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

General Information of Drug (ID: DMSTA36)

Drug Name

Intedanib Drug Info

Synonyms

Nintedanib; Vargatef; 656247-17-5; BIBF-1120; BIBF 1120; 928326-83-4; BIBF1120; Nintedanib (BIBF 1120); OFEV; UNII-G6HRD2P839; (Z)-methyl 3-((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenylamino)(phenyl)methylene)-2-oxoindoline-6-carboxylate; G6HRD2P839; CHEBI:85164; 1160294-26-7; Methyl (3z)-3-{[(4-{methyl[(4-Methylpiperazin-1-Yl)acetyl]amino}phenyl)amino](Phenyl)methylidene}-2-Oxo-2,3-Dihydro-1h-Indole-6-Carboxylate

Indication

Disease Entry	ICD 11	Status	REF
Colorectal cancer	2B91.Z	Approved	[1]
Idiopathic pulmonary fibrosis	CB03.4	Approved	[2]
Mesothelioma	2C51.2	Phase 3	[3]
Non-small-cell lung cancer	2C25.Y	Phase 3	[4]
Ovarian cancer	2C73	Phase 2	[4]

Cross-matching ID

PubChem CID: 135423438
ChEBI ID: CHEBI:85164
CAS Number: CAS 656247-17-5
TTD Drug ID: DMSTA36
VARIDT Drug ID: DR00137

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Fibroblast growth factor receptor 1 (FGFR1)	TTRLW2X	FGFR1_HUMAN	Modulator	[1]
Fms-like tyrosine kinase 3 (FLT-3)	TTGJCWZ	FLT3_HUMAN	Inhibitor	[1]
Platelet-derived growth factor receptor (PDGFR)	TTI2WET	NOUNIPROTAC	Modulator	[1]
Vascular endothelial growth factor receptor (VEGFR)	TTVJ1D8	NOUNIPROTAC	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	[5]

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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
Fibroblast growth factor receptor 1 (FGFR1)	DTT	FGFR1	5.32	6.548	5.908	6.126
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

Colorectal cancer

ICD Disease Classification

2B91.Z

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Fibroblast growth factor receptor 1 (FGFR1)	DTT	FGFR1	5.16E-02	1.24E-03	4.64E-03
Fms-like tyrosine kinase 3 (FLT-3)	DTT	FLT3	2.64E-120	3.41	4.96
P-glycoprotein 1 (ABCB1)	DTP	P-GP	4.70E-06	-5.80E-02	-1.98E-01

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
2	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
3	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
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: 5936).
5	Effects of Ketoconazole and Rifampicin on the Pharmacokinetics of Nintedanib in Healthy Subjects. Eur J Drug Metab Pharmacokinet. 2018 Oct;43(5):533-541.