Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DM3INX7)

• Drug Name: EPZ015666 Drug Info
• Synonyms: EPZ-015666; EPZ 015666

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 90241673
  ChEBI ID: CHEMBL4060831
  TTD Drug ID: DM3INX7

Molecule-Related Drug Atlas

Drug(s) Targeting Protein arginine methyltransferase 5 (PRMT5)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
GSK3326595	DMJRD7A	Breast cancer	2C60-2C65	Phase 2	[5]
AMG 193	DMU9K8N	Aggressive cancer	2A00-2F9Z	Phase 2	[6]
PRT811	DMW3MCX	Glioma	2A00.0	Phase 1	[7]
PRT543	DMHNZ3U	Hematologic tumour	2B33.Y	Phase 1	[8]
JNJ-64619178	DMDBW2N	Myelodysplastic syndrome	2A37	Phase 1	[9]
PF-06939999	DM7BOFR	Solid tumour/cancer	2A00-2F9Z	Phase 1	[10]
DS-437	DME3WBQ	Discovery agent	N.A.	Investigative	[11]
cmp5	DMBT2ZW	Discovery agent	N.A.	Investigative	[12]

Drug(s) Affected By Myc proto-oncogene protein (MYC)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[13]
Sertraline	DM0FB1J	Coronary heart disease	BA80.Z	Approved	[14]
Fulvestrant	DM0YZC6	Breast cancer	2C60-2C65	Approved	[15]
Gefitinib	DM15F0X	Colon adenocarcinoma		Approved	[16]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[17]
Selenium	DM25CGV	N. A.	N. A.	Approved	[18]
Ribavirin	DMEYLH9	Hepatitis C virus infection	1E51.1	Approved	[19]
Trametinib	DM2JGQ3	Melanoma	2C30	Approved	[20]
Sulindac	DM2QHZU	Acute myelogenous leukaemia	2A41	Approved	[21]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[22]

Drug(s) Affected By Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Quercetin	DM3NC4M	Obesity	5B81	Approved	[23]
2-deoxyglucose	DMIAHVU	Solid tumour/cancer	2A00-2F9Z	Approved	[24]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[25]
Cannabidiol	DM0659E	Dravet syndrome	8A61.11	Approved	[26]
Ofloxacin	DM0VQN3	Acute gonococcal cervicitis		Approved	[27]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[28]
Ciprofloxacin XR	DM2NLS9	Acute gonococcal cervicitis		Approved	[27]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[29]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[30]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[31]

Drug(s) Affected By Small ribosomal subunit protein eS6 (RPS6)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Cannabidiol	DM0659E	Dravet syndrome	8A61.11	Approved	[32]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[33]
Crizotinib	DM4F29C	Non-small-cell lung cancer	2C25.Y	Approved	[34]
Glucosamine	DM4ZLFD	Osteoarthritis	FA00-FA05	Approved	[35]
Arsenic trioxide	DM61TA4	Acute lymphoblastic leukaemia	2A85	Approved	[36]
Aspirin	DM672AH	Acute coronary syndrome	BA41	Approved	[37]
Testosterone	DM7HUNW	Hot flushes	GA30	Approved	[38]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[39]
Capivasertib	DM9SKW8	Breast cancer	2C60-2C65	Approved	[40]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[41]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Protein arginine methyltransferase 5 (PRMT5)	TTR1D7X	ANM5_HUMAN	Inhibitor	[2]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Myc proto-oncogene protein (MYC)	OTPV5LUK	MYC_HUMAN	Gene/Protein Processing	[3]
Small ribosomal subunit protein eS6 (RPS6)	OTT4D1LN	RS6_HUMAN	Post-Translational Modifications	[4]
Solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1)	OTA675TJ	GTR1_HUMAN	Gene/Protein Processing	[4]

References

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• [2] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1256).
• [3] Role of protein arginine methyltransferase 5 in group 3 (MYC-driven) Medulloblastoma. BMC Cancer. 2019 Nov 6;19(1):1056. doi: 10.1186/s12885-019-6291-z.
• [4] Selective PRMT5 Inhibitors Suppress Human CD8(+) T Cells by Upregulation of p53 and Impairment of the AKT Pathway Similar to the Tumor Metabolite MTA. Mol Cancer Ther. 2020 Feb;19(2):409-419. doi: 10.1158/1535-7163.MCT-19-0189. Epub 2019 Nov 11.
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• [7] Clinical pipeline report, company report or official report of Prelude Therapeutics.
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• [22] The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
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• [26] Cannabidiol Displays Proteomic Similarities to Antipsychotics in Cuprizone-Exposed Human Oligodendrocytic Cell Line MO3.13. Front Mol Neurosci. 2021 May 28;14:673144. doi: 10.3389/fnmol.2021.673144. eCollection 2021.
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• [29] Phenotypic characterization of retinoic acid differentiated SH-SY5Y cells by transcriptional profiling. PLoS One. 2013 May 28;8(5):e63862.
• [30] Differential gene expression in human hepatocyte cell lines exposed to the antiretroviral agent zidovudine. Arch Toxicol. 2014 Mar;88(3):609-23. doi: 10.1007/s00204-013-1169-3. Epub 2013 Nov 30.
• [31] Essential role of cell cycle regulatory genes p21 and p27 expression in inhibition of breast cancer cells by arsenic trioxide. Med Oncol. 2011 Dec;28(4):1225-54.
• [32] Cannabidiol Reduces Leukemic Cell Size - But Is It Important?. Front Pharmacol. 2017 Mar 24;8:144. doi: 10.3389/fphar.2017.00144. eCollection 2017.
• [33] Global molecular effects of tocilizumab therapy in rheumatoid arthritis synovium. Arthritis Rheumatol. 2014 Jan;66(1):15-23.
• [34] Crizotinib-resistant mutants of EML4-ALK identified through an accelerated mutagenesis screen. Chem Biol Drug Des. 2011 Dec;78(6):999-1005. doi: 10.1111/j.1747-0285.2011.01239.x. Epub 2011 Oct 31.
• [35] D-glucosamine down-regulates HIF-1alpha through inhibition of protein translation in DU145 prostate cancer cells. Biochem Biophys Res Commun. 2009 Apr 24;382(1):96-101. doi: 10.1016/j.bbrc.2009.02.129. Epub 2009 Feb 28.
• [36] Proteomics-based identification of differentially abundant proteins from human keratinocytes exposed to arsenic trioxide. J Proteomics Bioinform. 2014 Jul;7(7):166-178.
• [37] Potential anti-aging agents suppress the level of constitutive mTOR- and DNA damage- signaling. Aging (Albany NY). 2012 Dec;4(12):952-65. doi: 10.18632/aging.100521.
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