General Information of the Drug (ID: M6APDG02602)
Name
Irinotecan
Synonyms
(+)-Irinotecan; (4S)-4,11-DIETHYL-4-HYDROXY-3,14-DIOXO-3,4,12,14-TETRAHYDRO-1H-PYRANO[3',4':6,7]INDOLIZINO[1,2-B]QUINOLIN-9-YL 1,4'-BIPIPERIDINE-1'-CARBOXYLATE; (4S)-4,11-Diethyl-4-hydroxy-3,14-dioxo-4,12-dihydro-1H-pyrano[3,4-f]quinolino[2,3-a]indolizin-9-yl 4-piperidylpiperidinecarboxylate; Biotecan; Biotecan (TN); CP0; Campto (TN); Camptosar; Camptosar (TN); Camptosar, Campto, CPT-11, Irinotecan; IRINOTECAN HYDROCHLORIDE Trihydrate; IRINOTECAN, CPT-11; Irinotecan (INN); Irinotecan (TOPO1 inhibitor); Irinotecan Hcl; Irinotecan [INN:BAN]; Irinotecan hydrochloride; Irinotecanum; Irinotecanum [INN-Latin]
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Status
Approved
Structure
Formula
C33H38N4O6
InChI
1S/C33H38N4O6/c1-3-22-23-16-21(43-32(40)36-14-10-20(11-15-36)35-12-6-5-7-13-35)8-9-27(23)34-29-24(22)18-37-28(29)17-26-25(30(37)38)19-42-31(39)33(26,41)4-2/h8-9,16-17,20,41H,3-7,10-15,18-19H2,1-2H3/t33-/m0/s1
InChIKey
UWKQSNNFCGGAFS-XIFFEERXSA-N
PubChem CID
60838
VARIDT Drug ID
DR00112
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.
Breast cancer resistance protein (ABCG2)
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Breast cancer resistance protein (ABCG2) is a therapeutic target for Irinotecan. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Irinotecan through regulating the expression of Breast cancer resistance protein (ABCG2). [1], [2]
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 Irinotecan. The Insulin-like growth factor 2 mRNA-binding protein 3 (IGF2BP3) has potential in affecting the response of Irinotecan through regulating the expression of P-glycoprotein 1 (ABCB1). [3], [4]
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 Irinotecan. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Irinotecan through regulating the expression of P-glycoprotein 1 (ABCB1). [1], [4]
References
Ref 1 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.
Ref 2 Cyclosporin A, tacrolimus and sirolimus are potent inhibitors of the human breast cancer resistance protein (ABCG2) and reverse resistance to mitoxantrone and topotecan. Cancer Chemother Pharmacol. 2006 Sep;58(3):374-83. doi: 10.1007/s00280-005-0173-6. Epub 2006 Jan 11.
Ref 3 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 4 Intestinal transport of irinotecan in Caco-2 cells and MDCK II cells overexpressing efflux transporters Pgp, cMOAT, and MRP1. Drug Metab Dispos. 2002 Jul;30(7):763-70. doi: 10.1124/dmd.30.7.763.