Details of the Drug

General Information of Drug (ID: DMVZXIA)

Drug Name

ASTX029

Indication

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

Drug Type

Small molecular drug

Cross-matching ID

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Extracellular signal-regulated kinase 1 (ERK1)	TT1MG9E	MK03_HUMAN	Inhibitor	[2]
Extracellular signal-regulated kinase 2 (ERK2)	TT4TQBX	MK01_HUMAN	Inhibitor	[2]

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Molecular Interaction Atlas (MIA)

Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease

Solid tumour/cancer

ICD Disease Classification

2A00-2F9Z

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Extracellular signal-regulated kinase 2 (ERK2)	DTT	MAPK1	6.78E-05	1.12	2.73

Molecular Expression Atlas (MEA)

Jump to Detail Molecular Expression Atlas of This Drug

References

1	ClinicalTrials.gov (NCT03520075) Study of ASTX029 in Subjects With Advanced Solid Tumors. U.S. National Institutes of Health.
2	Clinical pipeline report, company report or official report of Astex Pharmaceuticals.
3	DOI: 10.1158/1538-7445.AM2015-4693
4	Clinical pipeline report, company report or official report of HaiHe Biopharma.
5	WO patent application no. 2013,1850,32, Nanotherapeutics for drug targeting.
6	ERK Mutations Confer Resistance to Mitogen-Activated Protein Kinase Pathway Inhibitors
7	National Cancer Institute Drug Dictionary (drug name JSI1187).
8	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
9	Corchorusin-D directed apoptosis of K562 cells occurs through activation of mitochondrial and death receptor pathways and suppression of AKT/PKB pathway. Cell Physiol Biochem. 2012;30(4):915-26.
10	Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors. J Med Chem. 2005 Feb 10;48(3):710-22.
11	Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes. 2003 Mar;52(3):588-95.
12	How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
13	Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.