amivantamab   Click here for help

GtoPdb Ligand ID: 10505

Synonyms: amivantamab-vmjw | JNJ-61186372 | JNJ-6372 | JNJ61186372 | Rybrevant®
Approved drug
amivantamab is an approved drug (FDA & EMA (2021))
Compound class: Antibody
Comment: Amivantamab (JNJ-61186372) is a bispecific monoclonal that targets EGFR and MET [2,4,7]. Examination of binding by surface plasmon resonance confirms that JNJ-61186372 can bind to EGFR and MET simultaneously [2]. JNJ-61186372 binding inhibits phosphorylation of both of the target receptor tyrosine kinases in vitro. Tackling the tyrosine kinases from outside the cell is hypothesised to override the issue of treatment resistance due to kinase mutations that frequently arise during therapy with intracellulary-acting small molecule kinase inhibitors [3,5-6].
Annotated peptide sequences for this antibody are available from its IMGT/mAb-DB record.
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
References
1. Chon K, Larkins E, Chatterjee S, Mishra-Kalyani PS, Aungst S, Wearne E, Subramaniam S, Li Y, Liu J, Sun J et al.. (2023)
FDA Approval Summary: Amivantamab for the Treatment of Patients with Non-Small Cell Lung Cancer with EGFR Exon 20 Insertion Mutations.
Clin Cancer Res, 29 (17): 3262-3266. [PMID:37022784]
2. Jarantow SW, Bushey BS, Pardinas JR, Boakye K, Lacy ER, Sanders R, Sepulveda MA, Moores SL, Chiu ML. (2015)
Impact of Cell-surface Antigen Expression on Target Engagement and Function of an Epidermal Growth Factor Receptor × c-MET Bispecific Antibody.
J Biol Chem, 290 (41): 24689-704. [PMID:26260789]
3. Nagasaka M, Zhu VW, Lim SM, Greco M, Wu F, Ou SI. (2021)
Beyond Osimertinib: The Development of Third-Generation EGFR Tyrosine Kinase Inhibitors For Advanced EGFR+ NSCLC.
J Thorac Oncol, 16 (5): 740-763. [PMID:33338652]
4. Neijssen J, Cardoso RMF, Chevalier KM, Wiegman L, Valerius T, Anderson GM, Moores SL, Schuurman J, Parren PWHI, Strohl WR et al.. (2021)
Discovery of amivantamab (JNJ-61186372), a bispecific antibody targeting EGFR and MET.
J Biol Chem, 296: 100641. [PMID:33839159]
5. Vijayaraghavan S, Lipfert L, Chevalier K, Bushey BS, Henley B, Lenhart R, Sendecki J, Beqiri M, Millar HJ, Packman K et al.. (2020)
Amivantamab (JNJ-61186372), an Fc Enhanced EGFR/cMet Bispecific Antibody, Induces Receptor Downmodulation and Antitumor Activity by Monocyte/Macrophage Trogocytosis.
Mol Cancer Ther, 19 (10): 2044-2056. [PMID:32747419]
6. Yun J, Lee SH, Kim SY, Jeong SY, Kim JH, Pyo KH, Park CW, Heo SG, Yun MR, Lim S et al.. (2020)
Antitumor Activity of Amivantamab (JNJ-61186372), an EGFR-MET Bispecific Antibody, in Diverse Models of EGFR Exon 20 Insertion-Driven NSCLC.
Cancer Discov, 10 (8): 1194-1209. [PMID:32414908]
7. Zheng S, Moores S, Jarantow S, Pardinas J, Chiu M, Zhou H, Wang W. (2016)
Cross-arm binding efficiency of an EGFR x c-Met bispecific antibody.
MAbs, 8 (3): 551-61. [PMID:26761634]