tak-448

TAK-448 (MVT-602), a potent and full KISS1R agonist with an IC50 of 460 pM and an EC50 of 632 pM, has been studied in trials for the treatment of Prostate Cancer, Low Testosterone, Prostatic Neoplasms, and Hypogonadotropic Hypogonadism.

TAK-448 is an investigational oligopeptide analog of kisspeptin and a potent agonist of the GPR54 receptor. In animals, acute TAK-448 administration stimulates LH FSH release, whereas continuous sc exposure rapidly down-regulates the pituitary-gonadal axis, with rapid reduction of T levels in a dose-dependent manner. TAK-448 has exhibited potent antitumor activity in rat androgen-dependent prostate cancer models. Therefore, TAK-448 may be useful in the treatment of PC in humans..

TAK-448 acetate (MVT-602 acetate) 是一种小分子 KISS1R 激动剂，是一种和 kisspeptin 类似的合成肽。TAK-448 acetate 具有抗肿瘤活性，抑制 VCaP 细胞增殖，可用于研究前列腺癌。