Rociletinib

Rociletinib is a medication developed to treat non-small cell lung carcinomas with a specific mutation. It is a third-generation epidermal growth factor receptor tyrosine kinase inhibitor.[1] It was being developed by Clovis Oncology as a potential treatment for non-small-cell lung cancer.[1] In May 2016, development of rociletinib was halted, along with its associated clinical trials, and Clovis Oncology withdrew its marketing authorisation application from the European Medicines Agency.[1]

Rociletinib
Clinical data
Trade namesXegafri
Other namesCO-1686, AVL-301
Routes of
administration		By mouth
ATC code
Identifiers
IUPAC name
  • N-(3-{[2-{[4-(4-Acetyl-1-piperazinyl)-2-methoxyphenyl]amino}-5-(trifluoromethyl)-4-pyrimidinyl]amino}phenyl)acrylamide
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
Chemical and physical data
FormulaC27H28F3N7O3
Molar mass555.562 g·mol−1
3D model (JSmol)
SMILES
  • CC(=O)N1CCN(CC1)c2ccc(c(c2)OC)Nc3ncc(c(n3)Nc4cccc(c4)NC(=O)C=C)C(F)(F)F
InChI
  • InChI=1S/C27H28F3N7O3/c1-4-24(39)32-18-6-5-7-19(14-18)33-25-21(27(28,29)30)16-31-26(35-25)34-22-9-8-20(15-23(22)40-3)37-12-10-36(11-13-37)17(2)38/h4-9,14-16H,1,10-13H2,2-3H3,(H,32,39)(H2,31,33,34,35)
  • Key:HUFOZJXAKZVRNJ-UHFFFAOYSA-N

References
  1. Van Der Steen N, Caparello C, Rolfo C, Pauwels P, Peters GJ, Giovannetti E (2016). "New developments in the management of non-small-cell lung cancer, focus on rociletinib: what went wrong?". OncoTargets and Therapy. 9: 6065–6074. doi:10.2147/OTT.S97644. PMC 5063481. PMID 27785053.


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