Margetuximab

Margetuximab
Monoclonal antibody
Type	Whole antibody
Source	Chimeric (mouse/human)
Target	HER2
Clinical data
Trade names	Margenza
Other names	margetuximab-cmkb, MGAH22
License data	US DailyMed: Margetuximab
Pregnancy category	Not recommended. Margetuximab can cause fetal harm when administered to a pregnant woman.^[1]
Routes of administration	Intravenous
Drug class	HER2/neu receptor antagonist
ATC code	L01FD06 (WHO)
Legal status
Legal status	US: ℞-only^[1]^[2]
Identifiers
CAS Number	1350624-75-7
DrugBank	DB14967
ChemSpider	None
UNII	K911R84KEW
KEGG	D10446
Chemical and physical data
Formula	C₆₄₈₄H₁₀₀₁₀N₁₇₂₆O₂₀₂₄S₄₂
Molar mass	145873.98 g·mol⁻¹

Margetuximab, sold under the brand name Margenza, is a chimeric IgG monoclonal antibody medication against HER2 used for the treatment of cancer.^[3]^[4]

The most common adverse drug reactions in combination with chemotherapy are fatigue/asthenia, nausea, diarrhea, vomiting, constipation, headache, pyrexia, alopecia, abdominal pain, peripheral neuropathy, arthralgia/myalgia, cough, decreased appetite, dyspnea, infusion-related reactions, palmar-plantar erythrodysesthesia, and extremity pain.^[2]

This drug was created by Raven biotechnologies, which was later acquired by MacroGenics. It was engineered to increase affinity for CD16A polymorphisms and decrease affinity for FcγRIIB (CD32B), an inhibitory receptor.^[4]

It binds to the same target (epitope) as trastuzumab,^[5] on the HER2 receptor.

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Medical uses

Margetuximab is indicated, in combination with chemotherapy, for the treatment of adults with metastatic HER2-positive breast cancer who have received two or more prior anti-HER2 regimens, at least one of which was for metastatic disease.^[1]^[2]^[6]

History

It is in phase III clinical trials for combination therapy in metastatic breast cancer^[7] in collaboration with Merck.^[8] Phase II trials are also in progress for gastric cancer and esophageal cancer.^[9]^{[needs update]}

In June 2020, it received orphan drug designation from the U.S. Food and Drug Administration (FDA).^[10]

Efficacy was evaluated in SOPHIA (NCT02492711), a randomized, multicenter, open-label trial of 536 participants with IHC 3+ or ISH-amplified HER2+ metastatic breast cancer who had received prior treatment with other anti-HER2 therapies.^[2]^[11] Participants were randomized (1:1) to margetuximab plus chemotherapy or trastuzumab plus chemotherapy.^[2] Randomization was stratified by chemotherapy choice (capecitabine, eribulin, gemcitabine, or vinorelbine), number of lines of therapy in the metastatic setting (≤ 2, > 2), and number of metastatic sites (≤ 2, > 2).^[2] The trial was conducted at 166 sites in the United States and 16 other countries.^[11]

It was approved for medical use in the United States in December 2020.^[2]^[12]^[11]

References

^ ^a ^b ^c "Margenza FDA label" (PDF).
^ ^a ^b ^c ^d ^e ^f ^g "FDA approves margetuximab for metastatic HER2-positive breast cancer". U.S. Food and Drug Administration (FDA). 16 December 2020. Retrieved 25 December 2020. This article incorporates text from this source, which is in the public domain.
^ Statement On A Nonproprietary Name Adopted By The USAN Council - Margetuximab, American Medical Association.
^ ^a ^b "Margenza". NCI Drug Dictionary. National Cancer Institute. Retrieved 17 December 2020.
^ "Pegram Discusses Promise of Margetuximab/Chemo Combo for HER2+ Breast Cancer. Jan 2017". Archived from the original on 2018-07-31. Retrieved 2017-02-27.
^ Markham A (March 2021). "Margetuximab: First Approval". Drugs. 81 (5): 599–604. doi:10.1007/s40265-021-01485-2. PMID 33761116. S2CID 232329257.
^ Clinical trial number NCT02492711 at ClinicalTrials.gov
^ "MacroGenics and Merck to Collaborate on Immuno-Oncology Study Evaluating Margetuximab in Combination with KEYTRUDA® (pembrolizumab) for Advanced Gastric Cancer". Merck & Co., Inc. Archived from the original on 10 May 2017.
^ Clinical trial number NCT02689284 at ClinicalTrials.gov
^ "Margetuximab Orphan Drug Designations and Approvals". U.S. Food and Drug Administration (FDA). 3 June 2020. Retrieved 6 June 2020.
^ ^a ^b ^c "Drug Trials Snapshot: Margenza". U.S. Food and Drug Administration (FDA). 16 December 2020. Retrieved 6 January 2021. This article incorporates text from this source, which is in the public domain.
^ "Margenza: FDA-Approved Drugs". U.S. Food and Drug Administration (FDA). Retrieved 17 December 2020.

External links

"Margetuximab". Drug Information Portal. U.S. National Library of Medicine.

Monoclonal antibodies for tumors

Tumor

Human	Adecatumumab^§ Amivantamab Ascrinvacumab^§ Atezolizumab Balstilimab^† Botensilimab Cixutumumab^§ Conatumumab^§ Daratumumab Drozitumab^§ Duligotumab^§ Dusigitumab^§ Enfortumab vedotin Enoticumab^§ Figitumumab^§ Flanvotumab^§ Ganitumab^† Glembatumumab vedotin^† Intetumumab^§ Ipilimumab Iratumumab^§ Istiratumab Icrucumab^§ Lexatumumab^§ Lucatumumab^§ Mapatumumab^§ Narnatumab^§ Necitumumab Nesvacumab^§ Nivolumab^# Ofatumumab Olaratumab^† Panitumumab Patritumab^§ Pembrolizumab^# Pritumumab^§ Radretumab^§ Ramucirumab Rilotumumab^† Robatumumab^§ Seribantumab^§ Tarextumab^§ Tisotumab vedotin Teprotumumab^† Tovetumab^§ Vantictumab^§ Votumumab^§ Zalutumumab^†
Mouse	Abagovomab Altumomab pentetate Anatumomab mafenatox Arcitumomab Bectumomab Blinatumomab Capromab pendetide Detumomab Edrecolomab Ibritumomab tiuxetan Igovomab Lilotomab Minretumomab Mitumomab Nacolomab tafenatox Moxetumomab pasudotox Naptumomab estafenatox Oregovomab Pemtumomab^† Racotumomab Satumomab pendetide Solitomab Taplitumomab paptox Nofetumomab merpentan Pintumomab Tenatumomab Tositumomab
Chimeric	Amatuximab^§ Bavituximab^§ Brentuximab vedotin Carotuximab^† Cetuximab Derlotuximab biotin^§ Dinutuximab Ecromeximab^§ Ensituximab^§ Futuximab^§ Girentuximab^† Indatuximab ravtansine^§ Isatuximab Loncastuximab tesirine Margetuximab Mirvetuximab soravtansine Rituximab^# Siltuximab Ublituximab
Humanized	Abituzumab^§ Alemtuzumab Belantamab mafodotin Bevacizumab Bivatuzumab mertansine^§ Brontictuzumab^§ Cantuzumab mertansine^§ Cantuzumab ravtansine^§ Cirmtuzumab Citatuzumab bogatox^§ Clivatuzumab tetraxetan Cofetuzumab pelidotin Dacetuzumab^§ Demcizumab^§ Dalotuzumab^§ Denintuzumab mafodotin^§ Elotuzumab Emactuzumab Emibetuzumab^§ Enoblituzumab^§ Epcoritamab Etaracizumab^§ Farletuzumab^§ Ficlatuzumab^§ Flotetuzumab^§ Gemtuzumab ozogamicin Glofitamab Imgatuzumab^§ Inotuzumab ozogamicin Labetuzumab^§ Lifastuzumab vedotin^§ Lintuzumab^§ Lorvotuzumab mertansine^§ Lumretuzumab^§ Matuzumab^§ Milatuzumab^§ Naxitamab Nimotuzumab^† Obinutuzumab Ocaratuzumab^§ Otlertuzumab^§ Onartuzumab^§ Oportuzumab monatox^† Parsatuzumab^§ Pertuzumab Pinatuzumab vedotin^§ Polatuzumab vedotin Rosmantuzumab Rovalpituzumab tesirine^† Sacituzumab govitecan Sibrotuzumab^§ Simtuzumab^§ Sofituzumab vedotin^§ Tacatuzumab tetraxetan^§ Tigatuzumab^§ Trastuzumab^# (+deruxtecan / +emtansine) Tucotuzumab celmoleukin^§ Vandortuzumab vedotin^§ Vanucizumab^§ Veltuzumab^§ Vorsetuzumab mafodotin^§
Rat/mouse hybrid	Catumaxomab Ertumaxomab^§
Chimeric + humanized	Depatuxizumab mafodotin^† Duvortuxizumab Ontuxizumab^§

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

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