Margetuximab
Monoclonal antibody | |
---|---|
Type | ? |
Source | Chimeric (mouse/human) |
Target | HER2 |
Clinical data | |
Trade names | Margenza |
Other names | margetuximab-cmkb, MGAH22 |
License data |
|
Pregnancy category |
|
Routes of administration | Intravenous |
Drug class | HER2/neu receptor antagonist |
ATC code |
|
Legal status | |
Legal status | |
Identifiers | |
CAS Number |
|
DrugBank | |
ChemSpider |
|
UNII | |
KEGG | |
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 . 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[]
- ^ 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
- ^ 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.
- Drugs not assigned an ATC code
- Monoclonal antibodies for tumors
- Orphan drugs
- Receptor tyrosine kinase inhibitors
- Monoclonal antibody stubs