Canertinib
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Preferred IUPAC name N-{4-(3-Chloro-4-fluoroanilino)-7-[3-(morpholin-4-yl)propoxy]quinazolin-6-yl}prop-2-enamide | |
Other names CI-1033; PD-183805 | |
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Properties | |
Chemical formula | C24H25ClFN5O3 |
Molar mass | 485.94 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). N verify (what is YN ?) Infobox references |
Chemical compound
Canertinib (CI-1033) is an experimental drug candidate for the treatment of cancer. It is an irreversible tyrosine-kinase inhibitor with activity against EGFR (IC50 0.8 nM), HER-2 (IC50 19 nM) and ErbB-4 (IC50 7 nM).[1][2] By 2015, Pfizer had discontinued development of the drug.[3]
Canertinib has been reported as a substrate for the transporter protein OATP1B3. Interaction of canertinib with OATP1B3 may alter its hepatic disposition and can lead to transporter mediated drug-drug interactions.[4] Canertinib is not an inhibitor of the OATP1B1 or OATP1B3 transporters.[5]
References
- ^ Smaill, JB; Rewcastle, GW; Loo, JA; Greis, KD; Chan, OH; Reyner, EL; Lipka, E; Showalter, HD; et al. (2000). "Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido3,2-dpyrimidine-6-acrylamides bearing additional solubilizing functions". Journal of Medicinal Chemistry. 43 (7): 1380–97. doi:10.1021/jm990482t. PMID 10753475.
- ^ CI-1033 (Canertinib), Selleck Chemicals
- ^ "Canertinib - AdisInsight".
- ^ Khurana V, Minocha M, Pal D, Mitra AK (March 2014). "Role of OATP-1B1 and/or OATP-1B3 in hepatic disposition of tyrosine kinase inhibitors". Drug Metabol Drug Interact. 29 (3): 179–90. doi:10.1515/dmdi-2013-0062. PMC 4407685. PMID 24643910.
- ^ Khurana V, Minocha M, Pal D, Mitra AK (May 2014). "Inhibition of OATP-1B1 and OATP-1B3 by tyrosine kinase inhibitors". Drug Metabol Drug Interact. 29 (4): 249–59. doi:10.1515/dmdi-2014-0014. PMC 4407688. PMID 24807167.
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- Agonists: Angiopoietin 1
- Angiopoietin 4
- Antagonists: Angiopoietin 2
- Angiopoietin 3
- Kinase inhibitors: Altiratinib
- CE-245677
- Rebastinib
- Antibodies: Evinacumab (against angiopoietin 3)
- Nesvacumab (against angiopoietin 2)
EGF (ErbB1/HER1) |
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ErbB2/HER2 |
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ErbB3/HER3 |
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ErbB4/HER4 |
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FGFR1 | |
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FGFR2 |
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FGFR3 | |
FGFR4 | |
Unsorted |
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- Agonists: Fosgonimeton
- Hepatocyte growth factor
- Potentiators: Dihexa (PNB-0408)
- Kinase inhibitors: Altiratinib
- AM7
- AMG-458
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- BMS-777607
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- INCB28060
- JNJ-38877605
- K252a
- MK-2461
- PF-04217903
- PF-2341066
- PHA-665752
- SU-11274
- Tivantinib
- Volitinib
- Antibodies: Emibetuzumab
- Ficlatuzumab
- Flanvotumab
- Onartuzumab
- Rilotumumab
- Telisotuzumab
- Telisotuzumab vedotin
IGF-1 |
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IGF-2 |
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Others |
- Antagonists: ALE-0540
- Dexamethasone
- EVT-901 (SAR-127963)
- Testosterone
- Antibodies: Against NGF: ABT-110 (PG110)
- ASP-6294
- Fasinumab
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- Aptamers: Against NGF: RBM-004
- Decoy receptors: LEVI-04 (p75NTR-Fc)
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- Kinase inhibitors: Agerafenib
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- Ripretinib
- Sunitinib
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- Antibodies: Olaratumab
- Ramucirumab
- Tovetumab
GFRα1 |
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GFRα2 |
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GFRα3 |
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GFRα4 |
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Unsorted |
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- See here instead.
TrkA |
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TrkB |
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TrkC |
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- Agonists: Placental growth factor (PGF)
- Ripretinib
- Telbermin
- VEGF (A, B, C, D (FIGF))
- Allosteric modulators: Cyclotraxin B
- Kinase inhibitors: Agerafenib
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- WHI-P 154
- Antibodies: Alacizumab pegol
- Bevacizumab
- Icrucumab
- Ramucirumab
- Ranibizumab
- Decoy receptors: Aflibercept
- Additional growth factors: Adrenomedullin
- Colony-stimulating factors (see here instead)
- Connective tissue growth factor (CTGF)
- Ephrins (A1, A2, A3, A4, A5, B1, B2, B3)
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- Glucose-6-phosphate isomerase (GPI; PGI, PHI, AMF)
- Glia maturation factor (GMF)
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- Pleiotrophin
- Renalase
- Thrombopoietin (see here instead)
- Wnt signaling proteins
- Additional growth factor receptor modulators: Cerebrolysin (neurotrophin mixture)
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