Healthy VolunteersPhase 1NCT03811834

A Study to Assess Absolute Bioavailability (ABA) of Mobocertinib (TAK-788) and to Characterize Mass Balance, Pharmacokinetics (PK), Metabolism, and Excretion of Carbon-14 ([14C])-Mobocertinib in Male Healthy Participants

A Phase 1 study testing Mobocertinib in people with Healthy Volunteers, run by Millennium Pharmaceuticals, Inc. at 1 site in United States.

Completed

Finished. The study has ended and is not enrolling. Results may be posted on the official record.

Official record

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Trial summary

The purpose of this study is to determine: Period 1 (ABA): ABA of mobocertinib following single microdose intravenous administration of 50 microgram (mcg) (approximately 2 microcurie [mcCi]) [14 C]-]-mobocertinib and single oral administration of 160 milligram (mg) mobocertinib. Read more about this study

Who is it for?: Ages 19 to 55 years, men onlyHealthy volunteers can take part
Conditions the study is for: Healthy Volunteers
What is being tested?: Mobocertinib
Type of treatment: Pill or oral medicine, Injection or infusion
Could I receive a placebo?: No, everyone receives an active treatment
How many people: 7 participants
Where: 1 siteUnited States
Study dates: 22 Jan 2019to 11 Mar 2019
Phase: Phase 1
Are there results?: Yes, posted in the registrySummary in the doctors' view

Key requirements

Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.

Ages 19 to 55 years
Men only
Healthy volunteers accepted
Adult

Who may be able to join

Continuous non smoker who has not used nicotine containing products for at least 20 years prior to the first dosing and throughout the study, based on subject self-reporting.
Body mass index greater than or equal to (>=)18 and less than (˂) 30.0 kilogram per square meter (kg/m^2) at screening.

Who cannot join

Is mentally or legally incapacitated or has significant emotional problems at the time of the screening visit or expected during the conduct of the study.
Has history or presence of alcoholism or drug abuse within the past 2 years prior to the first dosing.
Has positive urine drug or alcohol results at screening or first check in.
Estimated creatinine clearance < 80 milliliter per minute (mL/min) at screening.
Has tattoo(s) or scarring at or near the site of intravenous (IV) infusion or any other condition which may interfere with infusion site examination, in the opinion of the investigator.
Has infrequent bowel movements (less than approximately once per day) within 30 days prior to first dosing.

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Has recent history of abnormal bowel movements, such as diarrhea, loose stools, or constipation, within 2 weeks of first dosing.
Has received radiolabeled substances or has been exposed to radiation sources within 12 months of first dosing or is likely to receive radiation exposure or radioisotopes within 12 months of first dosing such that participation in this study would increase their total exposure beyond the recommended levels considered safe (that is., weighted annual limit recommended by the Commission on Radiological Protection [ICRP] of 3000 millirem).
Donation of blood or significant blood loss within 56 days prior to the first dosing.
Plasma donation within 7 days prior to the first dosing.

Trial locations and contacts

1 site in 1 country.

United States1 site

Celerion
Lincoln, Nebraska, 68502

Other trials in United States

About this study

Official title: A Phase 1 Study to Assess Absolute Bioavailability of TAK-788 and to Characterize Mass Balance, Pharmacokinetics, Metabolism, and Excretion of [14C]-TAK-788 in Male Healthy Subjects

The purpose of this study is to determine:

Period 1 (ABA): ABA of mobocertinib following single microdose intravenous administration of 50 microgram (mcg) (approximately 2 microcurie [mcCi]) [14 C]-]-mobocertinib and single oral administration of 160 milligram (mg) mobocertinib.

Period 2 (absorption, distribution, metabolism, and elimination [ADME]): the mass balance and metabolic profile of mobocertinib in plasma, urine, and feces, to characterize the PK of mobocertinib and its metabolites (AP32960 and AP32914) in plasma, whole blood, and urine, and total radioactivity concentration equivalents in plasma and whole blood following a single oral administration of 160 mg (approximately 100 mcCi) [14C]-mobocertinib solution.

Read the detailed description

The drug being tested in this study is called mobocertinib. The study will determine ABA of mobocertinib following single microdose of 50 mcg [14C]-mobocertinib and single oral administration of 160 mg mobocertinib and will assess the mass balance and metabolic profile of mobocertinib in plasma, urine, and feces following a single oral administration of 160 mg [14C]-mobocertinib solution, and will characterize the PK of mobocertinib and its metabolites in plasma, whole blood, and urine, and total radioactivity concentration equivalents in plasma and whole blood following a single dose of 160 mg [14C]-mobocertinib.

The study will enroll approximately 6 participants. The study is designed to consist of 2 periods: Period 1 (ABA study period) and Period 2 (ADME study period). In Period 1, all participants will receive single unlabeled oral 160 mg dose of mobocertinib as capsules. At 3.75 hours post oral dosing, participants will receive 15-minute intravenous infusion of a microdose of 50 mcg (approximately 2mcCi) [14C]-mobocertinib. In Period 2, participants will receive single dose of 160 mg (approximately 100 mcCi) [14C]-mobocertinib as an oral solution.

This single center trial will be conducted in the United States. The overall time to participate in this study is approximately 65 days including screening period. Participants will be contacted approximately 30 days after the last dose of study drug for a follow-up assessment.

Conditions: Healthy Volunteers
Being tested: Mobocertinib
Keywords: Drug Therapy

What participants receive

What participants receive. In a randomised study each person is assigned to one group by chance.

MobocertinibDrug
Also called TAK-788
Mobocertinib capsule, [14C]-Mobocertinib intravenous infusion, [14C]-Mobocertinib oral solution.

Study groups in NCT03811834
Study group	Role	What they receive
Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg + [14C]-Mobocertinib 160 mg	Experimental	Mobocertinib 160 mg, capsule, orally, once under fasted state, followed by [14C]-mobocertinib 50 mcg (approximately 2 microcurie [mcCi]), infusion, intravenously, once on Day 1 of Period 1, further followed by a washout period of 9 days, followed by [14C]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2. Receives: Drug: Mobocertinib

What is being measured

The primary outcome is the main question the study is designed to answer.

Period 1: Percent Absolute Oral Bioavailability (%F) for Mobocertinib
Absolute bioavailability (F), defined as the fraction or percentage of the unchanged, orally administered dose that is systemically available, relative to the total dose administered intravenously. Percent Absolute Oral Bioavailability (%F) was calculated as dose of [14C]-mobocertinib intravenous in mg*AUC∞ of mobocertinib (oral)/dose of mobocertinib (oral)* AUC∞ of [14C]-mobocertinib (intravenous)*100.
Measured: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Period 2: Percentage of Total Radioactivity (Cum%Dose) Recovered in Urine Relative to the Administered Radioactive Dose
Measured: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2: Percentage of Total Radioactivity (Cum%Dose) Recovered in Feces Relative to the Administered Radioactive Dose
Measured: Day 1 pre-dose and at multiple time points (up to 432 hours) post-dose
Period 2: Amount of Total Radioactivity Excreted in Urine (Ae[UR])
Measured: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2: Amount of Total Radioactivity Excreted in Feces (Ae[Fe])
Measured: Day 1 pre-dose and at multiple time points (up to 432 hours) post-dose
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib
Measured: Day 1: Pre-dose, 0-12 hours (hrs), 12-24 hrs, 24-48 hrs, 48-72 hrs, 72-96 hrs, 96-120 hrs, 120-144 hrs, 144-168 hrs, 168-192 hrs, 192-216 hrs, 216-240 hrs post-dose
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib
Measured: Day 1: at Pre-dose, 0-24 hours (hrs), 24-48 hrs, 48-72 hrs, 72-96 hrs, 96-120 hrs, 120-144 hrs, 144-168 hrs, 168-192 hrs, 192-216 hrs, 216-240 hrs; 240-264 hrs, 264-288 hrs, 288-312 hrs, 213-408 hrs and 408-432 hrs
Period 2, Cmax: Maximum Observed Plasma and Whole Blood Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914)
Measured: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2, Tmax: Time to Reach the Maximum Plasma and Whole Blood Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914)
Measured: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2: t(1/2): Terminal Disposition Phase Half-life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma and Whole Blood
Measured: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2, AUC∞: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914)
Measured: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2, AUClast: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914)
Measured: Day 1 pre-dose at multiple time points (up to 240 hours) post-dose
Period 2, AUCt: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Time t for Mobocertinib and Its Metabolites (AP32960 and AP32914)
Measured: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2, Cmax: Maximum Observed Plasma Radioactivity Concentration Equivalents for [14C]-Mobocertinib
Measured: Day 1 pre-dose at multiple time points (up to 240 hours) post-dose
Period 2, Cmax: Maximum Observed Whole Blood Radioactivity Concentration Equivalents for [14C]-Mobocertinib
Measured: Day 1 pre-dose at multiple time points (up to 240 hours) post-dose
Period 2, Tmax: Time to Reach the Maximum Plasma and Whole Blood Radioactivity Concentration (Cmax) Equivalents for [14C]-Mobocertinib
Measured: Day 1 pre-dose at multiple time points (up to 240 hours) post-dose
Period 2, t(1/2z): Terminal Disposition Phase Half-life of Plasma and Whole Blood Radioactivity Concentration Equivalents for [14C]-Mobocertinib
Measured: Day 1 pre-dose at multiple time points (up to 240 hours) post-dose
Period 2, AUC∞: Area Under the Plasma Radioactivity Concentration Equivalents-time Curve From Time 0 to Infinity for [14C]-Mobocertinib
Measured: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2, AUC∞: Area Under the Whole Blood Radioactivity Concentration Equivalents-time Curve From Time 0 to Infinity for [14C]-Mobocertinib
Measured: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2, AUClast: Area Under the Plasma Radioactivity Concentration Equivalents -Time Curve From Time 0 to Last Quantifiable Concentration for [14C]-Mobocertinib
Measured: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2, AUClast: Area Under the Whole Blood Radioactivity Concentration Equivalents -Time Curve From Time 0 to Last Quantifiable Concentration for [14C]- Mobocertinib
Measured: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2, AUCt : Area Under the Plasma Radioactivity Concentration Equivalents-time Curve From Time 0 to Time t for [14C]-Mobocertinib
Measured: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2, AUCt : Area Under the Whole Blood Radioactivity Concentration Equivalents-time Curve From Time 0 to Time t for [14C]-Mobocertinib
Measured: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914)
Measured: Day 1: at Pre-dose, 0-12 hours (hrs), 12-24 hrs, 24-48 hrs, 48-72 hrs, 72-96 hrs, 96-120 hrs, 120-144 hrs, 144-168 hrs, 168-192 hrs, 192-216 hrs and 216-240 hrs post dose
Period 2, CLR: Renal Clearance for Mobocertinib and Its Metabolites (AP32960 and AP32914)
Measured: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio)
Measured: At 0.5 hours (hrs), 1 hr, 2 hrs, 3 hrs, 4 hrs, 5 hrs, 6 hrs, 8 hrs, 12 hrs, 24 hrs, 36 hrs, 48 hrs, 72 hrs, 96 hrs, 120 hrs, 144 hrs, 168 hrs, 192 hrs, 216 hrs and 240 hrs post-dose

Secondary outcomes (14)

Period 1, Ceoi: Plasma Concentration at the End of Infusion for [14C]-Mobocertinib, and Its Metabolites ([14C]-AP32960 and [14C]-AP32914)
Measured: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Period 1, Cmax: Maximum Observed Plasma Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration
Measured: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Period 1, Cmax: Maximum Observed Plasma Concentration for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration
Measured: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Period 1, Time to Reach the Maximum Plasma Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral, and [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration
Data for mobocertinib and its metabolites (AP32960 and AP32914) is reported following the oral administration, and data for [14C]-mobocertinib and its metabolites ([14C]-AP32960 and [14C]-AP32914) is reported following intravenous administration.
Measured: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Period 1, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration
Measured: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Period 1, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) After Intravenous Administration
Measured: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Period 1, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration
Measured: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Period 1, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to Last Quantifiable Concentration for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration
Measured: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Period 1, AUCt: Area Under the Plasma Concentration-time Curve From Time 0 to Time t for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration
Measured: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Period 1, t(1/2):Terminal Disposition Phase Half-Life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma After Oral, and [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) in Plasma After Intravenous Administration
Data for mobocertinib and its metabolites (AP32960 and AP32914) is reported following the oral administration, and data for [14C]-mobocertinib and its metabolites ([14C]-AP32960 and [14C]-AP32914) is reported following intravenous administration.
Measured: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Number of Participants Reporting One or More Treatment-emergent Adverse Events (TEAEs)
Measured: Baseline up to 30 days after last dose of study drug in Period 2 (Day 41)
Number of Participants With Clinically Significant Change From Baseline in 12-lead Electrocardiogram (ECG) Findings
Measured: Baseline up to 30 days after last dose of study drug in Period 2 (Day 41)
Number of Participants With Clinically Significant Change From Baseline in Vital Signs
Measured: Baseline up to 30 days after last dose of study drug in Period 2 (Day 41)
Number of Participants With Clinically Significant Change From Baseline in Laboratory Values
Measured: Baseline up to 30 days after last dose of study drug in Period 2 (Day 41)

Timeline

From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.

22 Jan 201911 Mar 2019

First posted22 Jan 2019
Study start22 Jan 2019
Primary completion11 Mar 2019
Study completion11 Mar 2019

Resources

Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
Posted resultsParticipant flow, outcome measures and adverse events reported by the sponsor.
Publications (1)Papers the sponsor has linked to this study.
Other trials for Healthy VolunteersStudies of the same condition, open and under way.
What the trial phases meanHow a treatment moves from first tests in people to approval.

More details

For doctors and researchers: how the study is designed, who runs it, and its registry IDs.

Study design

Study type: Interventional
Phase: Phase 1
Primary purpose: Other
Allocation: Not applicable
Intervention model: Single group
Masking: None (open label)
Enrolment: 7 participants (actual)

IDs, dates and publications

ClinicalTrials.gov ID: NCT03811834
Sponsor's protocol ID: TAK-788-1002
Other IDs: U1111-1223-7593
Status last verified: Feb 2024
First submitted: 18 Jan 2019
Last updated: 12 Feb 2024
Results posted: Yes, on ClinicalTrials.gov
Data monitoring committee: No
FDA-regulated drug: Yes
FDA-regulated device: No
Individual data sharing: No: De-identified individual participant data from this particular study will not be shared as there is a reasonable likelihood that individual patients could be re-identified (due to the limited number of study participants/study sites)

Publications

Hanley MJ, Zhang S, Griffin R, Zhu SX, Fram RJ, Lin J, Venkatakrishnan K, Gupta N. A phase 1 study to assess the absolute bioavailability, mass balance, pharmacokinetics, metabolism, and excretion of [14C]-mobocertinib, an oral inhibitor of EGFR exon 20 insertion mutations, in healthy participants. Invest New Drugs. 2024 Aug;42(4):343-352. doi: 10.1007/s10637-024-01446-y. Epub 2024 May 24.
PubMed 38789848

Want to know more?

The sponsor has not listed a contact. The official record may have more details.

Talk to your doctor first and take this page with you. Only the study team can confirm whether you can join.

Questions to ask the study team

What is the study trying to find out?
What would I need to do, and how often would I visit?
Could I receive a placebo instead of the treatment?
What are the possible risks and benefits for me?
Will it cost me anything? Are travel or time paid for?
Can I keep seeing my own doctor during the study?
What happens when the study ends?

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Study at a glance

From the registry record, last updated by the sponsor on 12 Feb 2024. Recruitment status is as the sponsor reported it: confirm with the study team.

Official title: A Phase 1 Study to Assess Absolute Bioavailability of TAK-788 and to Characterize Mass Balance, Pharmacokinetics, Metabolism, and Excretion of [14C]-TAK-788 in Male Healthy Subjects
ClinicalTrials.gov ID: NCT03811834
Acronym / sponsor ID: TAK-788-1002
Conditions: Healthy Volunteers
Keywords: Drug Therapy
Phase: Phase 1
Study type: Interventional
Recruitment status: Completed
Enrolment: 7 participants (actual)
Lead sponsor: Millennium Pharmaceuticals, Inc.Industry (pharma, biotech, devices)
Study start: 22 Jan 2019 (actual)
Primary completion: 11 Mar 2019 (actual)
Study completion: 11 Mar 2019 (actual)
First posted: 22 Jan 2019 (actual)
Results: Posted 30 Jul 2021

Clinical summary

The research question as the sponsor registered it. This describes what the study plans to test, not what it found.

The purpose of this study is to determine:

Detailed description

Study design

Primary purpose: Other
Allocation: Not applicable
Intervention model: Single group
Masking: None (open label)
Number of arms: 1

Arm	Type	Receives
Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg + [14C]-Mobocertinib 160 mg	Experimental	Drug: MobocertinibMobocertinib 160 mg, capsule, orally, once under fasted state, followed by [14C]-mobocertinib 50 mcg (approximately 2 microcurie [mcCi]), infusion, intravenously, once on Day 1 of Period 1, further followed by a washout period of 9 days, followed by [14C]-mobocertinib 160 mg (approximately 100 mcCi), solution, orally, once under fasted state on Day 1 of Period 2.

Who may qualify

Ages: 19 to 55 years
Sex: Male only
Healthy volunteers: Accepted
Age groups: Adult

Key inclusion criteria (2 listed)

Continuous non smoker who has not used nicotine containing products for at least 20 years prior to the first dosing and throughout the study, based on subject self-reporting.
Body mass index greater than or equal to (>=)18 and less than (˂) 30.0 kilogram per square meter (kg/m^2) at screening.

Key exclusion criteria (10 listed)

Is mentally or legally incapacitated or has significant emotional problems at the time of the screening visit or expected during the conduct of the study.
Has history or presence of alcoholism or drug abuse within the past 2 years prior to the first dosing.
Has positive urine drug or alcohol results at screening or first check in.
Estimated creatinine clearance < 80 milliliter per minute (mL/min) at screening.
Has tattoo(s) or scarring at or near the site of intravenous (IV) infusion or any other condition which may interfere with infusion site examination, in the opinion of the investigator.

Eligibility is decided by the study team after screening; this overview does not establish that a patient qualifies. Full inclusion and exclusion criteria.

Interventions

Intervention	Type	Arms
MobocertinibAlso: TAK-788Mobocertinib capsule, [14C]-Mobocertinib intravenous infusion, [14C]-Mobocertinib oral solution.	Drug	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg + [14C]-Mobocertinib 160 mg

Primary outcome

Period 1: Percent Absolute Oral Bioavailability (%F) for Mobocertinib
Time frame: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Absolute bioavailability (F), defined as the fraction or percentage of the unchanged, orally administered dose that is systemically available, relative to the total dose administered intravenously. Percent Absolute Oral Bioavailability (%F) was calculated as dose of [14C]-mobocertinib intravenous in mg*AUC∞ of mobocertinib (oral)/dose of mobocertinib (oral)* AUC∞ of [14C]-mobocertinib (intravenous)*100.
Period 2: Percentage of Total Radioactivity (Cum%Dose) Recovered in Urine Relative to the Administered Radioactive Dose
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2: Percentage of Total Radioactivity (Cum%Dose) Recovered in Feces Relative to the Administered Radioactive Dose
Time frame: Day 1 pre-dose and at multiple time points (up to 432 hours) post-dose
Period 2: Amount of Total Radioactivity Excreted in Urine (Ae[UR])
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2: Amount of Total Radioactivity Excreted in Feces (Ae[Fe])
Time frame: Day 1 pre-dose and at multiple time points (up to 432 hours) post-dose
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Urine for Mobocertinib
Time frame: Day 1: Pre-dose, 0-12 hours (hrs), 12-24 hrs, 24-48 hrs, 48-72 hrs, 72-96 hrs, 96-120 hrs, 120-144 hrs, 144-168 hrs, 168-192 hrs, 192-216 hrs, 216-240 hrs post-dose
Period 2: Percentage of Administered Radioactive Dose (%Dose) Excreted in Feces for Mobocertinib
Time frame: Day 1: at Pre-dose, 0-24 hours (hrs), 24-48 hrs, 48-72 hrs, 72-96 hrs, 96-120 hrs, 120-144 hrs, 144-168 hrs, 168-192 hrs, 192-216 hrs, 216-240 hrs; 240-264 hrs, 264-288 hrs, 288-312 hrs, 213-408 hrs and 408-432 hrs
Period 2, Cmax: Maximum Observed Plasma and Whole Blood Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914)
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2, Tmax: Time to Reach the Maximum Plasma and Whole Blood Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914)
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2: t(1/2): Terminal Disposition Phase Half-life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma and Whole Blood
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2, AUC∞: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914)
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2, AUClast: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914)
Time frame: Day 1 pre-dose at multiple time points (up to 240 hours) post-dose
Period 2, AUCt: Area Under the Plasma and Whole Blood Concentration-time Curve From Time 0 to Time t for Mobocertinib and Its Metabolites (AP32960 and AP32914)
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2, Cmax: Maximum Observed Plasma Radioactivity Concentration Equivalents for [14C]-Mobocertinib
Time frame: Day 1 pre-dose at multiple time points (up to 240 hours) post-dose
Period 2, Cmax: Maximum Observed Whole Blood Radioactivity Concentration Equivalents for [14C]-Mobocertinib
Time frame: Day 1 pre-dose at multiple time points (up to 240 hours) post-dose
Period 2, Tmax: Time to Reach the Maximum Plasma and Whole Blood Radioactivity Concentration (Cmax) Equivalents for [14C]-Mobocertinib
Time frame: Day 1 pre-dose at multiple time points (up to 240 hours) post-dose
Period 2, t(1/2z): Terminal Disposition Phase Half-life of Plasma and Whole Blood Radioactivity Concentration Equivalents for [14C]-Mobocertinib
Time frame: Day 1 pre-dose at multiple time points (up to 240 hours) post-dose
Period 2, AUC∞: Area Under the Plasma Radioactivity Concentration Equivalents-time Curve From Time 0 to Infinity for [14C]-Mobocertinib
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2, AUC∞: Area Under the Whole Blood Radioactivity Concentration Equivalents-time Curve From Time 0 to Infinity for [14C]-Mobocertinib
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2, AUClast: Area Under the Plasma Radioactivity Concentration Equivalents -Time Curve From Time 0 to Last Quantifiable Concentration for [14C]-Mobocertinib
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2, AUClast: Area Under the Whole Blood Radioactivity Concentration Equivalents -Time Curve From Time 0 to Last Quantifiable Concentration for [14C]- Mobocertinib
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2, AUCt : Area Under the Plasma Radioactivity Concentration Equivalents-time Curve From Time 0 to Time t for [14C]-Mobocertinib
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2, AUCt : Area Under the Whole Blood Radioactivity Concentration Equivalents-time Curve From Time 0 to Time t for [14C]-Mobocertinib
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2, Aet1-t2: Amount of Unchanged Drug Excreted in the Urine in Each Collection Interval From t1 to t2 for Mobocertinib and Its Metabolites (AP32960 and AP32914)
Time frame: Day 1: at Pre-dose, 0-12 hours (hrs), 12-24 hrs, 24-48 hrs, 48-72 hrs, 72-96 hrs, 96-120 hrs, 120-144 hrs, 144-168 hrs, 168-192 hrs, 192-216 hrs and 216-240 hrs post dose
Period 2, CLR: Renal Clearance for Mobocertinib and Its Metabolites (AP32960 and AP32914)
Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Period 2, Percentage Change of [14C]-Radioactivity in Whole Blood Relative to Plasma Over the Time for [14C]-Mobocertinib, (Whole Blood : Plasma Partitioning Ratio)
Time frame: At 0.5 hours (hrs), 1 hr, 2 hrs, 3 hrs, 4 hrs, 5 hrs, 6 hrs, 8 hrs, 12 hrs, 24 hrs, 36 hrs, 48 hrs, 72 hrs, 96 hrs, 120 hrs, 144 hrs, 168 hrs, 192 hrs, 216 hrs and 240 hrs post-dose

14 secondary outcomes

Period 1, Ceoi: Plasma Concentration at the End of Infusion for [14C]-Mobocertinib, and Its Metabolites ([14C]-AP32960 and [14C]-AP32914)
Time frame: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Period 1, Cmax: Maximum Observed Plasma Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration
Time frame: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Period 1, Cmax: Maximum Observed Plasma Concentration for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration
Time frame: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Period 1, Time to Reach the Maximum Plasma Concentration (Cmax) for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral, and [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration
Time frame: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Period 1, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration
Time frame: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Period 1, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) After Intravenous Administration
Time frame: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Period 1, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to Last Quantifiable Concentration for Mobocertinib and Its Metabolites (AP32960 and AP32914) After Oral Administration
Time frame: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Period 1, AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to Last Quantifiable Concentration for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration
Time frame: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Period 1, AUCt: Area Under the Plasma Concentration-time Curve From Time 0 to Time t for [14C]-Mobocertinib and Its Metabolites ([14C]-AP32960 and [14C]-AP32914) After Intravenous Administration
Time frame: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Period 1, t(1/2):Terminal Disposition Phase Half-Life of Mobocertinib and Its Metabolites (AP32960 and AP32914) in Plasma After Oral, and [14C]-Mobocertinib and Its Metabolites ( [14C]-AP32960 and [14C]-AP32914) in Plasma After Intravenous Administration
Time frame: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose
Number of Participants Reporting One or More Treatment-emergent Adverse Events (TEAEs)
Time frame: Baseline up to 30 days after last dose of study drug in Period 2 (Day 41)
Number of Participants With Clinically Significant Change From Baseline in 12-lead Electrocardiogram (ECG) Findings
Time frame: Baseline up to 30 days after last dose of study drug in Period 2 (Day 41)
Number of Participants With Clinically Significant Change From Baseline in Vital Signs
Time frame: Baseline up to 30 days after last dose of study drug in Period 2 (Day 41)
Number of Participants With Clinically Significant Change From Baseline in Laboratory Values
Time frame: Baseline up to 30 days after last dose of study drug in Period 2 (Day 41)

Results and safety

Results posted to the registry on 30 Jul 2021, as reported by the sponsor. Figures are copied from the record, not re-analysed. Full results on ClinicalTrials.gov.

Participant flow

Group	Started	Completed
Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg + [14C]-Mobocertinib 160 mg	7	6

Primary outcome: Period 1: Percent Absolute Oral Bioavailability (%F) for Mobocertinib

Time frame: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose. Geometric mean (90% Confidence Interval). Unit: percentage bioavailability

Measure	Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg n = 6
Value	36.7 (22.4 to 60.2)

Population analysed: The pharmacokinetic (PK) set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This outcome measure (OM) was planned to be assessed only in Period 1.

Primary outcome: Period 2: Percentage of Total Radioactivity (Cum%Dose) Recovered in Urine Relative to the Administered Radioactive Dose

Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose. Geometric mean (Geometric Coefficient of Variation). Unit: percentage of radioactive dose

Measure	[14C]-Mobocertinib 160 mg n = 6
Value	3.57 (12.6)

Population analysed: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.

Primary outcome: Period 2: Percentage of Total Radioactivity (Cum%Dose) Recovered in Feces Relative to the Administered Radioactive Dose

Time frame: Day 1 pre-dose and at multiple time points (up to 432 hours) post-dose. Geometric mean (Geometric Coefficient of Variation). Unit: percentage of radioactive dose

Measure	[14C]-Mobocertinib 160 mg n = 6
Value	76.0 (6.5)

Population analysed: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.

Primary outcome: Period 2: Amount of Total Radioactivity Excreted in Urine (Ae[UR])

Time frame: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose. Geometric mean (Geometric Coefficient of Variation). Unit: milligram equivalent (mg eq)

Measure	[14C]-Mobocertinib 160 mg n = 6
Value	5.777 (12.6)

Population analysed: The PK set included all participants who complied sufficiently with the protocol and displayed an evaluable PK profile. This OM was planned to be assessed only in Period 2.

14 secondary outcomes are reported in the full results.

Adverse events

Time frame: Treatment-emergent adverse events are adverse events that started after the first dose of study drug until 30 days after last dose of study drug in Period 2 (up to Day 41). Other adverse events reported at 0% frequency or more

Group	Serious adverse events	Other adverse events	Deaths
Mobocertinib 160 mg and [14C]-Mobocertinib 50 mcg	0 of 7 (0%)	6 of 7 (85.7%)	0 of 7
[14C]-Mobocertinib 160 mg	0 of 6 (0%)	4 of 6 (66.7%)	0 of 6

Loading the posted results from ClinicalTrials.gov…

Research links

Official record on ClinicalTrials.govLast updated by the sponsor 12 Feb 2024.
Posted resultsParticipant flow, baseline, all outcome measures and adverse events.
Derived from this study: PubMed 38789848Hanley MJ, Zhang S, Griffin R, Zhu SX, Fram RJ, Lin J, Venkatakrishnan K, Gupta N. A phase 1 study to assess the absolute bioavailability, mass balance, pharmacokinetics, metabolism, and excretion of [14C]-mobocertinib, an oral inhibitor of EGFR exon 20 insertion mutations, in healthy participants. Invest New Drugs. 2024 Aug;42(4):343-352. doi: 10.1007/s10637-024-01446-y. Epub 2024 May 24.
Individual participant dataSharing planned: No. De-identified individual participant data from this particular study will not be shared as there is a reasonable likelihood that individual patients could be re-identified (due to the limited number of study participants/study sites)

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Referral and contact

AzTrials does not enrol participants or take referrals. Contact the study team or a site listed below; they decide who can take part. This study is not recruiting at the moment.

Medical Director study director

Millennium Pharmaceuticals, Inc.

1 site in 1 country: see every site and its status.

Questions about this trial

What is this clinical trial studying?

A Phase 1 study testing Mobocertinib in people with Healthy Volunteers, run by Millennium Pharmaceuticals, Inc. at 1 site in United States.

The full registered description is in the About this study section and the official record.

Who may be eligible to take part?

The sponsor lists 2 inclusion and 10 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.

Is this clinical trial currently recruiting?

The record says: finished, as of the sponsor's last update on 12 Feb 2024. Status can change between updates, so confirm with the study contact before making plans.

Where is the study taking place?

The record lists 1 site in United States. Whether a site is taking part right now should be confirmed with that site. See every site.

What are the possible benefits and risks?

They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.

What does this phase mean?

Phase 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.

Not every study follows the same path, and some studies (observational studies, device studies) have no phase.

Are results available for this study?

Yes. Results are posted in the registry (first posted 30 Jul 2021). A summary is in the For doctors view, and the full results are on ClinicalTrials.gov.

How can a doctor refer a patient or contact the research team?

The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.

What does the primary outcome measure?

Period 1: Percent Absolute Oral Bioavailability (%F) for Mobocertinib (time frame: Day 1 pre-dose and at multiple time points (up to 144 hours) post-dose). The study lists 26 primary outcomes in all. It is what the study was designed to measure, not a finding.

Where can I read the original study information?

On the ClinicalTrials.gov record for NCT03811834, which also lists 1 linked publication.

Does a listing mean the treatment is approved or proven to work?

No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.

How often is this information updated?

AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 12 Feb 2024.