Cobimetinib

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Cobimetinib
Cobimetinib.svg
Systematic (IUPAC) name
[3,4-Difluoro-2-(2-fluoro-4-iodoanilino)phenyl]{3-hydroxy-3-[(2S)-piperidin-2-yl]azetidin-1-yl} methanone
Clinical data
  • Investigational
Identifiers
934660-93-2
None
PubChem CID 16222096
ChemSpider 17349374
ChEMBL CHEMBL2146883
Chemical data
Formula C21H21F3IN3O2
531.3 g/mol

Cobimetinib (GDC-0973, XL-518) is a MEK inhibitor being developed by Exelixis and Roche. It is being studied in combination with BRAF inhibitors to treat several cancers. Early data showed that administration of Cobimetinib in combination with the BRAF inhibitor vemurafenib increased progression-free survival in melanoma patients with a BRAF V600 mutation by 3.7 months compared to vemurafenib alone.[1] Phase 3 clinical trials are ongoing and expected to complete by 2017.[2] After good results in 2014 the combination has been submitted to EC and FDA for marketing approval.[3]

References[edit]

  1. ^ Larkin, J., Ascierto, P.A., Dreno, B., Atkinson, V., Liszkay, G., Maio, M., Mandala, M., Demidov, L., Stroyakovskiy, D., Thomas, L., de la Cruz-Merino, L., Dutriaux, C., Garbe, C., Sovak, M.A., Chang, I., Choong, N., Hack, S.P., McArthur, G.A., Ribas, A., "Combined Vemurafenib and Cobimetinib in BRAF-Mutated Melanoma" NEJM, 2014, 371, doi:10.1056/NEJMoa1408868
  2. ^ coBRIM: A Phase 3 Study Comparing GDC-0973 (Cobimetinib), a MEK Inhibitor, in Combination With Vemurafenib vs Vemurafenib Alone in Patients With Metastatic Melanoma
  3. ^ Cobimetinib at exelixis.com

External links[edit]