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TAK-788

Phase 3

Advanced/Metastatic Non-Small Cell Lung Cancer (NSCLC) | Small molecule | Oncology |Takeda Pharmaceutical Company Limited|Last Updated: Mar 30, 2026

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Trial Design
RandomizedACTIVE_CONTROLLEDDMC
Total Trials1
Total Enrollment354
FDA Designations
No designations recorded
Clinical trial landscape

TAK-788 · 5 trials · 4 indications

Phase 3 1Phase 1 4
NCT04129502TAK-788 as First-Line Treatment Versus Platinum-Based Chemotherapy for Non-Small Cell Lung Cancer (NSCLC) With EGFR Exon 20 Insertion MutationsAdvanced/Metastatic Non-Small Cell Lung Cancer (NSCLC)
ACTIVE NOT_RECRUITING354 Analytics
PHASE3ACTIVE NOT_RECRUITING
TAK-788 as First-Line Treatment Versus Platinum-Based Chemotherapy for Non-Small Cell Lung Cancer (NSCLC) With EGFR Exon 20 Insertion Mutations
Advanced/Metastatic Non-Small Cell Lung Cancer (NSCLC)Unlock trial analytics
Study Endpoints
Primary Endpoints
Progression Free Survival (PFS) as Assessed by Blinded Independent Review Committee (IRC) per Response Evaluation Criteria in Solid Tumors (RECIST) Version 1.1
Up to approximately 40 months after the first participant is randomized

PFS is defined as the time interval from the date of randomization until the first date at which the criteria for progressive disease (PD) according to RECIST Version 1.1 are met or death, whichever occurs first.

Part A, Cmax: Geometric Mean Maximum Observed Plasma Concentration (Cmax) for Midazolam Administered Orally With Mobocertinib (Cycle 1 Day 24) and Without Mobocertinib (Cycle 1 Day 1)
Cycle 1: Days 1 and 24 pre-dose and at multiple time points (up to 24 hours) post-dose (Cycle length is equal to [=] 30 days)

As planned, this pharmacokinetic (PK) outcome measure was only assessed in Part A.

Part A, AUC∞: Geometric Mean Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Midazolam Administered Orally With Mobocertinib (Cycle 1 Day 24) and Without Mobocertinib (Cycle 1 Day 1)
Cycle 1: Days 1 and 24 pre-dose and at multiple time points (up to 24 hours) post-dose (Cycle length = 30 days)

As planned, this PK outcome measure was only assessed in Part A.

Part A, Cmax: Geometric Mean Maximum Observed Plasma Concentration (Cmax) for Midazolam Administered Intravenously With Mobocertinib (Cycle 1 Day 25) and Without Mobocertinib (Cycle 1 Day 2)
Cycle 1: Days 2 and 25 pre-dose and at multiple time points (up to 24 hours) post-dose (Cycle length = 30 days)

As planned, this PK outcome measure was only assessed in Part A.

Part A, AUC∞: Geometric Mean Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Midazolam Administered Intravenously With Mobocertinib (Cycle 1 Day 25) and Without Mobocertinib (Cycle 1 Day 2)
Cycle 1: Days 2 and 25 pre-dose and at multiple time points (up to 24 hours) post-dose (Cycle length = 30 days)

As planned, this PK outcome measure was only assessed in Part A.

Part A, Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for Midazolam Administered Orally With Mobocertinib (Cycle 1 Day 24) and Without Mobocertinib (Cycle 1 Day 1)
Cycle 1: Days 1 and 24 pre-dose and at multiple time points (up to 24 hours) post-dose (Cycle length = 30 days)

As planned, this PK outcome measure was only assessed in Part A for midazolam 3 mg oral solution.

Part A, Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for Midazolam Administered Intravenously With Mobocertinib (Cycle 1 Day 25) and Without Mobocertinib (Cycle 1 Day 2)
Cycle 1: Days 2 and 25 pre-dose and at multiple time points (up to 24 hours) post-dose (Cycle length = 30 days)

As planned, this PK outcome measure was only assessed in Part A for midazolam 1 mg intravenous infusion.

Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for Mobocertinib
Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Cmax: Maximum Observed Plasma Concentration for Mobocertinib
Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Mobocertinib
Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Mobocertinib
Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose
Part 1: Number of Participants Reporting One or More Treatment-emergent Adverse Events (TEAEs)
Baseline up to 30 days after the last dose of study drug (Day 31)
Part 1: Number of Participants With One or More Serious Adverse Events (SAEs)
Baseline up to 30 days after the last dose of study drug (Day 31)
Part 1: Number of Participants With Clinically Significant Abnormal Laboratory Values
Baseline up to 30 days after the last dose of study drug (Day 31)
Part 1: Number of Participants With Clinically Significant Abnormal Vital Signs
Baseline up to 30 days after the last dose of study drug (Day 31)
Part 2, Cmax: Maximum Observed Plasma Concentration for TAK-788
Day 1 pre-dose and at multiple time points (up to 168 hours) post-dose
Part 3, Cmax: Maximum Observed Plasma Concentration for TAK-788
Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose
Part 2, Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-788
Day 1 pre-dose and at multiple time points (up to 168 hours) post-dose
Part 3, Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for TAK-788
Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose
Part 2, AUCt: Area Under the Plasma Concentration-time Curve From Time 0 to Time t for TAK-788
Day 1 pre-dose and at multiple time points (up to 168 hours) post-dose
Part 3, AUCt: Area Under the Plasma Concentration-time Curve From Time 0 to Time t for TAK-788
Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose
Part 2, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for TAK-788
Day 1 pre-dose and at multiple time points (up to 168 hours) post-dose
Part 3, AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for TAK-788
Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose
Part 2, t1/2z: Terminal Disposition Phase Half-life (t1/2z) for TAK-788
Day 1 pre-dose and at multiple time points (up to 168 hours) post-dose
Part 3, t1/2z: Terminal Disposition Phase Half-life (t1/2z) for TAK-788
Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose
Part 1, Dose Escalation Component: Recommended Phase 2 Dose (RP2D) of Orally Administered TAK-788
Cycle 1 (Cycle length is equal to [=] 28 days)
Part 2, Expansion Cohorts 1, 2, 4, 5 and 7: Confirmed Objective Response Rate (ORR) Assessed by the Investigator
Up to 36 months after first dose
Part 2, Expansion Cohort 3: Intracranial ORR (iORR) Assessed by Independent Review Committee (IRC)
Up to 36 months after first dose
Part 2, Expansion Cohort 6: Confirmed ORR Assessed by IRC
Up to 36 months after first dose
Part 3, Extension Cohort: Confirmed ORR Assessed by IRC
Up to 36 months after first dose
Secondary Endpoints
Confirmed Objective Response Rate (ORR) as Assessed by Blinded Independent Review Committee (IRC) per RECIST Version 1.1
Up to approximately 40 months after the first participant is randomized
Overall Survival (OS)
Up to approximately 40 months after the first participant is randomized
Progression Free Survival (PFS) as Assessed by the Investigator
Up to approximately 40 months after the first participant is randomized
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Study Design & Arms
AllocationRANDOMIZED
MaskingNONE
ModelPARALLEL
PurposeTREATMENT
Treatment Arms
ArmTypeDescription
TAK-788 Group (Arm A)EXPERIMENTALTAK-788 160 milligram (mg) with or without food, capsules, orally, once daily until the participants experience PD as assessed by blinded IRC, intolerable toxicity, or another discontinuation criteria.
Platinum-based Chemotherapy Group (Arm B)ACTIVE_COMPARATORPemetrexed 500 milligram per meter square (mg/m\^2) plus cisplatin 75 mg/m\^2, infusion, IV, once on Day 1 of 21-day cycle pemetrexed 500 mg/m\^2 plus carboplatin, infusion, IV, once at a dose calculated to produce area under curve (AUC) of 5 milligram\*minute per milliliter (mg\*min/mL) on Day 1 of 21-day cycle until the participants experience PD as assessed by blinded IRC, intolerable toxicity, or another discontinuation criteria. Pemetrexed/cisplatin or pemetrexed/carboplatin will be repeated every 3 weeks for 4 cycles, followed by maintenance treatment with pemetrexed 500 mg/m\^2, on Day 1 of a 21-day cycle thereafter.
Part A: Midazolam + TAK-788EXPERIMENTALMidazolam 3 mg, solution, orally, once on Days 1 and 24 and midazolam 1 mg, infusion, intravenously, once on Days 2 and 25 along with TAK-788 160 mg, capsule, orally, once daily from Day 3 through 30 in Cycle 1.
Part B: TAK-788EXPERIMENTALTAK-788 160 mg, capsules, orally, once daily in a 28-day treatment cycle from Cycle 2 to Cycle 24, or until progressive disease (PD), intolerable toxicity, or another discontinuation criterion is met, whichever is sooner. Eligible participants from Part A may enter into Part B. Based on the investigator's opinion, if a participant continues to experience clinical benefit, treatment with TAK-788 may be continued after PD.
TAK-788 160 mg Fasted + TAK-788 160 mg FedEXPERIMENTALTAK-788 160 milligram (mg), capsule, orally, once on Day 1 of Period 1 under fasted conditions (Treatment A), followed by 10 days washout period, followed by TAK-788 160 mg, capsule, orally, once on Day 1 of Period 2 under fed conditions (Treatment B).
TAK-788 160 mg Fed + TAK-788 160 mg FastedEXPERIMENTALTAK-788 160 mg, capsule, orally, once on Day 1 of Period 1 under fed conditions (Treatment B), followed by 10 days washout period, followed by TAK-788 160 mg, capsule, orally, once on Day 1 of Period 2 under fasted conditions (Treatment A).
Part 1 Cohort 1: TAK-788EXPERIMENTALTAK-788, capsule, orally or TAK-788 matching placebo capsule, orally, once under fasted conditions on Day 1.
Part 1 Cohort 2: TAK-788EXPERIMENTALTAK-788, capsule, orally or TAK-788 matching placebo capsule, orally, once under fasted conditions on Day 1 following review of safety data from Cohort 1.
Part 1 Cohort 3: TAK-788EXPERIMENTALTAK-788, capsule, orally or TAK-788 matching placebo capsule, orally, once under fasted conditions on Day 1 following review of safety data from Cohort 2.
Part 1 Cohort 4: TAK-788EXPERIMENTALTAK-788, capsule, orally or TAK-788 matching placebo capsule, orally, once under fasted conditions on Day 1 following review of safety data from Cohort 3.
Part 1 Cohort 5: TAK-788EXPERIMENTALTAK-788, capsule, orally or TAK-788 matching placebo capsule, orally, once under fasted conditions on Day 1 following review of safety data from Cohort 4.
Part 2: TAK-788 Fed + TAK-788 FastedEXPERIMENTALTAK-788, capsule, orally, once on Day 1 of Intervention Period 1 under fed conditions with low-fat meal (Treatment A), followed by at least 7 days washout period, further followed by TAK-788, capsule, orally, once on Day 1 of Intervention Period 2 under fasted conditions (Treatment B). TAK-788 dose will be determined based on review of safety and tolerability data from cohorts of Part 1.
Part 2: TAK-788 Fasted + TAK-788 FedEXPERIMENTALTAK-788, capsule, orally, once on Day 1 of Intervention Period 1 under fasted conditions (Treatment B), followed by at least 7 days washout period, further followed by TAK-788, capsule, orally, once on Day 1 of Intervention Period 2 under fed conditions with low-fat meal (Treatment A). TAK-788 dose will be determined based on review of safety and tolerability data from cohorts of Part 1.
Part 3: TAK-788 DiC (reference) + TAK-788 DiC (test)EXPERIMENTALTAK-788 160 mg, DiC A (reference), orally, under fasted condition, once on Day 1 of Intervention Period 1, followed by at least 7 days washout period, further followed by TAK-788 160 mg, DiC B (test), orally, under fasted condition, once on Day 1 of Intervention Period 2.
Part 3: TAK-788 DiC (test) + TAK-788 DiC (reference)EXPERIMENTALTAK-788 160 mg, DiC B (test), orally, under fasted condition, once, on Day 1 of Intervention Period 1, followed by at least 7 days washout period, further followed by TAK-788 160 mg, DiC A (reference), orally, under fasted condition, once on Day 1 of Intervention Period 2.
Part 1: Dose Escalation ComponentEXPERIMENTALTAK-788 treatment for participants with advanced NSCLC.
Part 2: Expansion Cohort 1EXPERIMENTALTAK-788 treatment for NSCLC participants with EGFR exon 20 activating insertions, who have either not received or not shown an objective response to an EGFR tyrosine kinase inhibitors (TKI), and who have no active, measurable central nervous system (CNS) metastases.
Part 2: Expansion Cohort 2EXPERIMENTALTAK-788 treatment for NSCLC participants with HER2 exon 20 activating insertions or point mutations and no active, measurable CNS metastases.
Part 2: Expansion Cohort 3EXPERIMENTALTAK-788 treatment for NSCLC participants with EGFR exon 20 activating insertions or HER2 exon 20 activating insertions or point mutations and active, measurable CNS metastases.
Part 2: Expansion Cohort 4EXPERIMENTALTAK-788 treatment for NSCLC participants with other targets against which TAK-788 is active (examples include EGFR exon 19 deletions or exon 21 substitutions \[with or without T790M mutations\] and other uncommon EGFR activating mutations), without active CNS metastases.
Part 2: Expansion Cohort 5EXPERIMENTALTAK-788 treatment for NSCLC participants with EGFR exon 20 activating insertions, who have previously shown an objective response to an EGFR TKI and subsequently progressed without active CNS metastases.
Part 2: Expansion Cohort 6EXPERIMENTALTAK-788 treatment NSCLC participants with EGFR exon 20 activating insertions, who have not received prior systemic anticancer treatment for locally advanced or metastatic disease without active CNS metastases
Part 2: Expansion Cohort 7EXPERIMENTALTAK-788 treatment for participants with solid tumors other than NSCLC with EGFR/HER2 mutations against which TAK-788 is active without active CNS metastases.
Part 3: Extension CohortEXPERIMENTALTAK-788 treatment for participants with previously treated locally advanced or metastatic NSCLC whose tumors harbor EGFR exon 20 insertion mutations.
Interventions
NameTypeDescription
TAK-788DRUGTAK-788 capsule
PemetrexedDRUGPemetrexed IV infusion
CisplatinDRUGCisplatin IV infusion
CarboplatinDRUGCarboplatin IV infusion
MidazolamDRUGMidazolam Oral Solution and Midazolam Intravenous Infusion.
PlaceboDRUGTAK-788 placebo-matching capsules.
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Eligibility Criteria
Age Range18 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites134

Inclusion Criteria: * Male or female adult patients (aged 18 years or older) * Histologically or cytologically confirmed nonsquamous cell locally advanced not suitable for definitive therapy, recurrent, or metastatic (Stage IV) NSCLC * Documented epidermal growth factor receptor (EGFR) in-frame exo...

Countries:United StatesAustraliaAustriaBelgiumCanadaChinaFranceGermanyGreeceHong KongIsraelItalyJapanNetherlandsPortugalRussiaSingaporeSouth KoreaSpainSwedenTaiwanTurkey (Türkiye)UkraineUnited KingdomPuerto Rico
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Recent Changes (Last 90 Days)
LOWMay 26, 2026NCT02716116primaryCompletionDate: changed
LOWMay 26, 2026NCT04129502primaryCompletionDate: changed
LOWMay 24, 2026NCT02716116studyFirstPostDate: changed
LOWMay 24, 2026NCT04129502studyFirstPostDate: changed