanNon-randomized trialActivity measurement
In women, the estimated cetrorelix concentration for half-maximal FSH suppression was 7.25 ng/mL.
In plain wordsIn women, the estimated cetrorelix concentration for half-maximal FSH suppression was 7.25 ng/mL.
Peptide
Cetrorelix
Outcome
Not applicableFSH suppression IC50
Study
n: not reported in source
Outcome group
Receptor activity and mechanism · Pharmacology
Studied dose
1, 3, and 5 mg · subcutaneous · single doseAs given in this study (human).
Measurements
IC50
7.25 ng/mL
FSH suppression
Source sentences
Summary
The suppression of follicle-stimulating hormone was described by a similar Emax model, with an inhibitory concentration of 50% of 7.25 ng/mL.
1 context sentence(design, population, supporting numbers)
Summary · context
In a placebo-controlled study, single subcutaneous doses of 1, 3, and 5 mg of cetrorelix were given to 36 subjects on day 8 of the natural menstrual cycle.
Report a problemFND-1118002207

AI wrote and checked these results. AI can make mistakes, so check important results against the source.

Version history

PepBank keeps every version of the data on this study. Status changes from Retraction Watch, Europe PMC and Crossref are listed with their source.

Version 2Current
28 Oct 2026, 02:03 UTC
Study results updated
Version 1
27 Oct 2026, 16:35 UTC
First added · source update from Europe PMC

Subjects

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MeSH terms

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