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DM1, a maytansinoid derivative, is a common payload toxin in antibody-drug conjugates (ADCs). It binds to tubulin, hinders microtubule assembly, arrests cell division, and induces apoptosis, but has off-target toxicity. ADCs like T-DM1 have shown good efficacy in HER2-positive cancers. For recent progress, many new DM1-containing ADCs are under development. For example, GQ1001 has entered Phase I clinical trials for HER2+ advanced solid tumors, and some have demonstrated antitumor activity in T-DM1-resistant models in preclinical studies.