Novel formulations of cetrorelix acetate in healthy men: pharmacodynamic effects and noncompartmental pharmacokinetics.

Erb K, Junge K, Pechstein B, Schneider E, Derendorf H, Hermann R

Journal of clinical pharmacology1 Sept 2002Cited by 1 (Europe PMC)

PMID12211225DOI10.1177/0091270002042009006PepBankPUB-12211225

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 study11

11 results from studies that gave the peptide. 11 results from people.

01HumanRandomized controlled trialEfficacy outcome
In healthy men, 10 mg CET/glu produced the deepest testosterone suppression among treatments.
In plain wordsIn healthy men, 10 mg CET/glu suppressed testosterone more deeply than the other treatments.
Peptide
Cetrorelix
Outcome
DecreaseDepth of testosterone suppression
Study
n = 36
Comparator
5 mg CET/glu and 10 mg CET/wat
Outcome group
Sex hormones and fertility · Endocrine and hormones
Studied dose
10 mg CET/glu · subcutaneous · Once weekly for 4 weeksAs given in this study (human).
Source sentences
Summary
Deepest and longest testosterone suppression was achieved by 10 mg CET/glu.
1 context sentence(design, population, supporting numbers)
Summary · context
In a randomized parallel-group study, single subcutaneous doses of cetrorelix acetate (concentration: 2.5 mg peptide base/ml) dissolved in aqueous gluconic acid (CET/glu, dose: 5 or 10 mg peptide base) or in water (CET/wat, dose: 10 mg peptide base) were given to 36 subjects once weekly in the morning for 4 weeks.
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02HumanRandomized controlled trialEfficacy outcome
In healthy men, the median duration of at least half-maximum testosterone suppression was 82 hours after the first dose and 122 hours after the fourth dose, and 10 mg CET/glu gave the longest suppression.
In plain wordsIn healthy men, half-maximum testosterone suppression lasted a median of 82 hours after dose one and 122 hours after dose four.
Peptide
Cetrorelix
Outcome
IncreaseDuration of testosterone suppression
Study
n = 36
Comparator
5 mg CET/glu and 10 mg CET/wat
Outcome group
Sex hormones and fertility · Endocrine and hormones
Studied dose
10 mg CET/glu · subcutaneous · Once weekly for 4 weeksAs given in this study (human).
Measurements
Median duration of at least half-maximum testosterone suppression
82 hours
After first dose, treatment group not specified in source
Median duration of at least half-maximum testosterone suppression
122 hours
After fourth dose, treatment group not specified in source
Source sentences
Summary
Duration of atleasthalf-maximum suppression was after the first dose median of 82 hours and after the fourth dose median of 122 hours, respectively.
2 context sentences(design, population, supporting numbers)
Summary · context
Deepest and longest testosterone suppression was achieved by 10 mg CET/glu.
Summary · context
In a randomized parallel-group study, single subcutaneous doses of cetrorelix acetate (concentration: 2.5 mg peptide base/ml) dissolved in aqueous gluconic acid (CET/glu, dose: 5 or 10 mg peptide base) or in water (CET/wat, dose: 10 mg peptide base) were given to 36 subjects once weekly in the morning for 4 weeks.
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03HumanRandomized controlled trialPharmacokinetics
In healthy men, tmax did not differ significantly between cetrorelix formulations.
In plain wordsIn healthy men, time to peak drug levels did not differ significantly between cetrorelix formulations.
Peptide
Cetrorelix
Outcome
No significant changetmax
Study
n = 36
Comparator
Other cetrorelix formulations
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
CET/glu 5 or 10 mg peptide base; CET/wat 10 mg peptide base · subcutaneous · Once weekly for 4 weeksAs given in this study (human).
Source sentences
Summary
For tmax and t1/2, no significant differences were found between formulations.
1 context sentence(design, population, supporting numbers)
Summary · context
In a randomized parallel-group study, single subcutaneous doses of cetrorelix acetate (concentration: 2.5 mg peptide base/ml) dissolved in aqueous gluconic acid (CET/glu, dose: 5 or 10 mg peptide base) or in water (CET/wat, dose: 10 mg peptide base) were given to 36 subjects once weekly in the morning for 4 weeks.
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04HumanRandomized controlled trialPharmacokinetics
In healthy men, half-life did not differ significantly between cetrorelix formulations.
In plain wordsIn healthy men, drug half-life did not differ significantly between cetrorelix formulations.
Peptide
Cetrorelix
Outcome
No significant changeHalf-life
Study
n = 36
Comparator
Other cetrorelix formulations
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
CET/glu 5 or 10 mg peptide base; CET/wat 10 mg peptide base · subcutaneous · Once weekly for 4 weeksAs given in this study (human).
Source sentences
Summary
For tmax and t1/2, no significant differences were found between formulations.
1 context sentence(design, population, supporting numbers)
Summary · context
In a randomized parallel-group study, single subcutaneous doses of cetrorelix acetate (concentration: 2.5 mg peptide base/ml) dissolved in aqueous gluconic acid (CET/glu, dose: 5 or 10 mg peptide base) or in water (CET/wat, dose: 10 mg peptide base) were given to 36 subjects once weekly in the morning for 4 weeks.
Report a problemFND-1221122511
05HumanRandomized controlled trialPharmacokinetics
In healthy men, Cmax nearly doubled after single-dose 10 mg CET/glu compared with 10 mg CET/wat.
In plain wordsIn healthy men, peak drug levels nearly doubled after single-dose 10 mg CET/glu compared with 10 mg CET/wat.
Peptide
Cetrorelix
Outcome
IncreaseCmax after single dose
Study
n: not reported in source
Comparator
10 mg CET/wat
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
10 mg CET/glu · subcutaneous · Once weekly for 4 weeksAs given in this study (human).
Source sentences
Summary
On average, Cmax was nearly doubled after single and multiple doses, and AUC(tau) was increased by about 50% after single doses and about 30% after multiple doses of 10 mg CET/glu as compared to 10 mg CET/wat.
1 context sentence(design, population, supporting numbers)
Summary · context
In a randomized parallel-group study, single subcutaneous doses of cetrorelix acetate (concentration: 2.5 mg peptide base/ml) dissolved in aqueous gluconic acid (CET/glu, dose: 5 or 10 mg peptide base) or in water (CET/wat, dose: 10 mg peptide base) were given to 36 subjects once weekly in the morning for 4 weeks.
Report a problemFND-1221122506
06HumanRandomized controlled trialPharmacokinetics
In healthy men, Cmax nearly doubled after multiple doses of 10 mg CET/glu compared with 10 mg CET/wat.
In plain wordsIn healthy men, peak drug levels nearly doubled after multiple doses of 10 mg CET/glu compared with 10 mg CET/wat.
Peptide
Cetrorelix
Outcome
IncreaseCmax after multiple doses
Study
n: not reported in source
Comparator
10 mg CET/wat
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
10 mg CET/glu · subcutaneous · Once weekly for 4 weeksAs given in this study (human).
Source sentences
Summary
On average, Cmax was nearly doubled after single and multiple doses, and AUC(tau) was increased by about 50% after single doses and about 30% after multiple doses of 10 mg CET/glu as compared to 10 mg CET/wat.
1 context sentence(design, population, supporting numbers)
Summary · context
In a randomized parallel-group study, single subcutaneous doses of cetrorelix acetate (concentration: 2.5 mg peptide base/ml) dissolved in aqueous gluconic acid (CET/glu, dose: 5 or 10 mg peptide base) or in water (CET/wat, dose: 10 mg peptide base) were given to 36 subjects once weekly in the morning for 4 weeks.
Report a problemFND-1221122507
07HumanRandomized controlled trialPharmacokinetics
In healthy men, single-dose 10 mg CET/glu increased AUC(tau) by about 50% compared with 10 mg CET/wat.
In plain wordsIn healthy men, single-dose 10 mg CET/glu increased drug exposure by about 50% compared with 10 mg CET/wat.
Peptide
Cetrorelix
Outcome
IncreaseAUC after single dose
Study
n: not reported in source
Comparator
10 mg CET/wat
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
10 mg CET/glu · subcutaneous · Once weekly for 4 weeksAs given in this study (human).
Measurements
AUC(tau) increase after single dose
≈ 50%
10 mg CET/glu versus 10 mg CET/wat
Source sentences
Summary
On average, Cmax was nearly doubled after single and multiple doses, and AUC(tau) was increased by about 50% after single doses and about 30% after multiple doses of 10 mg CET/glu as compared to 10 mg CET/wat.
1 context sentence(design, population, supporting numbers)
Summary · context
In a randomized parallel-group study, single subcutaneous doses of cetrorelix acetate (concentration: 2.5 mg peptide base/ml) dissolved in aqueous gluconic acid (CET/glu, dose: 5 or 10 mg peptide base) or in water (CET/wat, dose: 10 mg peptide base) were given to 36 subjects once weekly in the morning for 4 weeks.
Report a problemFND-1221122508
08HumanRandomized controlled trialPharmacokinetics
In healthy men, multiple doses of 10 mg CET/glu increased AUC(tau) by about 30% compared with 10 mg CET/wat.
In plain wordsIn healthy men, multiple doses of 10 mg CET/glu increased drug exposure by about 30% compared with 10 mg CET/wat.
Peptide
Cetrorelix
Outcome
IncreaseAUC after multiple doses
Study
n: not reported in source
Comparator
10 mg CET/wat
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
10 mg CET/glu · subcutaneous · Once weekly for 4 weeksAs given in this study (human).
Measurements
AUC(tau) increase after multiple doses
≈ 30%
10 mg CET/glu versus 10 mg CET/wat
Source sentences
Summary
On average, Cmax was nearly doubled after single and multiple doses, and AUC(tau) was increased by about 50% after single doses and about 30% after multiple doses of 10 mg CET/glu as compared to 10 mg CET/wat.
1 context sentence(design, population, supporting numbers)
Summary · context
In a randomized parallel-group study, single subcutaneous doses of cetrorelix acetate (concentration: 2.5 mg peptide base/ml) dissolved in aqueous gluconic acid (CET/glu, dose: 5 or 10 mg peptide base) or in water (CET/wat, dose: 10 mg peptide base) were given to 36 subjects once weekly in the morning for 4 weeks.
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09HumanNon-randomized trialEfficacy outcome
In healthy men, all cetrorelix formulations started at least half-maximum testosterone suppression within less than 1 day.
In plain wordsIn healthy men, all cetrorelix formulations started substantial testosterone suppression within less than 1 day.
Peptide
Cetrorelix
Outcome
DecreaseOnset of testosterone suppression
Study
n = 36
Outcome group
Sex hormones and fertility · Endocrine and hormones
Studied dose
CET/glu 5 or 10 mg peptide base; CET/wat 10 mg peptide base · subcutaneous · Once weekly for 4 weeksAs given in this study (human).
Measurements
Onset of at least half-maximum testosterone suppression
< 1 day
All treatments
Source sentences
Summary
At least half-maximum testosterone suppression started with all treatments within less than 1 day.
1 context sentence(design, population, supporting numbers)
Summary · context
In a randomized parallel-group study, single subcutaneous doses of cetrorelix acetate (concentration: 2.5 mg peptide base/ml) dissolved in aqueous gluconic acid (CET/glu, dose: 5 or 10 mg peptide base) or in water (CET/wat, dose: 10 mg peptide base) were given to 36 subjects once weekly in the morning for 4 weeks.
Report a problemFND-1221122501
10HumanNon-randomized trialEfficacy outcome
In healthy men, cetrorelix substantially suppressed LH.
In plain wordsIn healthy men, cetrorelix substantially suppressed LH.
Peptide
Cetrorelix
Outcome
DecreaseLH suppression
Study
n = 36
Outcome group
Sex hormones and fertility · Endocrine and hormones
Studied dose
CET/glu 5 or 10 mg peptide base; CET/wat 10 mg peptide base · subcutaneous · Once weekly for 4 weeksAs given in this study (human).
Source sentences
Summary
Substantial suppression was also evidentfor luteinizing hormone (LH) and, to a lesser extent, forfollicle-stimulating hormone (FSH).
1 context sentence(design, population, supporting numbers)
Summary · context
In a randomized parallel-group study, single subcutaneous doses of cetrorelix acetate (concentration: 2.5 mg peptide base/ml) dissolved in aqueous gluconic acid (CET/glu, dose: 5 or 10 mg peptide base) or in water (CET/wat, dose: 10 mg peptide base) were given to 36 subjects once weekly in the morning for 4 weeks.
Report a problemFND-1221122504
11HumanNon-randomized trialEfficacy outcome
In healthy men, cetrorelix suppressed FSH to a lesser extent than LH.
In plain wordsIn healthy men, cetrorelix suppressed FSH less than LH.
Peptide
Cetrorelix
Outcome
DecreaseFSH suppression
Study
n = 36
Outcome group
Sex hormones and fertility · Endocrine and hormones
Studied dose
CET/glu 5 or 10 mg peptide base; CET/wat 10 mg peptide base · subcutaneous · Once weekly for 4 weeksAs given in this study (human).
Source sentences
Summary
Substantial suppression was also evidentfor luteinizing hormone (LH) and, to a lesser extent, forfollicle-stimulating hormone (FSH).
1 context sentence(design, population, supporting numbers)
Summary · context
In a randomized parallel-group study, single subcutaneous doses of cetrorelix acetate (concentration: 2.5 mg peptide base/ml) dissolved in aqueous gluconic acid (CET/glu, dose: 5 or 10 mg peptide base) or in water (CET/wat, dose: 10 mg peptide base) were given to 36 subjects once weekly in the morning for 4 weeks.
Report a problemFND-1221122505

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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

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