General Information of the Drug (ID: M6APDG03286)
Name
Lapatinib ditosylate
Synonyms
Lapatinib (GW-572016) Ditosylate; Lapatinib (ditosylate); Lapatinib Ditosylate; Tykerb Ditosylate; 388082-77-7; 4WK72K94MC; AK-47669; GW-57201; GW-572016F Ditosylate; N-(3-CHLORO-4-((3-FLUOROBENZYL)OXY)PHENYL)-6-(5-(((2-(METHYLSULFONYL)ETHYL)AMINO)METHYL)FURAN-2-YL)QUINAZOLIN-4-AMINE BIS(4-METHYLBENZENESULFONATE); N-{3-chloro-4-[(3-fluorophenyl)methoxy]phenyl}-6-(5-{[(2-methanesulfonylethyl)amino]methyl}furan-2-yl)quinazolin-4-amine; UNII-4WK72K94MC; bis(4-methylbenzene-1-sulfonic acid)
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Status
Approved
Structure
3D MOL
Formula
C43H42ClFN4O10S3
InChI
1S/C29H26ClFN4O4S.2C7H8O3S/c1-40(36,37)12-11-32-16-23-7-10-27(39-23)20-5-8-26-24(14-20)29(34-18-33-26)35-22-6-9-28(25(30)15-22)38-17-19-3-2-4-21(31)13-19;2*1-6-2-4-7(5-3-6)11(8,9)10/h2-10,13-15,18,32H,11-12,16-17H2,1H3,(H,33,34,35);2*2-5H,1H3,(H,8,9,10)
InChIKey
UWYXLGUQQFPJRI-UHFFFAOYSA-N
PubChem CID
9941095
INTEDE Drug ID
DR0917
Target Gene(s) and Their Upstream m6A Regulator, Together with the Effect of Target Gene(s) in Drug Response
The target genes involved in drug-target interaction (such as drug-metabolizing enzymes, drug transporters and therapeutic targets) and drug-mediated cell death signaling (including modulating DNA damage and repair capacity, escaping from drug-induced apoptosis, autophagy, cellular metabolic reprogramming, oncogenic bypass signaling, cell microenvironment, cell stemness, etc.) could be regulated by m6A regulator(s) and affected their corresponding drug response. You can browse detailed information on drug-related target gene(s) mediated by m6A regulators.
Cytochrome P450 2C8 (CYP2C8)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for Lapatinib ditosylate. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of Lapatinib ditosylate through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [1], [2]
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for Lapatinib ditosylate. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of Lapatinib ditosylate through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [1], [2]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for Lapatinib ditosylate. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Lapatinib ditosylate through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [1], [2]
YTH domain-containing protein 2 (YTHDC2)
In total 1 mechanisms lead to this potential drug response
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for Lapatinib ditosylate. The YTH domain-containing protein 2 (YTHDC2) has potential in affecting the response of Lapatinib ditosylate through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [1], [2]
References
Ref 1 Methylation of adenosine at the N(6) position post-transcriptionally regulates hepatic P450s expression. Biochem Pharmacol. 2020 Jan;171:113697. doi: 10.1016/j.bcp.2019.113697. Epub 2019 Nov 7.
Ref 2 Mechanism-based inactivation of cytochrome P450 3A4 by lapatinib. Mol Pharmacol. 2010 Oct;78(4):693-703. doi: 10.1124/mol.110.065839. Epub 2010 Jul 12.