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CompletedNCT04056455Updated Jan 8, 2024Results posted

A Study of Mobocertinib Capsules in People With Severe Kidney Problems and People With Healthy Kidneys

A Phase 1 interventional study of Mobocertinib in Renal Impairment and Healthy Volunteers, sponsored by Millennium Pharmaceuticals, Inc.. Completed at 2 sites in United States. Open to participants aged 18 Years to 81 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2024-01-08.

Sponsored by Millennium Pharmaceuticals, Inc. · Phase 1, Interventional, and Other

Phase
Phase 1
Study type
Interventional
Enrollment
26
Allocation
Non-randomized
Ages
18 Years to 81 Years
Sex
All
01

Study summary

It is hoped that mobocertinib will eventually help people with cancer with severely reduced kidney function. The main aim of this study is to learn about the levels of mobocertinib in the blood and urine of participants with severely reduced kidney function and participants with healthy kidneys. These participants do not have cancer. The information from this study will be used to work out the best dose of mobocertinib for people with cancer with severely reduced kidney function in the future.

At the first visit, the study doctor will check who can take part. Participants who can take part will be placed into 1 of 2 treatment groups. Participants with severely reduced kidney function will be in 1 group. Participants with healthy kidneys will be in the other group. Participants in both groups will receive the same treatment and the group results will be compared.

Participants from both groups will take 1 capsule of mobocertinib. They will stay in the clinic for 10 days so the study doctors can check the amount of mobocertinib in the blood and urine of these participants over time. The study doctors will also check if the participants have any side effects from this treatment.

The clinic will call the participants 30 days after they took mobocertinib to check if they have any more side effects from their treatment.

Read the detailed description

The drug being tested in this study is called mobocertinib. This study is to assess the pharmacokinetic (PK) of mobocertinib and its active metabolites (AP32960 and AP32914) in participants with severe RI compared to matched-healthy participants with normal renal function.

The study will enroll approximately 24 participants. Participants will be assigned to 1 of the following 2 treatment groups:

  • Severe RI: Mobocertinib 80 mg
  • Normal Renal Function: Mobocertinib 80 mg

Healthy participants with normal renal function will be recruited to match severe RI by age (mean plus or minus [+-] 10 years), gender (+-2 participants per gender), and body mass index (BMI), (mean +- 10 percent [%]). All participants will be asked to take single dose of mobocertinib on Day 1.

This multi-center trial will be conducted in the United States. The overall time to participate in this study is 51 days. Participants will be contacted by telephone 30 days after the last dose of study drug for a follow-up assessment.

02

Conditions studied

  • Renal Impairment
  • Healthy Volunteers

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Keywords

  • Drug Therapy
03

In context

Renal Insufficiency

1,995 studies on the registry are indexed under Renal Insufficiency; 173 are open to participants now.

This study's enrollment of 26 is below the median of 43 across 1,504 interventional studies indexed under Renal Insufficiency.

Browse Renal Insufficiency studies →

Lead sponsor

Millennium Pharmaceuticals, Inc. is the lead sponsor of 173 studies on the registry; none are open to participants now.

Of its 73 completed or terminated interventional studies of FDA-regulated products, 72 (99%) have results posted.

Counted across the registry records on this site, refreshed daily.

04

Who can participate

Ages eligible
18 Years to 81 Years
Sexes eligible
All
Accepts healthy volunteers
Yes

Eligibility criteria

Inclusion Criteria:

Inclusion Criteria for Healthy Participants:

  1. Continuous non-smoker or moderate smoker (less than or equal to [\<=] 10 cigarettes/day or the equivalent) before screening. Participant must agree to consume no more than 5 cigarettes or equivalent/day from the 7 days prior to mobocertinib dosing and throughout the period of PK sample collection.
  2. Body mass index (BMI) greater than or equal to (>=) 18.0 and \<=39.0 kilogram per square meter (kg/m\^2), at screening. Participants will be matched to RI participants by BMI (mean +- 10%) at screening. At least 50% of the participants will be required to be of BMI >=18.0 and \<=35.0 kg/m\^2, at screening.
  3. Medically healthy with no clinically significant medical history, physical examination, laboratory profiles, vital signs or ECGs, as deemed by the Investigator or designee. Has liver function tests including alanine aminotransferase (ALT), Aspartate Aminotransferase (AST), Alkaline phosphatase (ALP), and total bilirubin within the upper limit of normal at screening and at check-in.
  4. Baseline estimated glomerular filtration rate (eGFR) >=90 milliliter per minute per 1.73 square meter (mL/min/1.73 m\^2) based on the Modification of Diet in Renal Disease (MDRD) equation at screening divided by standard body surface area (BSA) value of 1.73 m\^2. For participants with non-standard BSA, the eGFR value calculated by MDRD formula will be multiplied by the individual's BSA calculated using appropriate formula and divided by 1.73 m\^2.

Inclusion Criteria for Participants with RI:

  1. Continuous non-smoker or moderate smoker (\<=10 cigarettes/day or the equivalent) before screening. Participant must agree to consume no more than 5 cigarettes or equivalent/day from the 7 days prior to dose of mobocertinib and throughout the period of PK sample collection.
  2. BMI >=18.0 and \<=39.0 kg/m\^2, at screening. At least 50% of the participants will be required to be of BMI >=18.0 and \<=35.0 kg/m\^2, at screening.
  3. Aside from RI, be sufficiently healthy for study participation based upon medical history, physical examination, vital signs, ECGs, and screening clinical laboratory profiles, as deemed by the Investigator or designee.
  4. Baseline eGFR 15-29 milliliter (mL) not on dialysis based on the MDRD equation at screening divided by standard BSA value of 1.73 m\^2. For participants with non-standard BSA, the eGFR value calculated by MDRD formula will be multiplied by the individual's BSA calculated using appropriate formula and divided by 1.73 m\^2.
  5. Has a diagnosis of chronic (greater than [>] 6 months), stable (no significant changes in renal function [less than [\<] 30%] in the 30 days preceding screening; no acute episodes of illness within the previous 2 months due to deterioration in renal function) renal insufficiency. Participants with RI may have related medical conditions consistent with their disease (example, mild diabetes) that are stable for at least 3 months prior to screening, in the opinion of the Investigator or designee.

Exclusion Criteria

  1. Positive results at screening for human immunodeficiency virus (HIV), Hepatitis B surface antigen (HBsAg), or hepatitis C virus (HCV).
  2. Positive test result for coronavirus disease 2019 (COVID-19) testing at screening or check-in.
  3. Seated heart rate is lower than 40 beats per minute (bpm) or higher than 99 bpm at screening.
  4. Seated blood pressure is less than 90/40 millimeters of mercury (mmHg) or greater than 180/100 mmHg at screening.
  5. Healthy participants: QT interval with Fridericia's correction (QTcF) interval is >=450 millisecond (msec) in males or >=470 msec in females or has ECG findings deemed abnormal with clinical significance by the Investigator or designee at screening
  6. RI participants: QTcF interval is >500 msec or has ECG findings deemed abnormal with clinical significance by the Investigator or designee at screening.
  7. Unable to refrain from or anticipates the use of any medication or substance (including prescription or over-the-counter, vitamin supplements, natural or herbal supplements) as indicated in (Prohibitions and Concomitant Medication) for the prohibited time period.
  8. Been on a diet incompatible with the on-study diet, in the opinion of the Investigator or designee, within the 30 days prior to dosing and throughout the study.
  9. Donation of blood or significant blood loss within 56 days prior to dosing.
  10. Plasma donation within 7 days prior to dosing.
05

Study design

Phase
Phase 1
Primary purpose
Other
Allocation
Non-randomized
Intervention model
Parallel assignment
Masking
None (open label)
Enrollment
26 participants (actual)

Study arms

  • Experimental
    Severe Renal Impairment: Mobocertinib 80 mg

    Participants with severe renal impairment received a single dose of mobocertinib 80 mg, capsule, orally, on Day 1.

    Drug: Mobocertinib

  • Experimental
    Normal Renal Function: Mobocertinib 80 mg

    Participants with normal renal function received a single dose of mobocertinib 80 mg, capsule, orally, on Day 1.

    Drug: Mobocertinib

Interventions

  • DrugMobocertinib

    Mobocertinib capsule.

    Also known as: TAK-788, AP32788

06

What researchers measure

Primary outcomes

  1. Cmax: Maximum Observed Plasma Concentration for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)

    Time frame: Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose

  2. Cmax,u: Maximum Observed Unbound Plasma Concentration for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)

    Time frame: Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose

  3. AUCinf: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)

    Time frame: Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose

  4. AUCinf,u: Area Under the Unbound Plasma Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)

    Time frame: Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose

  5. AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)

    Time frame: Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose

  6. AUClast,u: Area Under the Unbound Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)

    Time frame: Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose

  7. Combined Molar Cmax,u: Combined Molar Unbound Cmax for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)

    Time frame: Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose

  8. Combined Molar AUClast,u: Combined Molar Unbound AUClast for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)

    Time frame: Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose

  9. Combined Molar AUCinf,u: Combined Molar Unbound AUCinf for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)

    Time frame: Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose

  10. Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)

    Time frame: Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose

  11. t1/2z: Terminal Disposition Phase Half-life for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)

    Time frame: Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose

  12. λz: Terminal Elimination Phase Rate Constant for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)

    Terminal elimination rate constant (λz) is a mathematical estimate calculated using log-linear regression of the terminal portions of a plasma concentration against time curve.

    Time frame: Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose

  13. CL/F: Apparent Clearance After Extravascular Administration for Mobocertinib

    Time frame: Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose

  14. CLu/F: Apparent Clearance for Unbound Drug After Extravascular Administration for Mobocertinib

    Time frame: Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose

  15. Vz/F: Apparent Volume of Distribution During the Terminal Disposition Phase After Extravascular Administration for Mobocertinib

    Time frame: Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose

  16. Vz,u/F: Apparent Volume of Distribution for Unbound Drug During the Terminal Disposition Phase After Extravascular Administration for Mobocertinib

    Time frame: Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose

  17. CumAe: Cumulative Amount of Mobocertinib and Its Active Metabolites (AP32960 and AP32914) Excreted in the Urine

    Time frame: Day 1 pre-dose and at multiple time points (up to 120 hours) post-dose

  18. Cumfe: Cumulative Fraction of Mobocertinib Excreted in the Urine

    Time frame: Day 1 pre-dose and at multiple time points (up to 120 hours) post-dose

  19. CLR: Renal Clearance of Mobocertinib and Its Active Metabolites (AP32960 and AP32914)

    Time frame: Day 1 pre-dose and at multiple time points (up to 120 hours) post-dose

Secondary outcomes

  1. Plasma Protein Binding of Mobocertinib and Its Active Metabolites (AP32960 and AP32914)

    Time frame: Day 1 at multiple time points (up to 24 hours) post-dose

  2. Number of Participants Reporting One or More Treatment-emergent Adverse Events (TEAEs)

    An Adverse Event (AE) is defined as any untoward medical occurrence in a clinical investigation participant administered a drug; it does not necessarily have to have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign (eg, a clinically significant abnormal laboratory finding), symptom, or disease temporally associated with the use of a drug, whether or not it is considered related to the drug. A Treatment-emergent Adverse Event (TEAE) is defined as an adverse event with an onset that occurs after receiving study drug.

    Time frame: From first dose of study drug up to end of study (EOS) (up to 40 days)

07

Results

Posted Jan 8, 2024

Participant flow

Participants took part in the study at 3 investigative sites in the United States from 04 March 2020 to 20 April 2022.

Participant flow — Overall Study
MilestoneSevere Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mg
Started1412
Safety analysis set1412
Pharmacokinetic (pk) analysis set1312
Completed1312
Not completed10
Withdrew: Adverse event10

Outcome measures

PrimaryCmax: Maximum Observed Plasma Concentration for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Time frame:
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
Reported as:
Geometric mean · nanograms per milliliter(ng/mL)
Cmax: Maximum Observed Plasma Concentration for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
nanograms per milliliter(ng/mL)Severe Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mg
Mobocertinib17.1 ± 32611.2 ± 69.8
AP3296012.2 ± 51.47.92 ± 45.8
AP329142.24 ± 73.91.51 ± 45.4
PrimaryCmax,u: Maximum Observed Unbound Plasma Concentration for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Time frame:
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
Reported as:
Geometric mean · ng/mL
Cmax,u: Maximum Observed Unbound Plasma Concentration for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
ng/mLSevere Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mg
Mobocertinib0.188 ± 2520.137 ± 106
AP329600.149 ± 53.70.0904 ± 63.9
AP329140.0112 ± 1080.0144 ± 82.7
PrimaryAUCinf: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Time frame:
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
Reported as:
Geometric mean · ng*hours(hr)/mL
AUCinf: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
ng*hours(hr)/mLSevere Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mg
Mobocertinib720 ± 97.8255 ± 58.1
AP32960328 ± 43.6184 ± 36.7
AP3291493.6 ± 73.642.3 ± 33.2
PrimaryAUCinf,u: Area Under the Unbound Plasma Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Time frame:
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
Reported as:
Geometric mean · ng*hr/mL
AUCinf,u: Area Under the Unbound Plasma Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
ng*hr/mLSevere Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mg
Mobocertinib7.61 ± 77.43.16 ± 91.9
AP329604.00 ± 53.22.15 ± 56.6
AP329140.469 ± 1340.461 ± 67.3
PrimaryAUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Time frame:
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
Reported as:
Geometric mean · ng*hr/mL
AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
ng*hr/mLSevere Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mg
Mobocertinib463 ± 184219 ± 70.3
AP32960305 ± 44.4159 ± 42.4
AP3291443.8 ± 12418.7 ± 75.0
PrimaryAUClast,u: Area Under the Unbound Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Time frame:
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
Reported as:
Geometric mean · ng*hr/mL
AUClast,u: Area Under the Unbound Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
ng*hr/mLSevere Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mg
Mobocertinib5.10 ± 1452.68 ± 105
AP329603.72 ± 53.71.82 ± 63.5
AP329140.219 ± 1400.172 ± 132
PrimaryCombined Molar Cmax,u: Combined Molar Unbound Cmax for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Time frame:
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
Reported as:
Geometric mean · nanomolar (nM)
Combined Molar Cmax,u: Combined Molar Unbound Cmax for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
nanomolar (nM)Severe Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mg
Combined Molar Cmax,u: Combined Molar Unbound Cmax for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)0.708 ± 83.70.419 ± 85.2
PrimaryCombined Molar AUClast,u: Combined Molar Unbound AUClast for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Time frame:
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
Reported as:
Geometric mean · nanomolar*hour(nM*hr)
Combined Molar AUClast,u: Combined Molar Unbound AUClast for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
nanomolar*hour(nM*hr)Severe Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mg
Combined Molar AUClast,u: Combined Molar Unbound AUClast for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)16.9 ± 79.58.14 ± 86.2
PrimaryCombined Molar AUCinf,u: Combined Molar Unbound AUCinf for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Time frame:
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
Reported as:
Geometric mean · nM*hr
Combined Molar AUCinf,u: Combined Molar Unbound AUCinf for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
nM*hrSevere Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mg
Combined Molar AUCinf,u: Combined Molar Unbound AUCinf for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)30.1 ± 49.016.8 ± 36.7
PrimaryTmax: Time to Reach the Maximum Plasma Concentration (Cmax) for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Time frame:
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
Reported as:
Median · hours (hr)
Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
hours (hr)Severe Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mg
Mobocertinib6.00 (2.00 to 96.0)6.00 (4.00 to 8.00)
AP329604.00 (2.00 to 12.0)6.00 (2.00 to 6.00)
AP329146.00 (2.00 to 12.0)6.00 (4.00 to 8.00)
Primaryt1/2z: Terminal Disposition Phase Half-life for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Time frame:
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
Reported as:
Geometric mean · hr
t1/2z: Terminal Disposition Phase Half-life for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
hrSevere Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mg
Mobocertinib28.0 ± 41.523.2 ± 24.3
AP3296040.1 ± 38.731.7 ± 23.3
AP3291420.6 ± 58.014.6 ± 37.8
Primaryλz: Terminal Elimination Phase Rate Constant for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)

Terminal elimination rate constant (λz) is a mathematical estimate calculated using log-linear regression of the terminal portions of a plasma concentration against time curve.

Time frame:
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
Reported as:
Geometric mean · per hour (1/hr)
λz: Terminal Elimination Phase Rate Constant for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
per hour (1/hr)Severe Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mg
Mobocertinib0.0248 ± 41.50.0299 ± 24.3
AP329600.0173 ± 38.70.0219 ± 23.3
AP329140.0336 ± 58.00.0475 ± 37.8
PrimaryCL/F: Apparent Clearance After Extravascular Administration for Mobocertinib
Time frame:
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
Reported as:
Geometric mean · Liters per hour (L/hr)
CL/F: Apparent Clearance After Extravascular Administration for Mobocertinib
Liters per hour (L/hr)Severe Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mg
CL/F: Apparent Clearance After Extravascular Administration for Mobocertinib111 ± 97.8314 ± 58.1
PrimaryCLu/F: Apparent Clearance for Unbound Drug After Extravascular Administration for Mobocertinib
Time frame:
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
Reported as:
Geometric mean · L/hr
CLu/F: Apparent Clearance for Unbound Drug After Extravascular Administration for Mobocertinib
L/hrSevere Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mg
CLu/F: Apparent Clearance for Unbound Drug After Extravascular Administration for Mobocertinib10500 ± 77.425300 ± 91.9
PrimaryVz/F: Apparent Volume of Distribution During the Terminal Disposition Phase After Extravascular Administration for Mobocertinib
Time frame:
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
Reported as:
Geometric mean · Liters (L)
Vz/F: Apparent Volume of Distribution During the Terminal Disposition Phase After Extravascular Administration for Mobocertinib
Liters (L)Severe Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mg
Vz/F: Apparent Volume of Distribution During the Terminal Disposition Phase After Extravascular Administration for Mobocertinib4480 ± 85.010500 ± 48.4
PrimaryVz,u/F: Apparent Volume of Distribution for Unbound Drug During the Terminal Disposition Phase After Extravascular Administration for Mobocertinib
Time frame:
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
Reported as:
Geometric mean · Liters (L)
Vz,u/F: Apparent Volume of Distribution for Unbound Drug During the Terminal Disposition Phase After Extravascular Administration for Mobocertinib
Liters (L)Severe Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mg
Vz,u/F: Apparent Volume of Distribution for Unbound Drug During the Terminal Disposition Phase After Extravascular Administration for Mobocertinib424000 ± 61.5847000 ± 87.7
PrimaryCumAe: Cumulative Amount of Mobocertinib and Its Active Metabolites (AP32960 and AP32914) Excreted in the Urine
Time frame:
Day 1 pre-dose and at multiple time points (up to 120 hours) post-dose
Reported as:
Mean · milligrams (mg)
CumAe: Cumulative Amount of Mobocertinib and Its Active Metabolites (AP32960 and AP32914) Excreted in the Urine
milligrams (mg)Severe Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mg
Mobocertinib0.271 ± 0.2160.357 ± 0.200
AP329600.108 ± 0.04570.296 ± 0.129
AP329140.0360 ± 0.02460.0895 ± 0.0361
PrimaryCumfe: Cumulative Fraction of Mobocertinib Excreted in the Urine
Time frame:
Day 1 pre-dose and at multiple time points (up to 120 hours) post-dose
Reported as:
Mean · percentage of dose
Cumfe: Cumulative Fraction of Mobocertinib Excreted in the Urine
percentage of doseSevere Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mg
Cumfe: Cumulative Fraction of Mobocertinib Excreted in the Urine0.339 ± 0.2690.446 ± 0.251
PrimaryCLR: Renal Clearance of Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Time frame:
Day 1 pre-dose and at multiple time points (up to 120 hours) post-dose
Reported as:
Mean · L/hr
CLR: Renal Clearance of Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
L/hrSevere Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mg
Mobocertinib0.694 ± 0.8271.78 ± 1.57
AP329600.373 ± 0.1721.77 ± 0.848
AP329140.683 ± 0.4273.11 ± 1.42
SecondaryPlasma Protein Binding of Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Time frame:
Day 1 at multiple time points (up to 24 hours) post-dose
Reported as:
Mean · percentage bound
Plasma Protein Binding of Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
percentage boundSevere Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mg
Mobocertinib98.8 ± 0.28798.7 ± 0.420
AP3296098.7 ± 0.40298.8 ± 0.401
AP3291499.3 ± 0.46999.2 ± 0.524
SecondaryNumber of Participants Reporting One or More Treatment-emergent Adverse Events (TEAEs)

An Adverse Event (AE) is defined as any untoward medical occurrence in a clinical investigation participant administered a drug; it does not necessarily have to have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign (eg, a clinically significant abnormal laboratory finding), symptom, or disease temporally associated with the use of a drug, whether or not it is considered related to the drug. A Treatment-emergent Adverse Event (TEAE) is defined as an adverse event with an onset that occurs after receiving study drug.

Time frame:
From first dose of study drug up to end of study (EOS) (up to 40 days)
Reported as:
Count of participants · Participants
Number of Participants Reporting One or More Treatment-emergent Adverse Events (TEAEs)
ParticipantsSevere Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mg
Number of Participants Reporting One or More Treatment-emergent Adverse Events (TEAEs)50

Adverse events

Collected over From first dose of study drug up to EOS (up to 40 days). Non-serious events are listed at a 5% frequency threshold.

Adverse event summary by group
GroupDeathsSeriousOther
Severe Renal Impairment: Mobocertinib 80 mg0/14 (0%)1/14 (7.1%)5/14 (35.7%)
Normal Renal Function: Mobocertinib 80 mg0/12 (0%)0/12 (0%)0/12 (0%)
Most frequent serious events
Most frequent serious events
EventSevere Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mg
Acute myocardial infarctionCardiac disorders1/140/12
Atrial fibrillationCardiac disorders1/140/12
HypotensionVascular disorders1/140/12
Most frequent other events
Most frequent other events
EventSevere Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mg
Atrial fibrillationCardiac disorders1/140/12
DiarrhoeaGastrointestinal disorders1/140/12
GoutMusculoskeletal and connective tissue disorders1/140/12
HyperkalaemiaMetabolism and nutrition disorders1/140/12
HypertensionVascular disorders1/140/12
NauseaGastrointestinal disorders1/140/12
VomitingGastrointestinal disorders1/140/12

Baseline characteristics

Safety Analysis Set included all participants who received the dose of study drug.

Age, Continuous
Age, Continuous(years)Severe Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mgTotal
Mean63.4 ± 11.8659.7 ± 3.5561.7 ± 9.07
Sex: Female, Male
Sex: Female, Male(Participants)Severe Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mgTotal
Female459
Male10717
Ethnicity (NIH/OMB)
Ethnicity (NIH/OMB)(Participants)Severe Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mgTotal
Hispanic or Latino6410
Not Hispanic or Latino8816
Unknown or Not Reported000
Race (NIH/OMB)
Race (NIH/OMB)(Participants)Severe Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mgTotal
American Indian or Alaska Native000
Asian000
Native Hawaiian or Other Pacific Islander000
Black or African American7714
White7512
More than one race000
Unknown or Not Reported000
Region of Enrollment
Region of Enrollment(Participants)Severe Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mgTotal
United States141226
Height
Height(cm)Severe Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mgTotal
Mean165.1 ± 6.53171.5 ± 6.32168.1 ± 7.10
Weight
Weight(kg)Severe Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mgTotal
Mean84.30 ± 13.71288.63 ± 6.99786.30 ± 11.143
Body Mass Index (BMI)
Body Mass Index (BMI)(kg/m^2)Severe Renal Impairment: Mobocertinib 80 mgNormal Renal Function: Mobocertinib 80 mgTotal
Mean30.896 ± 4.546630.108 ± 1.506630.532 ± 3.4508
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Study locations

2 sites
  • Clinical Pharmacology of Miami
    Hialeah, Florida 33014, United States
  • Orlando Clinical Research Center
    Orlando, Florida 32809, United States
09

References and documents

Related links

Study documents

  • Study protocol · Dec 14, 2020
  • Statistical analysis plan · Feb 18, 2021

Documents are hosted by the registry — open the source record to download them.

Individual participant data

Plan to share: Yes — Takeda provides access to the de-identified individual participant data (IPD) for eligible studies to aid qualified researchers in addressing legitimate scientific objectives (Takeda's data sharing commitment is available on https://clinicaltrials.takeda.com/takedas-commitment?commitment=5). These IPDs will be provided in a secure research environment following approval of a data sharing request, and under the terms of a data sharing agreement.

Supporting information: Study protocol, Sap, Icf, Csr

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Updates

Tracking since Sep 25, 2026
No changes since tracking began. The registry record was last updated on Jan 8, 2024, before this site started recording changes on Sep 25, 2026. Its history is on ClinicalTrials.gov ↗
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Registry details

Key details

Study ID
NCT04056455
Lead sponsor
Millennium Pharmaceuticals, Inc.
Responsible party
Sponsor
First posted
Aug 14, 2019
Start date
Mar 4, 2020
Primary completion
Apr 20, 2022
Completion
Apr 20, 2022
Results posted
Jan 8, 2024
Last update
Jan 8, 2024

Study contacts

Study Director
study director · Millennium Pharmaceuticals, Inc.

Oversight

Data monitoring committee
No
FDA-regulated drug
Yes
FDA-regulated device
No
View the source record on ClinicalTrials.gov ↗

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This study is completed, as verified in Mar 2023. You cannot join it, but the record below documents what was studied.

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