EP4704913A2 - Conjugués anticorps-médicament utilisant de nouveaux systèmes lieur-charge utile pour le ciblage amélioré d'antigènes associés au cancer - Google Patents
Conjugués anticorps-médicament utilisant de nouveaux systèmes lieur-charge utile pour le ciblage amélioré d'antigènes associés au cancerInfo
- Publication number
- EP4704913A2 EP4704913A2 EP24725410.5A EP24725410A EP4704913A2 EP 4704913 A2 EP4704913 A2 EP 4704913A2 EP 24725410 A EP24725410 A EP 24725410A EP 4704913 A2 EP4704913 A2 EP 4704913A2
- Authority
- EP
- European Patent Office
- Prior art keywords
- seq
- paired
- antibody
- cdr2
- cdr3
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Classifications
-
- 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
- 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
- A61K47/6851—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
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- 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
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
- C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
- C07K16/28—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
- C07K16/2896—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against molecules with a "CD"-designation, not provided for elsewhere
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/20—Immunoglobulins specific features characterized by taxonomic origin
- C07K2317/24—Immunoglobulins specific features characterized by taxonomic origin containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/50—Immunoglobulins specific features characterized by immunoglobulin fragments
- C07K2317/56—Immunoglobulins specific features characterized by immunoglobulin fragments variable (Fv) region, i.e. VH and/or VL
- C07K2317/565—Complementarity determining region [CDR]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/70—Immunoglobulins specific features characterized by effect upon binding to a cell or to an antigen
- C07K2317/77—Internalization into the cell
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/90—Immunoglobulins specific features characterized by (pharmaco)kinetic aspects or by stability of the immunoglobulin
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/90—Immunoglobulins specific features characterized by (pharmaco)kinetic aspects or by stability of the immunoglobulin
- C07K2317/92—Affinity (KD), association rate (Ka), dissociation rate (Kd) or EC50 value
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/90—Immunoglobulins specific features characterized by (pharmaco)kinetic aspects or by stability of the immunoglobulin
- C07K2317/94—Stability, e.g. half-life, pH, temperature or enzyme-resistance
Landscapes
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Immunology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Genetics & Genomics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Cell Biology (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Peptides Or Proteins (AREA)
- Medicinal Preparation (AREA)
- Saccharide Compounds (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Un conjugué anticorps-médicament (ADC) est fourni et comprend un anticorps qui se lie au sialyl Tn (STn) ou à un glycane terminé par un acide sialique à liaison alpha 2,6, conjugué à un médicament par l'intermédiaire d'un lieur, le lieur comprenant un lieur clivable, et le médicament comprenant un agent inhibiteur de croissance qui est l'exatécan, le déruxtécan ou un dérivé correspondant. Le conjugué anticorps-médicament (ADC) de l'invention comprend un lieur clivable par la glucuronidase, par exemple, le lieur comprend une fraction β-glucuronide, telle que représentée dans la formule I : Formule (I). Le conjugué anticorps-médicament (ADC) comprend un lieur qui est lié, ou est modifié pour se lier, au médicament par l'intermédiaire d'une liaison carbamate, ou un lieur qui est lié, ou est modifié pour se lier, au médicament par l'intermédiaire d'une liaison de sel d'ammonium quaternaire. Le conjugué anticorps-médicament (ADC) peut comprendre un lieur qui est PEGylé avec un groupe comprenant du polyéthylène glycol (PEG). De nouveaux lieurs destinés à être utilisés dans des ADC sont également décrits.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB2306706.9A GB202306706D0 (en) | 2023-05-05 | 2023-05-05 | Antibody-drug conjugates employing novel linker-payload systems for enhanced targeting of cancer-associated glycan antigens |
| GBGB2306730.9A GB202306730D0 (en) | 2023-05-06 | 2023-05-06 | Antibody-drug conjugates employing novel linker-payload systems for enhanced targeting of cancer-associated antigens |
| PCT/EP2024/062120 WO2024231224A2 (fr) | 2023-05-05 | 2024-05-02 | Conjugués anticorps-médicament utilisant de nouveaux systèmes lieur-charge utile pour le ciblage amélioré d'antigènes associés au cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EP4704913A2 true EP4704913A2 (fr) | 2026-03-11 |
Family
ID=91076529
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EP24725410.5A Pending EP4704913A2 (fr) | 2023-05-05 | 2024-05-02 | Conjugués anticorps-médicament utilisant de nouveaux systèmes lieur-charge utile pour le ciblage amélioré d'antigènes associés au cancer |
Country Status (4)
| Country | Link |
|---|---|
| EP (1) | EP4704913A2 (fr) |
| JP (1) | JP2026514252A (fr) |
| CN (1) | CN121219019A (fr) |
| WO (1) | WO2024231224A2 (fr) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN121401440B (zh) * | 2025-10-21 | 2026-05-29 | 北京晟日昭阳生物科技有限公司 | 一种靶向治疗胰腺癌的抗体偶联物及其制备方法和应用 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB2183662B (en) | 1985-04-01 | 1989-01-25 | Celltech Ltd | Transformed myeloma cell-line and a process for the expression of a gene coding for a eukaryotic polypeptide employing same |
| PT3057585T (pt) * | 2013-10-15 | 2020-10-21 | Seagen Inc | Fármaco-ligadores peguilados para farmacocinética melhorada de conjugados de fármaco-ligando |
| HRP20241124T1 (hr) * | 2014-09-11 | 2024-11-22 | Seagen Inc. | Ciljana isporuka lijekovitih tvari koje sadrže tercijarni amin |
| US11229708B2 (en) * | 2015-12-04 | 2022-01-25 | Seagen Inc. | Conjugates of quaternized tubulysin compounds |
| WO2018103739A1 (fr) | 2016-12-09 | 2018-06-14 | 凯惠科技发展(上海)有限公司 | Conjugué anticorps-médicament, procédé de préparation, intermédiaire, composition pharmaceutique et utilisation |
| KR20240044544A (ko) * | 2017-03-03 | 2024-04-04 | 씨젠 인크. | 글리칸-상호작용 화합물 및 사용 방법 |
| PT110526B (pt) | 2018-01-26 | 2021-02-04 | Univ Nova De Lisboa | Anticorpo, fragmento funcional ou sonda do mesmo contra antigénios tumorais |
| US20250122282A2 (en) | 2020-09-04 | 2025-04-17 | Merck Patent Gmbh | Anti-ceacam5 antibodies and conjugates and uses thereof |
| EP4331616A4 (fr) | 2021-05-13 | 2026-03-18 | Univ Tsinghua | Conjugué anticorps-médicament, procédé de préparation s'y rapportant et utilisation associée |
| MX2023012920A (es) | 2021-06-02 | 2023-11-13 | Sichuan Kelun Biotech Biopharmaceutical Co Ltd | Conjugado anticuerpo-farmaco y metodo de preparacion y uso del mismo. |
| GB2619976A (en) | 2022-06-24 | 2023-12-27 | Cellmabs S A | Humanised antibodies or functional fragments thereof against tumour antigens |
| CN115160403B (zh) * | 2022-07-05 | 2025-06-27 | 博石丰生命科技(南通)有限公司 | 特异性拓扑异构酶抑制剂和可用于抗体药物偶联物及其制备方法 |
-
2024
- 2024-05-02 WO PCT/EP2024/062120 patent/WO2024231224A2/fr not_active Ceased
- 2024-05-02 EP EP24725410.5A patent/EP4704913A2/fr active Pending
- 2024-05-02 CN CN202480030574.5A patent/CN121219019A/zh active Pending
- 2024-05-02 JP JP2025564147A patent/JP2026514252A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| CN121219019A (zh) | 2025-12-26 |
| JP2026514252A (ja) | 2026-05-07 |
| WO2024231224A3 (fr) | 2024-12-26 |
| WO2024231224A2 (fr) | 2024-11-14 |
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| PUAI | Public reference made under article 153(3) epc to a published international application that has entered the european phase |
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