Afatinib

Kinase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Afatinib is an onp drug in the Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2013. Its mechanism of action is classified as Protein Kinase Inhibitors. DrugCentral lists 45 molecular targets, including EGFR, ERBB2 and ERBB4. Recorded indications include Non-small cell lung cancer, positive for epidermal growth factor receptor expression.

• Approval status: onp (first approved 2013 by the FDA).
• Drug class: Kinase Inhibitor.
• Mechanism of action: Protein Kinase Inhibitors.
• Molecular targets: EGFR, ERBB2, ERBB4 and GAK (45 listed in DrugCentral).
• Indications: Non-small cell lung cancer, positive for epidermal growth factor receptor expression.
• ATC code: L01EB03 (Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors).
• Molecular formula: C24H25ClFN5O3; molecular weight 485.95 g/mol.

Indications & contraindications

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

Indications (1)

• Non-small cell lung cancer, positive for epidermal growth factor receptor expression

Mechanism & targets

• Mechanism of action (MoA): Protein Kinase Inhibitors
• Established pharmacologic class: Kinase Inhibitor

Molecular targets (45)

Target	Gene	Action	Activity
Epidermal growth factor receptor	EGFR	inhibitor	Kd 10.00
Receptor tyrosine-protein kinase erbB-2	ERBB2	inhibitor	Kd 8.30
Receptor tyrosine-protein kinase erbB-4	ERBB4	inhibitor	Kd 8.20
Cyclin-G-associated kinase	GAK	unknown	Kd 7.10
Tyrosine-protein kinase Blk	BLK	unknown	Kd 6.66
Tyrosine-protein kinase ABL1	ABL1	unknown	Kd 6.64
Interleukin-1 receptor-associated kinase 1	IRAK1	unknown	Kd 6.62
Ephrin type-A receptor 6	EPHA6	unknown	Kd 6.47
Homeodomain-interacting protein kinase 4	HIPK4	unknown	Kd 6.44
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform	PHKG2	unknown	Kd 6.33
Tyrosine-protein kinase Lck	LCK	unknown	Kd 6.24
Tyrosine-protein kinase Lyn	LYN	unknown	IC50 6.13
MAP kinase-activated protein kinase 2	MAPKAPK2	unknown	Kd 6.09
Dual specificity tyrosine-phosphorylation-regulated kinase 1A	DYRK1A	unknown	Kd 6.01
Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform	PHKG1	unknown	Kd 5.89
Mitogen-activated protein kinase 14	MAPK14	unknown	Kd 5.89
Casein kinase I isoform epsilon	CSNK1E	unknown	Kd 5.89
Dual specificity mitogen-activated protein kinase kinase 5	MAP2K5	unknown	Kd 5.89
Tyrosine-protein kinase FRK	FRK	unknown	Kd 5.85
Receptor-type tyrosine-protein kinase FLT3	FLT3	unknown	Kd 5.85

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2013-09-25	EMA	—	—
2013-07-12	FDA	—	BOEHRINGER INGELHEIM	Yes

ATC classification

ATC code	Therapeutic hierarchy
L01EB03	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
Malignant neoplasm progression	4783.0
Diarrhoea	2024.1
Paronychia	1328.8
Metastases to central nervous system	731.8
Rash	480.3
Stomatitis	391.1
Dermatitis acneiform	376.8
EGFR gene mutation	306.9
Metastases to meninges	270.3
Decreased appetite	255.2
Drug resistance	235.4
Skin toxicity	225.7

Chemical structure

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

• Molecular formula: C₂₄H₂₅ClFN₅O₃
• Molecular weight: 485.95 g/mol
• CAS number: —
• InChIKey: ULXXDDBFHOBEHA-CWDCEQMOSA-N
• PubChem CID: 10184653

CN(C)C\C=C\C(=O)NC1=CC2=C(C=C1O[C@H]1CCOC1)N=CN=C2NC1=CC(Cl)=C(F)C=C1

Frequently asked questions

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

What is Afatinib used for?

DrugCentral lists the following indications for Afatinib: Non-small cell lung cancer, positive for epidermal growth factor receptor expression.

How does Afatinib work?

Afatinib is classified as Protein Kinase Inhibitors; its molecular targets in DrugCentral include EGFR (inhibitor), ERBB2 (inhibitor), ERBB4 (inhibitor) and GAK.

When was Afatinib first approved?

Afatinib was first approved by the FDA in 2013.

What drug class does Afatinib belong to?

Afatinib is in the Kinase Inhibitor class.

What is the chemical formula of Afatinib?

Afatinib has the molecular formula C24H25ClFN5O3 and a molecular weight of 485.95 g/mol.

Sources

• DrugCentral drug card 4318 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1173655 — compound record and bioactivity
• PubChem CID 10184653 — chemical identifiers
• DrugBank DB08916 — drug record
• FDA UNII 41UD74L59M — substance identity
• DailyMed: FDA labels for Afatinib — current prescribing information (label search)
• UniProt P00533 (EGFR) — target protein
• UniProt P04626 (ERBB2) — target protein
• UniProt Q15303 (ERBB4) — target protein
• UniProt O14976 (GAK) — target protein
• UniProt P51451 (BLK) — target protein
• UniProt P00519 (ABL1) — 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.