Tigapotide (also known as PCK3145) is a synthetic peptide that is derived from the natural sequence of amino acids of the prostate secretory protein (PSP94), one of three predominant proteins found in human seminal fluid. PSP94 expression in the prostate is downregulated in patients with advanced prostate cancer and believed to be a survival mechanism for the cancer cells. Tigapotide can exert anticancer activity not only on prostate but also on breast and colon cancer cells, possibly through laminin receptor-mediated activation of MEK and ERK1/2 phosphorylation. However, the exact molecular mechanisms of action of Tigapotide against prostate cancer tumor growth and metastasis, and tumor-associated angiogenesis remain poorly understood. In preclinical trials, Tigapotide shows potent anticancer activity and reduces prostate cancer growth in PC3 xenograft mouse model and the Dunning rat R-3327 MLL model. Phase II a clinical trial results with Tigapotide confirmed its therapeutic safety and tolerability for metastatic hormone-refractory prostate cancer. This effect was in part correlated to a marked reduction in the high levels of plasma MMP-9, a gelatinase B enzyme involved in extracellular matrix degradation and tumor invasion, of patients receiving Tigapotide, suggesting a biological effect possibly related to control metastasis.