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

General Information of Drug (ID: DM13AH8)

Drug Name

TAS-0728 Drug Info

Indication

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

Cross-matching ID

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

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Drug(s) Targeting Erbb2 tyrosine kinase receptor (HER2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Lapatinib	DM3BH1Y	Breast cancer	2C60-2C65	Approved	[3]
Dacomitinib	DMOH8VY	Non-small-cell lung cancer	2C25.Y	Approved	[4]
BIBW 2992	DMTKD7Q	Non-small-cell lung cancer	2C25.Y	Approved	[5]
Merimepodib	DM0HS92	Breast cancer	2C60-2C65	Approved	[6]
NERATINIB MALEATE	DMEDU7B	HER2/NEU overexpressing breast cancer	2C60-2C65	Approved	[7]
Margetuximab	DMKEY6S	HER2-positive breast cancer	2C60-2C65	Approved	[8]
Trastuzumab	DMZQOUX	Breast cancer	2C60-2C65	Approved	[9]
Tucatinib	DMBESUA	HER2-positive breast cancer	2C60-2C65	Approved	[10]
Pertuzumab	DMHJV0X	Adrenal gland neoplasm		Approved	[11]
Masoprocol	DMMVNZ0	Prostate cancer	2C82.0	Approved	[12]
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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
Erbb2 tyrosine kinase receptor (HER2)	TT6EO5L	ERBB2_HUMAN	Inhibitor	[2]

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References

1	ClinicalTrials.gov (NCT03410927) A Study of TAS0728 in Patients With Solid Tumors With HER2 or HER3 Abnormalities. U.S. National Institutes of Health.
2	TAS0728, A Covalent-binding, HER2-selective Kinase Inhibitor Shows Potent Antitumor Activity in Preclinical Models. Mol Cancer Ther. 2019 Apr;18(4):733-742.
3	Triple negative breast cancer--current status and prospective targeted treatment based on HER1 (EGFR), TOP2A and C-MYC gene assessment. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2009 Mar;153(1):13-7.
4	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. (Ligand id: 7422).
5	Boehringer Ingelheim. Product Development Pipeline. June 2 2009.
6	Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
7	2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
8	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
9	Her2/neu is not a commonly expressed therapeutic target in melanoma -- a large cohort tissue microarray study. Melanoma Res. 2004 Jun;14(3):207-10.
10	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
11	Clinical pipeline report, company report or official report of Roche (2009).
12	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.