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

General Information of Drug (ID: DMB920Z)

Drug Name

Ceritinib Drug Info

Synonyms

ceritinib; LDK378; 1032900-25-6; ZYKADIA; NVP-LDK378-NX; LDK-378; UNII-K418KG2GET; LDK378(Ceritinib); LDK 378; Eritinib (LDK378); 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine; K418KG2GET; CHEMBL2403108; CHEBI:78432; AK174337; ceritinib; C28H36ClN5O3S; 5-Chloro-N2-[2-isopropoxy-5-Methyl-4-(4-piperidyl)phenyl]-N4-(2-isopropylsulfonylphenyl)pyriMidine-2,4-diaMine; 5-Chloro-N2-(5-methyl-4-(piperidin-4-yl)-2-(propan-2-yloxy)phenyl)-N4-(2-(propane-2-sulfonyl)phenyl)pyrim

Indication

Disease Entry	ICD 11	Status	REF
Non-small-cell lung cancer	2C25.Y	Approved	[1]

Cross-matching ID

PubChem CID: 57379345
ChEBI ID: CHEBI:78432
CAS Number: CAS 1032900-25-6
TTD Drug ID: DMB920Z
VARIDT Drug ID: DR00228
ACDINA Drug ID: D00115

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
ALK tyrosine kinase receptor (ALK)	TTPMQSO	ALK_HUMAN	Modulator	[1]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Approved	[2]

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

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
ALK tyrosine kinase receptor (ALK)	DTT	ALK	5.329	3.897	4.178	4.943
P-glycoprotein 1 (ABCB1)	DTP	P-GP	7.009	6.988	7.442	8.135

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

Non-small-cell lung cancer

ICD Disease Classification

2C25.Y

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
ALK tyrosine kinase receptor (ALK)	DTT	ALK	7.19E-15	0.18	0.61
P-glycoprotein 1 (ABCB1)	DTP	P-GP	3.12E-33	-8.30E-01	-1.04E+00

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	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: 7397).
2	P-glycoprotein Mediates Ceritinib Resistance in Anaplastic Lymphoma Kinase-rearranged Non-small Cell Lung Cancer. EBioMedicine. 2015 Dec 12;3:54-66.