Margetuximab Explained

Type:mab
Mab Type:mab
Source:xi/o
Target:HER2
Tradename:Margenza
Dailymedid:Margetuximab
Pregnancy Category:Not recommended. Margetuximab can cause fetal harm when administered to a pregnant woman.
Routes Of Administration:Intravenous
Class:HER2/neu receptor antagonist
Atc Prefix:L01
Atc Suffix:FD06
Legal Us:Rx-only
Legal Us Comment:[1] [2]
Cas Number:1350624-75-7
Drugbank:DB14967
Chemspiderid:None
Unii:K911R84KEW
Kegg:D10446
Synonyms:margetuximab-cmkb, MGAH22
C:6484
H:10010
N:1726
O:2024
S:42

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.

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.

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.[6]

History

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

In June 2020, it received orphan drug designation from the U.S. Food and Drug Administration (FDA).[8]

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.[9] Participants were randomized (1:1) to margetuximab plus chemotherapy or trastuzumab plus chemotherapy. 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). The trial was conducted at 166 sites in the United States and 16 other countries.

It was approved for medical use in the United States in December 2020.[10]

Notes and References

  1. Web site: Margenza FDA label .
  2. Web site: FDA approves margetuximab for metastatic HER2-positive breast cancer . U.S. Food and Drug Administration (FDA) . 16 December 2020 . 25 December 2020.
  3. http://www.ama-assn.org/resources/doc/usan/margetuximab.pdf Statement On A Nonproprietary Name Adopted By The USAN Council - Margetuximab
  4. Web site: Margenza . NCI Drug Dictionary . National Cancer Institute . 17 December 2020.
  5. Web site: Pegram Discusses Promise of Margetuximab/Chemo Combo for HER2+ Breast Cancer. Jan 2017 . 2017-02-27 . 2018-07-31 . https://web.archive.org/web/20180731111202/https://www.targetedonc.com/news/pegram-discusses-promise-of-margetuximabchemo-combo-for-her2-breast-cancer . dead .
  6. Markham A . Margetuximab: First Approval . Drugs . 81. 5. 599–604. March 2021 . 33761116 . 10.1007/s40265-021-01485-2 . 232329257 .
  7. Web site: MacroGenics and Merck to Collaborate on Immuno-Oncology Study Evaluating Margetuximab in Combination with KEYTRUDA® (pembrolizumab) for Advanced Gastric Cancer . https://web.archive.org/web/20170510205146/http://www.mercknewsroom.com/news-release/prescription-medicine-news/macrogenics-and-merck-collaborate-immuno-oncology-study-eval . 10 May 2017 . Merck & Co., Inc .
  8. Web site: Margetuximab Orphan Drug Designations and Approvals . U.S. Food and Drug Administration (FDA) . 3 June 2020 . 6 June 2020.
  9. Web site: Drug Trials Snapshot: Margenza . U.S. Food and Drug Administration (FDA) . 16 December 2020 . 6 January 2021.
  10. Web site: Margenza: FDA-Approved Drugs . U.S. Food and Drug Administration (FDA) . 17 December 2020.