Tigapotide

Tigapotide (PCK-3145) is a synthetic 15-mer peptide derived from prostate-secretory protein, and acts as an antineoplastic agent. Tigapotide inhibits tumor growth, experimental bone metastasis, and malignancy-associated hypocalcemia. Tigapotide induces apoptosis in prostate cancer cells and tumors, and suppresses the growth of prostate cancer cells. Tigapotide inhibits the production of parathyroid hormone-related protein (PTHrP) in tumors and plasma. Tigapotide reduces plasma calcium levels in hypercalcemic tumor-bearing rats. Tigapotide is applicable for the research of prostate cancer and malignancy-associated hypercalcemia^[1][2]. In Vitro:Tigapotide causes dose-dependent inhibition of MatLyLu-PTHrP prostate cancer cell growth in in vitro^[2].
Tigapotide induces apoptosis in MatLyLu-PTHrP prostate cancer cells in vitro^[2]. In Vivo:Tigapotide (1-100 μg/kg/day; subcutaneous injection; daily administration; up to 15 days) dose-dependently inhibits the growth of primary prostate tumors in subcutaneous MatLyLu-PTHrP xenografts in male Copenhagen rats, reduces PTHrP levels in tumor tissues and plasma, decreases plasma calcium levels, induces tumor cell apoptosis, significantly delays the progression of hindlimb paralysis caused by prostate cancer bone metastasis in male rats, and reduces tumor burden in their lumbar vertebrae^[2].