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

General Information of Drug (ID: DMJVZBC)

Drug Name

TP-0184 Drug Info

Synonyms

Itacnosertib; UNII-22Z53X5LHF; 22Z53X5LHF; 1628870-27-8; methylpiperazin-1-yl)phenyl]pyrimidine-2,4-diamine; N4-([2,2'-bipyridin]-3-yl)-N2-[3-methoxy-4-(4-; 2-N-[3-methoxy-4-(4-methylpiperazin-1-yl)phenyl]-4-N-(2-pyridin-2-ylpyridin-3-yl)pyrimidine-2,4-diamine; Itacnosertib [INN]; SCHEMBL16129103; GTPL10632; TP0184; example 11 [WO2014151871A9]; 2,4-Pyrimidinediamine, N4-(2,2'-bipyridin)-3-yl-N2-(3-methoxy-4-(4-methyl-1-piperazinyl)phenyl)-; N2-(3-Methoxy-4-(4-methylpiperazin-1-yl)phenyl)-N4-(2-(pyridin-2-yl)pyridin-3-yl)pyrimidine-2,4-diamine

Indication

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

Cross-matching ID

PubChem CID: 86290265
CAS Number: CAS 1628870-27-8
TTD Drug ID: DMJVZBC

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Clinical Trial Drug(s)

Patented Agent(s)

Investigative Drug(s)

Preclinical Drug(s)

Discontinued Drug(s)

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Drug(s) Targeting Activin receptor-like kinase 2 (ALK-2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
INCB00928	DMFG8TI	Anemia	3A00-3A9Z	Phase 2	[3]
PMID27774822-Compound-Figure10Compound12	DMFAGOZ	N. A.	N. A.	Patented	[4]
PMID27774822-Compound-Figure10Compound4	DMMJVTW	N. A.	N. A.	Patented	[4]
PMID23639540C13d	DMSTQGH	Discovery agent	N.A.	Investigative	[5]
PMID23639540C13a	DMLXOAQ	Discovery agent	N.A.	Investigative	[5]
PMID23639540C13r	DMHBZ0N	Discovery agent	N.A.	Investigative	[5]
LDN-214117	DM57Z8J	Discovery agent	N.A.	Investigative	[6]
ML347	DMR8N36	Discovery agent	N.A.	Investigative	[5]
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Drug(s) Targeting TGF-beta receptor type I (TGFBR1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
LY2157299	DMP8HW1	Arteriosclerosis	BD40	Phase 2/3	[7]
TEW-7197	DM2LBC3	Myeloproliferative neoplasm	2A20	Phase 2	[8]
Metelimumab	DMENFD6	Scleroderma	4A42	Phase 1/2	[9]
P-2745	DMJ3PNS	Chronic myelogenous leukaemia	2A20.0	Phase 1	[10]
LY3200882	DMQP6VB	Solid tumour/cancer	2A00-2F9Z	Phase 1	[11]
PF-06952229	DMDQJEZ	Solid tumour/cancer	2A00-2F9Z	Phase 1	[12]
SB-431542	DM0YOXQ	Pulmonary fibrosis	CB03.4	Preclinical	[13]
SM-16	DMHXJV2	Fibrosis	GA14-GC01	Terminated	[14]
LF-984	DMIYMS2	Fibrosis	GA14-GC01	Terminated	[15]
PMID23639540C13d	DMSTQGH	Discovery agent	N.A.	Investigative	[5]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Activin receptor-like kinase 2 (ALK-2)	TTJNBQA	ACVR1_HUMAN	Inhibitor	[2]
TGF-beta receptor type I (TGFBR1)	TTP4520	TGFR1_HUMAN	Inhibitor	[2]

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References

1	ClinicalTrials.gov (NCT03429218) First-in-human Study of Oral TP-0184 in Patients With Advanced Solid Tumors. U.S. National Institutes of Health.
2	Clinical pipeline report, company report or official report of Sumitomo Dainippon Pharma.
3	Clinical pipeline report, company report or official report of Incyte.
4	Inhibitors of JAK-family kinases: an update on the patent literature 2013-2015, part 2.Expert Opin Ther Pat. 2017 Feb;27(2):145-161.
5	Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe. Bioorg Med Chem Lett. 2013 Jun 1;23(11):3248-52.
6	Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. J Med Chem. 2014 Oct 9;57(19):7900-15.
7	Cardiac Safety of TGF-beta Receptor I Kinase Inhibitor LY2157299 Monohydrate in Cancer Patients in a First-in-Human Dose Study. Cardiovasc Toxicol. 2015 Oct;15(4):309-23.
8	Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
9	Development of TGF-beta signalling inhibitors for cancer therapy. Nat Rev Drug Discov. 2004 Dec;3(12):1011-22.
10	Novel potent inhibitor of Bcr-Abl mutated imatinib resistant chronic myeloid leukemia cell lines. Cancer Research. 06/2012; 72(8 Supplement):1822-1822.
11	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
12	Targeting the TGF pathway for cancer therapy. Pharmacol Ther. 2015 Mar;147:22-31.
13	Pyrazolone based TGFbetaR1 kinase inhibitors. Bioorg Med Chem Lett. 2010 Jan 1;20(1):326-9.
14	TGF-beta type I receptor kinase inhibitor down-regulates rheumatoid synoviocytes and prevents the arthritis induced by type II collagen antibody. Int Immunol. 2007 Feb;19(2):117-26.
15	US patent application no. 2013,0028,978, Compositions and methods for wound treatment.