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Revision as of 19:52, 10 November 2011 editBeetstra (talk | contribs)Edit filter managers, Administrators172,031 edits Script assisted update of identifiers for the Chem/Drugbox validation project (updated: 'ChEMBL', 'CASNo').← Previous edit Latest revision as of 19:23, 7 April 2024 edit undoIsla (talk | contribs)Extended confirmed users2,404 edits added Category:Drugs developed by Pfizer using HotCat 
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{{Chembox {{Chembox
| Verifiedfields = changed
⚫ | verifiedrevid = 455350271
| Watchedfields = changed
⚫ | verifiedrevid = 460016047
| ImageFile = Canertinib.svg | ImageFile = Canertinib.svg
| ImageSize = 200px | ImageSize = 200px
| IUPACName = ''N''-{4--7-quinazolin-6-yl}prop-2-enamide | PIN = ''N''-<nowiki/>{4-(3-Chloro-4-fluoroanilino)-7-quinazolin-6-yl}prop-2-enamide
| OtherNames = CI-1033; PD-183805 | OtherNames = CI-1033; PD-183805
| Section1 = {{Chembox Identifiers |Section1={{Chembox Identifiers
| IUPHAR_ligand = 5675
⚫ | CASNo = <!-- blanked - oldvalue: 267243-28-7 -->
| UNII_Ref = {{fdacite|correct|FDA}} | CASNo_Ref = {{cascite|changed|??}}
⚫ | CASNo = 267243-28-7
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = C78W1K5ASF | UNII = C78W1K5ASF
| ChEBI_Ref = {{ebicite|correct|EBI}} | ChEBI_Ref = {{ebicite|correct|EBI}}
| ChEBI = 61399 | ChEBI = 61399
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 31965 | ChEMBL = 31965
| ChEMBL1_Ref = {{ebicite|changed|EBI}}
| ChEMBL1 = 545315
| PubChem = 156414 | PubChem = 156414
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 137741 | ChemSpiderID = 137741
| SMILES = Fc1ccc(cc1Cl)Nc4ncnc3cc(OCCCN2CCOCC2)c(NC(=O)\C=C)cc34 | SMILES = Fc1ccc(cc1Cl)Nc4ncnc3cc(OCCCN2CCOCC2)c(NC(=O)\C=C)cc34
| InChI = 1/C24H25ClFN5O3/c1-2-23(32)30-21-13-17-20(14-22(21)34-9-3-6-31-7-10-33-11-8-31)27-15-28-24(17)29-16-4-5-19(26)18(25)12-16/h2,4-5,12-15H,1,3,6-11H2,(H,30,32)(H,27,28,29) | InChI = 1/C24H25ClFN5O3/c1-2-23(32)30-21-13-17-20(14-22(21)34-9-3-6-31-7-10-33-11-8-31)27-15-28-24(17)29-16-4-5-19(26)18(25)12-16/h2,4-5,12-15H,1,3,6-11H2,(H,30,32)(H,27,28,29)
| InChIKey = OMZCMEYTWSXEPZ-UHFFFAOYAG | InChIKey = OMZCMEYTWSXEPZ-UHFFFAOYAG
| StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 1S/C24H25ClFN5O3/c1-2-23(32)30-21-13-17-20(14-22(21)34-9-3-6-31-7-10-33-11-8-31)27-15-28-24(17)29-16-4-5-19(26)18(25)12-16/h2,4-5,12-15H,1,3,6-11H2,(H,30,32)(H,27,28,29) | StdInChI = 1S/C24H25ClFN5O3/c1-2-23(32)30-21-13-17-20(14-22(21)34-9-3-6-31-7-10-33-11-8-31)27-15-28-24(17)29-16-4-5-19(26)18(25)12-16/h2,4-5,12-15H,1,3,6-11H2,(H,30,32)(H,27,28,29)
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = OMZCMEYTWSXEPZ-UHFFFAOYSA-N | StdInChIKey = OMZCMEYTWSXEPZ-UHFFFAOYSA-N
}} }}
| Section2 = {{Chembox Properties |Section2={{Chembox Properties
| C=24|H=25|Cl=1|F=1|N=5|O=3 | C=24 | H=25 | Cl=1 | F=1 | N=5 | O=3
| Appearance = | Appearance =
| Density = | Density =
| MeltingPt = | MeltingPt =
| BoilingPt = | BoilingPt =
| Solubility = | Solubility =
}} }}
| Section3 = {{Chembox Hazards |Section3={{Chembox Hazards
| MainHazards = | MainHazards =
| FlashPt = | FlashPt =
| Autoignition = | AutoignitionPt =
}} }}
}} }}


'''Canertinib''' ('''CI-1033''') is an experimental drug candidate for the treatment of cancer. It is an ] ] with activity against ] (IC<sub>50</sub> 0.8&nbsp;nM), ] (IC<sub>50</sub> 19&nbsp;nM) and ] (IC<sub>50</sub> 7&nbsp;nM).<ref>{{cite journal | pmid = 10753475 | year = 2000 | last1 = Smaill | first1 = JB | last2 = Rewcastle | first2 = GW | last3 = Loo | first3 = JA | last4 = Greis | first4 = KD | last5 = Chan | first5 = OH | last6 = Reyner | first6 = EL | last7 = Lipka | first7 = E | last8 = Showalter | first8 = HD | last9 = Vincent | first9 = PW | title = 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 | volume = 43 | issue = 7 | pages = 1380–97 | journal = Journal of medicinal chemistry}}</ref><ref>, Selleck Chemicals</ref> '''Canertinib''' ('''CI-1033''') is an experimental drug candidate for the treatment of cancer. It is an ] ] with activity against ] (IC<sub>50</sub> 0.8&nbsp;nM), ] (IC<sub>50</sub> 19&nbsp;nM) and ] (IC<sub>50</sub> 7&nbsp;nM).<ref>{{cite journal | pmid = 10753475 | year = 2000 | last1 = Smaill | first1 = JB | last2 = Rewcastle | first2 = GW | last3 = Loo | first3 = JA | last4 = Greis | first4 = KD | last5 = Chan | first5 = OH | last6 = Reyner | first6 = EL | last7 = Lipka | first7 = E | last8 = Showalter | first8 = HD | last9 = Vincent | first9 = PW | last10 = Elliott | first10 = William L | last11 = Denny | first11 = William A | title = 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 | volume = 43 | issue = 7 | pages = 1380–97 | journal = Journal of Medicinal Chemistry | doi=10.1021/jm990482t| display-authors = 8 }}</ref><ref>, Selleck Chemicals</ref> By 2015, Pfizer had discontinued development of the drug.<ref>{{Cite web|url=http://adisinsight.springer.com/drugs/800012072|title = Canertinib - AdisInsight}}</ref>

Canertinib has been reported as a substrate for the transporter protein ]. Interaction of canertinib with OATP1B3 may alter its hepatic disposition and can lead to transporter mediated drug-drug interactions.<ref name="pmid24643910">{{cite journal |vauthors=Khurana V, Minocha M, Pal D, Mitra AK | title = Role of OATP-1B1 and/or OATP-1B3 in hepatic disposition of tyrosine kinase inhibitors. | journal = Drug Metabol Drug Interact. | volume = 29| issue = 3 | pages = 179–90 |date=March 2014 | pmid = 24643910 | doi = 10.1515/dmdi-2013-0062 | pmc=4407685}}</ref> Canertinib is not an inhibitor of the ] or OATP1B3 transporters.<ref name="Khurana V_2014">{{cite journal |vauthors=Khurana V, Minocha M, Pal D, Mitra AK | title = Inhibition of OATP-1B1 and OATP-1B3 by tyrosine kinase inhibitors. | journal = Drug Metabol Drug Interact. | volume = 29| issue = 4 | pages = 249–59 |date=May 2014 | pmid = 24807167 | doi = 10.1515/dmdi-2014-0014 | pmc=4407688}}</ref>


==References== ==References==
{{reflist}} {{Reflist|2}}

{{Growth factor receptor modulators}}


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