General
Preferred name
ERLOTINIB
Synonyms
ERLOTINIB HYDROCHLORIDE ()
Erlotinib (mesylate) ()
CP-358774 (mesylate) ()
NSC 718781 (mesylate) ()
OSI-774 (mesylate) ()
RG-1415, Tarceva, OSI-774, R-1415, CP-358774, Ro-508231, CP-35877401, CP-358774-01, Erlotinib HCl ()
OSI-744 ()
R1415 ()
NSC 718781 ()
CP358774 ()
OSI-774 ()
Tarceva ()
CP-358774 ()
R 1415 ()
CP-358,774 ()
[6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl- phenyl)amine hydrochloride ()
Erlotinib (Hydrochloride) ()
CP-35877401 ()
R-1415 ()
RG-1415 ()
RO-508231 ()
CP-358774 (Hydrochloride) ()
NSC 718781 (Hydrochloride) ()
OSI-774 (Hydrochloride) ()
Erlotinib (OSI-774) HCl ()
Erlotinib (OSI-774) ()
CP358774, NSC 718781,OSI-774 HCl ()
CP358774, NSC 718781, Tarceva ()
Erlotinib mesylate ()
CP-358 ()
CP-358774-01 ()
CP-358,774-01 ()
Erlotinib hcl ()
Erlotinib-d6 (hydrochloride) ()
P&D ID
PD003356
CAS
183321-74-6
183319-69-9
1429636-49-6
248594-19-6
1189953-78-3
Tags
natural product
drug
available
Approved by
EMA
FDA
First approval
2004
Drug Status
investigational
approved
Drug indication
Colon cancer
Non-small-cell lung cancer
Pancreatic cancer
Max Phase
Phase 4
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
INDICATION
Erlotinib is indicated for:; ; - The treatment of metastatic non-small cell lung cancer (NSCLC) with tumors showing epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations [FDA label]. ; ; - In combination with first-line treatment for patients diagnosed with locally advanced, unresectable or metastatic pancreatic cancer [FDA label].; ; The safety and efficacy of erlotinib have not been established for patients with NSCLC whose tumors show other EGFR mutations. Additionally it is not recommended for use in combination with platinum-based chemotherapy. [FDA label]
DESCRIPTION
Erlotinib is a clinically approved type-1 inhibitor of the epidermal growth factor receptor (EGFR) receptor tyrosine kinase. This drug shows some selectivity for EGFR exon 19 deletion or exon 21 L858R mutations over the wild type receptor.
Subsequent studies have shown erlotinib to be a potent inhibitor of JAK2V617F activity. JAK2V617F, a mutant from of tyrosine kinase JAK2, is found in most patients with polycythemia vera (PV) and a substantial proportion of patients with idiopathic myelofibrosis or essential thrombocythemia. Study suggests that erlotinib may be used for treatment of JAK2V617F-positive PV and other myeloproliferative disorders. Specificity of inhibition with regard to other tyrosine kinase receptors remains to be fully characterized. Erlotinib is a Type-1 kinase inhibitor. (GtoPdb)
Subsequent studies have shown erlotinib to be a potent inhibitor of JAK2V617F activity. JAK2V617F, a mutant from of tyrosine kinase JAK2, is found in most patients with polycythemia vera (PV) and a substantial proportion of patients with idiopathic myelofibrosis or essential thrombocythemia. Study suggests that erlotinib may be used for treatment of JAK2V617F-positive PV and other myeloproliferative disorders. Specificity of inhibition with regard to other tyrosine kinase receptors remains to be fully characterized. Erlotinib is a Type-1 kinase inhibitor. (GtoPdb)
DESCRIPTION
inhibitor of EGFR and HER2
(Informer Set)
DESCRIPTION
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 with locally advanced, unresectable or metastatic pancreatic cancer.
(PKIDB)
DESCRIPTION
Highly potent JAK1 and JAK2 inhibitor; also inhibits JAK3 and Tyk2
(Tocris Bioactive Compound Library)
DESCRIPTION
Erlotinib is an EGFR inhibitor. The drug follows Iressa (gefitinib), which was the first drug of this type. Erlotinib specifically targets the epidermal growth factor receptor (EGFR) tyrosine kinase, which is highly expressed and occasionally mutated in various forms of cancer. It binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor. For the signal to be transmitted, two EGFR molecules need to come together to form a homodimer. These then use the molecule of ATP to trans-phosphorylate each other on tyrosine residues, which generates phosphotyrosine residues, recruiting the phosphotyrosine-binding proteins to EGFR to assemble protein complexes that transduce signal cascades to the nucleus or activate other cellular biochemical processes. By inhibiting the ATP, formation of phosphotyrosine residues in EGFR is not possible and the signal cascades are not initiated.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
212
Organisms
11
Compound Sets
39
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
ChEMBL Approved Drugs
ChEMBL Drugs
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
DrugMatrix
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
Informer Set
Ki Database
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
NCATS Inxight Approved Drugs
NIH Approved Oncology Drugs
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
PKIDB
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Welcome Trust Cancer Drugs
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
74
Molecular Weight
393.17
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
1
Rotatable Bonds
10
Ring Count
3
Aromatic Ring Count
3
cLogP
3.41
TPSA
74.73
Fraction CSP3
0.27
Chiral centers
0.0
Largest ring
6.0
QED
0.42
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
EGFR
ERBB2
Autophagy
EGFR, NR1I2
NR1I2
Autophagy,EGFR
Compound status
FDA
Pathway
EGFR signaling
JAK/STAT Signaling
Protein Tyrosine Kinase/RTK
Angiogenesis
Tyrosine Kinase/Adaptors
MOA
Inhibitor
Inhibitors of Signal Transduction Pathways
EGFR (HER1 or erbB1) Inhibitors
EGFR inhibitor
Member status
member
Indication
non-small cell lung cancer (NSCLC), pancreatic cancer
Therapeutic Class
Anticancer Agents
Source data
