EP4243931A4 - BIFUNCTIONAL ANTAGONISTS OF ACTIVIN/TGF-BETA AND RANKL AND USES THEREOF - Google Patents

BIFUNCTIONAL ANTAGONISTS OF ACTIVIN/TGF-BETA AND RANKL AND USES THEREOF

Info

Publication number
EP4243931A4
EP4243931A4 EP21892613.7A EP21892613A EP4243931A4 EP 4243931 A4 EP4243931 A4 EP 4243931A4 EP 21892613 A EP21892613 A EP 21892613A EP 4243931 A4 EP4243931 A4 EP 4243931A4
Authority
EP
European Patent Office
Prior art keywords
rankl
activin
tgf
bifunctional
antagonists
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
EP21892613.7A
Other languages
German (de)
English (en)
French (fr)
Other versions
EP4243931A1 (en
Inventor
Hq Han
Xiaolan Zhou
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.)
Individual
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of EP4243931A1 publication Critical patent/EP4243931A1/en
Publication of EP4243931A4 publication Critical patent/EP4243931A4/en
Pending legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/1703—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • A61K38/1709—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • C07K16/22—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against growth factors ; against growth regulators
    • 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
    • C07K16/2875—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the NGF/TNF superfamily, e.g. CD70, CD95L, CD153, CD154
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/30—Immunoglobulins specific features characterized by aspects of specificity or valency
    • C07K2317/31—Immunoglobulins specific features characterized by aspects of specificity or valency multispecific
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/60—Immunoglobulins specific features characterized by non-natural combinations of immunoglobulin fragments
    • C07K2317/62—Immunoglobulins specific features characterized by non-natural combinations of immunoglobulin fragments comprising only variable region components
    • C07K2317/622—Single chain antibody (scFv)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/60—Immunoglobulins specific features characterized by non-natural combinations of immunoglobulin fragments
    • C07K2317/64—Immunoglobulins specific features characterized by non-natural combinations of immunoglobulin fragments comprising a combination of variable region and constant region components
    • 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
    • C07K2317/76—Antagonist effect on antigen, e.g. neutralization or inhibition of binding
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Marine Sciences & Fisheries (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Medicinal Preparation (AREA)
EP21892613.7A 2020-11-11 2021-11-05 BIFUNCTIONAL ANTAGONISTS OF ACTIVIN/TGF-BETA AND RANKL AND USES THEREOF Pending EP4243931A4 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063112380P 2020-11-11 2020-11-11
US202063113922P 2020-11-15 2020-11-15
PCT/US2021/058181 WO2022103660A1 (en) 2020-11-11 2021-11-05 Bifunctional antagonists of activin/tgf-beta and rankl and uses thereof

Publications (2)

Publication Number Publication Date
EP4243931A1 EP4243931A1 (en) 2023-09-20
EP4243931A4 true EP4243931A4 (en) 2025-01-01

Family

ID=81601668

Family Applications (1)

Application Number Title Priority Date Filing Date
EP21892613.7A Pending EP4243931A4 (en) 2020-11-11 2021-11-05 BIFUNCTIONAL ANTAGONISTS OF ACTIVIN/TGF-BETA AND RANKL AND USES THEREOF

Country Status (7)

Country Link
EP (1) EP4243931A4 (https=)
JP (1) JP2023548346A (https=)
KR (1) KR20230118573A (https=)
AU (1) AU2021377176A1 (https=)
CA (1) CA3197104A1 (https=)
MX (1) MX2023005565A (https=)
WO (1) WO2022103660A1 (https=)

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010097394A1 (en) * 2009-02-24 2010-09-02 Glaxo Group Limited Multivalent and/or multispecific rankl-binding constructs
WO2014071212A2 (en) * 2012-11-01 2014-05-08 Abbvie Inc. Stable dual variable domain immunoglobulin protein formulations
WO2016039796A2 (en) * 2014-09-12 2016-03-17 Regeneron Pharmaceuticals, Inc. Treatment of fibrodysplasia ossificans progressiva
WO2018009732A1 (en) * 2016-07-08 2018-01-11 Regeneron Pharmaceuticals, Inc. Anti-activin a antibodies and methods of use thereof for treating pulmonary arterial hypertension
WO2018200918A1 (en) * 2017-04-28 2018-11-01 Amgen Inc. Formulations of human anti-rankl antibodies, and methods of using the same
WO2020113274A1 (en) * 2018-12-05 2020-06-11 The Council Of The Queensland Institute Of Medical Research Rank antagonists and uses therefor

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL142900A0 (en) * 1999-09-03 2002-04-21 Amgen Inc Compositions and methods for the prevention or treatment of cancer and bone loss associated with cancer
TR201901929T4 (tr) * 2005-02-08 2019-03-21 Genzyme Corp TGFBeta'ya antikorlar.
CL2007002567A1 (es) * 2006-09-08 2008-02-01 Amgen Inc Proteinas aisladas de enlace a activina a humana.
KR20100058509A (ko) * 2007-07-31 2010-06-03 메디뮨 엘엘씨 다중특이적 에피토프 결합 단백질 및 이의 용도
JP2011526792A (ja) * 2008-07-02 2011-10-20 エマージェント プロダクト デベロップメント シアトル， エルエルシー ＴＮＦ−αアンタゴニスト多重標的結合性タンパク質
EP2826789A1 (en) * 2009-03-19 2015-01-21 Chugai Seiyaku Kabushiki Kaisha Antibody constant region variant
EP3202459B1 (en) * 2009-09-09 2021-04-14 Acceleron Pharma Inc. Actriib antagonists and dosing and uses thereof for treating obesity or type 2 diabetes by regulating body fat content
CA3253628A1 (en) * 2010-03-05 2025-11-29 The Johns Hopkins University Compositions and methods for targeted immunomodulatory antibodies and fusion proteins
AU2012375257B2 (en) * 2012-03-31 2019-09-12 R-Pharm International, Limited Liability Company Osteoprotegerin derived composition and use thereof
UY35148A (es) * 2012-11-21 2014-05-30 Amgen Inc Immunoglobulinas heterodiméricas
JP6594855B2 (ja) * 2013-03-15 2019-10-23 ゼンコア インコーポレイテッド ヘテロ二量体タンパク質
TW201920262A (zh) * 2013-07-30 2019-06-01 美商再生元醫藥公司 抗活化素ａ之抗體及其用途
US10227411B2 (en) * 2015-03-05 2019-03-12 Xencor, Inc. Modulation of T cells with bispecific antibodies and FC fusions
EP3274457A4 (en) * 2015-03-26 2018-08-08 Acceleron Pharma Inc. Follistatin-related fusion proteins and uses thereof
WO2018026742A1 (en) * 2016-08-01 2018-02-08 Askgene Pharma Inc. Novel antibody-albumin-drug conjugates (aadc) and methods for using them
WO2019079762A1 (en) * 2017-10-20 2019-04-25 Children's National Medical Center METHODS OF DISCOVERING ANTIBODIES USING TRANSCRIPTOMES AND COMPOSITIONS DERIVED THEREFROM

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010097394A1 (en) * 2009-02-24 2010-09-02 Glaxo Group Limited Multivalent and/or multispecific rankl-binding constructs
WO2014071212A2 (en) * 2012-11-01 2014-05-08 Abbvie Inc. Stable dual variable domain immunoglobulin protein formulations
WO2016039796A2 (en) * 2014-09-12 2016-03-17 Regeneron Pharmaceuticals, Inc. Treatment of fibrodysplasia ossificans progressiva
WO2018009732A1 (en) * 2016-07-08 2018-01-11 Regeneron Pharmaceuticals, Inc. Anti-activin a antibodies and methods of use thereof for treating pulmonary arterial hypertension
WO2018200918A1 (en) * 2017-04-28 2018-11-01 Amgen Inc. Formulations of human anti-rankl antibodies, and methods of using the same
WO2020113274A1 (en) * 2018-12-05 2020-06-11 The Council Of The Queensland Institute Of Medical Research Rank antagonists and uses therefor

Non-Patent Citations (8)

* Cited by examiner, † Cited by third party
Title
HIYAMA ET AL: "Cross talk between Smad transcription factors and TNF-@a in intervertebral disc degeneration", BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, ELSEVIER, AMSTERDAM NL, vol. 369, no. 2, 26 February 2008 (2008-02-26), pages 679 - 685, XP022551997, ISSN: 0006-291X, DOI: 10.1016/J.BBRC.2008.02.087 *
KUNIHIRO TSUCHIDA ET AL: "Activin signaling as an emerging target for therapeutic interventions", CELL COMMUNICATION AND SIGNALING, vol. 7, no. 1, 1 January 2009 (2009-01-01), pages 15, XP055116810, ISSN: 1478-811X, DOI: 10.1186/1478-811X-7-15 *
OLSEN ODDRUN ELISE ET AL: "Activins as Dual Specificity TGF-[beta] Family Molecules: SMAD-Activation via Activin- and BMP-Type 1 Receptors", BIOMOLECULES, vol. 10, no. 4, 29 March 2020 (2020-03-29), CH, pages 519, XP093200563, ISSN: 2218-273X, DOI: 10.3390/biom10040519 *
See also references of WO2022103660A1 *
SUN HAIBIN ET AL: "TGF-[beta]1/T[beta]RII/Smad3 signaling pathway promotes VEGF expression in oral squamous cell carcinoma tumor-associated macrophages", BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, ELSEVIER, AMSTERDAM NL, vol. 497, no. 2, 17 February 2018 (2018-02-17), pages 583 - 590, XP085355078, ISSN: 0006-291X, DOI: 10.1016/J.BBRC.2018.02.104 *
WANG JUN ET AL: "Engineering and characterization of a humanized antibody targeting TNF-[alpha] and R", BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, ELSEVIER, AMSTERDAM NL, vol. 450, no. 1, 17 June 2014 (2014-06-17), pages 717 - 722, XP029037964, ISSN: 0006-291X, DOI: 10.1016/J.BBRC.2014.06.046 *
YAMADA CHIAKI ET AL: "TGF-[beta] in jaw tumor fluids induces RANKL expression in stromal fibroblasts", INTERNATIONAL JOURNAL OF ONCOLOGY, vol. 49, no. 2, 31 May 2016 (2016-05-31), GR, pages 499 - 508, XP093200272, ISSN: 1019-6439, DOI: 10.3892/ijo.2016.3548 *
YAMANE KENICHI ET AL: "Antagonistic Effects of TNF-[alpha] on TGF-[beta] Signaling Through Down-Regulation of TGF-[beta] Receptor Type II in Human Dermal Fibroblasts", THE JOURNAL OF IMMUNOLOGY, vol. 171, no. 7, 1 October 2003 (2003-10-01), US, pages 3855 - 3862, XP093200228, ISSN: 0022-1767, Retrieved from the Internet <URL:https://watermark.silverchair.com/3855.pdf?token=AQECAHi208BE49Ooan9kkhW_Ercy7Dm3ZL_9Cf3qfKAc485ysgAABbIwggWuBgkqhkiG9w0BBwagggWfMIIFmwIBADCCBZQGCSqGSIb3DQEHATAeBglghkgBZQMEAS4wEQQMTJ8noJwsRn918cfMAgEQgIIFZag1NIJY_zk2IohgVi6oHRERu4DkLR75edBX3x8Pa6ATTBv4zIXUXdHL_pkQVSlGoH18NRGIACOU-oBljVKrplOyEVvRuZL> DOI: 10.4049/jimmunol.171.7.3855 *

Also Published As

Publication number Publication date
AU2021377176A1 (en) 2023-06-22
JP2023548346A (ja) 2023-11-16
KR20230118573A (ko) 2023-08-11
MX2023005565A (es) 2024-02-23
CA3197104A1 (en) 2022-05-19
WO2022103660A1 (en) 2022-05-19
EP4243931A1 (en) 2023-09-20

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