m6A-centered Drug Response Information

General Information of the Drug (ID: M6APDG02860)
Name
EMD-128130
Synonyms
Sarizotan; Sarizotan [INN]; ZINC21067; (R)-(-)-2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]chroman; (r)-(+)-2-[5-(4-fluorphenyl)-3-pyridylmethylaminomethyl]-chromane; 1-(5-(4-Fluorophenyl)pyridin-3-yl)-N-((2R)-3,4,4a,8a-tetrahydro-2H-chromen-2-ylmethyl)methanamine; 3-Pyridinemethanamine, 5-(4-fluorophenyl)-N-(((2R)-3,4,4a,8a-tetrahydro-2H-1-benzopyran-2-yl)methyl)-; 351862-32-3; 467LU0UCUW; AC1OCFD8; ACM177975085; BDBM50027256; CHEMBL220808; HKFMQJUJWSFOLY-OAQYLSRUSA-N; SCHEMBL120080; UNII-467LU0UCUW
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Status
Phase 2/3
Structure
Formula
C22H21FN2O
InChI
1S/C22H21FN2O/c23-20-8-5-17(6-9-20)19-11-16(12-24-14-19)13-25-15-21-10-7-18-3-1-2-4-22(18)26-21/h1-6,8-9,11-12,14,21,25H,7,10,13,15H2/t21-/m1/s1
InChIKey
HKFMQJUJWSFOLY-OAQYLSRUSA-N
PubChem CID
6918388
INTEDE Drug ID
DR1872
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
 Regulator Info 
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for EMD-128130. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of EMD-128130 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
 Regulator Info 
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for EMD-128130. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of EMD-128130 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
 Regulator Info 
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for EMD-128130. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of EMD-128130 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
 Regulator Info 
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for EMD-128130. The YTH domain-containing protein 2 (YTHDC2) has potential in affecting the response of EMD-128130 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 In vitro characterization of sarizotan metabolism: hepatic clearance, identification and characterization of metabolites, drug-metabolizing enzyme identification, and evaluation of cytochrome p450 inhibition. Drug Metab Dispos. 2010 Jun;38(6):905-16. doi: 10.1124/dmd.109.029835. Epub 2010 Mar 10.