2021
DOI: 10.3390/pharmaceutics13040483
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Abstract: HER-3 is becoming an attractive target for antibody–drug conjugate (ADC)-based therapy. Indeed, this receptor and its ligands are found to be overexpressed in several malignancies, and re-activation of its downstream signaling axis is known to play a critical role in modulating the sensitivity of targeted therapeutics in different tumors. In this study, we generated a novel ADC named EV20/NMS-P945 by coupling the anti-HER-3 antibody EV20 with a duocarmycin-like derivative, the thienoindole (TEI) NMS-P528, a DN… Show more

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Cited by 7 publications
(3 citation statements)
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“…Furthermore, 1H11′s rapid internalization underscores its potential as an immunoconjugate therapy by being synthesized to drugs, toxins, or radioisotopes to potentiate cytotoxicity. Excitingly, 1H11 as a monotherapy demonstrates a more substantial antitumor effect on OVCAR8 tumor-bearing mice than an HER-3 targeting antibody-drug conjugate [ 64 ]. Taken together, our study revealing 1H11′s utility for integration with current mainstay drugs has wide implications on future combinatory cancer strategies in OC.…”
Section: Discussionmentioning
confidence: 99%
“…Furthermore, 1H11′s rapid internalization underscores its potential as an immunoconjugate therapy by being synthesized to drugs, toxins, or radioisotopes to potentiate cytotoxicity. Excitingly, 1H11 as a monotherapy demonstrates a more substantial antitumor effect on OVCAR8 tumor-bearing mice than an HER-3 targeting antibody-drug conjugate [ 64 ]. Taken together, our study revealing 1H11′s utility for integration with current mainstay drugs has wide implications on future combinatory cancer strategies in OC.…”
Section: Discussionmentioning
confidence: 99%
“…EV20/NMS-P945, a novel ADC targeting HER3, was composed of the EV20; the thienoindole (TEI) NMS-P528, a derivative of doxorubicin; and a cleavable linker. The preclinical study found that EV20/NMS-P945 had good anticancer activity on GC cells and mouse xenograft tumor models, which indicated that this agent could be a potent tool against HER3-expressing AGC ( 19 ).…”
Section: Adcs For the Treatment Of Agcmentioning
confidence: 99%
“…EV20-sss-vc/ MMAF demonstrated its efficacy in HER3 + liver cancer [249]. Recently, EV20/NMS-P945 showed cytotoxic activity on prostate, HNSCC, pancreatic, melanoma, gastric and ovarian cancer [250].…”
Section: In Preclinical Phasementioning
confidence: 99%