CN111801121B - 在psma靶向癌症成像或放疗期间用于健康组织保护的2-pmpa前药 - Google Patents

在psma靶向癌症成像或放疗期间用于健康组织保护的2-pmpa前药 Download PDF

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CN111801121B
CN111801121B CN201880034447.7A CN201880034447A CN111801121B CN 111801121 B CN111801121 B CN 111801121B CN 201880034447 A CN201880034447 A CN 201880034447A CN 111801121 B CN111801121 B CN 111801121B
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psma
pmpa
group
prodrug
cancer
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CN111801121A (zh
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芭芭拉·斯卢谢尔
迈克尔·内德尔科维奇
拉娜·赖斯
克莱门斯·克拉托齐维尔
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Adaga LLC
Johns Hopkins University
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Adaga LLC
Johns Hopkins University
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/0489—Phosphates or phosphonates, e.g. bone-seeking phosphonates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
    • A61K31/663—Compounds having two or more phosphorus acid groups or esters thereof, e.g. clodronic acid, pamidronic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/664—Amides of phosphorus acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/0402—Organic compounds carboxylic acid carriers, fatty acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/0497—Organic compounds conjugates with a carrier being an organic compounds

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
CN201880034447.7A 2017-04-11 2018-04-11 在psma靶向癌症成像或放疗期间用于健康组织保护的2-pmpa前药 Active CN111801121B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762484219P 2017-04-11 2017-04-11
US62/484,219 2017-04-11
PCT/US2018/027106 WO2018191376A2 (en) 2017-04-11 2018-04-11 Prodrugs of 2-pmpa for healthy tissue protection during psma-targeted cancer imaging or radiotherapy

Publications (2)

Publication Number Publication Date
CN111801121A CN111801121A (zh) 2020-10-20
CN111801121B true CN111801121B (zh) 2023-12-01

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Country Status (10)

Country Link
US (1) US12508271B2 (enExample)
EP (1) EP3609544B1 (enExample)
JP (3) JP2020530007A (enExample)
KR (1) KR102686172B1 (enExample)
CN (1) CN111801121B (enExample)
AU (1) AU2018250609B2 (enExample)
ES (1) ES3021195T3 (enExample)
IL (1) IL269969B2 (enExample)
SG (1) SG11201909513QA (enExample)
WO (1) WO2018191376A2 (enExample)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9951324B2 (en) 2010-02-25 2018-04-24 Purdue Research Foundation PSMA binding ligand-linker conjugates and methods for using
AU2014336638C1 (en) 2013-10-18 2020-09-17 Novartis Ag Labeled inhibitors of prostate specific membrane antigen (PSMA), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer
WO2015073678A1 (en) 2013-11-14 2015-05-21 Endocyte, Inc. Compounds for positron emission tomography
MX2020010813A (es) 2018-04-17 2021-01-08 Endocyte Inc Metodos de tratamiento de cancer.
JP7429688B2 (ja) * 2018-09-21 2024-02-08 エンドサイト・インコーポレイテッド シールド剤およびそれらの使用
EP3972627A4 (en) 2019-05-20 2023-06-21 Endocyte, Inc. Methods for preparing psma conjugates
WO2021202376A1 (en) * 2020-03-30 2021-10-07 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Method for blocking uptake of prostate-specific membrane antigen (psma)-targeted radionuclides by exocrine organs
US20230165980A1 (en) * 2020-04-29 2023-06-01 Novartis Ag Methods for radiolabeling psma binding ligands and their kits
IL297323A (en) * 2020-04-29 2022-12-01 Novartis Ag Methods for radiological labeling of psma-binding ligands and their kits
AU2021352915A1 (en) * 2020-10-01 2023-06-08 Cornell University Methods and compositions for increasing uptake, internalization, and/or retention of small molecule ligands
WO2022106629A1 (en) 2020-11-19 2022-05-27 Novartis Ag Synthesis of prostate specific membrane antigen (psma) ligands
CN113354709B (zh) * 2021-06-03 2023-06-09 江苏华益科技有限公司 一种转移性前列腺癌靶向性药物前体的固相合成方法
EP4536278A4 (en) 2022-06-07 2026-08-12 Actinium Pharmaceuticals Inc CHELETARIANS AND BIFUNCTIONAL CONJUGATES
WO2023239903A1 (en) * 2022-06-09 2023-12-14 Case Western Reserve University Compositions and methods for preventing retention of psma-targeted therapy
AU2024317528A1 (en) 2023-07-31 2026-03-05 Curium Us Llc [177 lu] lutetium-psma it composition and dosimetry, kit, method of making, and method of using thereof
WO2025167998A1 (zh) * 2024-02-06 2025-08-14 北京昌平实验室 膦酸酯骨架的psma靶向偶联物
WO2026120497A1 (en) 2024-12-05 2026-06-11 Novartis Ag Stable radionuclide complex solutions

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009046294A2 (en) * 2007-10-03 2009-04-09 Cornell University Treatment of proliferative disorders using antibodies to psma
WO2016022827A1 (en) * 2014-08-06 2016-02-11 The Johns Hopkins University Prodrugs of prostate specific membrane antigen (psma) inhibitor
WO2016022809A2 (en) * 2014-08-06 2016-02-11 The Johns Hopkins University Methods for treating inflammatory bowel disease using prostate specific membrane antigen (psma) inhibitors

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017530109A (ja) * 2014-09-08 2017-10-12 モレキュラ インサイト ファーマシューティカルズ インコーポレイテッド 前立腺癌についてのｐｓｍａを標的とした放射性核種治療中の臓器の保護

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009046294A2 (en) * 2007-10-03 2009-04-09 Cornell University Treatment of proliferative disorders using antibodies to psma
WO2016022827A1 (en) * 2014-08-06 2016-02-11 The Johns Hopkins University Prodrugs of prostate specific membrane antigen (psma) inhibitor
WO2016022809A2 (en) * 2014-08-06 2016-02-11 The Johns Hopkins University Methods for treating inflammatory bowel disease using prostate specific membrane antigen (psma) inhibitors

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
Discovery of Orally Available Prodrugs of the Glutamate Carboxypeptidase II (GCPII) Inhibitor 2‑Phosphonomethylpentanedioic Acid (2-PMPA);Pavel Majer et al;《J. Med. Chem.》;20160301;第59卷;第2810-2819页 *
PMPA for Nephroprotection in PSMA-Targeted Radionuclide Therapy of Prostate Cancer;Clemens Kratochwil et al;《THE JOURNAL OF NUCLEAR MEDICINE》;20150122;第56卷(第2期);第293-298页 *
Towards Personalized Treatment of Prostate Cancer: PSMA I&T, a Promising Prostate-Specific Membrane Antigen-Targeted Theranostic Agent;Kristell L.S. Chatalic et al;《Theranostics》;20160412;第6卷(第6期);第849-861页 *

Also Published As

Publication number Publication date
JP2020530007A (ja) 2020-10-15
JP2025028897A (ja) 2025-03-05
AU2018250609B2 (en) 2024-05-09
EP3609544C0 (en) 2025-04-09
EP3609544A2 (en) 2020-02-19
CA3059741A1 (en) 2018-10-18
JP2023093545A (ja) 2023-07-04
ES3021195T3 (en) 2025-05-26
WO2018191376A3 (en) 2018-12-27
KR102686172B1 (ko) 2024-07-17
WO2018191376A2 (en) 2018-10-18
KR20200059187A (ko) 2020-05-28
EP3609544B1 (en) 2025-04-09
IL269969B2 (en) 2023-04-01
US12508271B2 (en) 2025-12-30
AU2018250609A1 (en) 2019-10-31
SG11201909513QA (en) 2019-11-28
IL269969A (en) 2022-12-01
EP3609544A4 (en) 2020-12-23
US20200069706A1 (en) 2020-03-05
CN111801121A (zh) 2020-10-20

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