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valemetostat

Phase 1

Non-small Cell Lung Cancer | Small molecule | Oncology |Merck & Company, Inc.|Last Updated: Jul 28, 2026

Target and mechanism

Target class-Stat (Enzyme)
ModalitySmall molecule

Also known as valemetostat tosylate

Success Probability

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Market & Valuation

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Trial Design

RandomizedACTIVE_CONTROLLEDDMCBiomarker
Total Trials1
Total Enrollment137

FDA Designations

No designations recorded

Clinical trial landscape

valemetostat · 1 trial · 2 indications

Phase 1 1
NCT06644768A Study of Valemetostat Tosylate Plus Pembrolizumab Versus Pembrolizumab Alone in First-Line NSCLC Without Actionable Genomic AlterationsNon-small Cell Lung Cancer
ACTIVE NOT_RECRUITING137 Analytics
PHASE1ACTIVE NOT_RECRUITING
A Study of Valemetostat Tosylate Plus Pembrolizumab Versus Pembrolizumab Alone in First-Line NSCLC Without Actionable Genomic Alterations
Non-small Cell Lung CancerUnlock trial analytics

Study Endpoints

Primary Endpoints

Phase 1b: Number of Participants with Dose-Limiting Toxicities
From day of first dose on Day 1 to Day 21 in Cycle 1 (21 days), or before the administration of Cycle 2, up to 24 days

Total number of participants with A Dose-Limiting Toxicity (DLT) at each dose level of valemetostat in combination with pembrolizumab per National Cancer Institute - Common Terminology Criteria for Adverse Events version 5.0.

Phase 1b: Number of Participants with Treatment-Emergent Adverse Events
From date of first dose to 30 days after last dose, up to approximately 31 months

Incidence of TEAEs, Grade 3 or 4 TEAEs, deaths, TESAEs, TEAEs leading to dose modifications (including interruption, reduction, and discontinuation), and AESIs using the National Cancer Institute - Common Terminology Criteria for Adverse Events version 5.0

Phase 2: Progression-Free Survival by BICR
From date of randomization to the date of radiographic disease progression, or death from any cause, whichever occurs first, up to approximately 31 months

PFS is the time from the date of randomization to the date of radiographic disease progression as assessed by blinded independent central review (BICR) per RECIST v1.1 or death from any cause, whichever occurs first.

Secondary Endpoints

Phase 2: Objective Response Rate
From date of randomization to the date of radiographic disease progression, or death from any cause, whichever occurs first, up to approximately 31 months
Phase 2: Duration of Response
From date of randomization to the date of radiographic disease progression, or death from any cause, whichever occurs first, up to approximately 31 months
Phase 2: Disease Control Rate
From date of randomization up to approximately 31 months
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Study Design & Arms

AllocationRANDOMIZED
MaskingNONE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Phase 1b: Pembrolizumab + Valemetostat TosylateEXPERIMENTALParticipants will be provided with pembrolizumab at standard dose of 200 mg intravenously (IV) Q3W, and valemetostat will be provided per a dose escalation schedule, with an initial starting dose of 150 mg by mouth once daily.
Phase 2: Pembrolizumab + Valemetostat TosylateEXPERIMENTALParticipants will be provided with pembrolizumab at standard dose of 200 mg IV Q3W, and valemetostat will be provided per recommended phase 2 dose (RP2D)
Phase 2: PembrolizumabACTIVE_COMPARATORParticipants will be provided with pembrolizumab at standard dose of 200 mg IV Q3W

Interventions

NameTypeDescription
valemetostat tosylateDRUGValemetostat will be administered orally once daily until RP2D of valemetostat is determined.
pembrolizumabDRUGOne IV infusion Q3W on D1 of each 21-day cycle for a maximum of 35 cycles.
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Eligibility Criteria

Age Range18 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites35

Key Inclusion Criteria: 1. Has signed and dated the ICF, prior to the start of any trial-specific qualification procedures. 2. Is an adult ≥18 years of age or the minimum legal age (whichever is greater) at the time of informed consent. (Follow local regulatory requirements if the legal age of adul...

Countries:United StatesArgentinaBrazilChinaJapan
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Competitive Landscape -Non-Small Cell Lung Cancer 389 trials

Frequently asked questions about valemetostat

What is valemetostat used for?

Valemetostat is an investigational small molecule being studied for the treatment of non-small cell lung cancer (NSCLC). It is currently in Phase 1 clinical development as a combination therapy with pembrolizumab for first-line NSCLC without actionable genomic alterations.

What does valemetostat target?

Valemetostat is a -stat class enzyme inhibitor, meaning it works by inhibiting a specific enzyme. In the context of its clinical trial, it is being evaluated in combination with pembrolizumab for the treatment of non-small cell lung cancer.

Who makes valemetostat?

Valemetostat is being developed by Merck & Company, Inc., a pharmaceutical company traded on the New York Stock Exchange under the ticker symbol MRK.

What phase is valemetostat in?

Valemetostat is in Phase 1 clinical development. It is currently being studied in an active, not recruiting clinical trial for non-small cell lung cancer, and it is not yet approved by regulatory authorities.

What clinical trials is valemetostat in?

Valemetostat is being studied in one active Phase 1 clinical trial, NCT06644768, which evaluates valemetostat tosylate plus pembrolizumab versus pembrolizumab alone in first-line non-small cell lung cancer without actionable genomic alterations. The trial has an enrollment of 137 participants.

Is valemetostat the same as valemetostat tosylate?

Yes, valemetostat and valemetostat tosylate refer to the same drug. Valemetostat tosylate is the salt form of valemetostat, and the clinical trial NCT06644768 specifically studies valemetostat tosylate in combination with pembrolizumab.