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Cancelled developmental cancer drug
Rociletinib
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Trade names | Xegafri |
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Other names | CO-1686, AVL-301 |
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Routes of administration |
By mouth |
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ATC code | |
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N-(3-{[2-{[4-(4-Acetyl-1-piperazinyl)-2-methoxyphenyl]amino}-5-(trifluoromethyl)-4-pyrimidinyl]amino}phenyl)acrylamide
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CAS Number | |
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PubChem
CID | |
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DrugBank | |
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ChemSpider | |
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UNII | |
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KEGG | |
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Formula | C27H28F3N7O3 |
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Molar mass | 555.562 g·mol−1 |
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3D model (
JSmol) | |
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CC(=O)N1CCN(CC1)c2ccc(c(c2)OC)Nc3ncc(c(n3)Nc4cccc(c4)NC(=O)C=C)C(F)(F)F
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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
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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]
References
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CI
monoclonal antibodies ("-mab") | |
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Tyrosine kinase inhibitors ("-nib") |
Receptor tyrosine kinase |
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RET inhibitors:
Entrectinib (ALK, ROS1, NTRK),
Futibatinib (FGFR2),
Infigratinib,
Larotrectinib (NTRK),
Pemigatinib (FGFR),
Pralsetinib,
Repotrectinib (ROS1, TRK, ALK),
Selpercatinib (VEGFR, FGFR),
Vandetanib (VEGFR, EGFR).
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Non-receptor | |
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Other | |
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Angiopoietin | |
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CNTF | |
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EGF (ErbB) | |
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FGF |
FGFR1 | |
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FGFR2 |
- Agonists:
Ersofermin
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FGF (
1,
2 (bFGF),
3,
4,
5,
6,
7 (
KGF),
8,
9,
10 (KGF2),
17,
18,
22)
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Palifermin
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Repifermin
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Selpercatinib
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Sprifermin
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Trafermin
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FGFR3 | |
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FGFR4 | |
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Unsorted | |
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HGF (c-Met) | |
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IGF | |
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LNGF (p75NTR) | |
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PDGF | |
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RET (GFL) | |
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SCF (c-Kit) | |
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TGFβ | |
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Trk |
TrkA |
- Negative allosteric modulators:
VM-902A
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TrkB |
- Agonists:
3,7-DHF
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3,7,8,2'-THF
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4'-DMA-7,8-DHF
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7,3'-DHF
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7,8-DHF
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7,8,2'-THF
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7,8,3'-THF
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Amitriptyline
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BDNF
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BNN-20
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Deoxygedunin
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Deprenyl
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Diosmetin
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DMAQ-B1
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HIOC
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LM22A-4
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N-Acetylserotonin
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NT-3
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NT-4
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Norwogonin (5,7,8-THF)
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R7
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R13
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TDP6
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TrkC | |
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VEGF | |
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Others |
- Additional growth factors:
Adrenomedullin
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Colony-stimulating factors (see
here instead)
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Connective tissue growth factor (CTGF)
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Ephrins (
A1,
A2,
A3,
A4,
A5,
B1,
B2,
B3)
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Erythropoietin (see
here instead)
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Glucose-6-phosphate isomerase (GPI; PGI, PHI, AMF)
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Glia maturation factor (GMF)
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Hepatoma-derived growth factor (HDGF)
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Interleukins/
T-cell growth factors (see
here instead)
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Leukemia inhibitory factor (LIF)
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Macrophage-stimulating protein (MSP; HLP, HGFLP)
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Midkine (NEGF2)
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Migration-stimulating factor (MSF; PRG4)
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Oncomodulin
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Pituitary adenylate cyclase-activating peptide (PACAP)
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Pleiotrophin
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Renalase
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Thrombopoietin (see
here instead)
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Wnt signaling proteins
- Additional growth factor receptor modulators:
Cerebrolysin (neurotrophin mixture)
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