Characterization of the Pharmacokinetics and Mass Balance of a Single Oral Dose of Trofinetide in Healthy Male Subjects.

Darwish M, Nunez R, Youakim JM, Robertson P Jr

Clinical drug investigation28 Nov 2023Cited by 7 (Europe PMC)

PMID38017349PMCIDPMC10769996DOI10.1007/s40261-023-01322-2PepBankPUB-38017349

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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. Results still quote short attributed sentences.

Results from this study17

17 results from studies that gave the peptide. 17 results from people.

01HumanNon-randomized trialPharmacokinetics
In healthy men after trofinetide, blood drug and total radioactivity profiles were nearly superimposable through approximately 12 hours.
In plain wordsIn healthy men after trofinetide, blood drug and total radioactivity profiles were nearly identical through approximately 12 hours.
Peptide
Trofinetide
Outcome
Not applicableBlood parent and total radioactivity profiles
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
12 g, mixture of trofinetide and radiolabeled trofinetide · oral · single doseAs given in this study (human).
Source sentences
Summary
Blood concentration-time profiles of trofinetide and total radioactivity were almost superimposable up to ~12 h after dosing.
2 context sentences(design, population, supporting numbers)
Summary · context
This Phase 1, open-label, single-dose trial conducted in healthy male adults
Summary · context
following administration of an oral 12-g dose administered as a mixture of trofinetide and [¹⁴C]-trofinetide.
Report a problemFND-3801734901
02HumanNon-randomized trialPharmacokinetics
In healthy men after trofinetide, urine drug and total radioactivity concentration-time profiles were similar.
In plain wordsIn healthy men after trofinetide, urine drug and total radioactivity profiles were similar.
Peptide
Trofinetide
Outcome
Not applicableUrine parent and total radioactivity profiles
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
12 g, mixture of trofinetide and radiolabeled trofinetide · oral · single doseAs given in this study (human).
Source sentences
Summary
Urine concentration-time profiles of trofinetide and total radioactivity were similar.
2 context sentences(design, population, supporting numbers)
Summary · context
This Phase 1, open-label, single-dose trial conducted in healthy male adults
Summary · context
following administration of an oral 12-g dose administered as a mixture of trofinetide and [¹⁴C]-trofinetide.
Report a problemFND-3801734902
03HumanNon-randomized trialPharmacokinetics
In healthy men, trofinetide was rapidly absorbed and had an initial decline half-life of approximately 2.6 hours.
In plain wordsIn healthy men, trofinetide entered the blood rapidly and had an initial decline half-life of approximately 2.6 hours.
Peptide
Trofinetide
Outcome
Not applicableInitial decline half-life
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
12 g, mixture of trofinetide and radiolabeled trofinetide · oral · single doseAs given in this study (human).
Measurements
Alpha half-life
≈ 2.6 h
reported result
Source sentences
Summary
Trofinetide was rapidly absorbed into the circulation with an initial rapid decline (half-life [t_½] _alpha ~2.6 h), followed by a relatively slow terminal elimination phase (t_{½ beta} ~20 h).
2 context sentences(design, population, supporting numbers)
Summary · context
This Phase 1, open-label, single-dose trial conducted in healthy male adults
Summary · context
following administration of an oral 12-g dose administered as a mixture of trofinetide and [¹⁴C]-trofinetide.
Report a problemFND-3801734903
04HumanNon-randomized trialPharmacokinetics
In healthy men, trofinetide had a slower terminal elimination half-life of approximately 20 hours.
In plain wordsIn healthy men, trofinetide had a terminal elimination half-life of approximately 20 hours.
Peptide
Trofinetide
Outcome
Not applicableTerminal elimination half-life
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
12 g, mixture of trofinetide and radiolabeled trofinetide · oral · single doseAs given in this study (human).
Measurements
Beta half-life
≈ 20 h
reported result
Source sentences
Summary
Trofinetide was rapidly absorbed into the circulation with an initial rapid decline (half-life [t_½] _alpha ~2.6 h), followed by a relatively slow terminal elimination phase (t_{½ beta} ~20 h).
2 context sentences(design, population, supporting numbers)
Summary · context
This Phase 1, open-label, single-dose trial conducted in healthy male adults
Summary · context
following administration of an oral 12-g dose administered as a mixture of trofinetide and [¹⁴C]-trofinetide.
Report a problemFND-3801734904
05HumanNon-randomized trialPharmacokinetics
In healthy men after trofinetide, blood-to-plasma radioactivity ratios were 0.529-0.592, indicating little affinity for blood cells.
In plain wordsIn healthy men after trofinetide, radioactivity ratios suggested little affinity for blood cells.
Peptide
Trofinetide
Outcome
Not applicableBlood-to-plasma radioactivity ratio
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
12 g, mixture of trofinetide and radiolabeled trofinetide · oral · single doseAs given in this study (human).
Measurements
Blood-to-plasma radioactivity ratio
0.529 to 0.592 ratio
reported result
Source sentences
Summary
The blood-to-plasma total radioactivity ratios were 0.529-0.592, indicating a lack of affinity for the cellular portion of blood.
2 context sentences(design, population, supporting numbers)
Summary · context
This Phase 1, open-label, single-dose trial conducted in healthy male adults
Summary · context
following administration of an oral 12-g dose administered as a mixture of trofinetide and [¹⁴C]-trofinetide.
Report a problemFND-3801734905
06HumanNon-randomized trialPharmacokinetics
In healthy men after trofinetide, renal excretion accounted for 83.8% of the administered radiochemical dose.
In plain wordsIn healthy men after trofinetide, urine contained 83.8% of the administered radioactive dose.
Peptide
Trofinetide
Outcome
Not applicableRenal recovery of administered radioactivity
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
12 g, mixture of trofinetide and radiolabeled trofinetide · oral · single doseAs given in this study (human).
Measurements
Renal recovery
83.8%
administered radiochemical dose
Source sentences
Summary
Renal excretion accounted for 83.8% of the administered radiochemical dose; 15.1% was recovered in feces.
2 context sentences(design, population, supporting numbers)
Summary · context
This Phase 1, open-label, single-dose trial conducted in healthy male adults
Summary · context
following administration of an oral 12-g dose administered as a mixture of trofinetide and [¹⁴C]-trofinetide.
Report a problemFND-3801734906
07HumanNon-randomized trialPharmacokinetics
In healthy men after trofinetide, fecal recovery accounted for 15.1% of the administered radiochemical dose.
In plain wordsIn healthy men after trofinetide, feces contained 15.1% of the administered radioactive dose.
Peptide
Trofinetide
Outcome
Not applicableFecal recovery of administered radioactivity
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
12 g, mixture of trofinetide and radiolabeled trofinetide · oral · single doseAs given in this study (human).
Measurements
Fecal recovery
15.1%
administered radiochemical dose
Source sentences
Summary
Renal excretion accounted for 83.8% of the administered radiochemical dose; 15.1% was recovered in feces.
2 context sentences(design, population, supporting numbers)
Summary · context
This Phase 1, open-label, single-dose trial conducted in healthy male adults
Summary · context
following administration of an oral 12-g dose administered as a mixture of trofinetide and [¹⁴C]-trofinetide.
Report a problemFND-3801734907
08HumanNon-randomized trialPharmacokinetics
In healthy men after trofinetide, urine and fecal radioactivity recovery reached 99% of the dose at 168 hours.
In plain wordsIn healthy men after trofinetide, urine and feces contained 99% of the radioactive dose at 168 hours.
Peptide
Trofinetide
Outcome
Not applicableTotal radioactivity recovery
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
12 g, mixture of trofinetide and radiolabeled trofinetide · oral · single doseAs given in this study (human).
Measurements
Total recovery
99%
168 h after dosing
Source sentences
Summary
Urine and fecal recovery of radioactivity accounted for 99% of the administered dose at 168 h after dosing.
2 context sentences(design, population, supporting numbers)
Summary · context
This Phase 1, open-label, single-dose trial conducted in healthy male adults
Summary · context
following administration of an oral 12-g dose administered as a mixture of trofinetide and [¹⁴C]-trofinetide.
Report a problemFND-3801734908
09HumanNon-randomized trialPharmacokinetics
In healthy men after trofinetide, parent drug accounted for 88.4% of radiolabeled AUC in pooled blood over 0-12 hours.
In plain wordsIn healthy men after trofinetide, parent drug accounted for 88.4% of radioactive exposure in pooled blood over 0-12 hours.
Peptide
Trofinetide
Outcome
Not applicableParent drug in pooled blood
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
12 g, mixture of trofinetide and radiolabeled trofinetide · oral · single doseAs given in this study (human).
Measurements
Parent drug AUC fraction
88.4%
pooled blood; 0-12 h
Source sentences
Summary
Parent [¹⁴C]-trofinetide was the major radiolabeled entity in blood and plasma (88.4% and 93.1% in area under the concentration-time curves from 0 to 12 h [AUC_0-12] in pooled blood and plasma samples, respectively)
2 context sentences(design, population, supporting numbers)
Summary · context
This Phase 1, open-label, single-dose trial conducted in healthy male adults
Summary · context
following administration of an oral 12-g dose administered as a mixture of trofinetide and [¹⁴C]-trofinetide.
Report a problemFND-3801734909
10HumanNon-randomized trialPharmacokinetics
In healthy men after trofinetide, parent drug accounted for 93.1% of radiolabeled AUC in pooled plasma over 0-12 hours.
In plain wordsIn healthy men after trofinetide, parent drug accounted for 93.1% of radioactive exposure in pooled plasma over 0-12 hours.
Peptide
Trofinetide
Outcome
Not applicableParent drug in pooled plasma
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
12 g, mixture of trofinetide and radiolabeled trofinetide · oral · single doseAs given in this study (human).
Measurements
Parent drug AUC fraction
93.1%
pooled plasma; 0-12 h
Source sentences
Summary
Parent [¹⁴C]-trofinetide was the major radiolabeled entity in blood and plasma (88.4% and 93.1% in area under the concentration-time curves from 0 to 12 h [AUC_0-12] in pooled blood and plasma samples, respectively)
2 context sentences(design, population, supporting numbers)
Summary · context
This Phase 1, open-label, single-dose trial conducted in healthy male adults
Summary · context
following administration of an oral 12-g dose administered as a mixture of trofinetide and [¹⁴C]-trofinetide.
Report a problemFND-3801734910
11HumanNon-randomized trialPharmacokinetics
In healthy men after trofinetide, parent drug accounted for 91.5% of radiolabeled material in pooled urine over 0-48 hours.
In plain wordsIn healthy men after trofinetide, parent drug accounted for 91.5% of radioactive material in pooled urine over 0-48 hours.
Peptide
Trofinetide
Outcome
Not applicableParent drug in pooled urine
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
12 g, mixture of trofinetide and radiolabeled trofinetide · oral · single doseAs given in this study (human).
Measurements
Parent drug fraction
91.5%
0-48-h pooled urine
Source sentences
Summary
and the major entity excreted in urine (91.5% in 0-48-h pooled urine samples) and in feces (52.7% in 0-192-h pooled fecal samples).
2 context sentences(design, population, supporting numbers)
Summary · context
This Phase 1, open-label, single-dose trial conducted in healthy male adults
Summary · context
following administration of an oral 12-g dose administered as a mixture of trofinetide and [¹⁴C]-trofinetide.
Report a problemFND-3801734911
12HumanNon-randomized trialPharmacokinetics
In healthy men after trofinetide, parent drug accounted for 52.7% of radiolabeled material in pooled feces over 0-192 hours.
In plain wordsIn healthy men after trofinetide, parent drug accounted for 52.7% of radioactive material in pooled feces over 0-192 hours.
Peptide
Trofinetide
Outcome
Not applicableParent drug in pooled feces
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
12 g, mixture of trofinetide and radiolabeled trofinetide · oral · single doseAs given in this study (human).
Measurements
Parent drug fraction
52.7%
0-192-h pooled feces
Source sentences
Summary
and the major entity excreted in urine (91.5% in 0-48-h pooled urine samples) and in feces (52.7% in 0-192-h pooled fecal samples).
2 context sentences(design, population, supporting numbers)
Summary · context
This Phase 1, open-label, single-dose trial conducted in healthy male adults
Summary · context
following administration of an oral 12-g dose administered as a mixture of trofinetide and [¹⁴C]-trofinetide.
Report a problemFND-3801734912
13HumanNon-randomized trialPharmacokinetics
In healthy men after trofinetide, two minor metabolites each represented at most 2.24% of pooled blood and plasma AUC.
In plain wordsIn healthy men after trofinetide, two minor metabolites each represented at most 2.24% of blood and plasma exposure.
Peptide
Trofinetide
Outcome
Not applicableMinor metabolites in blood and plasma
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
12 g, mixture of trofinetide and radiolabeled trofinetide · oral · single doseAs given in this study (human).
Measurements
Minor metabolites
2 metabolites
reported result
Each metabolite AUC fraction
≤ 2.24%
0-12 h pool
Source sentences
Summary
In blood and plasma, only two minor metabolites were identified (each metabolite ≤ 2.24% of the AUC_0-12 pool).
2 context sentences(design, population, supporting numbers)
Summary · context
This Phase 1, open-label, single-dose trial conducted in healthy male adults
Summary · context
following administration of an oral 12-g dose administered as a mixture of trofinetide and [¹⁴C]-trofinetide.
Report a problemFND-3801734913
14HumanNon-randomized trialPharmacokinetics
In healthy men after trofinetide, the two minor circulating metabolites also appeared in urine and feces at no more than 2.41% of dose.
In plain wordsIn healthy men after trofinetide, the two minor metabolites also appeared in urine and feces at no more than 2.41% of dose.
Peptide
Trofinetide
Outcome
Not applicableMinor metabolites in urine and feces
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
12 g, mixture of trofinetide and radiolabeled trofinetide · oral · single doseAs given in this study (human).
Measurements
Metabolite recovery
≤ 2.41 % of dose
urine and feces
Source sentences
Summary
These two metabolites were also observed in urine and fecal samples (≤ 2.41% of dose).
3 context sentences(design, population, supporting numbers)
Summary · context
In blood and plasma, only two minor metabolites were identified (each metabolite ≤ 2.24% of the AUC_0-12 pool).
Summary · context
This Phase 1, open-label, single-dose trial conducted in healthy male adults
Summary · context
following administration of an oral 12-g dose administered as a mixture of trofinetide and [¹⁴C]-trofinetide.
Report a problemFND-3801734914
15HumanNon-randomized trialPharmacokinetics
In healthy men after trofinetide, one additional fecal metabolite represented 0.84% of dose.
In plain wordsIn healthy men after trofinetide, one additional fecal metabolite represented 0.84% of dose.
Peptide
Trofinetide
Outcome
Not applicableAdditional fecal metabolite
Study
n: not reported in source
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
12 g, mixture of trofinetide and radiolabeled trofinetide · oral · single doseAs given in this study (human).
Measurements
Additional fecal metabolite
0.84 % of dose
reported result
Source sentences
Summary
In feces, one additional metabolite (0.84% of dose) was identified.
2 context sentences(design, population, supporting numbers)
Summary · context
This Phase 1, open-label, single-dose trial conducted in healthy male adults
Summary · context
following administration of an oral 12-g dose administered as a mixture of trofinetide and [¹⁴C]-trofinetide.
Report a problemFND-3801734915
16HumanNon-randomized trialSafety outcome
In healthy men after trofinetide, two mild treatment-emergent adverse events occurred in two participants and were considered unrelated to treatment.
In plain wordsIn healthy men after trofinetide, two participants had mild adverse events that investigators considered unrelated to treatment.
Peptide
Trofinetide
Outcome
Not applicableTreatment-emergent adverse events
Study
n: not reported in source
Outcome group
Adverse events · Whole body
Studied dose
12 g, mixture of trofinetide and radiolabeled trofinetide · oral · single doseAs given in this study (human).
Measurements
TEAEs
2 events
reported result
Participants with TEAEs
2 participants
reported result
Source sentences
Summary
Two mild TEAEs were reported in two participants and were not considered related to trofinetide.
2 context sentences(design, population, supporting numbers)
Summary · context
This Phase 1, open-label, single-dose trial conducted in healthy male adults
Summary · context
following administration of an oral 12-g dose administered as a mixture of trofinetide and [¹⁴C]-trofinetide.
Report a problemFND-3801734916
17HumanNon-randomized trialSafety outcome
In healthy men after trofinetide, laboratory parameters, vital signs, physical findings and electrocardiogram results showed no clinically meaningful changes.
In plain wordsIn healthy men after trofinetide, laboratory tests, vital signs, examinations and heart tracings showed no clinically meaningful changes.
Peptide
Trofinetide
Outcome
Direction not reportedLaboratory parameters, vital signs, physical findings and ECG
Study
n: not reported in source
Outcome group
Adverse events · Whole body
Studied dose
12 g, mixture of trofinetide and radiolabeled trofinetide · oral · single doseAs given in this study (human).
Source sentences
Summary
There were no clinically meaningful changes in individual laboratory parameters, vital signs, physical findings, or electrocardiogram results.
2 context sentences(design, population, supporting numbers)
Summary · context
This Phase 1, open-label, single-dose trial conducted in healthy male adults
Summary · context
following administration of an oral 12-g dose administered as a mixture of trofinetide and [¹⁴C]-trofinetide.
Report a problemFND-3801734917

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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, 16:37 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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