JP7660186B2 - Fl118薬物が酸感受性リンカーに結合された複合体及びそれを用いた免疫複合体 - Google Patents
Fl118薬物が酸感受性リンカーに結合された複合体及びそれを用いた免疫複合体 Download PDFInfo
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- JP7660186B2 JP7660186B2 JP2023503070A JP2023503070A JP7660186B2 JP 7660186 B2 JP7660186 B2 JP 7660186B2 JP 2023503070 A JP2023503070 A JP 2023503070A JP 2023503070 A JP2023503070 A JP 2023503070A JP 7660186 B2 JP7660186 B2 JP 7660186B2
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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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/545—Heterocyclic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
- A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
- A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
- A61K47/68037—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a camptothecin [CPT] or derivatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
- A61K47/6849—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a receptor, a cell surface antigen or a cell surface determinant
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
- A61K47/6851—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
- A61K47/6855—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell the tumour determinant being from breast cancer cell
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
-
- 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
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
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- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cell Biology (AREA)
- Oncology (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR20200088005 | 2020-07-16 | ||
| KR10-2020-0088005 | 2020-07-16 | ||
| KR1020210060721A KR102349925B1 (ko) | 2020-07-16 | 2021-05-11 | Fl118 약물을 포함하는 화합물 및 이를 이용한 면역접합체 |
| KR10-2021-0060721 | 2021-05-11 | ||
| PCT/KR2021/009204 WO2022015110A1 (ko) | 2020-07-16 | 2021-07-16 | Fl118 약물이 산 민감성 링커에 연결된 접합체 및 이를 이용한 면역접합체 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2023534292A JP2023534292A (ja) | 2023-08-08 |
| JP2023534292A5 JP2023534292A5 (https=) | 2023-09-28 |
| JPWO2022015110A5 JPWO2022015110A5 (https=) | 2023-09-28 |
| JP7660186B2 true JP7660186B2 (ja) | 2025-04-10 |
Family
ID=79339522
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023503070A Active JP7660186B2 (ja) | 2020-07-16 | 2021-07-16 | Fl118薬物が酸感受性リンカーに結合された複合体及びそれを用いた免疫複合体 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20230270867A1 (https=) |
| EP (1) | EP4183418A4 (https=) |
| JP (1) | JP7660186B2 (https=) |
| KR (3) | KR102349925B1 (https=) |
| CN (1) | CN116075321A (https=) |
| AU (1) | AU2021308834A1 (https=) |
| CA (1) | CA3189462A1 (https=) |
| WO (1) | WO2022015110A1 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN119546346A (zh) * | 2022-05-04 | 2025-02-28 | 匹诺生物股份有限公司 | 与ddx5蛋白结合的喜树碱类药物与酸敏感性接头连接的缀合物及使用该缀合物的免疫缀合物 |
| JP2025523863A (ja) * | 2022-07-11 | 2025-07-25 | ピノットバイオ インコーポレイテッド | Ddx5タンパク質に結合するカンプトセシン誘導体およびそのプロドラッグ |
| KR20240031183A (ko) | 2022-08-30 | 2024-03-07 | 주식회사 피노바이오 | 캄토테신계 약물이, 항원 결합 친화도가 낮은 항체에 링커를 통해 연결된 항체-약물 접합체 |
| KR20250163350A (ko) * | 2023-03-28 | 2025-11-20 | 한서 바이오 엘엘씨 | 리간드-세포 독성 약물 접합체 및 이의 약학적 용도 |
| WO2025170834A1 (en) * | 2024-02-06 | 2025-08-14 | Canget Biotekpharma, Llc | Fl118 complexes for targeting ddx5, ube2t or usp2a |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015148415A2 (en) | 2014-03-26 | 2015-10-01 | Canget Biotekpharma, Llc | Use of the fl118 core chemical structure platform to generate fl118 derivatives for treatment of human disease |
| JP2016534092A (ja) | 2013-07-23 | 2016-11-04 | イミューノメディクス、インコーポレイテッドImmunomedics, Inc. | Cl2aリンカーを有する抗体−sn−38免疫複合体 |
| JP2017036285A (ja) | 2014-01-31 | 2017-02-16 | 第一三共株式会社 | 抗her2抗体−薬物コンジュゲート |
| WO2019236954A1 (en) | 2018-06-07 | 2019-12-12 | Seattle Genetics, Inc. | Camptothecin conjugates |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2632264B1 (en) * | 2010-10-29 | 2019-10-02 | Health Research, Inc. | Novel formulations of water-insoluble chemical compounds and methods of using a formulation of compound fl118 for cancer therapy |
| US10206918B2 (en) * | 2012-12-13 | 2019-02-19 | Immunomedics, Inc. | Efficacy of anti-HLA-DR antiboddy drug conjugate IMMU-140 (hL243-CL2A-SN-38) in HLA-DR positive cancers |
| SI2900277T1 (sl) * | 2012-12-13 | 2022-05-31 | Immunomedics, Inc. | Odmerki imunokonjugatov protiteles in SN-38 za boljšo učinkovitost in zmanjšano toksičnost |
| WO2015012904A2 (en) * | 2012-12-13 | 2015-01-29 | Immunomedics, Inc. | Antibody-sn-38 immunoconjugates with a cl2a linker |
-
2021
- 2021-05-11 KR KR1020210060721A patent/KR102349925B1/ko active Active
- 2021-07-16 US US18/016,331 patent/US20230270867A1/en active Pending
- 2021-07-16 WO PCT/KR2021/009204 patent/WO2022015110A1/ko not_active Ceased
- 2021-07-16 CA CA3189462A patent/CA3189462A1/en active Pending
- 2021-07-16 CN CN202180062303.4A patent/CN116075321A/zh active Pending
- 2021-07-16 KR KR1020210093769A patent/KR20220009916A/ko not_active Ceased
- 2021-07-16 AU AU2021308834A patent/AU2021308834A1/en not_active Abandoned
- 2021-07-16 JP JP2023503070A patent/JP7660186B2/ja active Active
- 2021-07-16 EP EP21841752.5A patent/EP4183418A4/en active Pending
- 2021-10-15 KR KR1020210137595A patent/KR102857180B1/ko active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2016534092A (ja) | 2013-07-23 | 2016-11-04 | イミューノメディクス、インコーポレイテッドImmunomedics, Inc. | Cl2aリンカーを有する抗体−sn−38免疫複合体 |
| JP2017036285A (ja) | 2014-01-31 | 2017-02-16 | 第一三共株式会社 | 抗her2抗体−薬物コンジュゲート |
| WO2015148415A2 (en) | 2014-03-26 | 2015-10-01 | Canget Biotekpharma, Llc | Use of the fl118 core chemical structure platform to generate fl118 derivatives for treatment of human disease |
| WO2019236954A1 (en) | 2018-06-07 | 2019-12-12 | Seattle Genetics, Inc. | Camptothecin conjugates |
Non-Patent Citations (3)
| Title |
|---|
| FL118, a novel camptothecin analogue, overcomes irinotecan and topotecan resistance in human tumor xenograft models,Am J Transl Res,2015年,7(10),pp.1765-1781,ISSN:1943-8141 |
| Induction of breast cancer resistance protein by the camptothecin derivative DX-8951f is associated with minor reduction of antitumour activity,British Journal of Cancer,2002年,87,pp.665-672 |
| The emergence of trophoblast cell-surface antigen 2 (TROP-2) as a novel cancer target,Oncotarget,2018年,Vol.9,No.48,pp.28989-29006,https://doi.org/10.18632/oncotarget.25615 |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2023534292A (ja) | 2023-08-08 |
| AU2021308834A2 (en) | 2023-10-19 |
| WO2022015110A1 (ko) | 2022-01-20 |
| KR102857180B1 (ko) | 2025-09-09 |
| KR102349925B1 (ko) | 2022-01-12 |
| US20230270867A1 (en) | 2023-08-31 |
| CA3189462A1 (en) | 2022-01-20 |
| KR20220009916A (ko) | 2022-01-25 |
| AU2021308834A1 (en) | 2023-02-16 |
| KR20220009928A (ko) | 2022-01-25 |
| CN116075321A (zh) | 2023-05-05 |
| EP4183418A4 (en) | 2025-02-12 |
| EP4183418A1 (en) | 2023-05-24 |
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