Kinetics and disposition of hexarelin, a peptidic growth hormone secretagogue, in rats.

Roumi M, Marleau S, du Souich P, Maggi T, Deghenghi R, Ong H

Drug metabolism and disposition: the biological fate of chemicals1 Jan 2000Cited by 9 (Europe PMC)

PMID10611139DOI10.1016/s0090-9556(24)11760-6PepBankPUB-10611139

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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 study15

15 results from studies that gave the peptide. No result from this study comes from people.

01AnimalAnimal study (in vivo)Pharmacokinetics
In rats given an intravenous bolus, hexarelin had a half-life of 75.9 min.
In plain wordsIn rats, hexarelin given into a vein had a half-life of 75.9 minutes.
Peptide
Hexarelin
Outcome
Not applicableHalf-life after i.v. bolus
Study
ratn: not reported in source
male Sprague-Dawley rats
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
5 microg/kg · intravenous bolus · single doseAs given in this study (rat).
Measurements
half-life
75.9 min
i.v. 5 microg/kg
Source sentences
Summary
After its i.v. injection, hexarelin displayed a half-life of 75.9 +/- 9.3 min, a systemic clearance of 7.6 +/- 0.7 ml/min/kg, and a volume of distribution at steady state of 744 +/- 81 ml/kg.
1 context sentence(design, population, supporting numbers)
Summary · context
To document the disposition of hexarelin, a peptidyl growth hormone secretagogue, male Sprague-Dawley rats received a 5-microg/kg bolus i.v. dose or three single s.c. doses of 5, 10, and 50 microg/kg.
Report a problemFND-1061113901
02AnimalAnimal study (in vivo)Pharmacokinetics
In rats given an intravenous bolus, hexarelin had a systemic clearance of 7.6 ml/min/kg.
In plain wordsIn rats, hexarelin given into a vein was cleared from the body at 7.6 ml per minute per kg.
Peptide
Hexarelin
Outcome
Not applicableSystemic clearance after i.v. bolus
Study
ratn: not reported in source
male Sprague-Dawley rats
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
5 microg/kg · intravenous bolus · single doseAs given in this study (rat).
Measurements
systemic clearance
7.6 ml/min/kg
i.v. 5 microg/kg
Source sentences
Summary
After its i.v. injection, hexarelin displayed a half-life of 75.9 +/- 9.3 min, a systemic clearance of 7.6 +/- 0.7 ml/min/kg, and a volume of distribution at steady state of 744 +/- 81 ml/kg.
1 context sentence(design, population, supporting numbers)
Summary · context
To document the disposition of hexarelin, a peptidyl growth hormone secretagogue, male Sprague-Dawley rats received a 5-microg/kg bolus i.v. dose or three single s.c. doses of 5, 10, and 50 microg/kg.
Report a problemFND-1061113902
03AnimalAnimal study (in vivo)Pharmacokinetics
In rats given an intravenous bolus, hexarelin had a volume of distribution at steady state of 744 ml/kg.
In plain wordsIn rats, hexarelin given into a vein had a steady-state distribution volume of 744 ml per kg.
Peptide
Hexarelin
Outcome
Not applicableVolume of distribution at steady state after i.v. bolus
Study
ratn: not reported in source
male Sprague-Dawley rats
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
5 microg/kg · intravenous bolus · single doseAs given in this study (rat).
Measurements
volume of distribution at steady state
744 ml/kg
i.v. 5 microg/kg
Source sentences
Summary
After its i.v. injection, hexarelin displayed a half-life of 75.9 +/- 9.3 min, a systemic clearance of 7.6 +/- 0.7 ml/min/kg, and a volume of distribution at steady state of 744 +/- 81 ml/kg.
1 context sentence(design, population, supporting numbers)
Summary · context
To document the disposition of hexarelin, a peptidyl growth hormone secretagogue, male Sprague-Dawley rats received a 5-microg/kg bolus i.v. dose or three single s.c. doses of 5, 10, and 50 microg/kg.
Report a problemFND-1061113903
04AnimalAnimal study (in vivo)Pharmacokinetics
In rats given subcutaneous doses, the area under the curve of hexarelin ranged from 477 to 3826 pmol.min/ml with increasing doses.
In plain wordsIn rats, blood exposure to hexarelin rose with the injected dose.
Peptide
Hexarelin
Outcome
Not applicableArea under the curve after s.c. doses
Study
ratn: not reported in source
male Sprague-Dawley rats
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
5, 10 and 50 microg/kg · subcutaneous · single doseAs given in this study (rat).
Measurements
AUC
477 to 3826 pmol.min/ml
s.c. doses
Source sentences
Summary
After s.c. administration, the area under the curve (477-3826 pmol.min/ml) estimated with increasing doses confirmed the absence of hexarelin accumulation.
1 context sentence(design, population, supporting numbers)
Summary · context
To document the disposition of hexarelin, a peptidyl growth hormone secretagogue, male Sprague-Dawley rats received a 5-microg/kg bolus i.v. dose or three single s.c. doses of 5, 10, and 50 microg/kg.
Report a problemFND-1061113904
05AnimalAnimal study (in vivo)Pharmacokinetics
In rats given subcutaneous doses, the area under the curve confirmed the absence of hexarelin accumulation.
In plain wordsIn rats, hexarelin did not build up in the body after injections under the skin.
Peptide
Hexarelin
Outcome
No significant changeAccumulation after s.c. doses
Study
ratn: not reported in source
male Sprague-Dawley rats
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
5, 10 and 50 microg/kg · subcutaneous · single doseAs given in this study (rat).
Source sentences
Summary
After s.c. administration, the area under the curve (477-3826 pmol.min/ml) estimated with increasing doses confirmed the absence of hexarelin accumulation.
1 context sentence(design, population, supporting numbers)
Summary · context
To document the disposition of hexarelin, a peptidyl growth hormone secretagogue, male Sprague-Dawley rats received a 5-microg/kg bolus i.v. dose or three single s.c. doses of 5, 10, and 50 microg/kg.
Report a problemFND-1061113905
06AnimalAnimal study (in vivo)Pharmacokinetics
In rats given subcutaneous doses, hexarelin clearance/F was dose independent at 12-15 ml/min/kg.
In plain wordsIn rats, how fast hexarelin was cleared after injection under the skin did not depend on the dose.
Peptide
Hexarelin
Outcome
No significant changeClearance/F after s.c. doses
Study
ratn: not reported in source
male Sprague-Dawley rats
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
5, 10 and 50 microg/kg · subcutaneous · single doseAs given in this study (rat).
Measurements
clearance/F
12 to 15 ml/min/kg
s.c. doses
Source sentences
Summary
Clearance/F (12-15 ml/min/kg) and volume of distribution/F (1208-1222 ml/kg) were dose independent.
1 context sentence(design, population, supporting numbers)
Summary · context
To document the disposition of hexarelin, a peptidyl growth hormone secretagogue, male Sprague-Dawley rats received a 5-microg/kg bolus i.v. dose or three single s.c. doses of 5, 10, and 50 microg/kg.
Report a problemFND-1061113906
07AnimalAnimal study (in vivo)Pharmacokinetics
In rats given subcutaneous doses, hexarelin volume of distribution/F was dose independent at 1208-1222 ml/kg.
In plain wordsIn rats, the volume hexarelin spread into after injection under the skin did not depend on the dose.
Peptide
Hexarelin
Outcome
No significant changeVolume of distribution/F after s.c. doses
Study
ratn: not reported in source
male Sprague-Dawley rats
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
5, 10 and 50 microg/kg · subcutaneous · single doseAs given in this study (rat).
Measurements
volume of distribution/F
1208 to 1222 ml/kg
s.c. doses
Source sentences
Summary
Clearance/F (12-15 ml/min/kg) and volume of distribution/F (1208-1222 ml/kg) were dose independent.
1 context sentence(design, population, supporting numbers)
Summary · context
To document the disposition of hexarelin, a peptidyl growth hormone secretagogue, male Sprague-Dawley rats received a 5-microg/kg bolus i.v. dose or three single s.c. doses of 5, 10, and 50 microg/kg.
Report a problemFND-1061113907
08AnimalAnimal study (in vivo)Pharmacokinetics
In rats, the bioavailability of subcutaneous hexarelin was 64%.
In plain wordsIn rats, 64% of hexarelin injected under the skin reached the blood.
Peptide
Hexarelin
Outcome
Not applicableSubcutaneous bioavailability
Study
ratn: not reported in source
male Sprague-Dawley rats
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
5, 10 and 50 microg/kg · subcutaneous · single doseAs given in this study (rat).
Measurements
bioavailability
64%
s.c.
Source sentences
Summary
Hexarelin bioavailability given s.c. was 64%.
1 context sentence(design, population, supporting numbers)
Summary · context
To document the disposition of hexarelin, a peptidyl growth hormone secretagogue, male Sprague-Dawley rats received a 5-microg/kg bolus i.v. dose or three single s.c. doses of 5, 10, and 50 microg/kg.
Report a problemFND-1061113908
09AnimalAnimal study (in vivo)Pharmacokinetics
In rats given [3H]hexarelin, the highest radioactivity levels were in the kidney, liver and duodenum.
In plain wordsIn rats, labelled hexarelin was found most in the kidney, liver and duodenum.
Peptide
Hexarelin
Outcome
Not applicableTissue distribution of radiolabelled hexarelin
Study
ratn: not reported in source
male Sprague-Dawley rats
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
1 microg/kgAs given in this study (rat).
Source sentences
Summary
The highest radioactivity levels were detected in the kidney, liver, and duodenum.
2 context sentences(design, population, supporting numbers)
Summary · context
To assess hexarelin tissue distribution and excretion, rats were given 1 microg/kg of [(3)H]hexarelin (9.4 Ci/mmol).
Summary · context
To document the disposition of hexarelin, a peptidyl growth hormone secretagogue, male Sprague-Dawley rats received a 5-microg/kg bolus i.v. dose or three single s.c. doses of 5, 10, and 50 microg/kg.
Report a problemFND-1061113909
10AnimalAnimal study (in vivo)Pharmacokinetics
In rats, the pattern of hexarelin excretion was similar after intravenous and subcutaneous administration.
In plain wordsIn rats, hexarelin left the body in a similar way after injection into a vein or under the skin.
Peptide
Hexarelin
Outcome
No significant changeExcretion pattern after i.v. or s.c. administration
Study
ratn: not reported in source
male Sprague-Dawley rats
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
Dose not stated · intravenous or subcutaneousAs given in this study (rat).
Source sentences
Summary
The pattern of hexarelin excretion was similar after i.v. or s.c. administrations.
1 context sentence(design, population, supporting numbers)
Summary · context
To document the disposition of hexarelin, a peptidyl growth hormone secretagogue, male Sprague-Dawley rats received a 5-microg/kg bolus i.v. dose or three single s.c. doses of 5, 10, and 50 microg/kg.
Report a problemFND-1061113910
11AnimalAnimal study (in vivo)Pharmacokinetics
In rats, 60% of the dose was recovered as radioactivity in bile.
In plain wordsIn rats, about 60% of the hexarelin dose left the body in bile.
Peptide
Hexarelin
Outcome
Not applicableBiliary excretion of radioactivity
Study
ratn: not reported in source
male Sprague-Dawley rats
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
Dose not stated
Measurements
radioactivity in bile
60 % of dose
bile
Source sentences
Summary
Total radioactivity in bile, urine, and feces corresponded to 60, 22, and 10% of the dose, respectively.
1 context sentence(design, population, supporting numbers)
Summary · context
To document the disposition of hexarelin, a peptidyl growth hormone secretagogue, male Sprague-Dawley rats received a 5-microg/kg bolus i.v. dose or three single s.c. doses of 5, 10, and 50 microg/kg.
Report a problemFND-1061113911
12AnimalAnimal study (in vivo)Pharmacokinetics
In rats, 22% of the dose was recovered as radioactivity in urine.
In plain wordsIn rats, about 22% of the hexarelin dose left the body in urine.
Peptide
Hexarelin
Outcome
Not applicableUrinary excretion of radioactivity
Study
ratn: not reported in source
male Sprague-Dawley rats
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
Dose not stated
Measurements
radioactivity in urine
22 % of dose
urine
Source sentences
Summary
Total radioactivity in bile, urine, and feces corresponded to 60, 22, and 10% of the dose, respectively.
1 context sentence(design, population, supporting numbers)
Summary · context
To document the disposition of hexarelin, a peptidyl growth hormone secretagogue, male Sprague-Dawley rats received a 5-microg/kg bolus i.v. dose or three single s.c. doses of 5, 10, and 50 microg/kg.
Report a problemFND-1061113912
13AnimalAnimal study (in vivo)Pharmacokinetics
In rats, 10% of the dose was recovered as radioactivity in feces.
In plain wordsIn rats, about 10% of the hexarelin dose left the body in feces.
Peptide
Hexarelin
Outcome
Not applicableFecal excretion of radioactivity
Study
ratn: not reported in source
male Sprague-Dawley rats
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
Dose not stated
Measurements
radioactivity in feces
10 % of dose
feces
Source sentences
Summary
Total radioactivity in bile, urine, and feces corresponded to 60, 22, and 10% of the dose, respectively.
1 context sentence(design, population, supporting numbers)
Summary · context
To document the disposition of hexarelin, a peptidyl growth hormone secretagogue, male Sprague-Dawley rats received a 5-microg/kg bolus i.v. dose or three single s.c. doses of 5, 10, and 50 microg/kg.
Report a problemFND-1061113913
14AnimalAnimal study (in vivo)Pharmacokinetics
In rats, 90% of the radioactivity excreted in bile was unchanged hexarelin.
In plain wordsIn rats, most hexarelin in bile (90%) was still intact.
Peptide
Hexarelin
Outcome
Not applicableUnchanged hexarelin in bile
Study
ratn: not reported in source
male Sprague-Dawley rats
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
Dose not stated
Measurements
unchanged hexarelin in bile
90%
bile
Source sentences
Summary
Of the radioactivity excreted in bile and urine, 90 and 71% was unchanged hexarelin, respectively.
1 context sentence(design, population, supporting numbers)
Summary · context
To document the disposition of hexarelin, a peptidyl growth hormone secretagogue, male Sprague-Dawley rats received a 5-microg/kg bolus i.v. dose or three single s.c. doses of 5, 10, and 50 microg/kg.
Report a problemFND-1061113914
15AnimalAnimal study (in vivo)Pharmacokinetics
In rats, 71% of the radioactivity excreted in urine was unchanged hexarelin.
In plain wordsIn rats, most hexarelin in urine (71%) was still intact.
Peptide
Hexarelin
Outcome
Not applicableUnchanged hexarelin in urine
Study
ratn: not reported in source
male Sprague-Dawley rats
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
Dose not stated
Measurements
unchanged hexarelin in urine
71%
urine
Source sentences
Summary
Of the radioactivity excreted in bile and urine, 90 and 71% was unchanged hexarelin, respectively.
1 context sentence(design, population, supporting numbers)
Summary · context
To document the disposition of hexarelin, a peptidyl growth hormone secretagogue, male Sprague-Dawley rats received a 5-microg/kg bolus i.v. dose or three single s.c. doses of 5, 10, and 50 microg/kg.
Report a problemFND-1061113915

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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
13 Oct 2026, 21:44 UTC
Study results updated
Version 1
13 Oct 2026, 16:31 UTC
First added · source update from Europe PMC

Subjects

Terms as the source lists them.

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MeSH terms

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