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Rociletinib

From Wikipedia, the free encyclopedia
Cancelled developmental cancer drug
Pharmaceutical compound
Rociletinib
Clinical data
Trade namesXegafri
Other namesCO-1686, AVL-301
Routes of
administration
By mouth
ATC code
Identifiers
  • N-(3-{[2-{[4-(4-Acetyl-1-piperazinyl)-2-methoxyphenyl]amino}-5-(trifluoromethyl)-4-pyrimidinyl]amino}phenyl)acrylamide
CAS Number
PubChemCID
DrugBank
ChemSpider
UNII
KEGG
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC27H28F3N7O3
Molar mass555.562 g·mol−1
3D model (JSmol)
  • CC(=O)N1CCN(CC1)c2ccc(c(c2)OC)Nc3ncc(c(n3)Nc4cccc(c4)NC(=O)C=C)C(F)(F)F
  • 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

Rociletinib is a medication developed to treatnon-small cell lung carcinomas with a specific mutation. It is a third-generationepidermal growth factor receptortyrosine kinase inhibitor.[1] It was beingdeveloped byClovis Oncology as a potential treatment fornon-small-cell lung cancer.[1] In May 2016, development of rociletinib was halted, along with its associated clinical trials, and Clovis Oncology withdrew itsmarketing authorisation application from theEuropean Medicines Agency.[1]

References

[edit]
  1. ^abcVan 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.
CImonoclonal antibodies ("-mab")
Receptor tyrosine kinase
Others for solid tumors
Leukemia/lymphoma
Other
Tyrosine kinase inhibitors ("-nib")
Receptor tyrosine kinase
Non-receptor
Other
Angiopoietin
CNTF
EGF (ErbB)
EGF
(ErbB1/HER1)
ErbB2/HER2
ErbB3/HER3
ErbB4/HER4
FGF
FGFR1
FGFR2
FGFR3
FGFR4
Unsorted
HGF (c-Met)
IGF
IGF-1
IGF-2
Others
LNGF (p75NTR)
PDGF
RET (GFL)
GFRα1
GFRα2
GFRα3
GFRα4
Unsorted
SCF (c-Kit)
TGFβ
Trk
TrkA
TrkB
TrkC
VEGF
Others


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