CTT2274

CTT2274 is a novel small molecule drug conjugate (SMDC) designed for the targeted treatment of prostate cancer, particularly metastatic castration-resistant prostate cancer. It consists of a prostate-specific membrane antigen (PSMA)-binding scaffold, a biphenyl motif, a pH-sensitive phosphoramidate linker, and the cytotoxic payload monomethyl auristatin E (MMAE). The PSMA-targeting scaffold enables selective binding to PSMA, which is overexpressed on prostate cancer cells. Upon internalization by tumor cells, the pH-sensitive linker releases MMAE intracellularly, minimizing off-target toxicity and side effects associated with free MMAE administration. Preclinical studies have demonstrated that CTT2274 provides sustained tumor suppression and improved survival in mouse models compared to free MMAE or saline controls. The drug is being developed by Cancer Targeted Technology and has received significant grant funding to support IND-enabling studies with first-in-human trials planned for 2026[1][2][3][4][5].