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Laprituximab emtansine (IMGN289) is an antibody-drug conjugate (ADC) developed for the treatment of cancers that overexpress the epidermal growth factor receptor (EGFR), such as squamous cell carcinoma of the head and neck (SCCHN) and non-small cell lung cancer (NSCLC). The drug consists of a humanized anti-EGFR monoclonal antibody covalently linked to DM1, a potent maytansinoid cytotoxic agent. Upon intravenous administration, the antibody component binds to EGFR on tumor cells, inhibiting EGFR-mediated signaling and potentially reducing tumor proliferation. The attached DM1 payload enables direct cytotoxicity by disrupting microtubule function in targeted cancer cells. This dual mechanism allows activity against tumors both sensitive and resistant to EGFR inhibition. IMGN289 was designed using ImmunoGen's Targeted Antibody Payload (TAP) technology. IMGN289 development was discontinued after phase 1 trials for solid tumors due to strategic reasons. It showed preclinical efficacy in models resistant to other EGFR inhibitors like cetuximab or gefitinib.
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