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Rociletinib

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Cancelled developmental cancer drug Pharmaceutical compound
Rociletinib
Clinical data
Trade namesXegafri
Other namesCO-1686, AVL-301
Routes of
administration
By mouth
ATC code
Identifiers
IUPAC name
  • N-(3-{amino}-5-(trifluoromethyl)-4-pyrimidinyl]amino}phenyl)acrylamide
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC27H28F3N7O3
Molar mass555.562 g·mol
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

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. It was being developed by Clovis Oncology as a potential treatment for non-small-cell lung cancer. 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.

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.
Targeted cancer therapy / antineoplastic agents (L01)
CI monoclonal antibodies ("-mab")
Receptor tyrosine kinase
Others for solid tumors
Leukemia/lymphoma
Other
Tyrosine kinase inhibitors ("-nib")
Receptor tyrosine kinase
Non-receptor
Other
Growth factor receptor modulators
Angiopoietin
CNTF
EGF (ErbB)
EGF
(ErbB1/HER1)
ErbB2/HER2
  • Agonists: Unknown/none
ErbB3/HER3
ErbB4/HER4
FGF
FGFR1
FGFR2
FGFR3
FGFR4
Unsorted
HGF (c-Met)
IGF
IGF-1
IGF-2
Others
LNGF (p75)
PDGF
RET (GFL)
GFRα1
GFRα2
GFRα3
GFRα4
Unsorted
SCF (c-Kit)
TGFβ
Trk
TrkA
  • Negative allosteric modulators: VM-902A
TrkB
TrkC
VEGF
Others
  • Additional growth factor receptor modulators: Cerebrolysin (neurotrophin mixture)


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