Literature DB >> 26452567

Cobimetinib: First Global Approval.

Karly P Garnock-Jones1.   

Abstract

Genentech (a subsidiary of Roche) and Exelixis are developing cobimetinib, an orally available small molecule, for the treatment of various cancers, including malignant melanoma and breast cancer. Cobimetinib inhibits the MEK (mitogen-activated protein kinase) component of the MAPK/ERK signalling pathway, which is frequently over-activated in human tumours. The product has been approved in Switzerland in combination with vemurafenib for the treatment of patients with unresectable or metastatic BRAF V600 mutation-positive melanoma, and is under regulatory review for the same indication in several countries, including the USA and the EU. This article summarizes the milestones in the development of cobimetinib leading to this first approval for unresectable or metastatic BRAF V600 mutation-positive melanoma melanoma.

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Year:  2015        PMID: 26452567     DOI: 10.1007/s40265-015-0477-8

Source DB:  PubMed          Journal:  Drugs        ISSN: 0012-6667            Impact factor:   9.546


  10 in total

1.  Combined vemurafenib and cobimetinib in BRAF-mutated melanoma.

Authors:  James Larkin; Paolo A Ascierto; Brigitte Dréno; Victoria Atkinson; Gabriella Liszkay; Michele Maio; Mario Mandalà; Lev Demidov; Daniil Stroyakovskiy; Luc Thomas; Luis de la Cruz-Merino; Caroline Dutriaux; Claus Garbe; Mika A Sovak; Ilsung Chang; Nicholas Choong; Stephen P Hack; Grant A McArthur; Antoni Ribas
Journal:  N Engl J Med       Date:  2014-09-29       Impact factor: 91.245

2.  Vemurafenib and cobimetinib in BRAF-mutated melanoma.

Authors:  Ahmadur Rahman
Journal:  Lancet Oncol       Date:  2014-10-10       Impact factor: 41.316

Review 3.  Achievements and challenges of molecular targeted therapy in melanoma.

Authors:  Ryan Sullivan; Patricia LoRusso; Scott Boerner; Reinhard Dummer
Journal:  Am Soc Clin Oncol Educ Book       Date:  2015

4.  Absolute bioavailability and effect of formulation change, food, or elevated pH with rabeprazole on cobimetinib absorption in healthy subjects.

Authors:  Luna Musib; Edna Choo; Yuzhong Deng; Steve Eppler; Isabelle Rooney; Iris T Chan; Mark J Dresser
Journal:  Mol Pharm       Date:  2013-09-30       Impact factor: 4.939

5.  Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973).

Authors:  Kenneth D Rice; Naing Aay; Neel K Anand; Charles M Blazey; Owen J Bowles; Joerg Bussenius; Simona Costanzo; Jeffry K Curtis; Steven C Defina; Larisa Dubenko; Stefan Engst; Anagha A Joshi; Abigail R Kennedy; Angie I Kim; Elena S Koltun; Julie C Lougheed; Jean-Claire L Manalo; Jean-Francois Martini; John M Nuss; Csaba J Peto; Tsze H Tsang; Peiwen Yu; Stuart Johnston
Journal:  ACS Med Chem Lett       Date:  2012-04-09       Impact factor: 4.345

6.  Bridging the gap between preclinical and clinical studies using pharmacokinetic-pharmacodynamic modeling: an analysis of GDC-0973, a MEK inhibitor.

Authors:  Harvey Wong; Laurent Vernillet; Amy Peterson; Joseph A Ware; Lillian Lee; Jean-Francois Martini; Peiwen Yu; Congfen Li; Geoffrey Del Rosario; Edna F Choo; Klaus P Hoeflich; Yongchang Shi; Blake T Aftab; Ron Aoyama; Sanh Tan Lam; Marcia Belvin; John Prescott
Journal:  Clin Cancer Res       Date:  2012-04-10       Impact factor: 12.531

7.  Combination of vemurafenib and cobimetinib in patients with advanced BRAF(V600)-mutated melanoma: a phase 1b study.

Authors:  Antoni Ribas; Rene Gonzalez; Anna Pavlick; Omid Hamid; Thomas F Gajewski; Adil Daud; Lawrence Flaherty; Theodore Logan; Bartosz Chmielowski; Karl Lewis; Damien Kee; Peter Boasberg; Ming Yin; Iris Chan; Luna Musib; Nicholas Choong; Igor Puzanov; Grant A McArthur
Journal:  Lancet Oncol       Date:  2014-07-15       Impact factor: 41.316

8.  Role of P-glycoprotein on the brain penetration and brain pharmacodynamic activity of the MEK inhibitor cobimetinib.

Authors:  Edna F Choo; Justin Ly; Jocelyn Chan; Sheerin K Shahidi-Latham; Kirsten Messick; Emile Plise; Cristine M Quiason; Lulu Yang
Journal:  Mol Pharm       Date:  2014-10-03       Impact factor: 4.939

9.  FDG-PET is a good biomarker of both early response and acquired resistance in BRAFV600 mutant melanomas treated with vemurafenib and the MEK inhibitor GDC-0973.

Authors:  Andreas R Baudy; Taner Dogan; Judith E Flores-Mercado; Klaus P Hoeflich; Fei Su; Nicholas van Bruggen; Simon-Peter Williams
Journal:  EJNMMI Res       Date:  2012-05-31       Impact factor: 3.138

Review 10.  MEK and the inhibitors: from bench to bedside.

Authors:  Akintunde Akinleye; Muhammad Furqan; Nikhil Mukhi; Pavan Ravella; Delong Liu
Journal:  J Hematol Oncol       Date:  2013-04-12       Impact factor: 17.388

  10 in total
  13 in total

Review 1.  The State-of-the-Art of Phase II/III Clinical Trials for Targeted Pancreatic Cancer Therapies.

Authors:  Andres Garcia-Sampedro; Gabriella Gaggia; Alexander Ney; Ismahan Mahamed; Pilar Acedo
Journal:  J Clin Med       Date:  2021-02-03       Impact factor: 4.241

Review 2.  Small-molecule inhibitors, immune checkpoint inhibitors, and more: FDA-approved novel therapeutic drugs for solid tumors from 1991 to 2021.

Authors:  Qing Wu; Wei Qian; Xiaoli Sun; Shaojie Jiang
Journal:  J Hematol Oncol       Date:  2022-10-08       Impact factor: 23.168

3.  Insights into the binding mode of MEK type-III inhibitors. A step towards discovering and designing allosteric kinase inhibitors across the human kinome.

Authors:  Zheng Zhao; Lei Xie; Philip E Bourne
Journal:  PLoS One       Date:  2017-06-19       Impact factor: 3.240

Review 4.  Receptor tyrosine kinases and downstream pathways as druggable targets for cancer treatment: the current arsenal of inhibitors.

Authors:  Wagner Ricardo Montor; Andrei Ronaldo Oliveira Silva Escartin Salas; Fabiana Henriques Machado de Melo
Journal:  Mol Cancer       Date:  2018-02-19       Impact factor: 27.401

5.  Development of ultra-short PCR assay to reveal BRAF V600 mutation status in Thai colorectal cancer tissues.

Authors:  Nunthawut Chat-Uthai; Pichpisith Vejvisithsakul; Sutthirat Udommethaporn; Puttarakun Meesiri; Chetiya Danthanawanit; Yannawan Wongchai; Chinachote Teerapakpinyo; Shanop Shuangshoti; Naravat Poungvarin
Journal:  PLoS One       Date:  2018-06-07       Impact factor: 3.240

6.  Isoform-selective activity-based profiling of ERK signaling.

Authors:  Myungsun Shin; Caroline E Franks; Ku-Lung Hsu
Journal:  Chem Sci       Date:  2018-02-06       Impact factor: 9.825

7.  Synthesis and Biological Evaluation of New Madecassic Acid Derivatives Targeting ERK Cascade Signaling.

Authors:  Ana S C Valdeira; Daniel A Ritt; Deborah K Morrison; James B McMahon; Kirk R Gustafson; Jorge A R Salvador
Journal:  Front Chem       Date:  2018-09-28       Impact factor: 5.221

Review 8.  The Role of Immune Checkpoint Blockade in Uveal Melanoma.

Authors:  Anja Wessely; Theresa Steeb; Michael Erdmann; Lucie Heinzerling; Julio Vera; Max Schlaak; Carola Berking; Markus Vincent Heppt
Journal:  Int J Mol Sci       Date:  2020-01-29       Impact factor: 5.923

Review 9.  Combination Strategies Using EGFR-TKi in NSCLC Therapy: Learning from the Gap between Pre-Clinical Results and Clinical Outcomes.

Authors:  Zheng Yang; Kin Yip Tam
Journal:  Int J Biol Sci       Date:  2018-02-05       Impact factor: 6.580

10.  STK405759 as a combination therapy with bortezomib or dexamethasone, in in vitro and in vivo multiple myeloma models.

Authors:  Gabriela Rozic; Lena Paukov; Ziv Cohen; Irit Shapira; Adrian Duek; Ohad Bejamini; Abraham Avigdor; Arnon Nagler; Igor Koman; Merav Leiba
Journal:  Oncotarget       Date:  2018-07-31
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