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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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CompTox Dashboard (EPA) | |
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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]
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CI monoclonal antibodies ("-mab") | |
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Tyrosine kinase inhibitors ("-nib") | Receptor tyrosine kinase |
- 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
- FGF (1, 2 (bFGF), 3, 4, 5, 6, 7 (KGF), 8, 9, 10 (KGF2), 17, 18, 22)
- Palifermin
- Repifermin
- Selpercatinib
- Sprifermin
- 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
- 3,7,8,2'-THF
- 4'-DMA-7,8-DHF
- 7,3'-DHF
- 7,8-DHF
- 7,8,2'-THF
- 7,8,3'-THF
- Amitriptyline
- BDNF
- BNN-20
- Deoxygedunin
- Deprenyl
- Diosmetin
- DMAQ-B1
- HIOC
- LM22A-4
- N-Acetylserotonin
- NT-3
- NT-4
- Norwogonin (5,7,8-THF)
- R7
- R13
- TDP6
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TrkC | |
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VEGF | |
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Others |
- Additional growth factors: Adrenomedullin
- Colony-stimulating factors (see here instead)
- Connective tissue growth factor (CTGF)
- Ephrins (A1, A2, A3, A4, A5, B1, B2, B3)
- Erythropoietin (see here instead)
- Glucose-6-phosphate isomerase (GPI; PGI, PHI, AMF)
- Glia maturation factor (GMF)
- Hepatoma-derived growth factor (HDGF)
- Interleukins/T-cell growth factors (see here instead)
- Leukemia inhibitory factor (LIF)
- Macrophage-stimulating protein (MSP; HLP, HGFLP)
- Midkine (NEGF2)
- Migration-stimulating factor (MSF; PRG4)
- Oncomodulin
- Pituitary adenylate cyclase-activating peptide (PACAP)
- Pleiotrophin
- Renalase
- Thrombopoietin (see here instead)
- Wnt signaling proteins
- Additional growth factor receptor modulators: Cerebrolysin (neurotrophin mixture)
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