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

General Information of Drug (ID: DMMPTLH)

Drug Name
Entrectinib Drug Info
Synonyms
1108743-60-7; RXDX-101; UNII-L5ORF0AN1I; Entrectinib (RXDX-101); L5ORF0AN1I; Benzamide, N-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl]-4-(4-methyl-1-piperazinyl)-2-[(tetrahydro-2H-pyran-4-yl)amino]-; Benzamide, N-(5-((3,5-difluorophenyl)methyl)-1H-indazol-3-yl)-4-(4-methyl-1-piperazinyl)-2-((tetrahydro-2H-pyran-4-yl)amino)-; Entrectinib [USAN:INN]; YMX; Kinome_2659; Entrectinib(rxdx-101); Entrectinib (USAN/INN); SCHEMBL3512601; GTPL8290; CHEMBL1983268; KS-00000TSK
Indication
Disease Entry ICD 11 Status REF
Non-small-cell lung cancer 2C25 Approved [1]
Colorectal cancer 2B91.Z Phase 2 [2]
Solid tumour/cancer 2A00-2F9Z Phase 2 [3]
Mammary analogue secretory carcinoma 2C60 Phase 1 [4]
Neuroblastoma 2D11.2 Phase 1 [2]
Cross-matching ID
PubChem CID
25141092
CAS Number
CAS 1108743-60-7
TTD Drug ID
DMMPTLH
INTEDE Drug ID
DR0582
ACDINA Drug ID
D01050

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 Inhibitor [1]
BDNF/NT-3 growth factors receptor (TrkB) TTKN7QR NTRK2_HUMAN Inhibitor [1]
NT-3 growth factor receptor (TrkC) TTXABCW NTRK3_HUMAN Inhibitor [1]
Proto-oncogene c-Ros (ROS1) TTSZ6Y3 ROS1_HUMAN Inhibitor [1]
Tropomyosin-related kinase A (TrkA) TTTDVOJ NTRK1_HUMAN Inhibitor [1]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [5]

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
NT-3 growth factor receptor (TrkC) DTT NTRK3 7.27 6.435 6.1 6.863
Tropomyosin-related kinase A (TrkA) DTT NTRK1 0.848 1.138 2.293 2.722
Proto-oncogene c-Ros (ROS1) DTT ROS1 5.511 4.406 4.973 4.823
ALK tyrosine kinase receptor (ALK) DTT ALK 5.329 3.897 4.178 4.943
BDNF/NT-3 growth factors receptor (TrkB) DTT NTRK2 4.65 5.231 6.555 4.672
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 11.692 6.58 4.984 9.089
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
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
NT-3 growth factor receptor (TrkC) DTT NTRK3 7.06E-04 -0.14 -0.43
Tropomyosin-related kinase A (TrkA) DTT NTRK1 8.72E-01 -0.04 -0.22
BDNF/NT-3 growth factors receptor (TrkB) DTT NTRK2 3.06E-01 -0.15 -0.31
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 1.04E-02 6.29E-02 3.54E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
2 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
3 ClinicalTrials.gov (NCT04589845) Tumor-Agnostic Precision Immuno-Oncology and Somatic Targeting Rational for You (TAPISTRY) Platform Study. U.S. National Institutes of Health.
4 Safety and Antitumor Activity of the Multitargeted Pan-TRK, ROS1, and ALK Inhibitor Entrectinib: Combined Results from Two Phase I Trials (ALKA-372... Cancer Discov. 2017 Apr;7(4):400-409.
5 Entrectinib: first global approval. Drugs. 2019 Sep;79(13):1477-1483.