dacomitinib
Trade name: vizimpro
Approved
Sep 27, 2018
Dacomitinib is an oral, once-daily, pan-HER inhibitor. It is an irreversible inhibitor of HER-1 (EGFR), HER-2 and HER-4 tyrosine kinases. Dacomtinib is being evaluated in phase 3 clinical trials against nonsmall-cell lung cancer. Direct comparison with erlotinib did not show superiority of dacomtinib, but subgroup analysis have demonstrated that subgroup with exon 19 deletion had favorable outcomes with dacomitinib. In addition to nonsmall-cell lung cancer dacomtinib is being evaluated against esophagus, head and neck and other neoplasms. Due to its ability to pass through blood-brain barrier, dacomitinib can be used to treat brain tumors. — NCATS
Clinical trial activity
52 trials · 36 clinical orgs · 1 marketing orgs
Earliest trial started Oct 1, 2005 (NCT00225121)
Timeline
2000s
Indications
Approved for
Studied for
- Adenocarcinoma · Phase 1
- Brain Neoplasms · Phase 2
- Breast Neoplasms · Phase 2
- Carcinoma, Large Cell · Phase 1
- Carcinoma, Non-Small-Cell Lung · Phase 3
- Carcinoma, Squamous Cell · Phase 2
- Colorectal Neoplasms · Phase 1/Phase 2
- Esophageal Neoplasms · Phase 2
- Esophageal Squamous Cell Carcinoma · Phase 2
- Glioblastoma · Phase 2
- Head and Neck Neoplasms · Phase 2
- Healthy Volunteers · Phase 1
- Liver Diseases · Phase 1
- Lung Neoplasms · Phase 3
- Mouth Neoplasms · Phase 1/Phase 2
- Mutation · Early Phase 1
- Neoplasm Metastasis · Phase 1
- Neoplasms · Phase 2
- Penile Neoplasms · Phase 2
- Small Cell Lung Carcinoma · Phase 4
- Squamous Cell Carcinoma of Head and Neck · Phase 2
- Stomach Neoplasms · Phase 2
Mechanism of action
EGFR inhibitor
Dacomitinib is an irreversible pan-ERBB inhibitor.
ERBB4 inhibitor
Dacomitinib is an irreversible pan-ERBB inhibitor.
ERBB2 inhibitor
Dacomitinib is an irreversible pan-ERBB inhibitor.
- Epidermal growth factor receptorINHIBITOR
Epidermal growth factor receptor inhibitor
Approval history
- approvedPriority reviewSep 27, 2018
Chemistry & pharmacology
SMILES
COc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1NC(=O)/C=C/CN1CCCCC1- Mol. weight
- 469.95 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL2110732 ↗
- WikipediaDacomitinib ↗
- NCATS2XJX250C20 ↗
- ChEMBLCHEMBL2105719 ↗
Also known as
- dacomitinib
- dacomitinib
- dacomitinib
- dacomitinib
- dacomitinib
- dacomitinib
- dacomitinib anhydrous
- dacomitinib anhydrous
- dacomitinib hydrate
- pf00299804
- pf00299804
- pf00299804
- pf 00299804
- pf-00299804
- pf-00299804
- pf-00299804
- pf-00299804
- pf-00299804-03
- pf-00299804-03
- pf-299804
- pf-299804
- pf804
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06486142 | Phase 3 | Sep 21, 2022 | Region Skane, Swedish Lung Cancer Study Group |
| NCT05271916 | Phase 1/Phase 2 (Phase 2) | Apr 1, 2022 | Jiao Tong University |
| NCT04946968 | Phase 2 | Aug 24, 2021 | Cancer Science Institute of Singapore, Government of Singapore, National University of Singapore, Singapore Translational Cancer Consortium |
| NCT04504071 | Phase 2 | Dec 8, 2020 | Jiao Tong University |
| NCT04675008 | Phase 2 | Dec 7, 2020 | Sungkyunkwan University |
| NCT04511533 | Phase 4 | Aug 27, 2020 | Pfizer |
| NCT04339829 | Phase 2 | Aug 1, 2020 | Guangdong Association of Clinical Trials |
| NCT04423185 | Phase 2 | Jul 1, 2020 | Chinese Academy of Medical Sciences |
| NCT04811001 | Phase 2 | Jun 12, 2020 | Fondazione Ricerca Traslazionale, University of Milan |
| NCT04027647 | Phase 2 | Aug 31, 2019 | Government of Singapore, Pfizer |
| NCT03865446 | Phase 1 | Apr 5, 2019 | Pfizer |
| NCT03810807 | Phase 1 | Jan 17, 2019 | Memorial Sloan-Kettering Cancer Center |
| NCT03755102 | Early Phase 1 (Phase 1) | Nov 21, 2018 | Memorial Sloan-Kettering Cancer Center |
| NCT02382796 | Phase 2 | Jul 1, 2015 | Pfizer |
| NCT02268747 | Phase 2 | Nov 1, 2014 | University of Milan |
| NCT02097433 | Phase 1 | Jul 1, 2014 | Pfizer |
| NCT02047747 | Phase 2 | Feb 1, 2014 | Pfizer, University of California, San Diego, University of California, San Francisco |
| NCT02039336 | Phase 1/Phase 2 (Phase 2) | Jan 1, 2014 | Erasmus University Rotterdam, Netherlands Cancer Institute, Pfizer, Utrecht University |
| NCT01920061 | Phase 1 | Sep 10, 2013 | Pfizer |
| NCT01918761 | Phase 1 | Aug 1, 2013 | Central European Cooperative Oncology Group, University of Vienna |