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

General Information of Drug (ID: DMBT2RJ)

• Drug Name: MC-2001 Drug Info
• Synonyms: MC-2002; MC-2006; Multiple selective kinase inhibitors (leukemia); Dual Flt3/ABL inhibitors, MaxoCore; Multiple selective kinase inhibitors (leukemia), Maxocore

Indication

Disease Entry	ICD 11	Status	REF
leukaemia	2A60-2B33	Preclinical	[1]

• Cross-matching ID: TTD Drug ID: DMBT2RJ

Molecule-Related Drug Atlas

Drug(s) Targeting Tyrosine-protein kinase ABL1 (ABL)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ponatinib	DMYGJQO	Acute lymphoblastic leukaemia	2A85	Approved	[3]
Bosutinib	DMTI8YE	Blast phase chronic myelogenous leukemia, BCR-ABL1 positive		Approved	[4]
SKI-758	DMQ8E9R	Ischemia	8B10-8B11	Approved	[5]
Adenosine triphosphate	DM79F6G	Malnutrition	5B50-5B71	Approved	[6]
Saracatinib	DMBLHGP	Hematologic tumour	2B33.Y	Phase 2	[7]
Flumatinib	DM0G5O6	Chronic myelogenous leukaemia	2A20.0	Phase 2	[8]
DCC-2036	DMJKFNU	Chronic myeloid leukaemia	2A20	Phase 1/2	[9]
ISIS-CRP	DMQDUG4	Cardiovascular disease	BA00-BE2Z	Phase 1	[10]
KW-2449	DMFO7RP	Acute myeloid leukaemia	2A60	Phase 1	[11]
IkT-148009	DMMJ9HY	Parkinson disease	8A00.0	Phase 1	[12]

Drug(s) Targeting Fms-like tyrosine kinase 3 (FLT-3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[13]
Ponatinib	DMYGJQO	Acute lymphoblastic leukaemia	2A85	Approved	[3]
Intedanib	DMSTA36	Colorectal cancer	2B91.Z	Approved	[14]
Midostaurin	DMI6E0R	Acute myeloid leukaemia	2A60	Approved	[4]
Gilteritinib	DMTI0ZO	Acute myeloid leukaemia	2A60	Approved	[15]
Pexidartinib	DMS2J0Z	Tenosynovial giant cell tumour	2F7B	Approved	[16]
Pacritinib	DM1T6ZN	Myelofibrosis	2A20.2	Approved	[13]
Quizartinib	DM8Y4JS	Acute myeloid leukaemia	2A60	Approved	[17]
Lestaurtinib	DMQ2AIJ	Acute myeloid leukaemia	2A60	Approved (orphan drug)	[18]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[19]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Fms-like tyrosine kinase 3 (FLT-3)	TTGJCWZ	FLT3_HUMAN	Inhibitor	[2]
Tyrosine-protein kinase ABL1 (ABL)	TT3PJMV	ABL1_HUMAN	Inhibitor	[2]

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 800021088)
• [2] Vascular endothelial growth factor and its receptors in multiple myeloma. Leukemia. 2003 Oct;17(10):1961-6.
• [3] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [4] 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.
• [5] Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles. J Med Chem. 2006 Dec 28;49(26):7868-76.
• [6] Targeted chronic myeloid leukemia therapy: Seeking a cure. Am J Health Syst Pharm. 2007 Dec 15;64(24 Suppl 15):S9-15.
• [7] Novel dual Src/Abl inhibitors for hematologic and solid malignancies.Expert Opin Investig Drugs.2010 Aug;19(8):931-45.
• [8] Flumatinib, a selective inhibitor of BCR-ABL/PDGFR/KIT, effectively overcomes drug resistance of certain KIT mutants. Cancer Sci. 2014 Jan;105(1):117-25.
• [9] Company report (Deciphera Pharmaceuticals: Tumor-Targeted Programs and Indications)
• [10] Structure-based optimization of pyrazolo[3,4-d]pyrimidines as Abl inhibitors and antiproliferative agents toward human leukemia cell lines. J Med Chem. 2008 Mar 13;51(5):1252-9.
• [11] KW-2449, a novel multikinase inhibitor, suppresses the growth of leukemia cells with FLT3 mutations or T315I-mutated BCR/ABL translocation. Blood. 2009 Aug 20;114(8):1607-17.
• [12] The c-Abl inhibitor IkT-148009 suppresses neurodegeneration in mouse models of heritable and sporadic Parkinson's disease. Sci Transl Med. 2023 Jan 18;15(679):eabp9352.
• [13] 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: 1807).
• [14] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [15] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [16] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [17] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [18] Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with ... Blood. 2008 Jun 15;111(12):5663-71.
• [19] Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.