Margetuximab

HER2/neu Receptor Antagonist — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Margetuximab is a drug in the HER2/neu Receptor Antagonist class catalogued in DrugCentral. It was first approved by the FDA in 2020. Its mechanism of action is classified as HER2/Neu/cerbB2 Antagonists. DrugCentral lists 2 molecular targets, including ERBB2 and FCGR3A. Recorded indications include Metastatic human epidermal growth factor 2 positive carcinoma of breast.

• Drug class: HER2/neu Receptor Antagonist.
• Mechanism of action: HER2/Neu/cerbB2 Antagonists.
• Molecular targets: ERBB2 and FCGR3A (2 listed in DrugCentral).
• Indications: Metastatic human epidermal growth factor 2 positive carcinoma of breast.
• ATC code: L01FD06 (HER2 (Human Epidermal Growth Factor Receptor 2) inhibitors).

Indications & contraindications

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

Indications (1)

• Metastatic human epidermal growth factor 2 positive carcinoma of breast

Mechanism & targets

• Mechanism of action (MoA): HER2/Neu/cerbB2 Antagonists
• Established pharmacologic class: HER2/neu Receptor Antagonist

Molecular targets (2)

Target	Gene	Action	Activity
Receptor tyrosine-protein kinase erbB-2	ERBB2	antagonist	Kd 8.55
Low affinity immunoglobulin gamma Fc region receptor III-A	FCGR3A	antagonist	Kd 7.05

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2020-12-16	FDA	—	MACROGENICS INC

ATC classification

ATC code	Therapeutic hierarchy
L01FD06	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES › HER2 (Human Epidermal Growth Factor Receptor 2) inhibitors

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label
• FDA label: ERBB2 · Testing Required
• FDA label: FCGR2A, FCGR2B, FCGR3A · No Clinical PGx
• HCSC label

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
Dry gangrene	57.4

Chemical structure

• Molecular formula: —
• Molecular weight: —
• CAS number: 1350624-75-7
• InChIKey: —
• PubChem CID: —

Frequently asked questions

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

What is Margetuximab used for?

DrugCentral lists the following indications for Margetuximab: Metastatic human epidermal growth factor 2 positive carcinoma of breast.

How does Margetuximab work?

Margetuximab is classified as HER2/Neu/cerbB2 Antagonists; its molecular targets in DrugCentral include ERBB2 (antagonist) and FCGR3A (antagonist).

When was Margetuximab first approved?

Margetuximab was first approved by the FDA in 2020.

What drug class does Margetuximab belong to?

Margetuximab is in the HER2/neu Receptor Antagonist class.

Sources

• DrugCentral drug card 5434 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL2364649 — compound record and bioactivity
• DrugBank DB14967 — drug record
• FDA UNII K911R84KEW — substance identity
• DailyMed: FDA labels for Margetuximab — current prescribing information (label search)
• UniProt P04626 (ERBB2) — target protein
• UniProt P08637 (FCGR3A) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

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