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

General Information of Drug (ID: DMEFW3G)

Drug Name

KD019 Drug Info

Synonyms

Tesevatinib; XL647; XL-647; 781613-23-8; EXEL-7647; UNII-F6XM2TN5A1; KD-019; XL 647; F6XM2TN5A1; 651031-01-5; 7-[[(3aS,6aR)-2-methyl-3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrol-5-yl]methoxy]-N-(3,4-dichloro-2-fluorophenyl)-6-methoxyquinazolin-4-amine; Tesevatinib [USAN:INN]; EXEL 7647; 874286-84-7; KD 019; 1000599-06-3; SCHEMBL721994; SCHEMBL721993; SCHEMBL721992; C24H25Cl2FN4O2; GTPL7944; CHEMBL3544983; EX-A172; QCR-153; MolPort-044-724-458; BCP23438; ZINC38912363; 2809AH; AKOS027255007

Indication

Disease Entry	ICD 11	Status	REF
Brain metastases	2D50	Phase 2	[1]
Meningioma metastases	2D51	Phase 2	[1]
Non-small-cell lung cancer	2C25.Y	Phase 2	[2]
Polycystic kidney disease	GB8Y	Phase 2	[3]
Recurrent glioblastoma	2A00.00	Phase 2	[1]

Cross-matching ID

PubChem CID: 10458325
CAS Number: CAS 781613-23-8
TTD Drug ID: DMEFW3G

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Ephrin type-B receptor 4 (EPHB4)	TTI4ZX2	EPHB4_HUMAN	Modulator	[4]
Tyrosine-protein kinase (PTK)	TTJSQEF	NOUNIPROTAC	Inhibitor	[1]

------------------------------------------------------------------------------------

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Ephrin type-B receptor 4 (EPHB4)	DTT	EPHB4	5.771	6.362	6.05	5.594

Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease

Brain metastases

ICD Disease Classification

2D50

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Ephrin type-B receptor 4 (EPHB4)	DTT	EPHB4	4.05E-01	6.00E-03	0.02

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
2	ClinicalTrials.gov (NCT01487174) KD019 Versus Erlotinib in Subjects With Stage IIIB/IV Non Small Cell Lung Cancer With Progression After First- or Second-Line Chemotherapy. U.S. National Institutes of Health.
3	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: 7944).
4	XL647--a multitargeted tyrosine kinase inhibitor: results of a phase II study in subjects with non-small cell lung cancer who have progressed after responding to treatment with either gefitinib or erlotinib. J Thorac Oncol. 2012 Jan;7(1):219-26.