DGIdb - DACOMITINIB Drug Record

DACOMITINIB chembl:CHEMBL2105719 ApprovedAntineoplastic

Alternate Names:

PF-00299804
VIZIMPRO
DACOMITINIB
PF-00299804-03

Drug Info:

Pharmaceutical Developer	Pfizer
Source Reported Drug Name(s)	PF-00299804/Dacomitinib
Drug Class	EGFR Inhibitor
Drug Class	Kinase Inhibitors
FDA Approval	not approved
Drug Class	small molecule
Drug Indications	antineoplastic agent

(11 More Sources)

Publications:

Ward RA et al., 2013, Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR)., J Med Chem
Yasuda et al., 2012, EGFR exon 20 insertion mutations in non-small-cell lung cancer: preclinical data and clinical implications., Lancet Oncol.
Engelman et al., 2007, PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib., Cancer Res.
Jänne et al., 2014, Dacomitinib as first-line treatment in patients with clinically or molecularly selected advanced non-small-cell lung cancer: a multicentre, open-label, phase 2 trial., Lancet Oncol.
Zahonero et al., 2015, Preclinical Test of Dacomitinib, an Irreversible EGFR Inhibitor, Confirms Its Effectiveness for Glioblastoma., Mol. Cancer Ther.
Ma et al., 2016, InsR/IGF1R Pathway Mediates Resistance to EGFR Inhibitors in Glioblastoma., Clin. Cancer Res.
Kobayashi et al., 2015, EGFR Exon 18 Mutations in Lung Cancer: Molecular Predictors of Augmented Sensitivity to Afatinib or Neratinib as Compared with First- or Third-Generation TKIs., Clin. Cancer Res.
Kobayashi et al., 2017, Characterization of EGFR T790M, L792F, and C797S Mutations as Mechanisms of Acquired Resistance to Afatinib in Lung Cancer., Mol. Cancer Ther.
Kosaka et al., 2017, Response Heterogeneity of EGFR and HER2 Exon 20 Insertions to Covalent EGFR and HER2 Inhibitors., Cancer Res.
Gerber et al., 2014, Management and future directions in non-small cell lung cancer with known activating mutations., Am Soc Clin Oncol Educ Book
Wu YL et al., 2017, Dacomitinib versus gefitinib as first-line treatment for patients with EGFR-mutation-positive non-small-cell lung cancer (ARCHER 1050): a randomised, open-label, phase 3 trial., Lancet Oncol
Sequist et al., 2011, Genotypic and histological evolution of lung cancers acquiring resistance to EGFR inhibitors., Sci Transl Med
Ramalingam et al., 2016, Dacomitinib versus erlotinib in patients with EGFR-mutated advanced nonsmall-cell lung cancer (NSCLC): pooled subset analyses from two randomized trials., Ann. Oncol.
Brzezniak C et al., 2013, Dacomitinib, a new therapy for the treatment of non-small cell lung cancer., Expert Opin Pharmacother
Fry et al., 1998, Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor., Proc. Natl. Acad. Sci. U.S.A.
Gonzales et al., 2008, Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor., Mol. Cancer Ther.
Kalous et al., 2012, Dacomitinib (PF-00299804), an irreversible Pan-HER inhibitor, inhibits proliferation of HER2-amplified breast cancer cell lines resistant to trastuzumab and lapatinib., Mol. Cancer Ther.
Kris et al., 2015, Targeting HER2 aberrations as actionable drivers in lung cancers: phase II trial of the pan-HER tyrosine kinase inhibitor dacomitinib in patients with HER2-mutant or amplified tumors., Ann. Oncol.
Nam et al., 2012, Evaluation of the antitumor effects and mechanisms of PF00299804, a pan-HER inhibitor, alone or in combination with chemotherapy or targeted agents in gastric cancer., Mol. Cancer Ther.

DACOMITINIB EGFR

Interaction Score: 2.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name PF-299804

Indication/Tumor Type non-small cell lung carcinoma

PMIDs:
23930994 21764376 18089823 25456362 25939761 26561558 26206867 27913578 28363995 24857124 28958502 21430269 26768165 23294134 9751783

Sources:
TALC DTC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions CIViC CancerCommons MyCancerGenomeClinicalTrial PharmGKB TTD FDA OncoKB
DACOMITINIB ERBB4

Interaction Score: 1.87

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name PF-299804

Novel drug target Novel Target

Direct Interaction yes

PMIDs:
None found

Sources:
TALC MyCancerGenome TdgClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial
DACOMITINIB ERBB2

Interaction Score: 1.09

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical - Cell culture

PMIDs:
18606718 22761403 25899785 22135232 28363995

Sources:
TALC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions CIViC MyCancerGenomeClinicalTrial TTD
DACOMITINIB ERBB3

Interaction Score: 0.82

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Epidermal growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions MyCancerGenomeClinicalTrial
DACOMITINIB PTEN

Interaction Score: 0.38

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BMS-754807 + Dacomitinib

Indication/Tumor Type glioblastoma multiforme

Response Type sensitive

PMIDs:
25939761 26561558

Sources:
JAX-CKB

CancerCommons: PF-00299804
- Version: 25-July-2013
Alternate Names:

11511120 PubChem Drug ID

Dacomitinib Drug Trade Name

Drug Info:

Drug Class EGFR Inhibitor

Source Reported Drug Name(s) PF-00299804/Dacomitinib

Pharmaceutical Developer Pfizer

Publications:
MyCancerGenome: DACOMITINIB
- Version: 20-Jun-2017
Alternate Names:

DACOMITINIB Generic Name

Drug Info:

Drug Class Kinase Inhibitors

Publications:
TdgClinicalTrial: DACOMITINIB
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antineoplastic agent

Drug Class small molecule

FDA Approval not approved

Publications:

DTC: DACOMITINIB

Version: 02-September-2020

Alternate Names:

CHEMBL2110732 ChEMBL Drug ID

Drug Info:

Publications:

Ward RA et al., 2013, Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR)., J Med Chem

JAX-CKB: Dacomitinib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Nam et al., 2012, Evaluation of the antitumor effects and mechanisms of PF00299804, a pan-HER inhibitor, alone or in combination with chemotherapy or targeted agents in gastric cancer., Mol. Cancer Ther.

Gonzales et al., 2008, Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor., Mol. Cancer Ther.

Kris et al., 2015, Targeting HER2 aberrations as actionable drivers in lung cancers: phase II trial of the pan-HER tyrosine kinase inhibitor dacomitinib in patients with HER2-mutant or amplified tumors., Ann. Oncol.

CIViC: DACOMITINIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

Ramalingam et al., 2016, Dacomitinib versus erlotinib in patients with EGFR-mutated advanced nonsmall-cell lung cancer (NSCLC): pooled subset analyses from two randomized trials., Ann. Oncol.

Wu YL et al., 2017, Dacomitinib versus gefitinib as first-line treatment for patients with EGFR-mutation-positive non-small-cell lung cancer (ARCHER 1050): a randomised, open-label, phase 3 trial., Lancet Oncol

Sequist et al., 2011, Genotypic and histological evolution of lung cancers acquiring resistance to EGFR inhibitors., Sci Transl Med

TTD: Dacomitinib
- Version: 2020.06.01
Alternate Names:

D06XXH TTD Drug ID

Drug Info:

Publications:
TALC: DACOMITINIB
- Version: 12-May-2016
Alternate Names:

DACOMITINIB Drug Generic Name

DACOMITINIB Primary Drug Name

PF299804 Drug Synonym

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL2105719
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL2105719
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
MyCancerGenomeClinicalTrial: DACOMITINIB
- Version: 30-February-2014
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL2110732
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
OncoKB: Dacomitinib
- Version: 23-July-2020
Alternate Names:

Drug Info:

Publications:
PharmGKB: dacomitinib
- Version: 18-August-2020
Alternate Names:

Drug Info:

Publications:
FDA: Dacomitinib
- Version: 04-September-2020
Alternate Names:

Drug Info:

Publications:

Novel drug target	Established target
Trial Name	PF-299804
Indication/Tumor Type	non-small cell lung carcinoma

Indication/Tumor Type	Advanced Solid Tumor
Response Type	sensitive
Approval Status	Preclinical - Cell culture

Mechanism of Interaction	Epidermal growth factor receptor inhibitor
Direct Interaction	yes

combination therapy	BMS-754807 + Dacomitinib
Indication/Tumor Type	glioblastoma multiforme
Response Type	sensitive

DACOMITINIB	Drug Generic Name
DACOMITINIB	Primary Drug Name
PF299804	Drug Synonym

DACOMITINIB Drug Record

DACOMITINIB chembl:CHEMBL2105719 ApprovedAntineoplastic

Alternate Names:

Drug Info:

Publications:

DACOMITINIB EGFR

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Novel drug target Established target Trial Name PF-299804 Indication/Tumor Type non-small cell lung carcinoma

PMIDs: 23930994 21764376 18089823 25456362 25939761 26561558 26206867 27913578 28363995 24857124 28958502 21430269 26768165 23294134 9751783

Sources: TALC DTC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions CIViC CancerCommons MyCancerGenomeClinicalTrial PharmGKB TTD FDA OncoKB

DACOMITINIB ERBB4

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name PF-299804 Novel drug target Novel Target Direct Interaction yes

PMIDs: None found

Sources: TALC MyCancerGenome TdgClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial

DACOMITINIB ERBB2

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type Advanced Solid Tumor Response Type sensitive Approval Status Preclinical - Cell culture

PMIDs: 18606718 22761403 25899785 22135232 28363995

Sources: TALC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions CIViC MyCancerGenomeClinicalTrial TTD

DACOMITINIB ERBB3

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Epidermal growth factor receptor inhibitor Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions MyCancerGenomeClinicalTrial

DACOMITINIB PTEN

Interaction Types & Directionality: n/a

Interaction Info: combination therapy BMS-754807 + Dacomitinib Indication/Tumor Type glioblastoma multiforme Response Type sensitive

PMIDs: 25939761 26561558

Sources: JAX-CKB

CancerCommons: PF-00299804

Alternate Names: 11511120 PubChem Drug ID Dacomitinib Drug Trade Name

Drug Info: Drug Class EGFR Inhibitor Source Reported Drug Name(s) PF-00299804/Dacomitinib Pharmaceutical Developer Pfizer

Publications:

MyCancerGenome: DACOMITINIB

Alternate Names: DACOMITINIB Generic Name

Drug Info: Drug Class Kinase Inhibitors

Publications:

TdgClinicalTrial: DACOMITINIB

Alternate Names:

Drug Info: Drug Indications antineoplastic agent Drug Class small molecule FDA Approval not approved

Publications:

DTC: DACOMITINIB

Alternate Names: CHEMBL2110732 ChEMBL Drug ID

Drug Info:

Publications: Ward RA et al., 2013, Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR)., J Med Chem

JAX-CKB: Dacomitinib

Alternate Names:

Drug Info:

CIViC: DACOMITINIB

Alternate Names:

Drug Info:

TTD: Dacomitinib

Alternate Names: D06XXH TTD Drug ID

Drug Info:

Publications:

TALC: DACOMITINIB

Alternate Names: DACOMITINIB Drug Generic Name DACOMITINIB Primary Drug Name PF299804 Drug Synonym

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL2105719

Alternate Names:

Drug Info:

Publications:

ChemblInteractions: CHEMBL2105719

Alternate Names:

Drug Info:

Publications:

MyCancerGenomeClinicalTrial: DACOMITINIB

Alternate Names:

Drug Info:

Publications:

ChemblInteractions: CHEMBL2110732

Alternate Names:

Drug Info:

Publications:

OncoKB: Dacomitinib

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name PF-299804

Indication/Tumor Type non-small cell lung carcinoma

PMIDs:
23930994 21764376 18089823 25456362 25939761 26561558 26206867 27913578 28363995 24857124 28958502 21430269 26768165 23294134 9751783

Sources:
TALC DTC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions CIViC CancerCommons MyCancerGenomeClinicalTrial PharmGKB TTD FDA OncoKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name PF-299804

Novel drug target Novel Target

Direct Interaction yes

PMIDs:
None found

Sources:
TALC MyCancerGenome TdgClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical - Cell culture

PMIDs:
18606718 22761403 25899785 22135232 28363995

Sources:
TALC MyCancerGenome TdgClinicalTrial JAX-CKB ChemblInteractions CIViC MyCancerGenomeClinicalTrial TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Epidermal growth factor receptor inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions MyCancerGenomeClinicalTrial

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy BMS-754807 + Dacomitinib

Indication/Tumor Type glioblastoma multiforme

Response Type sensitive

PMIDs:
25939761 26561558

Sources:
JAX-CKB

Alternate Names:

11511120 PubChem Drug ID

Dacomitinib Drug Trade Name

Drug Info:

Drug Class EGFR Inhibitor

Source Reported Drug Name(s) PF-00299804/Dacomitinib

Pharmaceutical Developer Pfizer

Alternate Names:

DACOMITINIB Generic Name

Drug Info:

Drug Class Kinase Inhibitors

Drug Info:

Drug Indications antineoplastic agent

Drug Class small molecule

FDA Approval not approved

Alternate Names:

CHEMBL2110732 ChEMBL Drug ID

Publications:

Ward RA et al., 2013, Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR)., J Med Chem

Alternate Names:

D06XXH TTD Drug ID

Alternate Names:

DACOMITINIB Drug Generic Name

DACOMITINIB Primary Drug Name

PF299804 Drug Synonym