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

General Information of Drug (ID: DMCBJSR)

Drug Name
Sunitinib Drug Info
Synonyms
Sunitanib; Sunitinibum; Sutent; PDGF TK antagonist; SU 11248; SU11248; KS-5022; SU-11248; SU-11248J; SU-12662; Su-011248; Sunitinib (INN); Sunitinib (free base); Sutent (TN); N-(2-diethylaminoethyl)-5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide; N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide; 5-(5-FLUORO-2-OXO-1,2-DIHYDRO-INDOL-3-YLIDENEMETHYL)-2,4-DIMETHYL-1H-PYRROLE-3-CARBOXYLIC ACID (2-DIETHYLAMINO-ETHYL)-AMIDE; Sunitinib (Pan-TK inhibitor)
Indication
Disease Entry ICD 11 Status REF
Acute undifferentiated leukemia Approved [1]
Chronic myelomonocytic leukemia Approved [1]
Classic Kaposi sarcoma Approved [1]
Gastrointestinal cancer 2C11 Approved [2]
Gastrointestinal stromal tumour 2B5B Approved [3]
Large granular lymphocytic leukemia 2A90.1 Approved [1]
Lung cancer 2C25.0 Approved [1]
Mast cell leukaemia 2A21.00 Approved [1]
Non-small-cell lung cancer 2C25.Y Approved [1]
Pancreatic cancer 2C10 Approved [1]
Primary myelofibrosis 2A20.2 Approved [1]
Prolymphocytic leukaemia 2A82.1 Approved [1]
Prostate adenocarcinoma Approved [1]
Refractory chronic myeloid leukaemia 2A20 Approved [1]
Salivary gland squamous cell carcinoma Approved [1]
Plexiform neurofibroma Investigative [1]
Therapeutic Class
Anticancer Agents
Cross-matching ID
PubChem CID
5329102
ChEBI ID
CHEBI:38940
CAS Number
CAS 557795-19-4
TTD Drug ID
DMCBJSR
VARIDT Drug ID
DR00454
INTEDE Drug ID
DR1519
ACDINA Drug ID
D00646

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Vascular endothelial growth factor receptor 2 (KDR) TTUTJGQ VGFR2_HUMAN Modulator [4]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
RalBP1-associated Eps domain-containing protein 2 (RALBP1) DTYEM9B REPS2_HUMAN Approved [5]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Approved [6]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Approved [7]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Approved [7]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Approved [8]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [9]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Approved [10]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Approved [10]

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
Breast cancer resistance protein (ABCG2) DTP BCRP 6.732 7.513 6.326 9.277
Organic anion transporting polypeptide 1B3 (SLCO1B3) DTP OATP1B3 8.873 2.17 2.485 3.322
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 9.79 0.485 3.511 2.07
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 10.08 7.207 5.403 9.211
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 Acute undifferentiated leukemia
ICD Disease Classification
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Vascular endothelial growth factor receptor 2 (KDR) DTT KDR 2.27E-01 0.03 0.14
P-glycoprotein 1 (ABCB1) DTP P-GP 4.70E-06 -5.80E-02 -1.98E-01
Breast cancer resistance protein (ABCG2) DTP BCRP 1.20E-13 -1.20E+00 -1.06E+00
Organic anion transporting polypeptide 1B3 (SLCO1B3) DTP OATP1B3 4.93E-05 -5.25E-02 -3.14E-01
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 9.49E-02 5.87E-03 5.86E-02
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 1.69E-01 2.37E-02 2.14E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 7.29E-03 -3.47E-02 -1.80E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Sunitinib FDA Label
2 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: 5713).
3 The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.
4 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
5 Rlip76 transports sunitinib and sorafenib and mediates drug resistance in kidney cancer. Int J Cancer. 2010 Mar 15;126(6):1327-38.
6 Double-transduced MDCKII cells to study human P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) interplay in drug transport across the blood-brain barrier. Mol Pharm. 2011 Apr 4;8(2):571-82.
7 Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clin Cancer Res. 2013 Mar 15;19(6):1458-66.
8 Interaction of the multikinase inhibitors sorafenib and sunitinib with solute carriers and ATP-binding cassette transporters. Clin Cancer Res. 2009 Oct 1;15(19):6062-9.
9 In vitro assessment of time-dependent inhibitory effects on CYP2C8 and CYP3A activity by fourteen protein kinase inhibitors. Drug Metab Dispos. 2014 Jul;42(7):1202-9.
10 Drug Interactions Flockhart Table