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

General Information of DTT (ID: TTGJCWZ)

• DTT Name: Fms-like tyrosine kinase 3 (FLT-3) DTT Info
• Gene Name: FLT3

Molecule-Related Drug & Molecule List

9 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Gilteritinib	DMTI0ZO	Acute myeloid leukaemia	2A60	Approved	[1]
Intedanib	DMSTA36	Colorectal cancer	2B91.Z	Approved	[2]
Lestaurtinib	DMQ2AIJ	Acute myeloid leukaemia	2A60	Approved (orphan drug)	[3]
Midostaurin	DMI6E0R	Acute myeloid leukaemia	2A60	Approved	[4]
Pacritinib	DM1T6ZN	Myelofibrosis	2A20.2	Approved	[5]
Pexidartinib	DMS2J0Z	Tenosynovial giant cell tumour	2F7B	Approved	[6]
Ponatinib	DMYGJQO	Acute lymphoblastic leukaemia	2A85	Approved	[7]
Quizartinib	DM8Y4JS	Acute myeloid leukaemia	2A60	Approved	[8]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[5]

18 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BMS-690514	DMX302C	Chronic pain	MG30	Phase 2	[9]
CDX-301	DMKRFCO	Hematopoietic stem cell transplantation	QB63	Phase 2	[10]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[11]
TAK-659	DMJH3U0	Diffuse large B-cell lymphoma	2A81	Phase 2	[8]
FF-10101	DM1XIMU	Acute myeloid leukaemia	2A60	Phase 1/2	[12]
HM43239	DMV1SDA	Acute myeloid leukaemia	2A60	Phase 1/2	[13]
MK-2461	DM21WBH	Alzheimer disease	8A20	Phase 1/2	[14]
SEL-24	DMH064K	Acute myeloid leukaemia	2A60	Phase 1/2	[8]
SEL24	DMD37Q5	Acute myeloid leukaemia	2A60	Phase 1/2	[15]
4SC-203	DM8XMPT	Solid tumour/cancer	2A00-2F9Z	Phase 1	[16]
AMG 427	DMI7JO6	Acute myeloid leukaemia	2A60	Phase 1	[17]
FF-10101-01	DMS1O56	Acute myeloid leukaemia	2A60	Phase 1	[8]
FN-1501	DM7BMD6	Solid tumour/cancer	2A00-2F9Z	Phase 1	[18]
IMC-EB10	DMCZQNJ	Acute myeloid leukaemia	2A60	Phase 1	[19]
Ki23819	DMIAVBL	Solid tumour/cancer	2A00-2F9Z	Phase 1	[20]
KW-2449	DMFO7RP	Acute myeloid leukaemia	2A60	Phase 1	[21]
MRX-2843	DMM5N8P	Solid tumour/cancer	2A00-2F9Z	Phase 1	[22]
SKI-G-801	DM4I92Z	Acute myeloid leukaemia	2A60	Phase 1	[23]

2 Patented Agent(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Carboxamide derivative 4	DMU5GKC	N. A.	N. A.	Patented	[24]
Pyridine derivative 18	DMBZMYT	N. A.	N. A.	Patented	[24]

3 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tandutinib	DMNU2MH	Anaplastic mixed oligoastrocytoma	2A00.0Y	Discontinued in Phase 2	[4]
AG1295	DMT10C2	N. A.	N. A.	Terminated	[26]
SU5614	DMO9UCK	Airway inflammation	CA05	Terminated	[27]

1 Preclinical Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
MC-2001	DMBT2RJ	leukaemia	2A60-2B33	Preclinical	[25]

27 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(1H-indol-2-yl)(5-methoxy-1H-indol-2-yl)methanone	DM21CXZ	Discovery agent	N.A.	Investigative	[28]
(1H-indol-2-yl)(5-phenoxy-1H-indol-2-yl)methanone	DM94XJ2	Discovery agent	N.A.	Investigative	[28]
(1H-indol-2-yl)(6-methoxy-1H-indol-2-yl)methanone	DM7KDNM	Discovery agent	N.A.	Investigative	[28]
(5-fluoro-1H-indol-2-yl)-(1H-indol-2-yl)methanone	DMIV4BU	Discovery agent	N.A.	Investigative	[28]
(5-hydroxy-1H-indol-2-yl)(1H-indol-2-yl)methanone	DMPBNYM	Discovery agent	N.A.	Investigative	[28]
(benzo[b]furan-2-yl)-(1H-indol-2-yl)methanone	DME80RK	Discovery agent	N.A.	Investigative	[26]
2-(3,4-dimethoxybenzamido)thiophene-3-carboxamide	DM3S26I	Discovery agent	N.A.	Investigative	[29]
4-(4-aminophenyl)-1H-indazol-3yl-amine	DMK1IWD	Discovery agent	N.A.	Investigative	[30]
AKN-028	DMANYU5	Acute myeloid leukaemia	2A60	Investigative	[5]
AST-487	DME76KU	Discovery agent	N.A.	Investigative	[31]
Bis(5-acetoxybenzo[b]furan-2-yl)methanone	DM36VKH	Discovery agent	N.A.	Investigative	[26]
Bis(5-aminobenzo[b]furan-2-yl)methanone	DMHRGTY	Discovery agent	N.A.	Investigative	[26]
Bis(5-hydroxybenzo[b]furan-2-yl)methanone	DMGRKDP	Discovery agent	N.A.	Investigative	[26]
Bis(6-hydroxybenzo[b]furan-2-yl)methanone	DMRGNSQ	Discovery agent	N.A.	Investigative	[26]
Bis(benzo[b]furan-2-yl)methanone	DMK2ZG4	Discovery agent	N.A.	Investigative	[26]
Bis-(5-hydroxy-1H-indol-2-yl)-methanone	DMTSEXB	Discovery agent	N.A.	Investigative	[28]
Di(1H-indol-2-yl)methanone	DM3DR6J	Discovery agent	N.A.	Investigative	[28]
G749	DMC7HIS	Discovery agent	N.A.	Investigative	[32]
GTP-14564	DMW23Y9	Discovery agent	N.A.	Investigative	[33]
IN1479	DM4JNUH	Discovery agent	N.A.	Investigative	[34]
JNJ-28312141	DMCMH7O	Discovery agent	N.A.	Investigative	[35]
N-[4-(3-amino-1H-indazol-4-yl)phenyl]benzamide	DMLV18K	Discovery agent	N.A.	Investigative	[30]
PMID21982499C14k	DM0VOXN	Discovery agent	N.A.	Investigative	[36]
PMID22765894C8h	DMH5RFU	Discovery agent	N.A.	Investigative	[37]
PMID24900538C2c	DM5PATM	Discovery agent	N.A.	Investigative	[38]
TCS-359	DMH6UN8	Discovery agent	N.A.	Investigative	[29]
URMC-099	DMCJXWK	Discovery agent	N.A.	Investigative	[39]

References

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• [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] 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).
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• [7] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
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• [9] Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2. J Pharm Sci. 2010 Aug;99(8):3579-93.
• [10] Efficacy and safety of CDX-301, recombinant human Flt3L, at expanding dendritic cells and hematopoietic stem cells in healthy human volunteers. Bone Marrow Transplant. 2015 Jul;50(7):924-30.
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• [12] A novel irreversible FLT3 inhibitor, FF-10101, shows excellent efficacy against AML cells with FLT3 mutations. Blood. 2018 Jan 25;131(4):426-438.
• [13] Clinical pipeline report, company report or official report of Hanmi Pharmaceutical.
• [14] MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
• [15] A novel, dual pan-PIM/FLT3 inhibitor SEL24 exhibits broad therapeutic potential in acute myeloid leukemia. Oncotarget. 2018 Mar 30;9(24):16917-16931.
• [16] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
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• [19] IMC-EB10, an anti-FLT3 monoclonal antibody, prolongs survival and reduces nonobese diabetic/severe combined immunodeficient engraftment of some acute lymphoblastic leukemia cell lines and primary leukemic samples. Cancer Res. 2006 May 1;66(9):4843-51.
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• [22] The MERTK/FLT3 inhibitor MRX-2843 overcomes resistance-conferring FLT3 mutations in acute myeloid leukemia. JCI Insight. 2016 Mar;1(3):e85630.
• [23] Clinical pipeline report, company report or official report of Genosco.
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• [28] Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase. J Med Chem. 2006 Jun 1;49(11):3101-15.
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• [30] Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted ... J Med Chem. 2007 Apr 5;50(7):1584-97.
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• [39] Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. J Med Chem. 2013 Oct 24;56(20):8032-48.