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

General Information of Drug (ID: DMSFWT7)

Drug Name
Famitinib Drug Info
Synonyms
Receptor tyrosine kinase inhibitors (cancer); SHR-1020; Receptor tyrosine kinase inhibitors (cancer), Shanghai Hengrui; Tyrosine-kinase inhibitor (oral, cancer), Jiangsu Hengrui; C-Kit/VEGFR2/PDGFR/VEGFR3/Flt1/Flt3 inhibitor (oral, cancer), Jiangsu Hengrui
Indication
Disease Entry ICD 11 Status REF
Solid tumour/cancer 2A00-2F9Z Phase 2 [1]
Cross-matching ID
PubChem CID
16662431
CAS Number
CAS 945380-27-8
TTD Drug ID
DMSFWT7
INTEDE Drug ID
DR1843

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Fms-like tyrosine kinase 3 (FLT-3) TTGJCWZ FLT3_HUMAN Inhibitor [2]
Platelet-derived growth factor receptor alpha (PDGFRA) TT8FYO9 PGFRA_HUMAN Inhibitor [2]
Platelet-derived growth factor receptor beta (PDGFRB) TTI7421 PGFRB_HUMAN Inhibitor [2]
Tyrosine-protein kinase Kit (KIT) TTX41N9 KIT_HUMAN Inhibitor [2]
Vascular endothelial growth factor receptor 1 (FLT-1) TT2Q6G1 VGFR1_HUMAN Inhibitor [2]
Vascular endothelial growth factor receptor 2 (KDR) TTUTJGQ VGFR2_HUMAN Inhibitor [2]
Vascular endothelial growth factor receptor 3 (FLT-4) TTDCBX5 VGFR3_HUMAN Inhibitor [2]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Phase 2 [3]
Cytochrome P450 1A1 (CYP1A1) DE6OQ3W CP1A1_HUMAN Phase 2 [3]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Phase 2 [3]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Phase 2 [3]

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Tyrosine-protein kinase Kit (KIT) DTT KIT 3.766 7.517 7.379 6.916
Platelet-derived growth factor receptor beta (PDGFRB) DTT PDGFRB 6.43 6.333 6.671 5.97
Vascular endothelial growth factor receptor 3 (FLT-4) DTT FLT4 3.053 3.655 3.766 4.986
Platelet-derived growth factor receptor alpha (PDGFRA) DTT PDGFRA 6.189 7.636 7.84 7.086
Vascular endothelial growth factor receptor 1 (FLT-1) DTT FLT1 4.802 4.95 4.597 3.17
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 10.036 5.779 6.508 6.481
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 10.08 7.207 5.403 9.211
Cytochrome P450 1A1 (CYP1A1) DME CYP1A1 5.952 6.384 4.897 6.293
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 Solid tumour/cancer
ICD Disease Classification 2A00-2F9Z
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Tyrosine-protein kinase Kit (KIT) DTT KIT 2.06E-01 -0.1 -0.14
Vascular endothelial growth factor receptor 2 (KDR) DTT KDR 1.98E-01 0.11 0.2
Platelet-derived growth factor receptor beta (PDGFRB) DTT PDGFRB 5.35E-10 0.36 0.89
Fms-like tyrosine kinase 3 (FLT-3) DTT FLT3 2.11E-01 -0.05 -0.16
Vascular endothelial growth factor receptor 3 (FLT-4) DTT FLT4 6.00E-01 -0.04 -0.23
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 7.36E-01 1.62E-02 1.08E-01
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 9.96E-01 -3.17E-03 -1.84E-02
Cytochrome P450 1A1 (CYP1A1) DME CYP1A1 6.83E-06 -1.42E-01 -4.93E-01
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 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: 7886).
2 Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
3 Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.