Last reviewed · How we verify
Margenza (MARGETUXIMAB)
Margenza works by blocking the HER2/neu receptor, which is overexpressed in certain breast cancer cells, to prevent them from growing and multiplying.
Margenza (margetuximab) is a HER2/neu Receptor Antagonist developed by MacroGenics Inc. It targets the receptor tyrosine-protein kinase erbB-2 to treat metastatic human epidermal growth factor 2 positive carcinoma of breast. Margenza is a small molecule modality that was FDA approved in 2020. It is currently owned and patented by MacroGenics Inc. Key safety considerations include its potential side effects, which should be carefully monitored by healthcare professionals.
At a glance
| Generic name | MARGETUXIMAB |
|---|---|
| Sponsor | Macrogenics Inc |
| Drug class | HER2/neu Receptor Antagonist [EPC] |
| Target | Receptor tyrosine-protein kinase erbB-2 |
| Modality | Monoclonal antibody |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 2020 |
Mechanism of action
Margetuximab-cmkb binds to the extracellular domain of the human epidermal growth factor receptor protein (HER2). Upon binding to HER2-expressing tumor cells, margetuximab-cmkb inhibits tumor cell proliferation, reduces shedding of the HER2 extracellular domain and mediates antibody-dependent cellular cytotoxicity (ADCC).In vitro, the modified Fc region of margetuximab-cmkb increases binding to activating Fc receptor FCGR3A (CD16A) and decreases binding to inhibitory Fc receptor FCGR2B (CD32B). These changes lead to greater in vitro ADCC and NK cell activation.
Approved indications
- Metastatic human epidermal growth factor 2 positive carcinoma of breast
Boxed warnings
- 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: Exposure to MARGENZA during pregnancy can cause embryo-fetal harm. Advise patients of the risk and need for effective contraception. ( 5.2 , 8.1 , 8.3 ) 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 [see Dosage and Administration (2.2) , Warnings and Precautions (5.1) , and Adverse Reactions (6.1) ]. Embryo-Fetal Toxicity: Exposure to MARGENZA during pregnancy can cause embryo-fetal harm. Advise patients of the risk and need for effective contraception [see Warnings and Precautions (5.2) , Use in Specific Populations (8.1 , 8.3) ].
Common side effects
- Fatigue/Asthenia
- Pyrexia
- Nausea
- Diarrhea
- Vomiting
- Constipation
- Abdominal pain
- Alopecia
- Palmar-plantar erythrodysesthesia
- Headache
- Peripheral neuropathy
- Cough
Key clinical trials
- Pilot Study of [68Ga]Ga-ABY-025 Imaging in Patients Undergoing Treatment With HER2-targeted Therapy (EARLY_PHASE1)
- MARGetuximab Or Trastuzumab (MARGOT) (PHASE2)
- Combination Margetuximab, Retifanlimab, Tebotelimab, and Chemotherapy Phase 2/3 Trial in HER2+ Gastric/GEJ Cancer (PHASE2,PHASE3)
- Margetuximab Plus Chemotherapy vs Trastuzumab Plus Chemotherapy in the Treatment of HER2+ Metastatic Breast Cancer (PHASE3)
- Combination Margetuximab and Pembrolizumab for Advanced, Metastatic HER2(+) Gastric or Gastroesophageal Junction Cancer (PHASE1,PHASE2)
- Phase 2 Study of the Monoclonal Antibody MGAH22 (Margetuximab) in Patients With Relapsed or Refractory Advanced Breast Cancer (PHASE2)
- Safety Study of MGAH22 in HER2-positive Carcinomas (PHASE1)
- Margetuximab Expanded Access Program
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Margenza CI brief — competitive landscape report
- Margenza updates RSS · CI watch RSS
- Macrogenics Inc portfolio CI