Title:
RADIOLABELED FAPα-AFFINITY COMPOUND AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/162946
Kind Code:
A1
Abstract:
The purpose of the present invention is to provide a medical agent which specifically binds to FAPα, is 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 tumors, thyroid cancer, uterine cancer, liver cancer, etc. (in particular, pancreatic cancer), and has a lower risk of prolonged side effects. The present invention provides a conjugate comprising: a bioactive part comprising an aryl group substituted with a radionuclide selected from among 211At, 210At, 131I, 125I, 124I, 123I, 77Br, and 76Br; and a bioactive part having affinity to fibroblast activation protein α (FAPα).
Inventors:
SHIRAKAMI YOSHIFUMI (JP)
KADONAGA YUICHIRO (JP)
KANEDA KAZUKO (JP)
WATABE TADASHI (JP)
FUKASE KOICHI (JP)
SHIMOYAMA ATSUSHI (JP)
ASO AYAKA (JP)
YOSHIYA TAKU (JP)
KADONAGA YUICHIRO (JP)
KANEDA KAZUKO (JP)
WATABE TADASHI (JP)
FUKASE KOICHI (JP)
SHIMOYAMA ATSUSHI (JP)
ASO AYAKA (JP)
YOSHIYA TAKU (JP)
Application Number:
PCT/JP2023/006110
Publication Date:
August 31, 2023
Filing Date:
February 21, 2023
Export Citation:
Assignee:
UNIV OSAKA (JP)
International Classes:
A61K47/54; A61K51/04; A61P35/00; C07D401/12; C07H15/26; C07K5/02
Domestic Patent References:
| WO2021197519A1 | 2021-10-07 | |||
| WO2019027059A1 | 2019-02-07 |
Foreign References:
| CN112023064A | 2020-12-04 | |||
| JP2021512949A | 2021-05-20 | |||
| JP2021500373A | 2021-01-07 |
Other References:
MA HUAN; LI FEIZE; SHEN GUOHUA; PAN LILI; LIU WEIHAO; LIANG RANXI; LAN TU; YANG YUANYOU; YANG JIJUN; LIAO JIALI; LIU NING: "In vitro and in vivo evaluation of 211At-labeled fibroblast activation protein inhibitor for glioma treatment", BIOORGANIC & MEDICINAL CHEMISTRY, ELSEVIER, AMSTERDAM, NL, vol. 55, 5 January 2022 (2022-01-05), AMSTERDAM, NL, pages 116600, XP086924678, ISSN: 0968-0896, DOI: 10.1016/j.bmc.2021.116600
MA HUAN, LI FEIZE, SHEN GUOHUA, CAI HUAWEI, LIU WEIHAO, LAN TU, YANG YUANYOU, YANG JIJUN, LIAO JIALI, LIU NING: "Synthesis and Preliminary Evaluation of 131 I-Labeled FAPI Tracers for Cancer Theranostics", MOLECULAR PHARMACEUTICS, AMERICAN CHEMICAL SOCIETY, US, vol. 18, no. 11, 1 November 2021 (2021-11-01), US , pages 4179 - 4187, XP093087205, ISSN: 1543-8384, DOI: 10.1021/acs.molpharmaceut.1c00566
MELETTA ROMANA, MüLLER HERDE ADRIENNE, CHIOTELLIS ARISTEIDIS, ISA MALSOR, RANCIC ZORAN, BOREL NICOLE, AMETAMEY SIMON, KRä: "Evaluation of the Radiolabeled Boronic Acid-Based FAP Inhibitor MIP-1232 for Atherosclerotic Plaque Imaging", MOLECULES, SPRINGER VERLAG, BERLIN, DE, vol. 20, no. 2, 1 January 2015 (2015-01-01), DE , pages 2081 - 2099, XP055832871, ISSN: 1433-1373, DOI: 10.3390/molecules20022081
ASO AYAKA, KANEDA-NAKASHIMA KAZUKO, NABETANI HINAKO, KADONAGA YUICHIRO, SHIRAKAMI YOSHIFUMI, WATABE TADASHI, YOSHIYA TAKU, MOCHIZU: "Substrate Study for Dihydroxyboryl Astatine Substitution Reaction with Fibroblast Activation Protein Inhibitor (FAPI)", CHEMISTRY LETTERS, CHEMICAL SOCIETY OF JAPAN,NIPPON KAGAKUKAI, JP, vol. 51, no. 11, 5 November 2022 (2022-11-05), JP , pages 1091 - 1094, XP093087207, ISSN: 0366-7022, DOI: 10.1246/cl.220391
MA HUAN, LI FEIZE, SHEN GUOHUA, CAI HUAWEI, LIU WEIHAO, LAN TU, YANG YUANYOU, YANG JIJUN, LIAO JIALI, LIU NING: "Synthesis and Preliminary Evaluation of 131 I-Labeled FAPI Tracers for Cancer Theranostics", MOLECULAR PHARMACEUTICS, AMERICAN CHEMICAL SOCIETY, US, vol. 18, no. 11, 1 November 2021 (2021-11-01), US , pages 4179 - 4187, XP093087205, ISSN: 1543-8384, DOI: 10.1021/acs.molpharmaceut.1c00566
MELETTA ROMANA, MüLLER HERDE ADRIENNE, CHIOTELLIS ARISTEIDIS, ISA MALSOR, RANCIC ZORAN, BOREL NICOLE, AMETAMEY SIMON, KRä: "Evaluation of the Radiolabeled Boronic Acid-Based FAP Inhibitor MIP-1232 for Atherosclerotic Plaque Imaging", MOLECULES, SPRINGER VERLAG, BERLIN, DE, vol. 20, no. 2, 1 January 2015 (2015-01-01), DE , pages 2081 - 2099, XP055832871, ISSN: 1433-1373, DOI: 10.3390/molecules20022081
ASO AYAKA, KANEDA-NAKASHIMA KAZUKO, NABETANI HINAKO, KADONAGA YUICHIRO, SHIRAKAMI YOSHIFUMI, WATABE TADASHI, YOSHIYA TAKU, MOCHIZU: "Substrate Study for Dihydroxyboryl Astatine Substitution Reaction with Fibroblast Activation Protein Inhibitor (FAPI)", CHEMISTRY LETTERS, CHEMICAL SOCIETY OF JAPAN,NIPPON KAGAKUKAI, JP, vol. 51, no. 11, 5 November 2022 (2022-11-05), JP , pages 1091 - 1094, XP093087207, ISSN: 0366-7022, DOI: 10.1246/cl.220391
Attorney, Agent or Firm:
KAMADA, Mitsunori et al. (JP)
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