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Mobocertinib

Phase 1

Hepatic Impairment | Small molecule | Gastrointestinal |Takeda Pharmaceutical Company Limited|Last Updated: May 14, 2026

Target and mechanism

Molecular targetEGFR
Target classInhibitor
ModalitySmall molecule

Success Probability

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Market & Valuation

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Trial Design

CONTROLLEDBiomarker
Total Trials1
Total Enrollment24

FDA Designations

No designations recorded

Clinical trial landscape

Mobocertinib · 3 trials · 4 indications

Phase 1 3
NCT04056468A Study to Evaluate Pharmacokinetics (PK) and Safety of Oral Mobocertinib in Participants With Moderate or Severe Hepatic Impairment (HI) and Normal Hepatic FunctionHepatic Impairment
COMPLETED24 Analytics
NCT04056455A Study of Mobocertinib Capsules in People With Severe Kidney Problems and People With Healthy KidneysRenal Impairment
COMPLETED26 Analytics
NCT03807778A Study of Mobocertinib in Japanese Adults With Non-Small Cell Lung CancerNon-Small Cell Lung Cancer
ACTIVE NOT_RECRUITING53 Analytics
PHASE1COMPLETED
A Study to Evaluate Pharmacokinetics (PK) and Safety of Oral Mobocertinib in Participants With Moderate or Severe Hepatic Impairment (HI) and Normal Hepatic Function
Hepatic ImpairmentUnlock trial analytics
PHASE1COMPLETED
A Study of Mobocertinib Capsules in People With Severe Kidney Problems and People With Healthy Kidneys
Renal ImpairmentUnlock trial analytics
PHASE1ACTIVE NOT_RECRUITING
A Study of Mobocertinib in Japanese Adults With Non-Small Cell Lung Cancer
Non-Small Cell Lung CancerUnlock trial analytics

Study Endpoints

Primary Endpoints

Cmax: Maximum Observed Plasma Concentration for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
Cmax,u: Maximum Observed Unbound Plasma Concentration for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
AUC∞,u: Area Under the Unbound Plasma Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
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)
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
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)
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
t1/2z: Terminal Disposition Phase Half-life for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
λz: Terminal Elimination Rate Constant for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose

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.

CL/F: Apparent Clearance After Extravascular Administration for Mobocertinib
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
CLu/F: Apparent Clearance for Unbound Drug After Extravascular Administration for Mobocertinib
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
Vz/F: Apparent Volume of Distribution During the Terminal Disposition Phase After Extravascular Administration for Mobocertinib
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
Vz,u/F: Apparent Volume of Distribution for Unbound Drug During the Terminal Disposition Phase After Extravascular Administration for Mobocertinib
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
AUCinf: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
AUCinf,u: Area Under the Unbound Plasma Concentration-time Curve From Time 0 to Infinity for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
Combined Molar Cmax,u: Combined Molar Unbound Cmax for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
Combined Molar AUClast,u: Combined Molar Unbound AUClast for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
Combined Molar AUCinf,u: Combined Molar Unbound AUCinf for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose
λz: Terminal Elimination Phase Rate Constant for Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Day 1 pre-dose and at multiple time points (up to 216 hours) post-dose

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.

CumAe: Cumulative Amount of Mobocertinib and Its Active Metabolites (AP32960 and AP32914) Excreted in the Urine
Day 1 pre-dose and at multiple time points (up to 120 hours) post-dose
Cumfe: Cumulative Fraction of Mobocertinib Excreted in the Urine
Day 1 pre-dose and at multiple time points (up to 120 hours) post-dose
CLR: Renal Clearance of Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Day 1 pre-dose and at multiple time points (up to 120 hours) post-dose
Phase 1 Part: Recommended Phase 2 Dose (RP2D) of Orally Administered Mobocertinib
Cycle 1 (Cycle length=28 days)

The RP2D was the maximum tolerated dose (MTD) or less. The MTD was declared when at least 9 participants were evaluable in the study and 6 participants were evaluable at the current dose, and the current dose was recommended for the next cohort. The dose recommended for use in phase 2 part was analyzed on the basis of the safety and tolerability data obtained in phase 1 part of the study.

Phase 2 Part: Confirmed Objective Response Rate (ORR) as Assessed by the Independent Review Committee (IRC)
From the first dose of the study drug until progressive disease (PD) (up to 2 years and 9 months)

Confirmed ORR is defined as percentage of participants who were confirmed to had achieved complete response (CR) or partial response (PR) per IRC using Response Evaluation Criteria in Solid Tumors (RECIST) version 1.1 after the initiation of study treatment. Confirmed responses were responses that persisted on repeat imaging \>=4 weeks after initial response. CR (target lesion response): disappearance of all extranodal target lesions, all pathological lymph nodes must have decreased to \<10 millimeter (mm) in short axis. CR (non-target lesion response): disappearance of all extranodal nontarget lesions, all lymph nodes must be nonpathological in size (\<10 mm short axis) and normalization of tumor marker level. PR (target lesions): at least 30% decrease in sum of the longest diameters (SLD) of target lesions, taking as reference baseline sum diameters. The SLD must also demonstrate an absolute increase of at least 5 mm.

Secondary Endpoints

Plasma Protein Binding of Mobocertinib and Its Active Metabolites (AP32960 and AP32914)
Day 1 at multiple time points (up to 24 hours) post-dose
Number of Participants Reporting One or More Treatment-emergent Adverse Events (TEAEs)
Baseline up to 30 days after last dose of study drug (up to Day 32)
Phase 1 Part: Number of Participants With Treatment-Emergent Adverse Events (TEAEs)
From first dose of study drug until 30 days after the last dose or before initiation of new anticancer therapy (whichever comes first) (Up to 2 years and 9 months, till data cut-off of 08 November 2021)
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Study Design & Arms

AllocationNON_RANDOMIZED
MaskingNONE
ModelPARALLEL
PurposeOTHER

Treatment Arms

ArmTypeDescription
Moderate HI (Child-Pugh B): Mobocertinib 40 mgEXPERIMENTALMobocertinib 40 milligram (mg), capsule, orally, a single dose on Day 1.
Severe HI (Child-Pugh C): Mobocertinib 40 mgEXPERIMENTALMobocertinib 40 mg, capsule, orally, a single dose on Day 1.
Normal Hepatic Function: Mobocertinib 40 mgEXPERIMENTALMobocertinib 40 mg, capsule, orally, a single dose on Day 1.
Severe Renal Impairment: Mobocertinib 80 mgEXPERIMENTALParticipants with severe renal impairment received a single dose of mobocertinib 80 mg, capsule, orally, on Day 1.
Normal Renal Function: Mobocertinib 80 mgEXPERIMENTALParticipants with normal renal function received a single dose of mobocertinib 80 mg, capsule, orally, on Day 1.
Mobocertinib, Phase 1 PartEXPERIMENTALMobocertinib 40 milligrams (mg) (as the starting dose), capsules, orally, once daily on Days 1-28 of each 28-day treatment cycle for up to disease progression or intolerable toxicity, or another discontinuation criterion, and increasing until 160 mg, once daily (for up to approximately 10-12 cycles).
Mobocertinib, Phase 2 PartEXPERIMENTALMobocertinib 160 mg, once daily, for up to approximately 10-12 cycles.

Interventions

NameTypeDescription
MobocertinibDRUGMobocertinib capsule.
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Eligibility Criteria

Age Range18 Years to 79 Years
SexALL
Healthy VolunteersYes
Study Sites2

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 mob...

Countries:United StatesJapan
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Frequently asked questions about Mobocertinib

What is mobocertinib used for?

Mobocertinib is being studied for use in non-small cell lung cancer, renal impairment, and hepatic impairment. It is an investigational small molecule being evaluated in clinical trials for these conditions. The drug is not approved and remains in clinical development.

What does mobocertinib target?

Mobocertinib is a kinase inhibitor, belonging to the -tinib class of drugs. Kinase inhibitors work by blocking specific enzymes involved in cell signaling. The drug is being studied in patients with non-small cell lung cancer, where kinase pathways are often implicated in tumor growth.

Who makes mobocertinib?

Mobocertinib is being developed by Takeda Pharmaceutical Company Limited, which trades under the ticker TAK. Takeda is conducting clinical trials to evaluate the drug's safety and efficacy in various patient populations.

What phase is mobocertinib in?

Mobocertinib is in Phase 1 clinical development. It is an investigational drug, meaning it has not been approved by regulatory authorities. The ongoing Phase 1 trials are assessing the drug in patients with non-small cell lung cancer, as well as in people with kidney or liver problems.

What clinical trials is mobocertinib in?

Mobocertinib has been studied in several Phase 1 trials. NCT03807778 is an active study in Japanese adults with non-small cell lung cancer. NCT04056455, a completed study, evaluated the drug in people with severe kidney problems and healthy volunteers. NCT04056468, also completed, assessed the drug in participants with moderate or severe hepatic impairment.

Is mobocertinib the same as Takeda's investigational lung cancer drug?

Mobocertinib is an investigational small molecule being developed by Takeda for non-small cell lung cancer. It is also being studied in people with renal and hepatic impairment to understand how the body processes the drug. The drug is currently in Phase 1 trials.