EA202092176A1 - 177Lu-DOTA-HYNIC-iPSMA В КАЧЕСТВЕ ТЕРАПЕВТИЧЕСКОГО РАДИОФАРМАЦЕВТИЧЕСКОГО СРЕДСТВА, НАЦЕЛЕННОГО НА ПРОСТАТИЧЕСКИЙ СПЕЦИФИЧЕСКИЙ МЕМБРАННЫЙ АНТИГЕН - Google Patents
177Lu-DOTA-HYNIC-iPSMA В КАЧЕСТВЕ ТЕРАПЕВТИЧЕСКОГО РАДИОФАРМАЦЕВТИЧЕСКОГО СРЕДСТВА, НАЦЕЛЕННОГО НА ПРОСТАТИЧЕСКИЙ СПЕЦИФИЧЕСКИЙ МЕМБРАННЫЙ АНТИГЕНInfo
- Publication number
- EA202092176A1 EA202092176A1 EA202092176A EA202092176A EA202092176A1 EA 202092176 A1 EA202092176 A1 EA 202092176A1 EA 202092176 A EA202092176 A EA 202092176A EA 202092176 A EA202092176 A EA 202092176A EA 202092176 A1 EA202092176 A1 EA 202092176A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- ipsma
- hynic
- dota
- radiopharmaceutical
- specific membrane
- Prior art date
Links
- 239000012217 radiopharmaceutical Substances 0.000 title abstract 5
- 229940127044 therapeutic radiopharmaceutical Drugs 0.000 title abstract 2
- 101710181478 Envelope glycoprotein GP350 Proteins 0.000 title 1
- 102100041003 Glutamate carboxypeptidase 2 Human genes 0.000 abstract 4
- 101000892862 Homo sapiens Glutamate carboxypeptidase 2 Proteins 0.000 abstract 4
- KOUZWQLNUJWNIA-UHFFFAOYSA-N 2-hydrazinylpyridine-3-carboxamide Chemical compound NNC1=NC=CC=C1C(N)=O KOUZWQLNUJWNIA-UHFFFAOYSA-N 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 2
- 229940121896 radiopharmaceutical Drugs 0.000 abstract 2
- 230000002799 radiopharmaceutical effect Effects 0.000 abstract 2
- WDLRUFUQRNWCPK-UHFFFAOYSA-N Tetraxetan Chemical compound OC(=O)CN1CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC1 WDLRUFUQRNWCPK-UHFFFAOYSA-N 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 230000002349 favourable effect Effects 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 238000001727 in vivo Methods 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- OHSVLFRHMCKCQY-NJFSPNSNSA-N lutetium-177 Chemical compound [177Lu] OHSVLFRHMCKCQY-NJFSPNSNSA-N 0.000 abstract 1
- 229920001481 poly(stearyl methacrylate) Polymers 0.000 abstract 1
- 230000003439 radiotherapeutic effect Effects 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 230000008685 targeting Effects 0.000 abstract 1
Classifications
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- 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
- A61K51/041—Heterocyclic compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/003—Compounds containing elements of Groups 3 or 13 of the Periodic Table without C-Metal linkages
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Physics & Mathematics (AREA)
- Optics & Photonics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Medicinal Preparation (AREA)
- Peptides Or Proteins (AREA)
Abstract
Настоящее изобретение относится к новому терапевтическому радиофармацевтическому средству на основе лютеция-177 в качестве ингибитора простатического специфического мембранного антигена (iPSMA), в котором 1,4,7,10-тетраазациклододекано-N,N',N'',N''''-тетрауксусная кислота (DOTA), связанная с гетероциклической молекулой гидразиноникотинамида (HYNIC), образует жесткую химическую структуру, которая минимизирует число конформеров и внутримолекулярных водородных связей, таким образом, приводя к пространственной ориентации активного сайта (Lys(Nal)-NH-CO-NH-Glu) в молекуле, благоприятной для биологического распознавания белком PSMA. Новое радиофармацевтическое средство 177Lu-DOTA-HYNIC-iPSMA аккумулируется с высокой аффинностью in vivo в опухолях, сверхэкспрессирующих белок PSMA, действуя как радиотерапевтическое средство. Задача настоящего изобретения состоит в обеспечении нового радиофармацевтического средства (радиофармацевтического средства, нацеленного на молекулярную мишень) для лечения опухолей со сверхэкспрессией PSMA.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| MX2018003175A MX2018003175A (es) | 2018-03-14 | 2018-03-14 | 177lu-dota-hynic-ipsma como un radiofarmaco terapeutico dirigido al antigeno prostatico especifico de membrana. |
| PCT/MX2019/000025 WO2019177449A1 (es) | 2018-03-14 | 2019-03-07 | 177lu-dota-hynic-ipsma como un radiofármaco terapéutico dirigido al antígeno prostático específico de membrana |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EA202092176A1 true EA202092176A1 (ru) | 2021-02-24 |
Family
ID=67907935
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA202092176A EA202092176A1 (ru) | 2018-03-14 | 2019-03-07 | 177Lu-DOTA-HYNIC-iPSMA В КАЧЕСТВЕ ТЕРАПЕВТИЧЕСКОГО РАДИОФАРМАЦЕВТИЧЕСКОГО СРЕДСТВА, НАЦЕЛЕННОГО НА ПРОСТАТИЧЕСКИЙ СПЕЦИФИЧЕСКИЙ МЕМБРАННЫЙ АНТИГЕН |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US12128114B2 (ru) |
| EP (1) | EP3766893B1 (ru) |
| CN (1) | CN112074526B (ru) |
| BR (1) | BR112020018155A2 (ru) |
| CA (1) | CA3093819A1 (ru) |
| EA (1) | EA202092176A1 (ru) |
| ES (1) | ES2960729T3 (ru) |
| MA (1) | MA52029A (ru) |
| MX (1) | MX2018003175A (ru) |
| WO (1) | WO2019177449A1 (ru) |
| ZA (1) | ZA202005600B (ru) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2799325C2 (ru) * | 2022-12-19 | 2023-07-04 | Федеральное государственное бюджетное учреждение "Национальный медицинский исследовательский центр радиологии" Министерства здравоохранения Российской Федерации (ФГБУ "НМИЦ радиологии" Минздрава России) | ЛИОФИЛИЗАТ ДЛЯ ПОЛУЧЕНИЯ ДИАГНОСТИЧЕСКОГО РАДИОФАРМАЦЕВТИЧЕСКОГО ЛЕКАРСТВЕННОГО ПРЕПАРАТА НА ОСНОВЕ РАДИОНУКЛИДА 99mTc |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL297423A (en) * | 2020-04-24 | 2022-12-01 | Radiomedix Inc | The composition, kit and method for the diagnosis and treatment of prostate cancer |
| WO2022101352A1 (en) * | 2020-11-12 | 2022-05-19 | Abx Advanced Biochemical Compounds Gmbh | Ligands of prostate specific membrane antigen (psma) containing heteroaromatic linker building blocks |
| CN112851637B (zh) * | 2021-01-22 | 2022-11-18 | 北京瑞达福明科技有限公司 | 一种psma抑制剂、化合物及其制备方法与用途 |
| AU2022227439A1 (en) * | 2021-02-26 | 2023-09-21 | Telix Pharmaceuticals (Innovations) Pty Ltd | Solid phase synthesis of glutamate-urea-lysine derived (gul derived) prostate-specific membrane antigen (psma) targeting conjugates and their use as precursors for therapeutic and / or diagnostic agents |
| CA3212963A1 (en) * | 2021-04-23 | 2022-10-27 | Reinier HERNANDEZ | Psma-targeting ligands with optimal properties for imaging and therapy |
| MX2021005088A (es) * | 2021-04-30 | 2022-11-01 | Instituto Nac De Investigaciones Nucleares | Nanoparticulas radioluminiscentes de sesquioxido de lutecio-177 funcionalizadas con peptidos para imagen optica. |
| CN118852043A (zh) * | 2021-09-03 | 2024-10-29 | 晶核生物医药科技(南京)有限公司 | 一种肽脲素衍生物、含其的药物组合物及其应用 |
| CN115260155B (zh) * | 2022-08-08 | 2023-11-10 | 北京师范大学 | 一种含三唑环和肼基尼古酰胺基的谷氨酸-脲衍生物及其应用 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1896086A1 (en) * | 2005-06-30 | 2008-03-12 | Bristol-Myers Squibb Pharma Company | Hydrazide conjugates as imaging agents |
| MX336322B (es) | 2010-04-08 | 2016-01-12 | Inst Nac De Investigaciones Nucleares | 99mtc-edda/hynic-ggc-aunp-manosa como un nuevo radiofarmaco para la deteccion del ganglio centinela en cancer de mama. |
| KR102210931B1 (ko) | 2013-10-18 | 2021-02-02 | 도이체스 크렙스포르슝스첸트룸 | 전립선 특이적 막 항원（ｐｓｍａ）의 표지된 억제제, 조영제로서의 이의 용도 및 전립선암 치료용 약제 |
| WO2016043793A1 (en) * | 2014-09-15 | 2016-03-24 | Shelterlogic Corp. | Shelter structure and methods of constructing same |
| GB201417067D0 (en) | 2014-09-26 | 2014-11-12 | South African Nuclear Energy | Radiopharmaceutical conjugate |
| IL237525A (en) | 2015-03-03 | 2017-05-29 | Shalom Eli | Method for labeling a prostate-specific membrane antigen with a radioactive isotope |
| US10688200B2 (en) * | 2015-12-31 | 2020-06-23 | Five Eleven Pharma Inc. | Urea-based prostate specific membrane antigen (PSMA) inhibitors for imaging and therapy |
| MX2016008466A (es) | 2016-06-24 | 2017-12-25 | Instituto Nac De Investigaciones Nucleares | 99mtc-edda/hynic-ipsma como un radiofarmaco para la deteccion de la sobre-expresion del antigeno prostatico de membrana. |
| AU2022227439A1 (en) * | 2021-02-26 | 2023-09-21 | Telix Pharmaceuticals (Innovations) Pty Ltd | Solid phase synthesis of glutamate-urea-lysine derived (gul derived) prostate-specific membrane antigen (psma) targeting conjugates and their use as precursors for therapeutic and / or diagnostic agents |
-
2018
- 2018-03-14 MX MX2018003175A patent/MX2018003175A/es unknown
-
2019
- 2019-03-07 MA MA052029A patent/MA52029A/fr unknown
- 2019-03-07 BR BR112020018155-2A patent/BR112020018155A2/pt unknown
- 2019-03-07 CN CN201980029761.0A patent/CN112074526B/zh active Active
- 2019-03-07 WO PCT/MX2019/000025 patent/WO2019177449A1/es unknown
- 2019-03-07 US US16/980,252 patent/US12128114B2/en active Active
- 2019-03-07 EA EA202092176A patent/EA202092176A1/ru unknown
- 2019-03-07 EP EP19768668.6A patent/EP3766893B1/en active Active
- 2019-03-07 CA CA3093819A patent/CA3093819A1/en active Pending
- 2019-03-07 ES ES19768668T patent/ES2960729T3/es active Active
-
2020
- 2020-09-09 ZA ZA2020/05600A patent/ZA202005600B/en unknown
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2799325C2 (ru) * | 2022-12-19 | 2023-07-04 | Федеральное государственное бюджетное учреждение "Национальный медицинский исследовательский центр радиологии" Министерства здравоохранения Российской Федерации (ФГБУ "НМИЦ радиологии" Минздрава России) | ЛИОФИЛИЗАТ ДЛЯ ПОЛУЧЕНИЯ ДИАГНОСТИЧЕСКОГО РАДИОФАРМАЦЕВТИЧЕСКОГО ЛЕКАРСТВЕННОГО ПРЕПАРАТА НА ОСНОВЕ РАДИОНУКЛИДА 99mTc |
Also Published As
| Publication number | Publication date |
|---|---|
| BR112020018155A2 (pt) | 2021-02-02 |
| MA52029A (fr) | 2021-01-20 |
| US20210015949A1 (en) | 2021-01-21 |
| EP3766893C0 (en) | 2023-07-19 |
| EP3766893B1 (en) | 2023-07-19 |
| EP3766893A1 (en) | 2021-01-20 |
| ES2960729T3 (es) | 2024-03-06 |
| MX2018003175A (es) | 2019-09-16 |
| WO2019177449A1 (es) | 2019-09-19 |
| CN112074526A (zh) | 2020-12-11 |
| US12128114B2 (en) | 2024-10-29 |
| CN112074526B (zh) | 2024-02-20 |
| EP3766893A4 (en) | 2022-02-16 |
| ZA202005600B (en) | 2021-08-25 |
| CA3093819A1 (en) | 2019-09-19 |
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