Absorption, distribution, metabolism, and excretion of tirzepatide in humans, rats, and monkeys.

Martin JA, Czeskis B, Urva S, Cassidy KC

European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences5 Sept 2024Cited by 8 (Europe PMC)

PMID39243911DOI10.1016/j.ejps.2024.106895PepBankPUB-39243911

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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: CC BY-NC-ND. Results still quote short attributed sentences.

Results from this study9

9 results from studies that gave the peptide. 6 results from people.

01HumanNon-randomized trialPharmacokinetics
In healthy men given a single subcutaneous dose of [14C]-tirzepatide, most of the excreted dose was recovered within 480 hours.
In plain wordsIn healthy men given one dose of tirzepatide, most of the dose that left the body did so within 480 hours.
Peptide
Tirzepatide
Outcome
Not applicableExcretion of radioactivity over time
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
approximately 2.9 mg (single dose) · subcutaneous · single doseAs given in this study (human).
Measurements
Time window for majority of excreted dose
480 h
human, single SC dose
Source sentences
Summary
Following a single SC dose of [¹⁴C]-tirzepatide in humans, the majority of the excreted dose was recovered within 480 h.
1 context sentence(design, population, supporting numbers)
Summary · context
Healthy male participants received a single subcutaneous dose of approximately 2.9 mg tirzepatide containing approximately 100 μCi of [¹⁴C]-tirzepatide.
Report a problemFND-3924391101
02HumanNon-randomized trialPharmacokinetics
In healthy men, about 66% of administered radioactivity was recovered in urine and about 33% in feces after a single tirzepatide dose.
In plain wordsIn healthy men, about two thirds of a tirzepatide dose left in urine and about one third in feces.
Peptide
Tirzepatide
Outcome
Not applicableRoute of elimination in humans
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
approximately 2.9 mg (single dose) · subcutaneous · single doseAs given in this study (human).
Measurements
Radioactivity recovered in urine
66%
human
Radioactivity recovered in feces
33%
human
Source sentences
Summary
Renal excretion was identified as a principal route of elimination in all species with approximately 66 % of the administered radioactivity recovered in urine, while approximately 33 % was eliminated in feces in humans.
1 context sentence(design, population, supporting numbers)
Summary · context
Healthy male participants received a single subcutaneous dose of approximately 2.9 mg tirzepatide containing approximately 100 μCi of [¹⁴C]-tirzepatide.
Report a problemFND-3924391102
03HumanNon-randomized trialPharmacokinetics
In healthy men, the parent drug was the major circulating component in plasma after a single tirzepatide dose.
In plain wordsIn healthy men, most of the tirzepatide in the blood was the original drug, not a breakdown product.
Peptide
Tirzepatide
Outcome
Not applicableCirculating components in human plasma
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
approximately 2.9 mg (single dose) · subcutaneous · single doseAs given in this study (human).
Source sentences
Summary
Metabolite analysis of tirzepatide revealed the parent drug was the major circulating component in human, rat, and monkey plasma.
1 context sentence(design, population, supporting numbers)
Summary · context
Healthy male participants received a single subcutaneous dose of approximately 2.9 mg tirzepatide containing approximately 100 μCi of [¹⁴C]-tirzepatide.
Report a problemFND-3924391104
04HumanNon-randomized trialPharmacokinetics
In healthy men, circulating metabolites of tirzepatide were similar to those in rats and monkeys, and none exceeded 10% of the total drug-related exposure.
In plain wordsIn healthy men, tirzepatide breakdown products in blood were similar to those in rats and monkeys, and none was a large share.
Peptide
Tirzepatide
Outcome
Not applicableCirculating metabolites in human plasma compared with rats and monkeys
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
approximately 2.9 mg (single dose) · subcutaneous · single doseAs given in this study (human).
Source sentences
Summary
Metabolites identified in human plasma were similar to circulating metabolites found in rats and monkeys with no circulating metabolites representing >10 % of the total radioactive drug-related exposure.
1 context sentence(design, population, supporting numbers)
Summary · context
Healthy male participants received a single subcutaneous dose of approximately 2.9 mg tirzepatide containing approximately 100 μCi of [¹⁴C]-tirzepatide.
Report a problemFND-3924391106
05HumanNon-randomized trialPharmacokinetics
In healthy men, intact tirzepatide was not observed in urine or feces.
In plain wordsIn healthy men, no unchanged tirzepatide was found in urine or feces.
Peptide
Tirzepatide
Outcome
Not applicableIntact tirzepatide in urine and feces in humans
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
approximately 2.9 mg (single dose) · subcutaneous · single doseAs given in this study (human).
Source sentences
Summary
Intact tirzepatide was not observed in urine or feces in any species.
1 context sentence(design, population, supporting numbers)
Summary · context
Healthy male participants received a single subcutaneous dose of approximately 2.9 mg tirzepatide containing approximately 100 μCi of [¹⁴C]-tirzepatide.
Report a problemFND-3924391107
06HumanNon-randomized trialMechanism
In the [14C]-tirzepatide study, tirzepatide was metabolized mainly by proteolytic cleavage of the amino acid backbone, beta-oxidation of the C20 diacid moiety and amide hydrolysis.
In plain wordsIn this study, the body broke tirzepatide down mainly by cutting its amino acid chain, oxidizing its fatty acid part and amide hydrolysis.
Peptide
Tirzepatide
Outcome
Not applicableMetabolic pathways of tirzepatide
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
approximately 2.9 mg (single dose) · subcutaneous · single doseAs given in this study (human).
Source sentences
Summary
Tirzepatide was primarily metabolized via proteolytic cleavage of the amino acid backbone, β-oxidation of the C20 diacid moiety, and amide hydrolysis.
1 context sentence(design, population, supporting numbers)
Summary · context
Healthy male participants received a single subcutaneous dose of approximately 2.9 mg tirzepatide containing approximately 100 μCi of [¹⁴C]-tirzepatide.
Report a problemFND-3924391109
07AnimalAnimal study (in vivo)Pharmacokinetics
In rats and monkeys given a single dose of [14C]-tirzepatide, renal excretion was a principal route of elimination.
In plain wordsIn rats and monkeys, the kidneys were a main way the body removed a single dose of tirzepatide.
Peptide
Tirzepatide
Outcome
Not applicableRoute of elimination in rats and monkeys
Study
Rat (Sprague Dawley, Long Evans) and cynomolgus monkeyn: not reported in source
in vivo
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
3 mg/kg (rats); 0.5 mg/kg (monkeys) · single doseAs given in this study (Rat (Sprague Dawley, Long Evans) and cynomolgus monkey).
Source sentences
Summary
Renal excretion was identified as a principal route of elimination in all species
1 context sentence(design, population, supporting numbers)
Summary · context
Preclinical studies were conducted in male Sprague Dawley and Long Evans rats administered a single dose of 3 mg kg^-1 (133 µCi/kg) of [¹⁴C]-tirzepatide, and male cynomolgus monkeys administered a single dose of 0.5 mg kg^-1 (20 µCi/kg) of [¹⁴C]-tirzepatide.
Report a problemFND-3924391103
08AnimalAnimal study (in vivo)Pharmacokinetics
In rats and monkeys, the parent drug was the major circulating component in plasma after a single dose of tirzepatide.
In plain wordsIn rats and monkeys, most of the tirzepatide in the blood was the original drug.
Peptide
Tirzepatide
Outcome
Not applicableCirculating components in rat and monkey plasma
Study
Rat (Sprague Dawley, Long Evans) and cynomolgus monkeyn: not reported in source
in vivo
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
3 mg/kg (rats); 0.5 mg/kg (monkeys) · single doseAs given in this study (Rat (Sprague Dawley, Long Evans) and cynomolgus monkey).
Source sentences
Summary
Metabolite analysis of tirzepatide revealed the parent drug was the major circulating component in human, rat, and monkey plasma.
1 context sentence(design, population, supporting numbers)
Summary · context
Preclinical studies were conducted in male Sprague Dawley and Long Evans rats administered a single dose of 3 mg kg^-1 (133 µCi/kg) of [¹⁴C]-tirzepatide, and male cynomolgus monkeys administered a single dose of 0.5 mg kg^-1 (20 µCi/kg) of [¹⁴C]-tirzepatide.
Report a problemFND-3924391105
09AnimalAnimal study (in vivo)Pharmacokinetics
In rats and monkeys, intact tirzepatide was not observed in urine or feces.
In plain wordsIn rats and monkeys, no unchanged tirzepatide was found in urine or feces.
Peptide
Tirzepatide
Outcome
Not applicableIntact tirzepatide in urine and feces in rats and monkeys
Study
Rat (Sprague Dawley, Long Evans) and cynomolgus monkeyn: not reported in source
in vivo
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
3 mg/kg (rats); 0.5 mg/kg (monkeys) · single doseAs given in this study (Rat (Sprague Dawley, Long Evans) and cynomolgus monkey).
Source sentences
Summary
Intact tirzepatide was not observed in urine or feces in any species.
1 context sentence(design, population, supporting numbers)
Summary · context
Preclinical studies were conducted in male Sprague Dawley and Long Evans rats administered a single dose of 3 mg kg^-1 (133 µCi/kg) of [¹⁴C]-tirzepatide, and male cynomolgus monkeys administered a single dose of 0.5 mg kg^-1 (20 µCi/kg) of [¹⁴C]-tirzepatide.
Report a problemFND-3924391108

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
12 Oct 2026, 12:58 UTC
Study results updated
Version 1
9 Oct 2026, 03:07 UTC
First added · source update from Europe PMC

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Terms as the source lists them.

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