General Information of the Drug (ID: M6APDG02474)
Name
Gepirone
Synonyms
Gepirone; 4,4-Dimethyl-1-(4-(4-(pyrimidin-2-yl)piperazin-1-yl)butyl)piperidine-2,6-dione; Gepirone ER; Gepironum [Latin]; Gepirone [INN]; Gepirona [Spanish]; UNII-JW5Y7B8Z18; BMY-13805; JW5Y7B8Z18; CHEMBL284092; MJ-13805; Variza; Ariza; Gepironum; AK115965; Gepirona; 4,4-dimethyl-1-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]piperidine-2,6-dione; Travivo; 2,6-Piperidinedione, 4,4-dimethyl-1-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-; BMY 13805; MJ 13805; gepiron ER; MJ 13805-1; ORG-13011(Gepirone); AC1L1IK6; AC1Q6F8Q
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Status
Phase 2
Structure
Formula
C19H29N5O2
InChI
1S/C19H29N5O2/c1-19(2)14-16(25)24(17(26)15-19)9-4-3-8-22-10-12-23(13-11-22)18-20-6-5-7-21-18/h5-7H,3-4,8-15H2,1-2H3
InChIKey
QOIGKGMMAGJZNZ-UHFFFAOYSA-N
PubChem CID
55191
VARIDT Drug ID
DR01722
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.
P-glycoprotein 1 (ABCB1)
Insulin-like growth factor 2 mRNA-binding protein 3 (IGF2BP3)
In total 1 mechanisms lead to this potential drug response
Response Summary P-glycoprotein 1 (ABCB1) is a therapeutic target for Gepirone. The Insulin-like growth factor 2 mRNA-binding protein 3 (IGF2BP3) has potential in affecting the response of Gepirone through regulating the expression of P-glycoprotein 1 (ABCB1). [1], [2]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary P-glycoprotein 1 (ABCB1) is a therapeutic target for Gepirone. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Gepirone through regulating the expression of P-glycoprotein 1 (ABCB1). [2], [3]
References
Ref 1 Binding of RNA m6A by IGF2BP3 triggers chemoresistance of HCT8 cells via upregulation of ABCB1. Am J Cancer Res. 2021 Apr 15;11(4):1428-1445. eCollection 2021.
Ref 2 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
Ref 3 METTL3 promotes adriamycin resistance in MCF-7 breast cancer cells by accelerating pri-microRNA-221-3p maturation in a m6A-dependent manner. Exp Mol Med. 2021 Jan;53(1):91-102. doi: 10.1038/s12276-020-00510-w. Epub 2021 Jan 8.