Dacomitinib

ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Dacomitinib is an onp drug catalogued in DrugCentral. It was first approved by the FDA in 2018. DrugCentral lists 10 molecular targets, including Egfr, EGFR and ERBB2. Recorded indications include EGFR mutation-positive, unresectable or recurrent non-small cell lung cancer and Non-small cell lung cancer, positive for epidermal growth factor receptor expression.

• Approval status: onp (first approved 2018 by the FDA).
• Molecular targets: Egfr, EGFR, ERBB2 and ERBB4 (10 listed in DrugCentral).
• Indications: EGFR mutation-positive, unresectable or recurrent non-small cell lung cancer and Non-small cell lung cancer, positive for epidermal growth factor receptor expression.
• ATC code: L01EB07 (Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors).
• Molecular formula: C24H25ClFN5O2; molecular weight 469.95 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (2)

• EGFR mutation-positive, unresectable or recurrent non-small cell lung cancer
• Non-small cell lung cancer, positive for epidermal growth factor receptor expression

Mechanism & targets

Molecular targets (10)

Target	Gene	Action	Activity
Epidermal growth factor receptor	Egfr	unknown	IC50 8.24
Epidermal growth factor receptor	EGFR	inhibitor	IC50 8.22
Receptor tyrosine-protein kinase erbB-2	ERBB2	inhibitor	IC50 7.34
Receptor tyrosine-protein kinase erbB-4	ERBB4	inhibitor	IC50 7.13
Tyrosine-protein kinase Lck	LCK	unknown	IC50 7.03
Proto-oncogene tyrosine-protein kinase Src	SRC	unknown	IC50 6.96
Cyclin-G-associated kinase	GAK	unknown	Kd 6.78
Receptor-interacting serine/threonine-protein kinase 2	RIPK2	unknown	Kd 6.00
Tyrosine-protein kinase JAK3	JAK3	unknown	IC50 5.45
Receptor-interacting serine/threonine-protein kinase 3	RIPK3	unknown	Kd 5.44

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2019-08-01	PMDA	—	PFIZER JAPAN INC.
2019-02-04	EMA	—	PFIZER EUROPE MA EEIG
2018-09-27	FDA	—	PFIZER INC	Yes

ATC classification

ATC code	Therapeutic hierarchy
L01EB07	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: EGFR · Testing Required
• FDA label: EGFR · Testing Required
• HCSC label: EGFR · Testing Required

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Neoplasm progression	136.4
Paronychia	116.3
Death	86.2
Diarrhoea	56.5

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Dacomitinib is on its molecule page.

• Molecular formula: C₂₄H₂₅ClFN₅O₂
• Molecular weight: 469.95 g/mol
• CAS number: 1110813-31-4
• InChIKey: LVXJQMNHJWSHET-AATRIKPKSA-N
• PubChem CID: 11511120

COC1=CC2=NC=NC(NC3=CC=C(F)C(Cl)=C3)=C2C=C1NC(=O)\C=C\CN1CCCCC1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Dacomitinib used for?

DrugCentral lists the following indications for Dacomitinib: EGFR mutation-positive, unresectable or recurrent non-small cell lung cancer and Non-small cell lung cancer, positive for epidermal growth factor receptor expression.

How does Dacomitinib work?

Its molecular targets in DrugCentral include Egfr, EGFR (inhibitor), ERBB2 (inhibitor) and ERBB4 (inhibitor).

When was Dacomitinib first approved?

Dacomitinib was first approved by the FDA in 2018.

What is the chemical formula of Dacomitinib?

Dacomitinib has the molecular formula C24H25ClFN5O2 and a molecular weight of 469.95 g/mol.

Sources

• DrugCentral drug card 5297 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL2105719 — compound record and bioactivity
• PubChem CID 11511120 — chemical identifiers
• DrugBank DB11963 — drug record
• FDA UNII 5092U85G58 — substance identity
• DailyMed: FDA labels for Dacomitinib — current prescribing information (label search)
• UniProt P00533 (EGFR) — target protein
• UniProt P04626 (ERBB2) — target protein
• UniProt Q15303 (ERBB4) — target protein
• UniProt P06239 (LCK) — target protein
• UniProt P12931 (SRC) — target protein
• UniProt O14976 (GAK) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.