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Compound class:
Antibody
Comment: MM-151 is a mixture of three fully human IgG1 monoclonal antibodies, each of which targets a distinct (and nonoverlapping) epitope on the extra-cellular domain of the EGFR [2]. This can be termed an oligoclonal agent. It was designed to target EGFRs with treatment-induced (acquired) resistance mutations that develop in cancer patients treated with the approved anti-EGFR monoclonals cetuximab or panitumumab. Development of the three antibody components is reported in [1].
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| Bioactivity Comments |
| We have tagged the EGFR as the primary molecular target of MM-151 based on preclinical results published in [2]. MM-151 antagonises high-affinity EGFR ligands more potently than cetuximab [2], and In cell viability studies, exhibits effective antiproliferative activity. The P1X antibody component of MM-151 has an EGFR dissociation Kd of 0.071nM, the Kd for P2X is 0.3nM and for P3X is 0.011nM [1]. |
| Selectivity at catalytic receptors | ||||||||||||||||||||||||||||||||||
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