Title:
SPECT CONTRAST AGENT FOR FAP-α-SPECIFIC TUMOR DIAGNOSIS
Document Type and Number:
WIPO Patent Application WO/2022/017375
Kind Code:
A1
Abstract:
A SPECT contrast agent for FAP-α-specific tumor diagnosis, said contrast agent being formed using a small molecule FAP-α inhibitor of a modified N-4-quinolinoyl-Gly-(2S)-cyanoPro scaffold as a precursor compound, using 99mTc as a radionuclide, and using N-tris (hydroxymethyl) methylglycine (Tricine) and triphenylphosphine trisulfonate (TPPTS) as synergistic ligands. Compared to current technology, the present contrast agent displays uniquely superior in vivo biodistribution, a higher tumor uptake, a higher tumor/organ uptake ratio, and a more stable coordination attribute, and further exhibits uniquely superior in vivo and in vitro stability; due to a special characteristic of a coordination structure of the present contrast agent, test kit technology using a one-step labeling method can be utilized, and therefor same possesses better drug developability, and is suitable for industrial production and clinical popularization.
Inventors:
JIA BING (CN)
YANG GUANGJIE (CN)
LI XIAODA (CN)
GAO HANNAN (CN)
YANG GUANGJIE (CN)
LI XIAODA (CN)
GAO HANNAN (CN)
Application Number:
PCT/CN2021/107347
Publication Date:
January 27, 2022
Filing Date:
July 20, 2021
Export Citation:
Assignee:
UNIV BEIJING (CN)
International Classes:
A61K51/04; A61K103/10
Domestic Patent References:
| WO2019154886A1 | 2019-08-15 | |||
| WO2018222987A1 | 2018-12-06 |
Foreign References:
| CN111991570A | 2020-11-27 | |||
| CN108144072A | 2018-06-12 | |||
| CN106581700A | 2017-04-26 | |||
| CN110743017A | 2020-02-04 | |||
| CN104667306A | 2015-06-03 | |||
| CN111228521A | 2020-06-05 |
Other References:
LINDNER THOMAS, ALTMANN ANNETTE, KRÄMER SUSANNE, KLEIST CHRISTIAN, LOKTEV ANASTASIA, KRATOCHWIL CLEMENS, GIESEL FREDERIK, MIER WAL: "Design and Development of 99m Tc-Labeled FAPI Tracers for SPECT Imaging and 188 Re Therapy", THE JOURNAL OF NUCLEAR MEDICINE, SOCIETY OF NUCLEAR MEDICINE, US, vol. 61, no. 10, 1 October 2020 (2020-10-01), US , pages 1507 - 1513, XP055888991, ISSN: 0161-5505, DOI: 10.2967/jnumed.119.239731
FREDERIK L. GIESEL, CLEMENS KRATOCHWIL, THOMAS LINDNER, MANFRED M. MARSCHALEK, ANASTASIA LOKTEV, WENCKE LEHNERT, JüRGEN DEBUS: "68 Ga-FAPI PET/CT: Biodistribution and Preliminary Dosimetry Estimate of 2 DOTA-Containing FAP-Targeting Agents in Patients with Various Cancers", THE JOURNAL OF NUCLEAR MEDICINE, SOCIETY OF NUCLEAR MEDICINE, US, vol. 60, no. 3, 1 March 2019 (2019-03-01), US , pages 386 - 392, XP055732757, ISSN: 0161-5505, DOI: 10.2967/jnumed.118.215913
FREDERIK L. GIESEL, CLEMENS KRATOCHWIL, THOMAS LINDNER, MANFRED M. MARSCHALEK, ANASTASIA LOKTEV, WENCKE LEHNERT, JüRGEN DEBUS: "68 Ga-FAPI PET/CT: Biodistribution and Preliminary Dosimetry Estimate of 2 DOTA-Containing FAP-Targeting Agents in Patients with Various Cancers", THE JOURNAL OF NUCLEAR MEDICINE, SOCIETY OF NUCLEAR MEDICINE, US, vol. 60, no. 3, 1 March 2019 (2019-03-01), US , pages 386 - 392, XP055732757, ISSN: 0161-5505, DOI: 10.2967/jnumed.118.215913
Attorney, Agent or Firm:
BEIJING ORIGINTELLIGENCE IP LAW FIRM (CN)
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