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

General Information of DTT (ID: TTRJB2G)

• DTT Name: Ephrin type-A receptor 2 (EPHA2) DTT Info
• UniProt ID: EPHA2_HUMAN
• Gene Name: EPHA2

Molecule-Related Drug & Molecule List

4 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BT5528	DMYBKMV	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[1]
CAR-T cells targeting EphA2	DMN3C2I	Malignant glioma	2A00.0	Phase 1/2	[2]
DS-8895	DM31VNC	Solid tumour/cancer	2A00-2F9Z	Phase 1	[3], [4]
MEDI-547	DM3WP70	Solid tumour/cancer	2A00-2F9Z	Phase 1	[5]

1 Preclinical Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
MEDI-543	DM7Q1PF	Solid tumour/cancer	2A00-2F9Z	Preclinical	[6]

4 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AMP-PNP	DMTOK1D	Discovery agent	N.A.	Investigative	[7]
PMID19788238C66	DMCVJK9	Discovery agent	N.A.	Investigative	[8]
PMID21561767C8h	DMABZH6	Discovery agent	N.A.	Investigative	[9]
PMID23489211C20	DMDYC4J	Discovery agent	N.A.	Investigative	[10]

References

• [1] MMAE Delivery Using the Bicycle Toxin Conjugate BT5528. Mol Cancer Ther. 2020 Jul;19(7):1385-1394.
• [2] ClinicalTrials.gov (NCT02575261) CAR-T Cell Immunotherapy for EphA2 Positive Malignant Glioma Patients
• [3] Clinical pipeline report, company report or official report of Daiichi Sankyo.
• [4] Therapeutic target database update 2012: a resource for facilitating target-oriented drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1128-36.
• [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: 1822).
• [6] Clinical and biological impact of EphA2 overexpression and angiogenesis in endometrial cancer. Cancer Biol Ther. 2010 Dec 15;10(12):1306-14.
• [7] The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
• [8] Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4). J Med Chem. 2009 Oct 22;52(20):6433-46.
• [9] Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3743-8.
• [10] Amino acid conjugates of lithocholic acid as antagonists of the EphA2 receptor. J Med Chem. 2013 Apr 11;56(7):2936-47.