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

General Information of Drug (ID: DM5WK0J)

Drug Name

ARQ 092 Drug Info

Synonyms

Miransertib

Indication

Disease Entry	ICD 11	Status	REF
Proteus syndrome	LD2C	Phase 2	[1]
Solid tumour/cancer	2A00-2F9Z	Phase 1	[2]

Cross-matching ID

PubChem CID: 53262401
CAS Number: CAS 1313881-70-7
TTD Drug ID: DM5WK0J

Molecule-Related Drug Atlas

Molecule Type:

DTT

DOT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

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Drug(s) Targeting RAC-alpha serine/threonine-protein kinase (AKT1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Capivasertib	DM9SKW8	Breast cancer	2C60-2C65	Approved	[6]
Enzastaurin	DM5H0R9	Diffuse large B-cell lymphoma	2A81	Phase 3	[6]
GDC-0068	DMWBZJD	Breast cancer	2C60-2C65	Phase 3	[6]
CI-1033	DMSI8N3	Lymphoma	2A80-2A86	Phase 2	[7]
CMX-2043	DMPSCVY	Cardiac disease	BA00-BE2Z	Phase 2	[8]
GSK2110183	DMZHB37	leukaemia	2A60-2B33	Phase 2	[9]
RX-0201	DMTBAV3	Pancreatic cancer	2C10	Phase 2	[10]
PTX-200	DM0ZIT2	Breast cancer	2C60-2C65	Phase 2	[6]
Triciribine prodrug	DMBN1XS	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[9]
M2698	DM3PVBJ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[6]
Capivasertib	DM9SKW8	Breast cancer	2C60-2C65	Approved	[20]
Nicotine	DMWX5CO	Lung cancer	2C25.0	Approved	[21]
Cannabidiol	DM0659E	Dravet syndrome	8A61.11	Approved	[22]
Beta-carotene	DM0RXBT	Vitamin deficiency	5B55-5B71	Approved	[23]
Gefitinib	DM15F0X	Colon adenocarcinoma		Approved	[24]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[25]
Imiquimod	DM1TMA3	Alopecia areata	ED70.2	Approved	[26]
Selenium	DM25CGV	N. A.	N. A.	Approved	[27]
Methimazole	DM25FL8	Hyperthyroidism	5A02	Approved	[28]
Ribavirin	DMEYLH9	Hepatitis C virus infection	1E51.1	Approved	[29]
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Drug(s) Targeting RAC-gamma serine/threonine-protein kinase (AKT3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Capivasertib	DM9SKW8	Breast cancer	2C60-2C65	Approved	[11]
MK-2206	DMT1OZ6	Rectal adenocarcinoma	2B92	Phase 2	[12]
GSK2141795	DMSHE70	Colorectal cancer	2B91.Z	Phase 2	[13]
M2698	DM3PVBJ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[6]
LYS-6KAKT1	DMLXGAI	Solid tumour/cancer	2A00-2F9Z	Phase 1	[14]
LY2780301	DM93AJW	Solid tumour/cancer	2A00-2F9Z	Phase 1	[15]
XL418	DME0F5W	Solid tumour/cancer	2A00-2F9Z	Phase 1	[16]
SR13668	DMO5760	Solid tumour/cancer	2A00-2F9Z	Phase 1	[17]
TCN-P	DMV0AH8	Acute myeloid leukaemia	2A60	Phase 1	[18]
GSK690693	DMRBVHE	Haematological malignancy	2B33.Y	Phase 1	[19]
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Drug(s) Affected By Tumor necrosis factor (TNF)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Indomethacin	DMSC4A7	Bursitis		Approved	[30]
Amphotericin B	DMTAJQE	Acne vulgaris	ED80	Approved	[31]
Fructose	DM43AN2	Vomiting	MD90	Approved	[32]
Ketoprofen	DMRKXPT	Bursitis		Approved	[32]
Cannabidiol	DM0659E	Dravet syndrome	8A61.11	Approved	[33]
Sertraline	DM0FB1J	Coronary heart disease	BA80.Z	Approved	[34]
Baclofen	DM0QV1J	Multiple sclerosis	8A40	Approved	[35]
Gefitinib	DM15F0X	Colon adenocarcinoma		Approved	[36]
Ganciclovir	DM1MBYQ	Cytomegalovirus infection	1D82	Approved	[37]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[38]
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Drug(s) Affected By Tumor necrosis factor receptor superfamily member 6 (FAS)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Beta-carotene	DM0RXBT	Vitamin deficiency	5B55-5B71	Approved	[39]
Hydrogen peroxide	DM1NG5W	Infectious disease	1A00-CA43.1	Approved	[40]
Nitric Oxide	DM1RBYG	Hypertension	BA00-BA04	Approved	[41]
Methotrexate	DM2TEOL	Anterior urethra cancer		Approved	[42]
Epinephrine	DM3KJBC	Acute asthma	CA23	Approved	[43]
Quercetin	DM3NC4M	Obesity	5B81	Approved	[44]
Troglitazone	DM3VFPD	Diabetic complication	5A2Y	Approved	[45]
Fructose	DM43AN2	Vomiting	MD90	Approved	[46]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[39]
Cyclophosphamide	DM4O2Z7	Advanced cancer	2A00-2F9Z	Approved	[47]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
RAC-alpha serine/threonine-protein kinase (AKT1)	TTWTSCV	AKT1_HUMAN	Inhibitor	[3]
RAC-gamma serine/threonine-protein kinase (AKT3)	TTAZ05C	AKT3_HUMAN	Modulator	[4]

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Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
RAC-alpha serine/threonine-protein kinase (AKT1)	OT8H2YY7	AKT1_HUMAN	Post-Translational Modifications	[5]
Tumor necrosis factor (TNF)	OT4IE164	TNFA_HUMAN	Protein Interaction/Cellular Processes	[5]
Tumor necrosis factor receptor superfamily member 6 (FAS)	OTP9XG86	TNR6_HUMAN	Protein Interaction/Cellular Processes	[5]

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References

1	ClinicalTrials.gov (NCT04316546) ARQ 092 (Miransertib) in Proteus Syndrome. U.S. National Institutes of Health.
2	ClinicalTrials.gov (NCT01473095) Phase 1 Dose Escalation Study of ARQ 092 in Adult Subjects With Advanced Solid Tumors and Recurrent Malignant Lymphoma. U.S. National Institutes of Health.
3	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4	Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
5	PI3K/AKT inhibitors aggravate death receptor-mediated hepatocyte apoptosis and liver injury. Toxicol Appl Pharmacol. 2019 Oct 15;381:114729. doi: 10.1016/j.taap.2019.114729. Epub 2019 Aug 22.
6	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
7	A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
8	Pre-clinical and Clinical Safety Studies of CMX-2043: a cytoprotective lipoic acid analogue for ischaemia-reperfusion injury. Basic Clin Pharmacol Toxicol. 2014 Nov;115(5):456-64.
9	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: 1479).
10	CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008.
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12	First-in-man clinical trial of the oral pan-AKT inhibitor MK-2206 in patients with advanced solid tumors.J Clin Oncol.2011 Dec 10;29(35):4688-95.
13	Inhibiting the akt pathway in cancer treatment: three leading candidates. P T. 2011 Apr;36(4):225-7.
14	DOI: 10.1016/S1359-6349(10)71767-5
15	A first-in-human phase I trial of LY2780301, a dual p70 S6 kinase and Akt Inhibitor, in patients with advanced or metastatic cancer. Invest New Drugs. 2015 Jun;33(3):710-9.
16	Targeting the phosphoinositide 3-kinase (PI3K) pathway in cancer
17	Phase 0 clinical chemoprevention trial of the Akt inhibitor SR13668. Cancer Prev Res (Phila). 2011 Mar;4(3):347-53.
18	Phase I pharmacokinetic and pharmacodynamic study of triciribine phosphate monohydrate, a small-molecule inhibitor of AKT phosphorylation, in adult subjects with solid tumors containing activated AKT.Invest New Drugs.2011 Dec;29(6):1381-9.
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20	Inhibition of cholesterol metabolism underlies synergy between mTOR pathway inhibition and chloroquine in bladder cancer cells. Oncogene. 2016 Aug 25;35(34):4518-28. doi: 10.1038/onc.2015.511. Epub 2016 Feb 8.
21	Nicotine-induced survival signaling in lung cancer cells is dependent on their p53 status while its down-regulation by curcumin is independent. Mol Cancer. 2010 Aug 20;9:220.
22	Role of miRNA in the regulation of cannabidiol-mediated apoptosis in neuroblastoma cells. Oncotarget. 2019 Jan 1;10(1):45-59. doi: 10.18632/oncotarget.26534. eCollection 2019 Jan 1.
23	-Carotene Induces Apoptosis in Human Esophageal Squamous Cell Carcinoma Cell Lines via the Cav-1/AKT/NF-B Signaling Pathway. J Biochem Mol Toxicol. 2016 Mar;30(3):148-57. doi: 10.1002/jbt.21773. Epub 2016 Jan 6.
24	Dihydromyricetin suppresses tumor growth via downregulation of the EGFR/Akt/survivin signaling pathway. J Biochem Mol Toxicol. 2023 Jun;37(6):e23328. doi: 10.1002/jbt.23328. Epub 2023 Feb 19.
25	Oxidative stress induces parallel autophagy and mitochondria dysfunction in human glioma U251 cells. Toxicol Sci. 2009 Aug;110(2):376-88. doi: 10.1093/toxsci/kfp101. Epub 2009 May 18.
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30	Indomethacin and juglone inhibit inflammatory molecules to induce apoptosis in colon cancer cells. J Biochem Mol Toxicol. 2020 Feb;34(2):e22433. doi: 10.1002/jbt.22433. Epub 2020 Jan 9.
31	A cell impedance-based real-time in vitro assay to assess the toxicity of amphotericin B formulations. Toxicol Appl Pharmacol. 2017 Nov 1;334:18-23. doi: 10.1016/j.taap.2017.08.017. Epub 2017 Sep 1.
32	ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
33	CBD Promotes Oral Ulcer Healing via Inhibiting CMPK2-Mediated Inflammasome. J Dent Res. 2022 Feb;101(2):206-215. doi: 10.1177/00220345211024528. Epub 2021 Jul 16.
34	Sertraline, an antidepressant, induces apoptosis in hepatic cells through the mitogen-activated protein kinase pathway. Toxicol Sci. 2014 Feb;137(2):404-15. doi: 10.1093/toxsci/kft254. Epub 2013 Nov 5.
35	Anti-inflammatory effects of the GABA(B) receptor agonist baclofen in allergic contact dermatitis. Exp Dermatol. 2010 Jul 1;19(7):661-6. doi: 10.1111/j.1600-0625.2010.01076.x. Epub 2010 Feb 25.
36	Frankincense myrrh attenuates hepatocellular carcinoma by regulating tumor blood vessel development through multiple epidermal growth factor receptor-mediated signaling pathways. World J Gastrointest Oncol. 2022 Feb 15;14(2):450-477. doi: 10.4251/wjgo.v14.i2.450.
37	Sulfasalazine unveils a contact-independent HSV-TK/ganciclovir gene therapy bystander effect in malignant gliomas. Int J Oncol. 2007 Jan;30(1):283-90.
38	Oxidative Stress Alters miRNA and Gene Expression Profiles in Villous First Trimester Trophoblasts. Biomed Res Int. 2015;2015:257090. doi: 10.1155/2015/257090. Epub 2015 Aug 3.
39	Beta-carotene and apocarotenals promote retinoid signaling in BEAS-2B human bronchioepithelial cells. Arch Biochem Biophys. 2006 Nov 1;455(1):48-60.
40	Gene expression after treatment with hydrogen peroxide, menadione, or t-butyl hydroperoxide in breast cancer cells. Cancer Res. 2002 Nov 1;62(21):6246-54.
41	Apoptotic signaling pathways induced by nitric oxide in human lymphoblastoid cells expressing wild-type or mutant p53. Cancer Res. 2004 May 1;64(9):3022-9. doi: 10.1158/0008-5472.can-03-1880.
42	Topotecan and methotrexate alter expression of the apoptosis-related genes BCL2, FAS and BCL2L12 in leukemic HL-60 cells. Biol Chem. 2006 Dec;387(12):1629-33. doi: 10.1515/BC.2006.203.
43	Carvedilol prevents epinephrine-induced apoptosis in human coronary artery endothelial cells: modulation of Fas/Fas ligand and caspase-3 pathway. Cardiovasc Res. 2000 Feb;45(3):788-94. doi: 10.1016/s0008-6363(99)00369-7.
44	Multifaceted preventive effects of single agent quercetin on a human prostate adenocarcinoma cell line (PC-3): implications for nutritional transcriptomics and multi-target therapy. Med Oncol. 2011 Dec;28(4):1395-404. doi: 10.1007/s12032-010-9603-3. Epub 2010 Jul 2.
45	Regulatory role of KEAP1 and NRF2 in PPAR expression and chemoresistance in human non-small-cell lung carcinoma cells. Free Radic Biol Med. 2012 Aug 15;53(4):758-68. doi: 10.1016/j.freeradbiomed.2012.05.041. Epub 2012 Jun 7.
46	Non-nutritional sweeteners effects on endothelial vascular function. Toxicol In Vitro. 2020 Feb;62:104694. doi: 10.1016/j.tiv.2019.104694. Epub 2019 Oct 23.
47	Transcriptome-based functional classifiers for direct immunotoxicity. Arch Toxicol. 2014 Mar;88(3):673-89.