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Larotrectinib

Phase 1

Solid Tumors Harboring NTRK Fusion | Small molecule | Oncology |Bayer AG|Last Updated: Feb 5, 2026

Target and mechanism

Molecular targetNTRK1, NTRK2, NTRK3
Target classInhibitor
ModalitySmall molecule

Also known as Larotrectinib (Vitrakvi, BAY2757556)

Success Probability

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Market & Valuation

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Trial Design

RandomizedCONTROLLED
Total Trials2
Total Enrollment229

FDA Designations

No designations recorded

Clinical trial landscape

Larotrectinib · 2 trials · 1 indication

Phase 1 2
NCT02637687A Study to Test the Safety and Efficacy of the Drug Larotrectinib for the Treatment of Tumors With NTRK-fusion in ChildrenSolid Tumors Harboring NTRK Fusion
ACTIVE NOT_RECRUITING154 Analytics
NCT02122913A Study to Test the Safety of the Investigational Drug Larotrectinib in Adults That May Treat CancerSolid Tumors Harboring NTRK Fusion
COMPLETED75 Analytics
PHASE1ACTIVE NOT_RECRUITING
A Study to Test the Safety and Efficacy of the Drug Larotrectinib for the Treatment of Tumors With NTRK-fusion in Children
Solid Tumors Harboring NTRK FusionUnlock trial analytics
PHASE1COMPLETED
A Study to Test the Safety of the Investigational Drug Larotrectinib in Adults That May Treat Cancer
Solid Tumors Harboring NTRK FusionUnlock trial analytics

Study Endpoints

Primary Endpoints

Phase 1: Number of participants in an assigned dose cohort with treatment emergent adverse events (TEAEs) by grade assessed by NCI-CTCAE v 4.03 who experience a DLT
From Day 1 to Day 28 of Cycle 1 (1 Cycle=28 days)

DLT: Dose-limiting toxicity. NCI-CTCAE: National Cancer Institute-Common Terminology Criteria for Adverse Events.

Phase 1: Number of participants with TEAEs
From first dose of larotrectinib up to 93 months
Phase 1: Severity of TEAEs
From first dose of larotrectinib up to 93 months
Phase 2: Overall response rate (ORR) by IRRC
From first dose of Larotrectinib to disease progression or subsequent therapy or surgical intervention or death, up to 76 months

Proportion of participants with a best overall response of complete response (CR) or partial response (PR) as determined by an independent radiology review committee (IRRC) based on Response Evaluation Criteria in Solid Tumours (RECIST) 1.1, Response Assessment in Neuro Oncology (RANO) or International Neuroblastoma Response Criteria (INRC) as appropriate to tumor type who express NTRK gene fusions.

Number of participants with adverse events
25 months
Severity of adverse events
25 months

The severity of adverse events will be assesssed according to the NCI CTCAE version 4.03.

Maximum tolerated dose (MTD)
25 months
Recommended dose for dose expansion
25 months

Secondary Endpoints

Phase 1: Maximum concentration of larotrectinib in plasma (Cmax)
Cohort 1 and 2: Cycle 1 Day 1 (C1D1) at 1 and 4 hours post-dose and C2D1 at pre-dose, and at 1 and 4 hours post-dose; Cohort 3 and Dose Expansion Cohort: C1D1 at 1 and 4 hours post-dose and C4D1 at pre-dose, 1 and 4 hours post-dose
Phase 1: Area under the concentration versus time curve from time 0 to t (AUC0-t) of larotrectinib in plasma
Cohort 1 and 2: C1D1 at 1 and 4 hours post-dose and C2D1 at pre-dose, and at 1 and 4 hours post-dose; Cohort 3 and Dose Expansion Cohort: C1D1 at 1 and 4 hours post-dose and C4D1 at pre-dose, 1 and 4 hours post-dose
Phase 1: Oral clearance (CL/F)
Cohort 1 and 2: C1D1 at 1 and 4 hours post-dose and C2D1 at pre-dose, and at 1 and 4 hours post-dose; Cohort 3 and Dose Expansion Cohort: C1D1 at 1 and 4 hours post-dose and C4D1 at pre-dose, 1 and 4 hours post-dos
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Study Design & Arms

AllocationNON_RANDOMIZED
MaskingNONE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Phase 1 dose escalationEXPERIMENTALPatients will receive the different levels of dose on Day 1 (BID in accordance with the cohort assignment). Each cycle will consist of 28 days of continuous dosing. Individual patients will continue daily larotrectinib dosing until PD, unacceptable toxicity, or other reason for treatment discontinuation. (arm closed)
Phase 1 dose expansionEXPERIMENTALPatients who are enrolled in the expansion cohort, following the formal dose escalation phase of the study. Distinct from the Phase 1 dose escalation cohort, the Phase 1 expansion cohort will enroll pediatric patients with advanced solid or primary CNS tumors with a documented NTRK gene fusion, or in the case of IFS, CMN or SBC with documented ETV6 rearrangement by FISH or RT-PCR or a documented NTRK fusion by NGS. This expansion cohort will follow the same schedule of assessments as the dose escalation cohorts. (arm closed)
Phase 2: Patients with tumors bearing NTRK fusions (IFS)_Cohort 1EXPERIMENTALPatients will receive larotrectinib dose on Day 1 (BID in accordance with the cohort assignment) at the recommended Phase 2 dose as determined in the Phase 1 portion of this study. Each cycle will consist of 28 days of continuous dosing. Individual patients will continue daily larotrectinib dosing until PD, unacceptable toxicity, or other reason for treatment discontinuation. (arm closed)
Phase 2: Other extra-cranial solid tumors_Cohort 2EXPERIMENTALPatients will receive larotrectinib dose on Day 1 (BID in accordance with the cohort assignment) at the recommended Phase 2 dose as determined in the Phase 1 portion of this study. Each cycle will consist of 28 days of continuous dosing. Individual patients will continue daily larotrectinib dosing until PD, unacceptable toxicity, or other reason for treatment discontinuation. (arm closed)
Phase 2: Primary CNS tumors_Cohort 3EXPERIMENTALPatients will receive larotrectinib dose on Day 1 (BID in accordance with the cohort assignment) at the recommended Phase 2 dose as determined in the Phase 1 portion of this study. Each cycle will consist of 28 days of continuous dosing. Individual patients will continue daily larotrectinib dosing until PD, unacceptable toxicity, or other reason for treatment discontinuation.
Phase 2: Bone health assessment_sub-cohortEXPERIMENTALPatients will receive larotrectinib dose on Day 1 (BID in accordance with the cohort assignment) at the recommended Phase 2 dose as determined in the Phase 1 portion of this study. Each cycle will consist of 28 days of continuous dosing. Individual patients will continue daily larotrectinib dosing until PD, unacceptable toxicity, or other reason for treatment discontinuation. Patients in this group will undergo bone health assessments in addition to all other efficacy and safety assessments.
Tumor patients_Dose 1EXPERIMENTALAdult patients with solid tumors receiving 50 mg of BAY2757556 once daily (dose escalation cohort).
Tumor patients_Dose 2EXPERIMENTALAdult patients with solid tumors receiving 100 mg of BAY2757556 once daily (dose escalation cohort).
Tumor patients_Dose 3EXPERIMENTALAdult patients with solid tumors receiving 100 mg of BAY2757556 twice daily (dose escalation cohort).
Tumor patients_Dose 4EXPERIMENTALAdult patients with solid tumors receiving 200 mg of BAY2757556 once daily (dose escalation cohort).
Tumor patients_Dose 5EXPERIMENTALAdult patients with solid tumors receiving 150 mg of BAY2757556 twice daily (dose escalation cohort).
Tumor patients_Dose 6EXPERIMENTALAdult patients with solid tumors receiving 200 mg of BAY2757556 twice daily (dose escalation cohort).
Tumor patients_ExpansionEXPERIMENTALAdults patients with solid tumors and neurotrophic tyrosine kinase (NTRK) genes or proteins of types 1 - 3 (dose expansion cohort). Patients receive either the recommended or maximum tolerated dose of BAY2757556 as determined in the dose escalation part.

Interventions

NameTypeDescription
Larotrectinib (Vitrakvi, BAY2757556)DRUGBAY2757556 will be administered orally as capsule or in liquid form over continuous 28-day cycles.
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Eligibility Criteria

Age RangeN/A to 21 Years
SexALL
Healthy VolunteersNo
Study Sites45

Inclusion Criteria: * Phase 1 (Closed): * Dose escalation: Birth through 21 years of age at C1D1 with a locally advanced or metastatic solid tumor or primary CNS tumor that has relapsed, progressed or was nonresponsive to available therapies and for which no standard or available systemic curati...

Countries:United StatesAustraliaCanadaChinaCzechiaDenmarkFranceGermanyIrelandIsraelItalyJapanNetherlandsPolandSouth KoreaSpainSwedenSwitzerlandTurkey (Türkiye)UkraineUnited Kingdom
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Frequently asked questions about Larotrectinib

What is Larotrectinib used for?

Larotrectinib is an investigational small molecule being developed for the treatment of solid tumors harboring NTRK fusion. It is a kinase inhibitor, and it is currently in Phase 1 clinical development for this indication.

What does Larotrectinib target?

Larotrectinib targets kinases, as it belongs to the -tinib class of kinase inhibitors. It is being studied in patients with solid tumors that harbor NTRK gene fusions, which are genetic alterations that can drive cancer growth.

Who makes Larotrectinib?

Larotrectinib is being developed by Bayer AG, a company traded under the ticker BAYRY. The drug is also known as Vitrakvi and BAY2757556.

What phase is Larotrectinib in?

Larotrectinib is in Phase 1 clinical development. It is an investigational drug and has not been approved by the FDA. It is being studied in clinical trials for solid tumors harboring NTRK fusion.

What clinical trials is Larotrectinib in?

Larotrectinib has been studied in two clinical trials. NCT02122913 is a completed Phase 1 study in adults with solid tumors harboring NTRK fusion. NCT02637687 is an active Phase 1 study in children with NTRK-fusion tumors, with 154 participants enrolled.

Is Larotrectinib the same as Vitrakvi?

Yes, Larotrectinib is also known as Vitrakvi and BAY2757556. These names refer to the same investigational drug being developed by Bayer AG for solid tumors harboring NTRK fusion.