Margetuximab

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Margetuximab
Monoclonal antibody
Type?
SourceChimeric (mouse/human)
TargetHER2
Clinical data
Trade namesMargenza
Other namesmargetuximab-cmkb, MGAH22
License data
Pregnancy
category
  • Not recommended. Margetuximab can cause fetal harm when administered to a pregnant woman.[1]
Routes of
administration
Intravenous
Drug classHER2/neu receptor antagonist
ATC code
  • None
Legal status
Legal status
Identifiers
CAS Number
DrugBank
ChemSpider
  • None
UNII
KEGG
Chemical and physical data
FormulaC6484H10010N1726O2024S42
Molar mass145873.98 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.

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

  1. ^ a b c "Margenza FDA label" (PDF).
  2. ^ 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. Public Domain This article incorporates text from this source, which is in the public domain.
  3. ^ Statement On A Nonproprietary Name Adopted By The USAN Council - Margetuximab, American Medical Association.
  4. ^ a b "Margenza". NCI Drug Dictionary. National Cancer Institute. Retrieved 17 December 2020.
  5. ^ Pegram Discusses Promise of Margetuximab/Chemo Combo for HER2+ Breast Cancer. Jan 2017
  6. ^ Markham A (March 2021). "Margetuximab: First Approval". Drugs. 81 (5): 599–604. doi:10.1007/s40265-021-01485-2. PMID 33761116. S2CID 232329257.
  7. ^ Clinical trial number NCT02492711 at ClinicalTrials.gov
  8. ^ "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.
  9. ^ Clinical trial number NCT02689284 at ClinicalTrials.gov
  10. ^ "Margetuximab Orphan Drug Designations and Approvals". U.S. Food and Drug Administration (FDA). 3 June 2020. Retrieved 6 June 2020.
  11. ^ a b c "Drug Trials Snapshot: Margenza". U.S. Food and Drug Administration (FDA). 16 December 2020. Retrieved 6 January 2021. Public Domain This article incorporates text from this source, which is in the public domain.
  12. ^ "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.