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

General Information of Drug (ID: DMW9MOK)

• Drug Name: Lomeguatrib Drug Info
• Synonyms: Patrin; AZD-5896; Patrin-2; O6-(4-bromothenylguanine), Cancer Research UK/KuDOS; 4-BTG (cancer), Paterson/Trinity/CRC/KuDOS/AstraZeneca

Indication

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 2	[1]

• Cross-matching ID:
  PubChem CID: 3025944
  CAS Number: CAS 192441-08-0
  TTD Drug ID: DMW9MOK

Molecule-Related Drug Atlas

Drug(s) Targeting Transferase unspecific (TF)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ademetionine	DMYQDBO	Hepatic fibrosis	DB93.0	Approved	[4]
BCX-25	DM4GEUF	Arthritis	FA20	Terminated	[5]

Drug(s) Affected By Methylated-DNA--protein-cysteine methyltransferase (MGMT)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
DTI-015	DMXZRW0	Brain cancer	2A00	Approved	[6]
Cyclophosphamide	DM4O2Z7	Advanced cancer	2A00-2F9Z	Approved	[7]
Acocantherin	DM7JT24	Atrial fibrillation	BC81.3	Approved	[8]
Ciclosporin	DMAZJFX	Graft-versus-host disease	4B24	Approved	[9]
Disulfiram	DMCL2OK	Alcohol dependence	6C40.2	Approved	[10]
Ivermectin	DMDBX5F	Intestinal strongyloidiasis due to nematode parasite	1F6B	Approved	[11]
Dexamethasone	DMMWZET	Acute adrenal insufficiency		Approved	[12]
Phenytoin	DMNOKBV	Epilepsy	8A60-8A68	Approved	[13]
Dacarbazine	DMNPZL4	Adenocarcinoma	2D40	Approved	[14]
Topotecan	DMP6G8T	Central nervous system neoplasm		Approved	[15]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Transferase unspecific (TF)	TTX2N1T	NOUNIPROTAC	Inhibitor	[2]

Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Methylated-DNA--protein-cysteine methyltransferase (MGMT)	OT40A9WH	MGMT_HUMAN	Gene/Protein Processing	[3]

References

• [1] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017888)
• [2] O6-methylguanine DNA methyltransferase as a promising target for the treatment of temozolomide-resistant gliomas. Cell Death Dis. 2013 Oct 24;4:e876.
• [3] O6-(4-bromothenyl)guanine reverses temozolomide resistance in human breast tumour MCF-7 cells and xenografts. Br J Cancer. 2005 Nov 14;93(10):1152-6. doi: 10.1038/sj.bjc.6602833.
• [4] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2013
• [5] CN patent application no. 1096855, Composition produced by treatment and induction of nitrogen mono oxide synthase expressed matter, and use thereof.
• [6] Tumor necrosis factor-alpha-induced protein 3 as a putative regulator of nuclear factor-kappaB-mediated resistance to O6-alkylating agents in human glioblastomas. J Clin Oncol. 2006 Jan 10;24(2):274-87. doi: 10.1200/JCO.2005.02.9405. Epub 2005 Dec 19.
• [7] Comparative gene expression analysis of a chronic myelogenous leukemia cell line resistant to cyclophosphamide using oligonucleotide arrays and response to tyrosine kinase inhibitors. Leuk Res. 2007 Nov;31(11):1511-20.
• [8] Ouabain induces apoptotic cell death in human prostate DU 145 cancer cells through DNA damage and TRAIL pathways. Environ Toxicol. 2019 Dec;34(12):1329-1339. doi: 10.1002/tox.22834. Epub 2019 Aug 21.
• [9] Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
• [10] Disulfiram is a direct and potent inhibitor of human O6-methylguanine-DNA methyltransferase (MGMT) in brain tumor cells and mouse brain and markedly increases the alkylating DNA damage. Carcinogenesis. 2014 Mar;35(3):692-702. doi: 10.1093/carcin/bgt366. Epub 2013 Nov 5.
• [11] Quantitative proteomics reveals a broad-spectrum antiviral property of ivermectin, benefiting for COVID-19 treatment. J Cell Physiol. 2021 Apr;236(4):2959-2975. doi: 10.1002/jcp.30055. Epub 2020 Sep 22.
• [12] Induction of the DNA repair gene O6-methylguanine-DNA methyltransferase by dexamethasone in glioblastomas. J Neurosurg. 2004 Oct;101(4):659-63. doi: 10.3171/jns.2004.101.4.0659.
• [13] Phenytoin may increase the efficacy of temozolomide by methylating DNA-repair enzyme, O6-methylguanine-DNA methyltransferase in patients with glioblastoma. Med Hypotheses. 2005;65(4):819-20. doi: 10.1016/j.mehy.2005.04.007.
• [14] Pharmacokinetic, biochemical and clinical effects of dimethyltriazenoimidazole-4-carboxamide-bischloroethylnitrosourea combination therapy in patients with advanced breast cancer. Int J Cancer. 2003 Feb 20;103(5):686-92. doi: 10.1002/ijc.10849.
• [15] Transcriptional repression of O6-methylguanine DNA methyltransferase gene rendering cells hypersensitive to N,N'-bis(2-chloroethyl)-N-nitrosurea in camptothecin-resistant cells. Mol Pharmacol. 2008 Aug;74(2):517-26. doi: 10.1124/mol.107.043620. Epub 2008 May 20.