123B9-L2-PTX

123B9-L2-PTX is a peptide-drug conjugate comprising the selective EphA2 agonist peptide 123B9 linked via a peptide linker (L2) to paclitaxel (PTX). The drug is designed for targeted cancer therapy, utilizing 123B9's selectivity for the EphA2 receptor, which is overexpressed in several malignancies. Binding to EphA2 triggers receptor activation and tyrosine phosphorylation, resulting in receptor internalization and promotion of cytotoxic effects via paclitaxel delivery. In preclinical models, especially in triple-negative breast cancer and prostate cancer, conjugation of 123B9 (usually in dimeric form) to paclitaxel significantly increased efficacy in reducing circulating tumor cells, inhibiting lung metastasis, and reducing tumor vasculature compared to conventional paclitaxel and Abraxane. The drug demonstrates in vivo stability and is more effective than paclitaxel alone for targeted tumor growth inhibition[1][2][5][6].