Pavel Strop, Thomas-Toan Tran, Magdalena Dorywalska, Kathy Delaria, Russell Dushin, Oi Kwan Wong, Wei-Hsien Ho, Dahui Zhou, Aidong Wu, Eugenia Kraynov, Laura Aschenbrenner, Bora Han, Christopher J O'Donnell, Jaume Pons, Arvind Rajpal, Dave L Shelton, Shu-Hui Liu
Trop-2, also known as TACSTD2, EGP-1, GA733-1, and M1S1, is frequently expressed on a variety of human carcinomas, and its expression is often associated with poor prognosis of the diseases. However, it is also present on the epithelium of several normal tissues. A comprehensively designed Trop-2-targeting antibody-drug conjugate (ADC), balancing both efficacy and toxicity, is therefore necessary to achieve clinical utility. To this end, we developed a cleavable Trop-2 ADC (RN927C) using a site-specific transglutaminase-mediated conjugation method and a proprietary microtubule inhibitor (MTI) linker-payload, PF-06380101...
November 2016: Molecular Cancer Therapeutics