Divinylpyrimidine reagents generate antibody–drug conjugates with excellent in vivo efficacy and tolerability

• DOI: 10.1039/d1cc06766d
• Publication Date: 2022-01-13T17:21:17Z
• Authors: Stephen J. Walsh; Soleilmane Omarjee; Friederike M. Dan...; Dominique-Laurent...; Dorentina Bexheti; Lee Mendil; Gemma Cronshaw; Toby Fewster; Charlotte Gregg; Cara Brodie; Jodi L. Miller; Richard Houghton; Jason S. Carroll; David R. Spring
• Keywords: Immunoconjugates; Trastuzumab; Proof of Concept Study; Xenograft Model Antitumor Assays; 01 natural sciences; 3. Good health; 0104 chemical sciences; Chemistry; Mice; Antineoplastic Agents, Immunological; Pyrimidines; Cell Line, Tumor; Animals; Humans; Indicators and Reagents

The development of divinylpyrimidine (DVP) reagents for the synthesis of antibody–drug conjugates (ADCs) with in vivo efficacy and tolerability is reported.