公开(公告)号：EP4483905A1

公开(公告)日：2025-01-01

申请号：EP23759947.7

申请日：2023-02-21

Applicant: OSAKA UNIVERSITY

Inventor： SHIRAKAMI, Yoshifumi ,  KADONAGA, Yuichiro ,  KANEDA, Kazuko ,  WATABE, Tadashi ,  FUKASE, Koichi ,  SHIMOYAMA, Atsushi ,  ASO, Ayaka ,  YOSHIYA, Taku

IPC: A61K47/54 ,  A61K51/04 ,  A61P35/00 ,  C07D401/12 ,  C07H15/26 ,  C07K5/02

Abstract: It is an object of the present invention to provide drugs that bind specifically to FAPα, are effective in the treatment and diagnosis of tumors or cancers expressing FAPα, for example, in the treatment and diagnosis of solid cancers such as pancreatic cancer, sarcoma, esophageal cancer, lung cancer, breast cancer, prostate cancer, head and neck cancer, ovarian cancer, colon cancer, neuroendocrine tumor, thyroid cancer, uterine cancer, liver cancer and the like (particularly, pancreatic cancer), and have a lower risk of prolonged side effects.
The present invention provides a conjugate comprising a radioactive moiety comprising an aryl group substituted with a radionuclide selected from 211 At, 210 At, 131 I, 125 I, 124 I, 123 I, 77 Br and 76 Br, and a bioactive moiety having an affinity for fibroblast activation protein α (FAPα).