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Binimetinib

Phase 2

Melanoma Stage III | Small molecule | Oncology |Pfizer, Inc.|Last Updated: Jun 4, 2026

Target and mechanism

Molecular targetMAP2K2, MAP2K1
Target classInhibitor
ModalitySmall molecule

Success Probability

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Market & Valuation

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Trial Design

UNCONTROLLEDDMCBiomarker
Total Trials1
Total Enrollment25

FDA Designations

No designations recorded

Clinical trial landscape

Binimetinib · 2 trials · 4 indications

Phase 2 2
NCT04598009Binimetinib and Imatinib for Unresectable Stage III-IV KIT-Mutant MelanomaMelanoma Stage III
RECRUITING25 Analytics
NCT03271047Study of Binimetinib + Nivolumab Plus or Minus Ipilimumab in Patients With Previously Treated Microsatellite-stable (MSS) Metastatic Colorectal Cancer With RAS MutationMSS
COMPLETED75 Analytics
PHASE2RECRUITING
Binimetinib and Imatinib for Unresectable Stage III-IV KIT-Mutant Melanoma
Melanoma Stage IIIUnlock trial analytics
PHASE2COMPLETED
Study of Binimetinib + Nivolumab Plus or Minus Ipilimumab in Patients With Previously Treated Microsatellite-stable (MSS) Metastatic Colorectal Cancer With RAS Mutation
MSSUnlock trial analytics

Study Endpoints

Primary Endpoints

Objective response rate (ORR)
Up to week 16

Defined as complete response (CR) or partial response (PR) by Response Evaluation Criteria in Solid Tumors (RECIST v1.1). The ORR at stages 1 and 2 will be estimated using the method of Whitehead, and the p-values for testing the null hypothesis at each stage will use the method of Koyama \& Chen and 90% confidence interval will be reported.

Phase 1b: Number of Participants With Dose-Limiting Toxicities (DLT)
Cycle 1: Day 1 up to Day 28

DLT:Adverse event(AE)/abnormal laboratory assessed unrelated-disease,disease progression,intercurrent illness/concomitant medication/therapies resulting inability tolerate 75% dose intensity in Cycle 1.Total bilirubin(TBL)grade(G)\>=3 (\>3.0\*upper limit of normal\[ULN)\]);AST/ALT\>5-8\*ULN\>5 days,\>8\*ULN,\>3\*ULN concurrent TBL\>2\*ULN;G\>=3 serum creatinine,CK elevation,ECG QTcF prolonged,G3 troponin,electrolyte\>72 hours,G3/4 amylase/lipase.G4 ANC,platelet count\>7 days;G3/4 platelet count,other AE except lymphopenia.G\>=3 retinopathy,other disorder\>21 days;G2 uveitis/eye pain/blurred vision/decreased visual acuity;G4 other disorder.Decrease LVEF\>10% G\>=3 cardiac disorders.G3/4 hypertension.G3 fatigue\>=7 days,hypersensitivity,infusion reaction,fever\>=72 hours/hemodynamic compromise,endocrinopathy.G\>=2 interstitial lung disease/pneumonitis;G3 bronchospasm.G3/4 rash,hand foot skin reaction,photosensitivity.G3 colitis;G3/4 diarrhea,nausea/vomiting.Neurologic G3.Other hematologic/nonhematolic G\>=3 AE.

Phase 2: Objective Response Rate (ORR) Per Response Evaluation Criteria in Solid Tumors (RECIST) Version (v) 1.1
From start of the treatment until disease progression, death or initiation of new anticancer therapy, whichever occurred first (Phase 2: maximum up to 26 months approximately)

ORR was defined as the percentage of participants who achieved a best overall response (BOR) of complete response (CR) or partial response (PR) as determined by investigator per RECIST v1.1. As per RECIST v1.1, CR was defined as disappearance of target and non-target lesions and normalization of tumor markers. Pathological lymph nodes must have short axis measures less than (\<)10 millimeter (mm). PR was defined as at least a 30% decrease in the sum of measures (longest diameter for tumor lesions and short axis measure for nodes) of target lesions, taking as reference baseline sum of diameters. Non-target lesions must be non-progressive disease (PD). PD was defined as at least a 20% increase in sum of diameters of target lesions, taking as reference the smallest sum on study. In addition to relative increase of 20%, the sum must also demonstrate an absolute increase of at least 5 mm. The appearance of one or more new lesions was considered progression.

Secondary Endpoints

Proportion of participants with treatment-related adverse events (AE)
Up to 2 years
Median duration of response
Up to 2 years
Progression-free survival (PFS)
Up to 2 years
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Study Design & Arms

AllocationNA
MaskingNONE
ModelSINGLE_GROUP
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Treatment (binimetinib, imatinib)EXPERIMENTALPatients receive binimetinib PO BID on days 1-28 and imatinib PO QD on days 1-28. Cycles repeat every 28 days
Phase 1b / Arm 1AEXPERIMENTALbinimetinib + nivolumab
Phase 1b / Arm 1BEXPERIMENTALbinimetinib + nivolumab + ipilimumab
Phase 2 / Arm 2AEXPERIMENTALbinimetinib + nivolumab
Phase 2 / Arm 2BEXPERIMENTALbinimetinib + nivolumab + ipilimumab

Interventions

NameTypeDescription
BinimetinibDRUGTaken orally (PO) twice a day (BID)
ImatinibDRUGTaken orally (PO) once a day (QD)
nivolumabDRUGIntravenously (IV) every 4 weeks (Q4W)
ipilimumabDRUGintravenously (IV) every 8 weeks (Q8W)
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Eligibility Criteria

Age Range18 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites2

Inclusion Criteria: * Eastern Cooperative Oncology Group (ECOG) performance status =\< 2 (Karnofsky \>= 60%) * Have histologically or cytologically confirmed melanoma * Have unresectable Stage III or Stage IV melanoma, as per American Joint Committee on Cancer 8th edition guidelines, not amenable t...

Countries:United StatesBelgiumNetherlandsSpainUnited Kingdom
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Frequently asked questions about Binimetinib

What is Binimetinib used for?

Binimetinib is an investigational small molecule being studied in oncology for advanced solid tumors, melanoma stage III, solid tumor and hematologic malignancies, epithelial ovarian cancer, MSS, and metastatic or unresectable cutaneous melanoma. It is currently in Phase 2 clinical development.

What does Binimetinib target?

Binimetinib targets MAP2K1 and MAP2K2, which are MEK1 and MEK2 kinases. It is an inhibitor of these targets, and its mechanism involves blocking the MEK signaling pathway that can drive tumor growth.

Who makes Binimetinib?

Binimetinib is being developed by Pfizer, Inc., which is listed on the New York Stock Exchange under the ticker symbol PFE.

What phase is Binimetinib in?

Binimetinib is in Phase 2 clinical development. It is an investigational drug and has not been approved by regulatory authorities. Clinical trials are ongoing to evaluate its safety and efficacy in various oncology indications.

What clinical trials is Binimetinib in?

Binimetinib has been studied in several clinical trials, including NCT01469130 in Japanese patients with advanced solid tumors, NCT01649336 in epithelial ovarian cancer, NCT01885195 in RAS/RAF/MEK activated tumors, and NCT01927341 in metastatic colorectal cancer. These trials are completed.

Is Binimetinib the same as MEK162?

Yes, Binimetinib is also known as MEK162. Clinical trials have used the name MEK162 to refer to this drug, and both names refer to the same investigational MEK inhibitor.