Drugs / Cobimetinib
last change Aug 2026 re-read 2 minutes ago

Cobimetinib

Small molecule targets MAP2K1, MAP2K2 via inhibition

Developed for
melanoma · cancer · metastatic melanoma · colorectal cancer · non-small cell lung carcinoma · plasma cell myeloma · acute myeloid leukemia · cutaneous melanoma
+62 more · female breast carcinoma · metastatic malignant neoplasm · neoplasm · ovarian cancer · pancreatic adenocarcinoma · pancreatic ductal adenocarcinoma · breast cancer · chronic myelomonocytic leukemia · digestive system cancer · Erdheim-Chester disease · estrogen-receptor positive breast cancer · gallbladder carcinoma · hematopoietic and lymphoid cell neoplasm · histiocytosis · intrahepatic cholangiocarcinoma · metastatic malignant neoplasm in the brain · non-Hodgkin lymphoma · ovarian carcinoma · primary peritoneal carcinoma · refractory malignant neoplasm · soft tissue sarcoma · thyroid gland papillary carcinoma · thyroid gland undifferentiated (anaplastic) carcinoma · appendix adenocarcinoma · arteriovenous hemangioma/malformation · biliary tract cancer · cancer of unknown primary site · central nervous system melanocytic neoplasm · colorectal neoplasm · digestive system carcinoma · distal biliary tract carcinoma · endometrial carcinoma · fallopian tube cancer · fallopian tube carcinoma · glioma · Her2-receptor negative breast cancer · histiocytic sarcoma · inflammatory breast carcinoma · juvenile xanthogranuloma · Langerhans cell histiocytosis · laryngeal neoplasm · lung cancer · malignant histiocytosis · malignant pancreatic neoplasm · melanoma of soft tissue · metastatic neoplasm · neoplastic disease or syndrome · neoplastic syndrome · neurodegenerative disease · ovarian neoplasm · pancreatic large cell neuroendocrine carcinoma · papillary craniopharyngioma · poorly differentiated thyroid gland carcinoma · prostate carcinoma · refractory plasma cell neoplasm · salivary gland cancer · sinus histiocytosis with massive lymphadenopathy · skin squamous cell carcinoma · small intestine adenocarcinoma · thyroid gland follicular carcinoma · urinary bladder cancer · uterine corpus cancer
Investigated by
Genentech, Inc. · Hoffmann-La Roche · National Cancer Institute (NCI) · Bristol-Myers Squibb · Eli Lilly and Company · M.D. Anderson Cancer Center
+120 more · OHSU Knight Cancer Institute · Oregon Health and Science University · Pfizer · AstraZeneca · Fondazione Melanoma Onlus · GlaxoSmithKline · Roche Pharma AG · The Netherlands Cancer Institute · Bayer · Boehringer Ingelheim · Cancer Research UK · City of Hope Medical Center · Hanmi Pharmaceutical Company Limited · Janssen, LP · Merck Sharp & Dohme LLC · Novartis · Peter MacCallum Cancer Centre, Australia · Royal Marsden NHS Foundation Trust · University of Birmingham · University of Manchester · ABM Therapeutics Corporation · AbbVie · Alliance for Clinical Trials in Oncology · American Association for Cancer Research · American Society of Clinical Oncology · Amgen · Amsterdam UMC, location VUmc · Asan Medical Center · Assistance Publique - Hôpitaux de Paris · Baylor College of Medicine · BioLineRx, Ltd. · Canadian Cancer Trials Group · Cardiff Oncology · Carl Allen · Celgene Corporation · Center Eugene Marquis · Centre Leon Berard · Clinical Research Technology S.r.l. · Clovis Oncology - Pharma and · Columbia University · Dana-Farber Cancer Institute · Dutch Cancer Society · Eisai Inc. · European Network of Gynaecological Oncological Trial Groups (ENGOT) · Exelixis · Fondazione per la Medicina Personalizzata · Foundation Medicine · GOG Foundation · Georgetown University · German Cancer Research Center · H. Lee Moffitt Cancer Center and Research Institute · Halozyme Therapeutics · Haukeland University Hospital · Helse Fonna · Helse Forde · Helse Møre og Romsdal HF · Helse Nord-Trøndelag HF · Helse Stavanger HF · Helsinki University Central Hospital · Hospital of Southern Norway Trust · ImmVira Pharma Co. Ltd · Incyte Corporation · Innlandet Hospital Trust · Inova Health Care Services · InxMed (Shanghai) Co., Ltd. · Ipsen · Isala · Karyopharm Therapeutics Inc · Kliniken Essen-Mitte · Lovisenberg Diakonale Hospital · Massachusetts General Hospital · Mayo Clinic · MedSIR · Melanoma Research Alliance · all 126 on the full record

Regulatory milestones approvals, filings & regulatory actions · 5 recorded

MilestoneJurisdictionBrandIndicationDateSentence it was read from
Label expansions (3) US (FDA) COTELLIC 2018-01-26 – 2022-10-28 fda.gov
Approved EU (EMA) Cotellic 2015-11-20 europa.eu
Approved US (FDA) COTELLIC 2015-11-10 fda.gov

Trials 109 · started per year

today
US approved 2015
EU approved 2015
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200720082009201020112012201320142015201620172018201920202021202220232024202520262027
PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 02 trials
Phase 0 NCT05238831 Jan 2023 → May 2026 female breast carcinoma, ovarian carcinoma, pancreatic ductal adenocarcinoma, pancreatic large cell neuroendocrine carcinoma +2 OHSU Knight Cancer Institute Withdrawn No outcome recorded
Phase 0 NCT04005690 Aug 2019 → Jun 2026 overdue pancreatic ductal adenocarcinoma OHSU Knight Cancer Institute Recruiting No outcome recorded
Phase 131 trials
Phase 1 NCT05691504 Sep 2023 → Feb 2027 expected endometrial carcinoma, fallopian tube carcinoma, ovarian carcinoma, primary peritoneal carcinoma +1 National Cancer Institute (NCI) Active not recruiting No outcome recorded
Phase 1 NCT05441514 Apr 2023 → Mar 2026 acute myeloid leukemia City of Hope Medical Center Completed No outcome recorded
Phase 1 NCT05034627 Aug 2022 → Dec 2025 overdue pancreatic adenocarcinoma OHSU Knight Cancer Institute Active not recruiting No outcome recorded
Phase 1 NCT04835805 May 2021 → Dec 2026 expected melanoma Genentech, Inc. Active not recruiting No outcome recorded
Phase 1 NCT04190628 Jun 2020 → Apr 2024 neoplastic disease or syndrome ABM Therapeutics Corporation Terminated No outcome recorded
Phase 1 NCT03878524 Apr → Dec 2020 acute myeloid leukemia, atypical chronic myeloid leukemia, BCR-ABL1 negative, blast phase chronic myelogenous leukemia, BCR-ABL1 positive, castration-resistant prostate carcinoma +14 OHSU Knight Cancer Institute Terminated No outcome recorded
Phase 1 NCT04109456 Mar 2020 → Dec 2024 metastatic melanoma InxMed (Shanghai) Co., Ltd. Completed No outcome recorded
Phase 1 NCT03695380 Jan 2019 → Jul 2023 ovarian cancer Hoffmann-La Roche Completed No outcome recorded
Phase 1 NCT03178851 Jun 2017 → May 2019 melanoma Hoffmann-La Roche Completed No outcome recorded
Phase 1 NCT03284502 May 2017 → Sep 2024 metastatic neoplasm Hanmi Pharmaceutical Company Limited Unknown No outcome recorded
Phase 1/214 trials
Phase 1/2 NCT04214418 Feb 2020 → Apr 2022 digestive system cancer Columbia University Terminated No outcome recorded
Phase 1/2 NCT04216953 Feb 2020 → Dec 2024 soft tissue sarcoma Centre Leon Berard Completed No outcome recorded
Phase 1/2 NCT03989115 Jul 2019 → Feb 2022 cancer Revolution Medicines, Inc. Completed No outcome recorded
Phase 1/2 NCT03732703 Apr 2019 → Dec 2024 refractory plasma cell neoplasm Multiple Myeloma Research Consortium Completed No outcome recorded
Phase 1/2 NCT03566485 Jul 2018 → Dec 2020 Her2-receptor negative breast cancer, estrogen-receptor positive breast cancer, female breast carcinoma Vanderbilt-Ingram Cancer Center Terminated No outcome recorded
Phase 1/2 NCT03337698 Dec 2017 → Oct 2025 non-small cell lung carcinoma Hoffmann-La Roche Terminated No outcome recorded
Phase 1/2 NCT03312530 Nov 2017 → May 2021 plasma cell myeloma Hoffmann-La Roche Completed No outcome recorded
Phase 1/2 NCT03281369 Oct 2017 → Oct 2025 digestive system carcinoma Hoffmann-La Roche Completed No outcome recorded
Phase 1/2 NCT03202940 Sep 2017 → Jan 2029 expected non-small cell lung carcinoma Massachusetts General Hospital Active not recruiting No outcome recorded
Phase 1/2 NCT03193190 Jul 2017 → Feb 2025 pancreatic adenocarcinoma Hoffmann-La Roche Completed No outcome recorded
Phase 254 trials
Phase 2 NCT07449754 Feb 2026 → Sep 2029 expected melanoma Hanmi Pharmaceutical Company Limited Recruiting No outcome recorded
Phase 2 NCT06813079 Apr 2025 → Feb 2028 expected pancreatic ductal adenocarcinoma University Health Network, Toronto Recruiting No outcome recorded
Phase 2 NCT06440850 Jul 2024 → Nov 2026 expected thyroid gland follicular carcinoma, thyroid gland papillary carcinoma City of Hope Medical Center Recruiting No outcome recorded
Phase 2 NCT05756556 Jun 2024 → Dec 2026 melanoma ImmVira Pharma Co. Ltd Suspended 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 NCT05125471 Jul 2022 → Sep 2025 arteriovenous hemangioma/malformation University of Arkansas Completed No outcome recorded
Phase 2 NCT04941287 Dec 2021 → Jan 2024 overdue distal biliary tract carcinoma, gallbladder carcinoma, intrahepatic cholangiocarcinoma National Cancer Institute (NCI) Active not recruiting No outcome recorded
Phase 2 NCT05159245 Dec 2021 → Nov 2026 expected cancer, hematopoietic and lymphoid cell neoplasm Helsinki University Central Hospital Recruiting No outcome recorded
Phase 2 NCT04551521 Oct 2021 → Dec 2024 cancer German Cancer Research Center Completed No outcome recorded
Phase 2 NCT04931342 Oct 2021 → Feb 2028 expected ovarian cancer Hoffmann-La Roche Active not recruiting No outcome recorded
Phase 2/32 trials
Phase 2/3 NCT05768178 Mar 2023 → Oct 2029 expected Erdheim-Chester disease, colorectal neoplasm, glioma, laryngeal neoplasm +6 Cancer Research UK Recruiting No outcome recorded
Phase 2/3 NCT05722886 Mar 2023 → Oct 2029 expected cancer, hematopoietic and lymphoid cell neoplasm Cancer Research UK Recruiting No outcome recorded
Phase 35 trials
Phase 3 NCT04007848 Jul 2019 → Oct 2021 histiocytosis Assistance Publique - Hôpitaux de Paris Completed No outcome recorded
Phase 3 NCT03768063 Feb 2019 → Jul 2028 expected cancer Hoffmann-La Roche Active not recruiting No outcome recorded
Phase 3 NCT03273153 Dec 2017 → Apr 2019 melanoma Hoffmann-La Roche Terminated No outcome recorded
Phase 3 NCT02788279 Jul 2016 → Mar 2018 colorectal cancer Hoffmann-La Roche Completed No outcome recorded
Phase 3 NCT01689519 Jan 2013 → May 2014 melanoma Hoffmann-La Roche Completed 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 2 trials
PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 3 NCT02908672 Background Jan 2017 → Oct 2019 melanoma Hoffmann-La Roche Completed No outcome recorded
Phase 3 NCT02427893 Comparator Aug 2015 → Nov 2016 melanoma Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins Withdrawn No outcome recorded

Press releases naming this drug 3 releases

DateIssuerRelease
2020-07-31 Roche Global Development FDA approves Roche’s Tecentriq plus Cotellic and Zelboraf for people with advanced melanoma roche.com
2019-12-13 Roche Global Development Roche announces positive Phase III study results for Tecentriq plus Cotellic and Zelboraf in people with previously untreated BRAF V600 mutation-positive advanced melanoma roche.com
2018-05-10 Roche Global Development Roche provides update on Phase III study of Tecentriq (atezolizumab) and Cotellic (cobimetinib) in people with heavily pre-treated locally advanced or metastatic colorectal cancer roche.com

Evidence & citations 16 cited values

Every value below carries the sentence it was read from. 113 sources stand behind the page.

FieldValueCited text
Known as Cobimetinib “Comparing Oral to Intravenous Administration of GDC-0973 (Cobimetinib)” NCT01249118
108

Cobimetinib 60 mg on days 1-21, break 7 days, cycle 28 days orally” NCT06229340

NCT04079179

NCT03108131

NCT04591431

NCT01988896

NCT04185831

NCT03363867

NCT07449754

NCT03284502

NCT02303951

NCT02414750

NCT03178851

NCT01249131

NCT02908672

NCT04190628

NCT02876224

NCT02091141

NCT05441514

NCT05159245

NCT01876641

NCT03395899

NCT03878524

NCT01986166

NCT03224208

NCT03224767

NCT01974258

NCT05768178

NCT03625141

NCT03312530

NCT02537600

NCT02583516

NCT02693535

NCT01562275

NCT03175432

NCT03600701

NCT03554083

NCT04109456

NCT05238831

NCT03181100

NCT02300025

NCT04341181

NCT04931342

NCT05034627

NCT05756556

NCT02639546

NCT03340558

NCT01495988

NCT02060188

NCT04214418

NCT02457793

NCT03281369

NCT04941287

NCT02968303

NCT03337698

NCT03273153

NCT02768207

NCT06813079

NCT04409639

NCT02036086

NCT02788279

NCT03201458

NCT04216953

NCT03695380

NCT00996892

NCT03989115

NCT04007848

NCT01813214

NCT03768063

NCT01689519

NCT02649972

NCT03193190

NCT01271803

NCT03297606

NCT02427893

NCT04005690

NCT02136524

NCT02721459

NCT02670044

NCT02902029

NCT04551521

NCT03005639

NCT04302025

NCT01959633

NCT04801966

NCT03498521

NCT05125471

NCT02230306

NCT05691504

NCT03202316

NCT03566485

NCT04722575

NCT02291289

NCT03264066

NCT03202940

NCT06440850

NCT05722886

NCT01928394

NCT03101254

NCT01277718

NCT02818023

NCT01929876

NCT04835805

NCT03732703

NCT03430947

NCT02925234

NCT00467779

NCT01656642

NCT02322814

Known as Cob cobimetinib (Cob) 60 mg IV once daily, 21 days on/7 days off schedule (21/7).” NCT01656642
Known as Cobimetinib = code number RO5514041/F04 Cobimetinib = code number RO5514041/F04NCT02537600
Known as COBIMETINIB FUMARATE ChEMBL registry synonym — accepted as the source's own label CHEMBL2146883
Known as Cobimetinib hemifumarate ChEMBL registry synonym — accepted as the source's own label CHEMBL2146883
Known as Cotellic “Zelboraf + Cotellic used outside of indication, based on biomarker” NCT04817956
Known as GDC-0973 “Cobimetinib (GDC-0973, XL518) is a potent and highly selective inhibitor of MEK1 and MEK2, central components of the RAS/RAF pathway.” NCT01813214
3

“Vemurafenib Plus Cobimetinib (GDC-0973)” NCT02414750

NCT01249118

NCT01711762

Known as Gdc-0973 hemifumarate ChEMBL registry synonym — accepted as the source's own label CHEMBL2146883
Known as RG 7420 ChEMBL registry synonym — accepted as the source's own label CHEMBL2146883
Known as Xl-518 hemifumarate ChEMBL registry synonym — accepted as the source's own label CHEMBL2146883
Known as XL518 “Cobimetinib (GDC-0973, XL518) is a potent and highly selective inhibitor of MEK1 and MEK2, central components of the RAS/RAF pathway.” NCT01813214
Action Inhibit “Dual specificity mitogen-activated protein kinase kinase 2 inhibitor” CHEMBL2146883
1

“MEK inhibition with cobimetinib” PMID 25037139 Jul 2014

Modality Small molecule “small-molecule inhibitor” NCT03395899
Route Oral “Repeating oral dose” NCT00467779
Target MAP2K1 “cobimetinib (GDC-0973), a highly selective inhibitor of MEK1” NCT02414750
Target MAP2K2 “Dual specificity mitogen-activated protein kinase kinase 2 inhibitor” CHEMBL2146883