Rx00096 - Erlotinib


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Rx00096
Primary Indication
Secondary Indication

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Disease prevalence from Electronic Health Records

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Disease A Disease B A∩B A∩¬B B∩¬A Odds-Ratio P-Value Adjusted P-Value
locally advanced non-small cell lung cancer metastatic non-small cell lung cancer 6927 6927 6927 582.492 0 0.0
metastatic pancreatic cancer locally advanced, unresectable pancreatic cancer 2521 2521 2521 1600.525 0 0.0
locally advanced pancreatic cancer locally advanced, unresectable pancreatic cancer 2521 2521 2521 1600.525 0 0.0
unresectable pancreatic cancer locally advanced, unresectable pancreatic cancer 2521 2521 2521 1600.525 0 0.0
non-small cell lung cancer locally advanced non-small cell lung cancer 6927 6927 6927 582.492 0 0.0
metastatic non-small cell lung cancer locally advanced non-small cell lung cancer 6927 6927 6927 582.492 0 0.0

Chemical, Pharmacological and Biological Annotations


ATC Code:
L01XE03
Category:
Protein Kinase Inhibitors
ChEBI ID:
114785
PubChem ID:
176870
KEGG Drug ID:
D07907
SMILE:
COCCOC1=C(OCCOC)C=C2C(NC3=CC=CC(=C3)C#C)=NC=NC2=C1
InChI:
1S/C22H23N3O4/c1-4-16-6-5-7-17(12-16)25-22-18-13-20(28-10-8-26-2)21(29-11-9-27-3)14-19(18)23-15-24-22/h1,5-7,12-15H,8-11H2,2-3H3,(H,23,24,25)
Classification:
Kingdom:
Organic Compounds
Superclass:
Heterocyclic Compounds
Class:
Naphthyridines
Subclass:
Quinazolines
Indication:
For the treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of at least one prior chemotherapy regimen. Also for use, in combination with gemcitabine, as the first-line treatment of patients wi...
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Pharmacodynamics:
Description:
Erlotinib hydrochloride (trade name Tarceva, Genentech/OSIP, originally coded as OSI-774) is a drug used to treat non-small cell lung cancer, pancreatic cancer and several other types of cancer. Similar to gefitinib, erlotinib specifically...
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Mechanism:
The mechanism of clinical antitumor action of erlotinib is not fully characterized. Erlotinib inhibits the intracellular phosphorylation of tyrosine kinase associated with the epidermal growth factor receptor (EGFR). Specificity of inhibiti...
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Adsorption, Distribution, Metabolism, Excretion and Toxicity


Human Intestinal Absorption:
+
Blood Brain Barrier:
+
Caco-2 permeable:
+
P-glycoprotein substrate:
Substrate
P-glycoprotein inhibitor I:
Inhibitor
P-glycoprotein inhibitor II:
Non-inhibitor
Renal organic cation transporter:
Non-inhibitor
CYP450 2C9 substrate:
Non-inhibitor
CYP450 2D6 substrate:
Non-inhibitor
CYP450 2C19 substrate:
Inhibitor
CYP450 inhibitory promiscuity:
High CYP Inhibitory Promiscuity
Ames test:
AMES toxic
Carcinogenicity:
Non-carcinogens
Biodegradation:
Not ready biodegradable
Rat acute toxicity:
2.3958 LD50, mol/kg
hERG inhibition (predictor I):
Weak inhibitor
hERG inhibition (predictor II):
Non-inhibitor

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Please contact us if you have questions or comments about RepurposeDB. You can also contact us if you need help in submitting your drug repositioning investigation to RepurposeDB.


Dudley Laboratory
Department of Genetics and Genomic Sciences
Icahn Institute for Genomics and Multiscale Biology
Icahn School of Medicine at Mount Sinai
One Gustave L. Levy Place, Box 1498
Manhattan, New York City, NY
repurposedb@dudleylab.org