DXd ADC is a novel ADC therapeutic designed with a potent DNA topoisomerase I inhibitor exatecan delivative. Raludotatug deruxtecan (R-DXd) is an ADC that is structurally composed of anti-CDH6 antibody with DXd-ADC technology. R-DXd demonstrated potent antitumor activity against CDH6-expressing tumors in mice and an acceptable safety profile in cynomolgus monkeys. CDH6 expression is increased in serous-type ovarian cancer and renal cell carcinoma, therefore these findings indicate the potential of R-DXd as a new treatment option for these patients in a clinical setting.

Endocrine therapies are a backbone treatment for estrogen receptor positive (ER+) breast cancer worldwide, however there remains an unmet need for treatments with improved efficacy, combinability, and tolerability. In this paper, Parisian et al. describe the development of palazestrant (OP-1250), a Complete ER Antagonist (CERAN) and Selective ER Degrader (SERD) that demonstrates full antagonism of ERα in vitro and potent tumor stasis or regression of ESR1...

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