Neratinib

Kinase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Neratinib is an onp drug in the Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2017. Its mechanism of action is classified as Kinase Inhibitors and P-Glycoprotein Inhibitors. DrugCentral lists 106 molecular targets, including MAP4K5, ERBB4 and STK24. Recorded indications include HER2-positive carcinoma of breast.

• Approval status: onp (first approved 2017 by the FDA).
• Drug class: Kinase Inhibitor.
• Mechanism of action: Kinase Inhibitors; P-Glycoprotein Inhibitors.
• Molecular targets: MAP4K5, ERBB4, STK24 and STK26 (106 listed in DrugCentral).
• Indications: HER2-positive carcinoma of breast.
• ATC code: L01EH02 (Human epidermal growth factor receptor 2 (HER2) tyrosine kinase inhibitors).
• Molecular formula: C30H29ClN6O3; molecular weight 557.05 g/mol.

Indications & contraindications

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

Indications (1)

• HER2-positive carcinoma of breast

Mechanism & targets

• Mechanism of action (MoA): Kinase Inhibitors; P-Glycoprotein Inhibitors
• Established pharmacologic class: Kinase Inhibitor

Molecular targets (106)

Target	Gene	Action	Activity
Mitogen-activated protein kinase kinase kinase kinase 5	MAP4K5	unknown	Kd 9.19
Receptor tyrosine-protein kinase erbB-4	ERBB4	inhibitor	Kd 8.62
Serine/threonine-protein kinase 24	STK24	unknown	Kd 8.19
Serine/threonine-protein kinase 26	STK26	unknown	Kd 8.13
Receptor tyrosine-protein kinase erbB-3	ERBB3	unknown	Kd 8.11
Mitogen-activated protein kinase kinase kinase kinase 3	MAP4K3	unknown	Kd 8.11
Serine/threonine-protein kinase 25	STK25	unknown	Kd 7.92
Serine/threonine-protein kinase 10	STK10	unknown	Kd 7.89
Dual specificity mitogen-activated protein kinase kinase 1	MAP2K1	unknown	Kd 7.85
Mitogen-activated protein kinase kinase kinase 19	MAP3K19	unknown	Kd 7.80
Dual specificity mitogen-activated protein kinase kinase 2	MAP2K2	unknown	Kd 7.59
Misshapen-like kinase 1	MINK1	unknown	Kd 7.54
Mitogen-activated protein kinase kinase kinase 4	MAP3K4	unknown	Kd 7.41
Serine/threonine-protein kinase 3	STK3	unknown	Kd 7.24
Receptor tyrosine-protein kinase erbB-2	ERBB2	inhibitor	IC50 7.23
Dual specificity mitogen-activated protein kinase kinase 5	MAP2K5	unknown	Kd 7.20
STE20-like serine/threonine-protein kinase	SLK	unknown	Kd 7.18
Serine/threonine-protein kinase PAK 2	PAK2	unknown	Kd 7.10
Tyrosine-protein kinase Blk	BLK	unknown	Kd 7.07
Epidermal growth factor receptor	EGFR	inhibitor	IC50 7.04

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2018-08-08	EMA	—	PUMA BIOTECH INC
2017-07-17	FDA	—	PUMA BIOTECH INC

ATC classification

ATC code	Therapeutic hierarchy
L01EH02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Human epidermal growth factor receptor 2 (HER2) tyrosine kinase inhibitors

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: ERBB2, ESR1, ESR2, PGR · Testing Required
• FDA label: ERBB2 · Testing Required
• FDA label: ESR1, ESR2, PGR
• HCSC label: ERBB2 · 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
Diarrhoea	1745.0
Nausea	414.3
Constipation	323.7
Drug titration	280.3
Fatigue	276.3
Decreased appetite	218.8
Vomiting	167.5
Disease progression	151.2
Off label use	137.8
Dehydration	107.8
Hyperchlorhydria	103.4
Breast cancer metastatic	93.8

Chemical structure

• Molecular formula: C₃₀H₂₉ClN₆O₃
• Molecular weight: 557.05 g/mol
• CAS number: —
• InChIKey: JWNPDZNEKVCWMY-VQHVLOKHSA-N
• PubChem CID: 9915743

CCOC1=CC2=NC=C(C#N)C(NC3=CC=C(OCC4=CC=CC=N4)C(Cl)=C3)=C2C=C1NC(=O)\C=C\CN(C)C

Frequently asked questions

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

What is Neratinib used for?

DrugCentral lists the following indications for Neratinib: HER2-positive carcinoma of breast.

How does Neratinib work?

Neratinib is classified as Kinase Inhibitors and P-Glycoprotein Inhibitors; its molecular targets in DrugCentral include MAP4K5, ERBB4 (inhibitor), STK24 and STK26.

When was Neratinib first approved?

Neratinib was first approved by the FDA in 2017.

What drug class does Neratinib belong to?

Neratinib is in the Kinase Inhibitor class.

What is the chemical formula of Neratinib?

Neratinib has the molecular formula C30H29ClN6O3 and a molecular weight of 557.05 g/mol.

Sources

• DrugCentral drug card 5252 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL180022 — compound record and bioactivity
• PubChem CID 9915743 — chemical identifiers
• DrugBank DB11828 — drug record
• FDA UNII JJH94R3PWB — substance identity
• DailyMed: FDA labels for Neratinib — current prescribing information (label search)
• UniProt Q9Y4K4 (MAP4K5) — target protein
• UniProt Q15303 (ERBB4) — target protein
• UniProt Q9Y6E0 (STK24) — target protein
• UniProt Q9P289 (STK26) — target protein
• UniProt P21860 (ERBB3) — target protein
• UniProt Q8IVH8 (MAP4K3) — 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.