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Cobimetinib

Cobimetinib
Clinical data
Pronunciation/ˌkoʊbɪˈmɛtɪnɪb/ KOH-bim-ET-i-nib
Trade namesCotellic
Other namesGDC-0973, XL-518
AHFS/Drugs.comMonograph
MedlinePlusa615057
License data
Pregnancy
category
Routes of
administration		By mouth[2]
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailabilityreported from 28%[6] to 46%[2]
Protein binding95%[2]
MetabolismIntestinal and low Liver clearance (mostly CYP3A4 oxidation and UGT2B7 glucuronidation)[2][6]
Elimination half-life44 hours (mean)[2]
ExcretionFeces (76–77%), urine (17.9–18%) (after oral and IV administration)[2][7]
Identifiers
  • (S)-[3,4-Difluoro-2-(2-fluoro-4-iodophenylamino)phenyl] [3-hydroxy-3-(piperidin-2-yl)azetidin-1-yl] methanone
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC21H21F3IN3O2
Molar mass531.318 g·mol−1
3D model (JSmol)
  • C1CCN[C@@H](C1)C2(CN(C2)C(=O)C3=C(C(=C(C=C3)F)F)NC4=C(C=C(C=C4)I)F)O
  • InChI=1S/C21H21F3IN3O2/c22-14-6-5-13(19(18(14)24)27-16-7-4-12(25)9-15(16)23)20(29)28-10-21(30,11-28)17-3-1-2-8-26-17/h4-7,9,17,26-27,30H,1-3,8,10-11H2/t17-/m0/s1
  • Key:BSMCAPRUBJMWDF-KRWDZBQOSA-N

Cobimetinib, sold under the brand name Cotellic, is an anti-cancer medication used in combination with vemurafenib (Zelboraf) alone or with both vemurafenib and atezolizumab (Tecentriq) to treat melanoma.[2][8] Cobimetinib is a MEK inhibitor.[2] Cotellic, Zelboraf, and Tecentriq are all marketed by Genentech.[2][8][9]

The most common side effects include diarrhea, rash, nausea (feeling sick), vomiting, pyrexia (fever), photosensitivity (light sensitivity) reaction, abnormal results for certain liver function tests (increased levels of alanine aminotransferase, aspartate aminotransferase) and abnormal results for an enzyme related to muscle breakdown (creatine phosphokinase).[5]

Cobimetinib was approved for medical use in the United States in November 2015.[10][11]

  1. ^ a b "Products". guildlink.com.au.
  2. ^ a b c d e f g h i j "Cotellic- cobimetinib tablet, film coated". DailyMed. 5 November 2019. Retrieved 19 October 2020.
  3. ^ "Prescription medicines: registration of new chemical entities in Australia, 2016". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 10 April 2023.
  4. ^ "Health Canada New Drug Authorizations: 2016 Highlights". Health Canada. 14 March 2017. Retrieved 7 April 2024.
  5. ^ a b Cite error: The named reference Cotellic EPAR was invoked but never defined (see the help page).
  6. ^ a b Takahashi RH, Choo EF, Ma S, Wong S, Halladay J, Deng Y, et al. (January 2016). "Absorption, Metabolism, Excretion, and the Contribution of Intestinal Metabolism to the Oral Disposition of [14C]Cobimetinib, a MEK Inhibitor, in Humans". Drug Metabolism and Disposition. 44 (1): 28–39. doi:10.1124/dmd.115.066282. PMID 26451002.
  7. ^ Choo E, Takahashi R, Rooney I, Gates M, Deng A, Musib L (January 30, 2014). "Abstract B160: Assessing Human Absorption, Metabolism, Routes of Excretion and the Contribution of Intestinal Metabolism to the Oral Clearance of Cobimetinib, a MEK Inhibitor". Molecular Cancer Therapeutics. 12 (11 Supplement): B160. doi:10.1158/1535-7163.TARG-13-B160.
  8. ^ a b "Tecentriq- atezolizumab injection, solution". DailyMed. Retrieved 21 September 2021.
  9. ^ "Zelboraf- vemurafenib tablet, film coated". DailyMed. Retrieved 21 September 2021.
  10. ^ "Cotellic (cobimetinib) tablet". U.S. Food and Drug Administration (FDA). 8 December 2015. Retrieved 21 September 2021.
  11. ^ "Drug Trials Snapshots: Cotellic". U.S. Food and Drug Administration (FDA). 30 July 2020. Retrieved 21 September 2021. Public Domain This article incorporates text from this source, which is in the public domain.

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