Chemical conjugates which comprise oligopeptides, having amino acid sequences that are selectively proteolytically cleaved by free prostate specific antigen (PSA) and known cytotoxic agents are disclosed. The conjugates of the invention are characterized by attachment of the cleavable oligopeptide to the oxygen atom at the 4-position on a vinca drug that has be desacetylated. Such conjugates are useful in the treatment of prostatic cancer and benign prostatic hypertrophy (BPH).
本发明公开了由寡肽组成的
化学共轭物,其
氨基酸序列可被游离的前列腺特异性抗原(P
SA)和已知的细胞毒剂选择性地蛋白
水解。本发明共轭物的特点是将可裂解的低聚肽连接到已去乙酰化的长春花类药物上 4 位的氧原子上。这种共轭物可用于治疗前列腺癌和良性前列腺肥大(BPH)。