JP2025506357A - 加水分解性マレイミドリンカーを有する抗体コンジュゲート化化学的分解誘導剤及びその方法 - Google Patents

加水分解性マレイミドリンカーを有する抗体コンジュゲート化化学的分解誘導剤及びその方法 Download PDF

Info

Publication number
JP2025506357A
JP2025506357A JP2024544690A JP2024544690A JP2025506357A JP 2025506357 A JP2025506357 A JP 2025506357A JP 2024544690 A JP2024544690 A JP 2024544690A JP 2024544690 A JP2024544690 A JP 2024544690A JP 2025506357 A JP2025506357 A JP 2025506357A
Authority
JP
Japan
Prior art keywords
antibody
cide
alkyl
hydrogen
conjugate
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
Application number
JP2024544690A
Other languages
English (en)
Japanese (ja)
Other versions
JP2025506357A5 (https=
Inventor
ダニエル ピー． サザーリン，
トンルー チャン，
ドックレー， サマー エー． ベーカー
ピーター スコット ドラゴビッチ，
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Genentech Inc
Original Assignee
Genentech Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Genentech Inc filed Critical Genentech Inc
Publication of JP2025506357A publication Critical patent/JP2025506357A/ja
Publication of JP2025506357A5 publication Critical patent/JP2025506357A5/ja
Pending legal-status Critical Current

Links

Images

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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Landscapes

  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP2024544690A 2022-01-26 2023-01-25 加水分解性マレイミドリンカーを有する抗体コンジュゲート化化学的分解誘導剤及びその方法 Pending JP2025506357A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202263303447P 2022-01-26 2022-01-26
US63/303,447 2022-01-26
PCT/US2023/061216 WO2023147328A1 (en) 2022-01-26 2023-01-25 Antibody-conjugated chemical inducers of degradation with hydolysable maleimide linkers and methods thereof

Publications (2)

Publication Number Publication Date
JP2025506357A true JP2025506357A (ja) 2025-03-11
JP2025506357A5 JP2025506357A5 (https=) 2026-02-02

Family

ID=85477901

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2024544690A Pending JP2025506357A (ja) 2022-01-26 2023-01-25 加水分解性マレイミドリンカーを有する抗体コンジュゲート化化学的分解誘導剤及びその方法

Country Status (7)

Country Link
US (1) US20250064968A1 (https=)
EP (1) EP4469090A1 (https=)
JP (1) JP2025506357A (https=)
CN (1) CN118591393A (https=)
AR (1) AR128330A1 (https=)
TW (1) TW202340146A (https=)
WO (1) WO2023147328A1 (https=)

Family Cites Families (76)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4816567A (en) 1983-04-08 1989-03-28 Genentech, Inc. Recombinant immunoglobin preparations
US5807715A (en) 1984-08-27 1998-09-15 The Board Of Trustees Of The Leland Stanford Junior University Methods and transformed mammalian lymphocyte cells for producing functional antigen-binding protein including chimeric immunoglobulin
US4676980A (en) 1985-09-23 1987-06-30 The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Target specific cross-linked heteroantibodies
US6548640B1 (en) 1986-03-27 2003-04-15 Btg International Limited Altered antibodies
EP0368684B2 (en) 1988-11-11 2004-09-29 Medical Research Council Cloning immunoglobulin variable domain sequences.
DE3920358A1 (de) 1989-06-22 1991-01-17 Behringwerke Ag Bispezifische und oligospezifische, mono- und oligovalente antikoerperkonstrukte, ihre herstellung und verwendung
US5091542A (en) * 1990-03-09 1992-02-25 Hybritech Incorporated Tris-maleimido compounds as intermediates in trifunctional antibody synthesis
US5571894A (en) 1991-02-05 1996-11-05 Ciba-Geigy Corporation Recombinant antibodies specific for a growth factor receptor
EP1400536A1 (en) 1991-06-14 2004-03-24 Genentech Inc. Method for making humanized antibodies
GB9114948D0 (en) 1991-07-11 1991-08-28 Pfizer Ltd Process for preparing sertraline intermediates
FI941572A7 (fi) 1991-10-07 1994-05-27 Oncologix Inc Anti-erbB-2-monoklonaalisten vasta-aineiden yhdistelmä ja käyttömenete lmä
WO1993008829A1 (en) 1991-11-04 1993-05-13 The Regents Of The University Of California Compositions that mediate killing of hiv-infected cells
CA2372813A1 (en) 1992-02-06 1993-08-19 L.L. Houston Biosynthetic binding protein for cancer marker
US5731168A (en) 1995-03-01 1998-03-24 Genentech, Inc. Method for making heteromultimeric polypeptides
US5869046A (en) 1995-04-14 1999-02-09 Genentech, Inc. Altered polypeptides with increased half-life
US7033827B2 (en) 1997-02-25 2006-04-25 Corixa Corporation Prostate-specific polynucleotide compositions
US20030185830A1 (en) 1997-02-25 2003-10-02 Corixa Corporation Compositions and methods for the therapy and diagnosis of prostate cancer
US6319688B1 (en) 1997-04-28 2001-11-20 Smithkline Beecham Corporation Polynucleotide encoding human sodium dependent phosphate transporter (IPT-1)
US20030060612A1 (en) 1997-10-28 2003-03-27 Genentech, Inc. Compositions and methods for the diagnosis and treatment of tumor
DK1034298T3 (da) 1997-12-05 2012-01-30 Scripps Research Inst Humanisering af murint antistof
US20020187472A1 (en) 2001-03-09 2002-12-12 Preeti Lal Steap-related protein
US20030064397A1 (en) 1998-05-22 2003-04-03 Incyte Genomics, Inc. Transmembrane protein differentially expressed in prostate and lung tumors
US6949245B1 (en) 1999-06-25 2005-09-27 Genentech, Inc. Humanized anti-ErbB2 antibodies and treatment with anti-ErbB2 antibodies
AU2001243142A1 (en) 2000-02-03 2001-08-14 Hyseq, Inc. Novel nucleic acids and polypeptides
AU2001249411B2 (en) 2000-03-24 2007-02-15 Fahri Saatcioglu Novel prostate-specific or testis-specific nucleic acid molecules, polypeptides,and diagnostic and therapeutic methods
US7279294B2 (en) 2000-04-03 2007-10-09 The United States Of America As Represented By The Secretary, Dept. Of Health And Human Services, Nih Tumor markers in ovarian cancer
JP2003531588A (ja) 2000-04-11 2003-10-28 ジェネンテック・インコーポレーテッド 多価抗体とその用途
CA2420140A1 (en) 2000-08-24 2002-02-28 Genentech, Inc. Compositions and methods for the diagnosis and treatment of tumor
US7208157B2 (en) 2000-09-08 2007-04-24 California Institute Of Technology Proteolysis targeting chimeric pharmaceutical
JP2005504513A (ja) 2001-05-09 2005-02-17 コリクサ コーポレイション 前立腺癌の治療及び診断のための組成物及び方法
WO2002102235A2 (en) 2001-06-18 2002-12-27 Eos Biotechnology Inc. Methods of diagnosis of ovarian cancer, compositions and methods of screening for modulators of ovarian cancer
EP2287186B1 (en) 2001-09-06 2014-12-31 Agensys, Inc. Nucleic acid and corresponding protein entitled STEAP-1 useful in treatment and detection of cancer
WO2003042661A2 (en) 2001-11-13 2003-05-22 Protein Design Labs, Inc. Methods of diagnosis of cancer, compositions and methods of screening for modulators of cancer
WO2003072736A2 (en) 2002-02-21 2003-09-04 Duke University Reagents and treatment methods for autoimmune diseases
US9770517B2 (en) 2002-03-01 2017-09-26 Immunomedics, Inc. Anti-Trop-2 antibody-drug conjugates and uses thereof
EP2258712A3 (en) 2002-03-15 2011-05-04 Multicell Immunotherapeutics, Inc. Compositions and Methods to Initiate or Enhance Antibody and Major-histocompatibility Class I or Class II-restricted T Cell Responses by Using Immunomodulatory, Non-coding RNA Motifs
EP1572916A4 (en) 2002-04-05 2007-05-30 Agensys Inc NUCLEIC ACID AND CORRESPONDING PROTEIN WITH THE NAME 98P4B6, SUITABLE FOR THE TREATMENT AND DETECTION OF CANCER
AU2003242633A1 (en) 2002-06-06 2003-12-22 Molecular Engines Laboratories Dudulin genes, non-human animal model: uses in human hematological disease
JP2004121218A (ja) 2002-08-06 2004-04-22 Jenokkusu Soyaku Kenkyusho:Kk 気管支喘息または慢性閉塞性肺疾患の検査方法
MXPA05001933A (es) 2002-08-19 2005-04-28 Genentech Inc Composiciones y metodos para el diagnostico y tratamiento de tumores.
AU2002951346A0 (en) 2002-09-05 2002-09-26 Garvan Institute Of Medical Research Diagnosis of ovarian cancer
AU2003288918A1 (en) 2002-10-04 2004-05-04 Van Andel Research Institute Molecular sub-classification of kidney tumors and the discovery of new diagnostic markers
WO2004065577A2 (en) 2003-01-14 2004-08-05 Bristol-Myers Squibb Company Polynucleotides and polypeptides associated with the nf-kb pathway
EP1740615B1 (en) 2004-03-31 2014-11-05 Genentech, Inc. Humanized anti-tgf-beta antibodies
JP2009541275A (ja) 2006-06-22 2009-11-26 ノボ・ノルデイスク・エー／エス 二重特異性抗体の生産
WO2008027236A2 (en) 2006-08-30 2008-03-06 Genentech, Inc. Multispecific antibodies
AR065404A1 (es) * 2007-02-21 2009-06-03 Medarex Inc Conjugados farmaco-ligando, los que se unen a citotoxinas potentes, composicion farmaceutica que los contienen y su uso para retardar o detener el crecimiento de un tumor en un mamifero
JP6157046B2 (ja) 2008-01-07 2017-07-05 アムジェン インコーポレイテッド 静電的ステアリング（ｅｌｅｃｔｒｏｓｔａｔｉｃｓｔｅｅｒｉｎｇ）効果を用いた抗体Ｆｃヘテロ二量体分子を作製するための方法
AU2009270988A1 (en) 2008-07-15 2010-01-21 Genentech, Inc. Anthracycline derivative conjugates, process for their preparation and their use as antitumor compounds
KR101860963B1 (ko) 2010-04-23 2018-05-24 제넨테크, 인크. 이종다량체 단백질의 생산
WO2013017705A1 (es) 2011-08-03 2013-02-07 Salvador Moreno Rufino Baltasar Sistema de panel para construccion con retroiluminacion a base de diodos electroluminosos
BR112014009050B1 (pt) 2011-10-14 2022-06-21 Medimmune Limited Conjugado anticorpo-fármaco de pirrolbenzodiazepinas, composição farmacêutica que compreende o mesmo, bem como compostos de pirrolbenzodiazepinas
KR102668696B1 (ko) 2012-01-12 2024-05-29 예일 유니버시티 E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법
WO2013106646A2 (en) 2012-01-12 2013-07-18 Yale University Compounds and methods for the inhibition of vcb e3 ubiquitin ligase
CN104540519B (zh) 2012-05-21 2018-06-01 基因泰克公司 抗Ly6E抗体和免疫缀合物及使用方法
US9492566B2 (en) 2012-12-13 2016-11-15 Immunomedics, Inc. Antibody-drug conjugates and uses thereof
US9089614B2 (en) 2012-12-21 2015-07-28 Bioalliance C.V. Hydrophilic self-immolative linkers and conjugates thereof
BR112016002829A2 (pt) 2013-08-12 2017-09-19 Genentech Inc Composto e processo para preparar o composto de conjugado anticorpo-¿droga, composição farmacêutica, método de tratamento do câncer, kit para o tratamento do câncer, intermediário ligante¿-droga, porção e composto de porção droga de dímero cbi
JP6671292B2 (ja) 2013-12-16 2020-03-25 ジェネンテック， インコーポレイテッド ペプチド模倣化合物及びその抗体−薬物コンジュゲート
KR102337414B1 (ko) 2013-12-16 2021-12-10 제넨테크, 인크. 펩타이드 모방체 화합물 및 이의 항체-약물 컨쥬게이트
WO2015095227A2 (en) 2013-12-16 2015-06-25 Genentech, Inc. Peptidomimetic compounds and antibody-drug conjugates thereof
RU2738833C9 (ru) 2014-04-14 2022-02-28 Арвинас, Оперэйшнз, Инк. Имидные модуляторы протеолиза и способы их применения
KR101957613B1 (ko) 2014-07-07 2019-03-12 쿠엔펭 첸 아릴 아민 치환된 퀸옥살린의 항암 약물로서 용도
WO2016025752A1 (en) * 2014-08-14 2016-02-18 Prolynx Llc Reagents for thiol conjugation and conjugates formed therefrom
US10508151B2 (en) 2014-11-19 2019-12-17 Genentech, Inc. Anti-transferrin receptor antibodies and methods of use
EP3319944A4 (en) 2015-07-10 2019-04-24 Arvinas, Inc. MDM2-BASED MODULATORS OF PROTEOLYSIS AND RELATED USE METHODS
US10772962B2 (en) 2015-08-19 2020-09-15 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
BR112018008918A8 (pt) 2015-11-02 2019-02-26 Univ Yale compostos de quimera proteólise dirigida e métodos para preparação e uso dos mesmos
CN118436801A (zh) 2016-05-20 2024-08-06 豪夫迈·罗氏有限公司 Protac抗体缀合物及其使用方法
US12605458B2 (en) * 2017-06-19 2026-04-21 Systimmune, Inc. Antibody-drug conjugate having acidic self-stabilization junction
US12539292B2 (en) 2018-04-01 2026-02-03 Arvinas Operations, Inc. BRM targeting compounds and associated methods of use
US20190300521A1 (en) 2018-04-01 2019-10-03 Arvinas Operations, Inc. Brm targeting compounds and associated methods of use
JP7708662B2 (ja) 2018-10-24 2025-07-15 エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト コンジュゲート化された化学的分解誘導物質および使用方法
JP7502425B2 (ja) 2019-10-01 2024-06-18 アルヴィナス・オペレーションズ・インコーポレイテッド Ｂｒｍ標的化化合物および関連使用方法
WO2021207291A1 (en) 2020-04-06 2021-10-14 Foghorn Therapeutics Inc. Compounds and uses thereof
PE20231104A1 (es) * 2020-07-21 2023-07-19 Genentech Inc Inductores quimicos de degradacion conjugados con anticuerpo de brm y metodos de estos

Also Published As

Publication number Publication date
TW202340146A (zh) 2023-10-16
US20250064968A1 (en) 2025-02-27
EP4469090A1 (en) 2024-12-04
WO2023147328A1 (en) 2023-08-03
AR128330A1 (es) 2024-04-17
CN118591393A (zh) 2024-09-03

Similar Documents

Publication Publication Date Title
JP7523506B2 (ja) 抗体－薬物コンジュゲート
US20230330249A1 (en) Antibody-conjugated chemical inducers of degradation of brm and methods thereof
JP6355641B2 (ja) スプライソスタチン類似体
CA2852860C (en) Cytotoxic peptides and antibody drug conjugates thereof
AU2019384136B2 (en) Bis-octahydrophenanthrene carboxamide derivatives and protein conjugates thereof for use as LXR agonists
KR20230004453A (ko) 캄프토테신 유도체 및 이의 접합체
TW202016081A (zh) 人類ｓｔｉｎｇ之小分子調節劑、結合物及治療應用
CN113056287A (zh) 缀合的化学降解诱导剂及使用方法
CN104530235A (zh) 一种抑制肿瘤生长的抗体药物衍生物及其制备方法和用途
JP2018123122A (ja) カリケアマイシン誘導体およびその抗体薬物コンジュゲート
JP2019507126A (ja) ツブリシン類似体およびこれらの調製のための方法
US20250073345A1 (en) Antibody-conjugated chemical inducers of degradation and methods thereof
US20250064968A1 (en) Antibody-conjugated chemical inducers of degradation with hydolysable maleimide linkers and methods thereof
RU2852712C1 (ru) Конъюгированные с антителом химические индукторы расщепления brm и связанные с ними способы
HK40088636A (zh) 降解brm的抗体缀合化学诱导剂及其方法
US20250282776A1 (en) Bicyclic TLR7 Agonists and Uses Thereof
WO2024193692A1 (zh) 连接子及其在配体药物偶联物中的应用
KR20260010741A (ko) 링커 화합물 및 리간드-약물 접합체, 이의 제조 방법 및 용도

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20260123

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20260123