General Information of Drug (ID: DM5GFIK)

Drug Name
Icotinib hydrochloride Drug Info
Synonyms Conmana; Conmanna; Icotinib; BPI-2009-H
Indication
Disease Entry ICD 11 Status REF
Non-small-cell lung cancer 2C25.Y Registered [1]
Cross-matching ID
PubChem CID
44609731
CAS Number
CAS 1204313-51-8
TTD Drug ID
DM5GFIK
INTEDE Drug ID
DR0851

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Epidermal growth factor receptor (EGFR) TTGKNB4 EGFR_HUMAN Antagonist [2]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Phase 3 [3]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Phase 3 [3]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Phase 3 [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
Epidermal growth factor receptor (EGFR) DTT EGFR 6.045 4.991 5.317 5.252
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 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.Y
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Epidermal growth factor receptor (EGFR) DTT EGFR 5.84E-05 0.32 0.55
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 7.26E-01 -3.16E-02 -1.31E-01
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 2.45E-13 -2.29E+00 -1.44E+00
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 5.04E-04 -9.90E-02 -3.91E-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: 7641).
2 Phase I study of icotinib hydrochloride (BPI-2009H), an oral EGFR tyrosine kinase inhibitor, in patients with advanced NSCLC and other solid tumors. Lung Cancer. 2011 Aug;73(2):195-202.
3 Metabolic pathway of icotinib in vitro: the differential roles of CYP3A4, CYP3A5, and CYP1A2 on potential pharmacokinetic drug-drug interaction. J Pharm Sci. 2018 Apr;107(4):979-983.