General Information of the Drug (ID: M6APDG03329)
Name
Apalutamide
Synonyms
Arn-509 (AR inhibitor)
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Status
Approved
Structure
Formula
C21H15F4N5O2S
InChI
1S/C21H15F4N5O2S/c1-27-17(31)13-4-3-11(8-15(13)22)30-19(33)29(18(32)20(30)5-2-6-20)12-7-14(21(23,24)25)16(9-26)28-10-12/h3-4,7-8,10H,2,5-6H2,1H3,(H,27,31)
InChIKey
HJBWBFZLDZWPHF-UHFFFAOYSA-N
PubChem CID
24872560
TTD Drug ID
D0S7LG
INTEDE Drug ID
DR0121
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.
Androgen receptor (AR)
ETS-related transcription factor Elf-3 (ELF3)
In total 1 mechanisms lead to this potential drug response
Response Summary Androgen receptor (AR) is a therapeutic target for Apalutamide. The ETS-related transcription factor Elf-3 (ELF3) has potential in affecting the response of Apalutamide through regulating the expression of Androgen receptor (AR). [1], [2]
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 Apalutamide. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of Apalutamide through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [3], [4]
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 Apalutamide. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of Apalutamide through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [3], [4]
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 Apalutamide. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Apalutamide through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [3], [4]
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 Apalutamide. The YTH domain-containing protein 2 (YTHDC2) has potential in affecting the response of Apalutamide through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [3], [4]
References
Ref 1 ELF3 is a repressor of androgen receptor action in prostate cancer cells. Oncogene. 2014 Feb 13;33(7):862-71. doi: 10.1038/onc.2013.15. Epub 2013 Feb 25.
Ref 2 Design and development of antisense drugs. Expert Opin. Drug Discov. 2008 3(10):1189-1207.
Ref 3 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 4 Apalutamide: First Global Approval. Drugs. 2018 Apr;78(6):699-705. doi: 10.1007/s40265-018-0900-z.