Drugs / Binimetinib
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Binimetinib

Small molecule targets MAP2K1, MAP2K2 via inhibition

Developed for
melanoma · non-small cell lung carcinoma · colorectal cancer · metastatic melanoma · cutaneous melanoma · cancer · metastatic malignant neoplasm in the brain · biliary tract cancer
+76 more · triple-negative breast carcinoma · female breast carcinoma · gastrointestinal stromal tumor · lung cancer · metastatic malignant neoplasm · refractory malignant neoplasm · uveal melanoma · colon carcinoma · colorectal carcinoma · endometrial carcinoma · exocrine pancreatic carcinoma · gallbladder carcinoma · hairy cell leukemia · leukemia · low grade glioma · lung adenocarcinoma · malignant pancreatic neoplasm · metastatic neoplasm · neoplasm · ovarian carcinoma · pancreatic adenocarcinoma · plasma cell myeloma · skin carcinoma · acral lentiginous melanoma · acute erythroid leukemia · acute myeloblastic leukemia with maturation · acute myeloblastic leukemia without maturation · acute myeloid leukemia · acute myeloid leukemia with 11q23 abnormalities · acute myeloid leukemia with abnormal bone marrow eosinophils inv(16)(p13q22) or t(16;16)(p13;q22) · acute myeloid leukemia with minimal differentiation · acute myeloid leukemia with t(8;21)(q22;q22) translocation · acute myeloid leukemia, del(5q31-q32) · acute myeloid leukemia, inv(16)(p13.1;q22) · acute myelomonocytic leukemia M4 · adamantinous craniopharyngioma · adult acute monocytic leukemia · adult lymphoma · anaplastic astrocytoma · anaplastic pleomorphic xanthoastrocytoma · biliary tract neoplasm · brain cancer · breast adenocarcinoma · cancer of unknown primary site · colon adenocarcinoma · differentiated thyroid carcinoma · distal biliary tract carcinoma · fallopian tube cancer · fallopian tube serous adenocarcinoma · gliosarcoma · hematopoietic and lymphoid cell neoplasm · Her2-receptor negative breast cancer · hilar cholangiocarcinoma · hormone receptor-positive breast cancer · malignant colon neoplasm · malignant epithelial tumor of ovary · malignant ovarian serous tumor · metastasis from malignant tumor of colon · metastatic carcinoma · metastatic malignant neoplasm in the lymph nodes · mucosal melanoma · myelodysplastic syndrome · neoplastic disease or syndrome · neurofibromatosis type 1 · ovarian serous adenocarcinoma · pancreatic ductal adenocarcinoma · peritoneum cancer · plexiform neurofibroma · primary brain neoplasm · primary peritoneal serous adenocarcinoma · RASopathy · rectal cancer · refractory plasma cell neoplasm · rheumatoid arthritis · soft tissue neoplasm · squamous cell lung carcinoma
Investigated by
Pfizer · National Cancer Institute (NCI) · Array BioPharma · Pierre Fabre Laboratories · Array BioPharma · M.D. Anderson Cancer Center
+105 more · Merck Sharp & Dohme LLC · Bristol-Myers Squibb · H. Lee Moffitt Cancer Center and Research Institute · Memorial Sloan Kettering Cancer Center · University Health Network, Toronto · Jonsson Comprehensive Cancer Center · Novartis Pharmaceuticals · Pierre Fabre Laboratories · University of California, San Francisco · Academic and Community Cancer Research United · Dana-Farber Cancer Institute · Deciphera Pharmaceuticals, LLC · European Organisation for Research and Treatment of Cancer - EORTC · Gilead Sciences · MFAR · Massachusetts General Hospital · Merck KGaA, Darmstadt, Germany · Ono Pharmaceutical Co., Ltd. · Peter MacCallum Cancer Centre, Australia · Pierre Fabre Ibérica, S.A. · Pierre Fabre Pharma GmbH · Spanish Melanoma Group · Taiho Oncology, Inc. · UNICANCER · AIO-Studien-gGmbH · AbbVie · Abramson Cancer Center at Penn Medicine · Accord Healthcare, Inc. · Acrotech Biopharma Inc. · Allist Pharmaceuticals, Inc. · Apices Soluciones S.L. · Beaumont Hospital · Belfast Health and Social Care Trust · Belgian Group of Digestive Oncology · Biotrial Inc. · Breast Cancer Research Foundation · Bruno C. Medeiros · CCTU- Cancer Theme · Cancer Research UK · Cancer Research UK & UCL Cancer Trials Centre · Children's Hospital Colorado · Children's Hospital Los Angeles · City of Hope Medical Center · Clinical Research Technology S.r.l. · Coordinating Centre for Clinical Trials Heidelberg · Dr. Ronnie Shapira · ECOG-ACRIN Cancer Research Group · European Association of Dermato Oncology · European Commission · European Georges Pompidou Hospital · Fondazione Melanoma Onlus · French Cooperative Thoracic Intergroup · Fundacion Oncosur · German Cancer Research Center · Hoosier Cancer Research Network · Hospital Vall d'Hebron · IDEAYA Biosciences · Inge Marie Svane · Jason J. Luke, MD · Johns Hopkins University · Laura Huppert, MD, BA · Leiden University Medical Center · Mayo Clinic · Merck Serono GmbH, Germany · Merck, S.L., Spain · N.N. Petrov National Medical Research Center of Oncology · NRG Oncology · National Cancer Center, Japan · National Cancer Institute (NCI) · National Cancer Institute, France · Nationwide Children's Hospital · OnKure, Inc. · Oxford University Hospitals NHS Trust · Pacific Pediatric Neuro-Oncology Consortium · all 111 on the full record

Regulatory milestones approvals, filings & regulatory actions · 6 recorded

MilestoneJurisdictionBrandIndicationDateSentence it was read from
Label expansions (4) US (FDA) MEKTOVI 2019-01-23 – 2025-03-12 fda.gov
Approved EU (EMA) Mektovi 2018-09-20 europa.eu
Approved US (FDA) MEKTOVI 2018-06-27 fda.gov

Trials 127 · started per year

today
US approved 2018
EU approved 2018
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20082009201020112012201320142015201620172018201920202021202220232024202520262027
PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 03 trials
Phase 0 NCT04870034 Jan 2024 → Sep 2025 colorectal carcinoma, lung adenocarcinoma Roswell Park Cancer Institute Withdrawn No outcome recorded
Phase 0 NCT04741997 May 2021 → Jul 2026 overdue metastatic melanoma H. Lee Moffitt Cancer Center and Research Institute Recruiting No outcome recorded
Phase 0 NCT03543969 Jun 2018 → Dec 2024 overdue cutaneous melanoma, skin carcinoma H. Lee Moffitt Cancer Center and Research Institute Active not recruiting No outcome recorded
Phase 135 trials
Phase 1 NCT05111561 Aug 2022 → Mar 2027 metastatic malignant neoplasm, triple-negative breast carcinoma National Cancer Institute (NCI) Suspended No outcome recorded
Phase 1 NCT05355701 Jul 2022 → Apr 2028 expected colorectal cancer, glioma, melanoma, non-small cell lung carcinoma +1 Pfizer Recruiting No outcome recorded
Phase 1 NCT04965818 Sep 2021 → Jun 2023 non-small cell lung carcinoma Taiho Oncology, Inc. Terminated No outcome recorded
Phase 1 NCT05103891 Sep → Nov 2021 metastatic melanoma Pierre Fabre Laboratories Unknown No outcome recorded
Phase 1 NCT04913285 Aug 2021 → Nov 2028 expected melanoma, non-small cell lung carcinoma Pierre Fabre Laboratories Active not recruiting No outcome recorded
Phase 1 NCT04892017 Jun 2021 → Mar 2026 metastatic neoplasm, non-small cell lung carcinoma Deciphera Pharmaceuticals, LLC Terminated No outcome recorded
Phase 1 NCT04800822 Mar 2021 → Jun 2024 neoplasm Pfizer Terminated No outcome recorded
Phase 1 NCT04759846 Jan 2021 → May 2023 metastatic melanoma Pierre Fabre Laboratories Withdrawn No outcome recorded
Phase 1 NCT04543188 Jan 2021 → Mar 2024 melanoma, non-small cell lung carcinoma, primary brain neoplasm Pfizer Terminated No outcome recorded
Phase 1 NCT04044430 Aug 2020 → Jul 2022 colon adenocarcinoma, rectum adenocarcinoma University of California, San Francisco Terminated No outcome recorded
Phase 1/223 trials
Phase 1/2 NCT05340621 May 2022 → Jan 2025 RASopathy, melanoma OnKure, Inc. Completed No outcome recorded
Phase 1/2 NCT05080621 Nov 2021 → Nov 2025 gastrointestinal stromal tumor Deciphera Pharmaceuticals, LLC Withdrawn No outcome recorded
Phase 1/2 NCT04655157 May 2021 → Aug 2022 melanoma Jason J. Luke, MD Terminated No outcome recorded
Phase 1/2 NCT04720976 Mar 2021 → Dec 2023 non-small cell lung carcinoma Allist Pharmaceuticals, Inc. Completed No outcome recorded
Phase 1/2 NCT04494958 Nov 2020 → Dec 2023 triple-negative breast carcinoma Fundacion Oncosur Completed No outcome recorded
Phase 1/2 NCT04585815 Nov 2020 → May 2023 non-small cell lung carcinoma Pfizer Terminated No outcome recorded
Phase 1/2 NCT04720768 Jun 2020 → Dec 2024 melanoma, metastatic neoplasm Peter MacCallum Cancer Centre, Australia Unknown No outcome recorded
Phase 1/2 NCT04292119 May 2020 → Dec 2022 non-small cell lung carcinoma, refractory malignant neoplasm Massachusetts General Hospital Unknown No outcome recorded
Phase 1/2 NCT03947385 Jun 2019 → Jan 2027 expected colorectal cancer, cutaneous melanoma, uveal melanoma IDEAYA Biosciences Recruiting No outcome recorded
Phase 1/2 NCT03843775 Feb 2019 → Sep 2023 neoplasm Memorial Sloan Kettering Cancer Center Completed No outcome recorded
Phase 255 trials
Phase 2 NCT06887088 May 2025 → Jan 2028 expected melanoma Spanish Melanoma Group Recruiting No outcome recorded
Phase 2 NCT05554354 Sep 2024 → Apr 2025 female breast carcinoma, hormone receptor-positive breast cancer National Cancer Institute (NCI) Terminated No outcome recorded
Phase 2 NCT06207656 Apr 2024 → Apr 2029 expected colorectal cancer Spanish Cooperative Group for the Treatment of Digestive Tumours (TTD) Recruiting No outcome recorded
Phase 2 NCT05564403 Feb 2024 → Oct 2026 expected distal biliary tract carcinoma, gallbladder carcinoma, hilar cholangiocarcinoma National Cancer Institute (NCI) Active not recruiting No outcome recorded
Phase 2 NCT05554367 Dec 2023 → Aug 2026 overdue exocrine pancreatic carcinoma, ovarian serous adenocarcinoma National Cancer Institute (NCI) Active not recruiting No outcome recorded
Phase 2 NCT06229340 Oct 2023 → Oct 2026 expected colorectal cancer, lung cancer, malignant pancreatic neoplasm, melanoma +1 N.N. Petrov National Medical Research Center of Oncology Recruiting No outcome recorded
Phase 2 NCT05304546 Sep 2023 → Jul 2025 metastatic melanoma Dr. Ronnie Shapira Completed No outcome recorded
Phase 2 NCT05926960 Jun 2023 → Feb 2026 melanoma Pfizer Terminated No outcome recorded
Phase 2 NCT05286788 Apr 2023 → Apr 2027 expected adamantinous craniopharyngioma Nationwide Children's Hospital Recruiting No outcome recorded
Phase 2 NCT05564377 Apr 2023 → Jul 2030 expected Her2-receptor negative breast cancer, endometrial carcinoma, fallopian tube carcinoma, female breast carcinoma +3 National Cancer Institute (NCI) Recruiting No outcome recorded
Phase 38 trials
Phase 3 NCT05615818 Jul 2024 → Jun 2027 expected biliary tract neoplasm UNICANCER Recruiting No outcome recorded
Phase 3 NCT05270044 May 2022 → Mar 2027 expected melanoma Pierre Fabre Laboratories Active not recruiting No outcome recorded
Phase 3 NCT04657991 Jan 2021 → Jan 2026 overdue melanoma Pfizer Active not recruiting No outcome recorded
Phase 3 NCT03803553 Apr 2020 → Dec 2026 expected metastasis from malignant tumor of colon Massachusetts General Hospital Recruiting No outcome recorded
Phase 3 NCT02928224 Oct 2016 → Feb 2019 Pfizer Completed No outcome recorded
Phase 3 NCT01909453 Sep 2013 → Nov 2016 melanoma Pfizer Completed No outcome recorded
Phase 3 NCT01763164 Jul 2013 → Dec 2015 cutaneous melanoma Pfizer Completed No outcome recorded
Phase 3 NCT01849874 Jun 2013 → Jan 2016 fallopian tube serous adenocarcinoma, malignant ovarian serous tumor, primary peritoneal serous adenocarcinoma Pfizer Terminated No outcome recorded
Phase 42 trials
Phase 4 NCT07092410 Aug 2025 → Aug 2030 melanoma SRH Wald-Klinikum Gera GmbH Withdrawn No outcome recorded
Phase 4 NCT05203172 Jul 2022 → Jul 2029 expected cancer Pfizer Recruiting No outcome recorded
Phase not applicable1 trial
NCT04801966 Sep 2021 → Dec 2022 cancer Peter MacCallum Cancer Centre, Australia Terminated No outcome recorded
Also used as a comparator or background therapy in 4 trials
PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 12 trials
Phase 1 NCT04903119 Background Jun 2022 → Jul 2028 expected metastatic melanoma Rina Plattner Recruiting No outcome recorded
Phase 1 NCT03864042 Background Jan 2018 → Jul 2022 cancer, metastatic melanoma Pfizer Completed No outcome recorded
Phase 22 trials
Phase 2 NCT06470880 Comparator Jun 2024 → Jun 2026 overdue melanoma The Christie NHS Foundation Trust Not yet recruiting No outcome recorded
Phase 2 NCT05370807 Background Oct 2022 → Dec 2024 metastatic melanoma University Hospital Brussels Unknown No outcome recorded

Press releases naming this drug 5 releases

DateIssuerRelease
2025-10-19 Pfizer Pfizer’s BRAFTOVI® + MEKTOVI® Shows Sustained Long-Term Survival in Patients with Advanced Lung Cancer pfizer.com
2024-09-14 Pfizer Pfizer’s BRAFTOVI® + MEKTOVI® Shows Long-Term Clinically Meaningful Response in Patients with BRAF V600E-Mutant Metastatic Non-Small Cell Lung Cancer pfizer.com
2023-10-12 Pfizer U.S. FDA Approves Pfizer’s BRAFTOVI® + MEKTOVI® for BRAF V600E-Mutant Metastatic Non-Small Cell Lung Cancer pfizer.com
2023-04-04 Pfizer FDA Accepts Pfizer’s Supplemental New Drug Applications for BRAFTOVI + MEKTOVI pfizer.com
2019-09-29 Pfizer Pfizer Presents Interim Analysis Results from Phase 3 BEACON CRC Trial of BRAFTOVI® (Encorafenib), MEKTOVI® (Binimetinib) and Cetuximab for the Treatment of BRAFV600E-Mutant Metastatic Colorectal Cancer pfizer.com

Evidence & citations 14 cited values

Every value below carries the sentence it was read from. 135 sources stand behind the page.

FieldValueCited text
Known as Binimetinib “Phase Ib/II Study of the Efficacy and Safety of Binimetinib (MEK162) Plus Panitumumab for Mutant or Wild-Type RAS Metastatic Colorectal Cancer.” PMID 37597246 Dec 2023
96

“The purpose of this study was to evaluate binimetinib, a potent MEK1/2 inhibitor with demonstrated activity across multiple cancers, in LGSOC.” PMID 32822286 Aug 2020

“Approved BRAF-/MEK- inhibitor combinations include dabrafenib/trametinib and encorafenib/binimetinib.” NCT05370807

“Encorafenib and binimetinib delivered to UK standard of care.” NCT06470880

Binimetinib: 45 mg (3 × 15 mg oral tablet) twice daily (BID)” NCT06207656

Binimetinib 45 mg 2 times a day daily orally” NCT06229340

“Drug: BinimetinibNCT03563729

BinimetinibNCT05615818

NCT04720768

NCT05564377

NCT03991819

NCT03374254

NCT03693170

NCT03637491

NCT04494958

NCT04759846

NCT04965818

NCT03170206

NCT03235245

NCT03231306

NCT03973918

NCT03839342

NCT05564403

NCT04324112

NCT04903119

NCT04735068

NCT05554354

NCT02185690

NCT02964689

NCT02928224

NCT05270044

NCT04913285

NCT04870034

NCT03911869

NCT02451865

NCT03843775

NCT02263898

NCT05554367

NCT05111561

NCT04390243

NCT02465060

NCT04598009

NCT05340621

NCT03981614

NCT04801966

NCT05195632

NCT04800822

NCT04292119

NCT05767879

NCT05097378

NCT05203172

NCT02910700

NCT03803553

NCT05355701

NCT04655157

NCT03898908

NCT04322383

NCT05103891

NCT03271047

NCT04585815

NCT04005144

NCT04375527

NCT04439344

NCT04526782

NCT05926960

NCT04132505

NCT04543188

NCT03475004

NCT05510895

NCT05097599

NCT04741997

NCT03971409

NCT02834364

NCT07092410

NCT02510001

NCT04221438

NCT04044430

NCT03864042

NCT06887088

NCT03106415

NCT04074096

NCT04892017

NCT05286788

NCT05304546

NCT04720976

NCT06159478

NCT03947385

NCT05170334

NCT03915951

NCT04657991

NCT05026983

NCT03543969

NCT05080621

NCT04061980

NCT03878719

NCT04511013

NCT02902042

Known as ARRY-162 “An Open-Label, Phase I/II Study of Nilotinib (Tasigna) and MEK-162 (ARRY-162) Used in Combination” NCT02225574
Known as ARRY-438162 ClinicalTrials.gov intervention name — accepted as the source's own label NCT00959127
1

NCT00650767

Known as BIN “Here, we present phase I safety results from an open-label, phase I/II study of pembrolizumab (PEM), encorafenib (ENC) and binimetinib (BIN) triplet therapy in advanced, B-Raf...” PMID 34655839 Oct 2021
1

binimetinib (BIN)” NCT04657991

Known as Bini “The BEACON CRC study demonstrated that encorafenib (Enco)+cetuximab (Cetux)±binimetinib (Bini) significantly improved overall survival (OS) versus” PMID 39313594 Sep 2024
Known as MEK162 “Binimetinib (also known as MEK162) is an orally bioavailable, selective and potent mitogenactivated protein (MAP) kinase (MEK1 and MEK2) inhibitor, which is approved for use in...” NCT04322383
35

“Phase Ib/II Study of the Efficacy and Safety of Binimetinib (MEK162) Plus Panitumumab for Mutant or Wild-Type RAS Metastatic Colorectal Cancer.” PMID 37597246 Dec 2023

MEK162 is not FDA approved or commercially available.” NCT02089230

“ARRY-438162 (MEK162), MEK inhibitor; oral” NCT00959127

NCT02041481

NCT01556568

NCT02094872

NCT02089230

NCT03158103

NCT01649336

NCT02773459

NCT01801358

NCT02276027

NCT02285439

NCT01320085

NCT01763164

NCT02050815

NCT02159066

NCT01449058

NCT01543698

NCT01337765

NCT02631447

NCT02105350

NCT01909453

NCT01352273

NCT02613650

NCT01562899

NCT02049801

NCT01469130

NCT01363232

NCT01859026

NCT01885195

NCT01991379

NCT01828034

NCT02225574

NCT01781572

Known as MEK162/ARRY-438162 “Binimetinib (MEK162/ARRY-438162) is an orally bioavailable, small molecule selective and potent mitogen-activated protein kinase (MEK) 1 and MEK 2 inhibitor.” NCT03475004
Known as MEKTOVI “The current commercially available MEKTOVI® (binimetinib) 15 mg tablets are provided as immediate release film-coated tablets for oral administration.” NCT05103891
Known as NVP-MEK162 ChEMBL registry synonym — accepted as the source's own label CHEMBL3187723
Action Inhibit “Dual specificity mitogen-activated protein kinase kinase 1 inhibitor” CHEMBL3187723
2

“Dual specificity mitogen-activated protein kinase kinase 2 inhibitor” CHEMBL3187723

“MEK inhibitor” NCT00650767

Modality Small molecule “MEK162, a small-molecule MEK1/2 inhibitor” PMID 23414587 Feb 2013
Route Oral “ARRY-438162, MEK inhibitor; oralNCT00650767
Target MAP2K1 “Dual specificity mitogen-activated protein kinase kinase 1 inhibitor” CHEMBL3187723
Target MAP2K2 “Dual specificity mitogen-activated protein kinase kinase 2 inhibitor” CHEMBL3187723