General Information of the Drug (ID: M6APDG02931)
Name
Omaveloxolone
Synonyms
RJCWBNBKOKFWNY-HGNIWHNWSA-N; N-((4aR,6aR,6bS,12aS,14aR,14bR)-11-cyano-2,2,6a,6b,9,9,12a-heptamethyl-10,14-dioxo-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,10,12a,14,14a,14b-octadecahydropicen-4a-yl)-2,2-difluoropropanamide; 1474034-05-3; AKOS030526563
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Status
Phase 2
Structure
Formula
C33H44F2N2O3
InChI
1S/C33H44F2N2O3/c1-27(2)11-13-33(37-26(40)32(8,34)35)14-12-31(7)24(20(33)17-27)21(38)15-23-29(5)16-19(18-36)25(39)28(3,4)22(29)9-10-30(23,31)6/h15-16,20,22,24H,9-14,17H2,1-8H3,(H,37,40)/t20-,22-,24-,29-,30+,31+,33-/m0/s1
InChIKey
RJCWBNBKOKFWNY-IDPLTSGASA-N
PubChem CID
71811910
TTD Drug ID
D0JB3H
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.
Nuclear factor erythroid 2-related factor 2 (Nrf2)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
Response Summary Nuclear factor erythroid 2-related factor 2 (Nrf2) is a therapeutic target for Omaveloxolone. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of Omaveloxolone through regulating the expression of Nuclear factor erythroid 2-related factor 2 (Nrf2). [1], [2]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Nuclear factor erythroid 2-related factor 2 (Nrf2) is a therapeutic target for Omaveloxolone. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Omaveloxolone through regulating the expression of Nuclear factor erythroid 2-related factor 2 (Nrf2). [2], [3]
YTH domain-containing family protein 1 (YTHDF1)
In total 1 mechanisms lead to this potential drug response
Response Summary Nuclear factor erythroid 2-related factor 2 (Nrf2) is a therapeutic target for Omaveloxolone. The YTH domain-containing family protein 1 (YTHDF1) has potential in affecting the response of Omaveloxolone through regulating the expression of Nuclear factor erythroid 2-related factor 2 (Nrf2). [2], [4]
YTH domain-containing protein 2 (YTHDC2)
In total 1 mechanisms lead to this potential drug response
Response Summary Nuclear factor erythroid 2-related factor 2 (Nrf2) is a therapeutic target for Omaveloxolone. The YTH domain-containing protein 2 (YTHDC2) has potential in affecting the response of Omaveloxolone through regulating the expression of Nuclear factor erythroid 2-related factor 2 (Nrf2). [1], [2]
References
Ref 1 Increased m6A RNA modification is related to the inhibition of the Nrf2-mediated antioxidant response in di-(2-ethylhexyl) phthalate-induced prepubertal testicular injury. Environ Pollut. 2020 Apr;259:113911. doi: 10.1016/j.envpol.2020.113911. Epub 2020 Jan 6.
Ref 2 Therapeutic targeting of the NRF2 and KEAP1 partnership in chronic diseases. Nat Rev Drug Discov. 2019 Apr;18(4):295-317. doi: 10.1038/s41573-018-0008-x.
Ref 3 METTL3-mediated M6A methylation modification is involved in colistin-induced nephrotoxicity through apoptosis mediated by Keap1/Nrf2 signaling pathway. Toxicology. 2021 Oct;462:152961. doi: 10.1016/j.tox.2021.152961. Epub 2021 Sep 21.
Ref 4 YTHDF1 links hypoxia adaptation and non-small cell lung cancer progression. Nat Commun. 2019 Oct 25;10(1):4892. doi: 10.1038/s41467-019-12801-6.