canertinib
Small moleculeexperimental
Canertinib (CI-1033) is an experimental drug candidate for the treatment of cancer. It is an irreversible tyrosine-kinase inhibitor with activity against EGFR (IC50 0.8 nM), HER-2 (IC50 19 nM) and ErbB-4 (IC50 7 nM). By 2015, Pfizer had discontinued development of the drug. — Wikipedia
Clinical trial activity
3 trials · 1 clinical orgs · 0 marketing orgs
Phase 1
1
Phase 2
2
Phase 3
0
Phase 4
0
Earliest trial started Dec 1, 2002 (NCT00174356)
Timeline
Indications
Mechanism of action
EGFR inhibitor
Canertinib is an irreversible pan-ErbB tyrosine kinase inhibitor.
ERBB4 inhibitor
Canertinib is an irreversible pan-ErbB tyrosine kinase inhibitor.
ERBB2 inhibitor
Canertinib is an irreversible pan-ErbB tyrosine kinase inhibitor.
Chemistry & pharmacology
Loading structure…
SMILES
C=CC(=O)Nc1cc2c(Nc3ccc(F)c(Cl)c3)ncnc2cc1OCCCN1CCOCC1- Mol. weight
- 485.95 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL31965 ↗
- WikipediaCanertinib ↗
- ChEMBLCHEMBL545315 ↗
Also known as
- canertinib
- canertinib
- canertinib
- canertinib
- canertinib dihydrochloride
- canertinib dihydrochloride
- canertinib dihydrochloride
- ci1033
- ci 1033
- ci-1033
- ci-1033
- ci-1033
- ci-1033
- ci 980
- ci-980
- pd-0183805
- pd-0183805
- pd183805
- pd 183805
- pd-183805
- pd-183805
- pd-183805
- sn-26606
- sn-26606
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT00050830 | Phase 2 | Jan 1, 2003 | Pfizer |
| NCT00051051 | Phase 2 | Dec 1, 2002 | Pfizer |
| NCT00174356 | Phase 1 | Dec 1, 2002 | Pfizer |
Showing 3 of 3 trials
Page 1 / 1
Organizations
Research & Development (1)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Pfizer | For profit | 3 | 3 | 2 | 2002 |
1 organizations
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