User:Mr. Ibrahem/Cobimetinib

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Mr. Ibrahem/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
  • AU: D
Routes of
administration		By mouth (tablets)[1]
Drug classMEK inhibitor[1]
Legal status
Legal status
Pharmacokinetic data
Bioavailabilityreported from 28%[3] to 46%[1]
Protein binding95%[1]
MetabolismIntestinal and low liver clearance (mostly CYP3A4 oxidation and UGT2B7 glucuronidation)[1][3]
Elimination half-life44 hours (mean)[1]
ExcretionFeces (76–77%), urine (17.9–18%) (after oral and IV administration)[1][4]
Identifiers
  • (S)-[3,4-Difluoro-2-(2-fluoro-4-iodophenylamino)phenyl] [3-hydroxy-3-(piperidin-2-yl)azetidin-1-yl] methanone
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 among others, is a medication used to treat melanoma.[1] Specifically it is used for advanced disease with either BRAF V600E or V600K mutation.[1] It is used together with vemurafenib.[1] Use is not recommended in the United Kingdom.[5] It is taken by mouth.[1]

Common side effects include diarrhea, rash, nausea, fever, sunburns, liver problems, or muscle damage.[2] Other side effects may include bleeding, heart damage, and retinal vein occlusion.[1] Use during pregnancy may harm the baby.[1] It is a MEK inhibitor.[1]

Cobimetinib was approved for medical use in the United States and Europe in 2015.[1][2] In the United Kingdom treatment for 4 weeks costs the NHS about £4,275 as of 2021.[5] This amount in the United States is about 7,300 USD.[6]

References[edit]

  1. ^ a b c d e f g h i j k l m n o p q r "Cotellic- cobimetinib tablet, film coated". DailyMed. 5 November 2019. Archived from the original on 4 August 2020. Retrieved 19 October 2020.
  2. ^ a b c d "Cotellic". Archived from the original on 20 January 2021. Retrieved 6 January 2022.
  3. ^ 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.
  4. ^ 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.
  5. ^ a b BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 1019. ISBN 978-0857114105.
  6. ^ "Cotellic Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 26 January 2021. Retrieved 6 January 2022.
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