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Data updated: May 26, 2026

MARGENZA (margetuximab-cmkb)

HER2/Neu/cerbB2 Antagonists Genetically Validated
Fast Track
Oncology Approved 2020-12-16

MARGENZA is a HER2/neu receptor antagonist indicated for use in combination with chemotherapy to treat adult patients with metastatic HER2-positive breast cancer. It is intended for patients who have already received two or more prior anti-HER2 regimens. At least one of these previous treatments must have been administered for metastatic disease.

Source: FDA Label • MACROGENICS INC • HER2/neu Receptor Antagonist

How MARGENZA Works

Margetuximab-cmkb binds to the extracellular domain of the HER2 protein, which inhibits tumor cell proliferation and reduces the shedding of the HER2 extracellular domain. The drug features a modified Fc region that increases binding to activating Fc receptors and decreases binding to inhibitory Fc receptors. These changes lead to enhanced antibody-dependent cellular cytotoxicity (ADCC) and natural killer (NK) cell activation against the tumor.

2
Indications
--
Phase 3 Trials
5
Years on Market

Details

Status
Prescription
First Approved
2020-12-16
Routes
INJECTION
Dosage Forms
INJECTABLE

Companies

Active Ingredient: MARGETUXIMAB-CMKB

MARGENZA Approval History

2021
2022
2023
2024
2025
2026
Original
New Indication
New Form
Label Update
3 FDA actions from 2020 to 2025 · 1 indication expansions
Jan 2025 SUPPL
Label · Labeling
May 2023 SUPPL
Efficacy
Dec 2020 ORIGINAL
New Drug · Type 1 - New Molecular Entity

What MARGENZA Treats

1 indications

MARGENZA is approved for 1 conditions since its original approval in 2020. These indications span multiple therapeutic areas including oncology, immunology, and more.

  • Breast Cancer
Source: FDA Label

MARGENZA Boxed Warning

LEFT VENTRICULAR DYSFUNCTION AND EMBRYO-FETAL TOXICITY WARNING: LEFT VENTRICULAR DYSFUNCTION AND EMBRYO-FETAL TOXICITY See full prescribing information for complete boxed warning. Left Ventricular Dysfunction: MARGENZA may lead to reductions in left ventricular ejection fraction (LVEF). Evaluate cardiac function prior to and during treatment. Discontinue MARGENZA treatment for a confirmed clinically significant decrease in left ventricular function. ( 2.2 , 5.1 , 6.1 ) Embryo-Fetal Toxicity: Exp...

MARGENZA Target & Pathway

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Target

HER2 (Human Epidermal Growth Factor Receptor 2) Growth Factor Receptor

A receptor tyrosine kinase that promotes cell growth and division. Approximately 20% of breast cancers overexpress HER2, leading to aggressive tumor growth. Targeting HER2 blocks these growth signals and can trigger immune-mediated destruction of cancer cells.

Pathway Context

HER2 forms dimers with other HER family members to activate growth signaling

HER3 (Human Epidermal Growth Factor Receptor 3)
EGFR (Epidermal Growth Factor Receptor) receptor

A receptor that triggers cell growth, proliferation, and survival when activated. Mutations or overexpression of EGFR drive many cancers, particularly lung cancer. Blocking EGFR stops the growth signals that fuel tumor progression.

MARGENZA Competitive Set

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Filters applied: drops same-active-ingredient (505(b)(2) reformulations), route-mismatch (topical vs systemic), and cross-therapeutic-area matches in same-indication rings.

What's emerging in MARGENZA's indications

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Phase 3 candidates targeting molecules with no FDA-approved drug, in indications MARGENZA treats. First-in-class if their pivotal trials read out positive.

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Active Pipeline

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Ongoing clinical trials by development phase

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Key Completed Trials

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Completed studies with published results, ranked by significance

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Trial Timeline

Full development history with FDA approval milestones

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Understanding FDA Approval Types
Count Type What it means
- ORIG Original approval - drug first enters market
- SUPPL - Efficacy New indication (new disease/condition approved)
- SUPPL - Labeling Label text changes (warnings, dosing updates)
- SUPPL - Manufacturing Production changes (new facility)
- SUPPL - Chemistry Formulation changes (new dosage strength)

Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.

MARGENZA FDA Label Details

Indications & Usage

FDA Label (PDF)

MARGENZA is indicated for the treatment of Breast Cancer.

⚠️ BOXED WARNING

WARNING: LEFT VENTRICULAR DYSFUNCTION AND EMBRYO-FETAL TOXICITY WARNING: LEFT VENTRICULAR DYSFUNCTION AND EMBRYO-FETAL TOXICITY See full prescribing information for complete boxed warning. Left Ventricular Dysfunction: MARGENZA may lead to reductions in left ventricular ejection fraction (LVEF). Eva...

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Data Sources

Data sourced from official FDA and NIH databases. Click links to verify on original sources.