Xiaofan Li, Sihong Zhou, Cristina L Abrahams, Stellanie Krimm, Jennifer Smith, Krishna Bajjuri, Heather T Stephenson, Robert Henningsen, Jeffrey Hanson, Tyler H Heibeck, Daniel Calarese, Cuong Tran, Gang Yin, Ryan L Stafford, Alice Y Yam, Toni Kline, Venita I De Almeida, Aaron K Sato, Mark Lupher, Kristin Bedard, Trevor J Hallam
STRO-002 is a novel homogeneous FolRα targeting antibody drug conjugate (ADC), currently being investigated in the clinic as a treatment for ovarian and endometrial cancers. Here we describe the discovery, optimization, and anti-tumor properties of STRO-002. STRO-002 was generated by conjugation of a novel cleavable 3-aminophenyl hemiasterlin linker-warhead (SC239) to the non-natural amino acid para-azidomethyl-L-phenylalanine (pAMF) incorporated at specific positions within a high affinity anti-FolRα antibody using Sutro's XpressCF+™, which resulted in a homogeneous ADC with a drug-antibody ratio (DAR) of 4...
November 30, 2022: Molecular Cancer Therapeutics