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NZ777273B2 - Factor XI antibodies and methods of use - Google Patents

Factor XI antibodies and methods of use

Info

Publication number
NZ777273B2
NZ777273B2 NZ777273A NZ77727316A NZ777273B2 NZ 777273 B2 NZ777273 B2 NZ 777273B2 NZ 777273 A NZ777273 A NZ 777273A NZ 77727316 A NZ77727316 A NZ 77727316A NZ 777273 B2 NZ777273 B2 NZ 777273B2
Authority
NZ
New Zealand
Prior art keywords
seq
variable region
chain variable
subject
heavy chain
Prior art date
Application number
NZ777273A
Other versions
NZ777273A (en
Inventor
Jorg Eder
Stefan Ewert
Ulrich Hassiepen
Yasser Khder
Lorenz M Mayr
Samu Melkko
Nikolaus Schiering
Original Assignee
Novartis Ag
Filing date
Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of NZ777273A publication Critical patent/NZ777273A/en
Publication of NZ777273B2 publication Critical patent/NZ777273B2/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K2039/505Medicinal preparations containing antigens or antibodies comprising antibodies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K39/395Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/36Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against blood coagulation factors
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/40Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against enzymes
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/20Immunoglobulins specific features characterized by taxonomic origin
    • C07K2317/21Immunoglobulins specific features characterized by taxonomic origin from primates, e.g. man
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/30Immunoglobulins specific features characterized by aspects of specificity or valency
    • C07K2317/33Crossreactivity, e.g. for species or epitope, or lack of said crossreactivity
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/30Immunoglobulins specific features characterized by aspects of specificity or valency
    • C07K2317/34Identification of a linear epitope shorter than 20 amino acid residues or of a conformational epitope defined by amino acid residues
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/50Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/55Fab or Fab'
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/50Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/56Immunoglobulins specific features characterized by immunoglobulin fragments variable (Fv) region, i.e. VH and/or VL
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/50Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/56Immunoglobulins specific features characterized by immunoglobulin fragments variable (Fv) region, i.e. VH and/or VL
    • C07K2317/565Complementarity determining region [CDR]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/70Immunoglobulins specific features characterized by effect upon binding to a cell or to an antigen
    • C07K2317/76Antagonist effect on antigen, e.g. neutralization or inhibition of binding
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/90Immunoglobulins specific features characterized by (pharmaco)kinetic aspects or by stability of the immunoglobulin
    • C07K2317/92Affinity (KD), association rate (Ka), dissociation rate (Kd) or EC50 value
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09Recombinant DNA-technology
    • C12N15/63Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression

Abstract

The present invention relates to monoclonal antibodies and antigen binding fragments thereof that bind to human Factor XI and activated Factor XI ("Factor XIa"), and pharmaceutical compositions and methods of treatment comprising the same.

Claims (25)

THE CLAIMS DEFINING THE INVENTION ARE AS FOLLOWS:
1. Use of an antibody or antigen-binding fragment thereof in the manufacture of a medicament for the treatment of a thromboembolic disorder in a subject afflicted with or at risk of developing a thromboembolic disorder, wherein the antibody or n-binding fragment thereof is to be administered to the subject at a dose of at least 90 mg, and wherein the antibody or antigen-binding nt thereof comprises: i. a heavy chain variable region CDR1 of SEQ ID NO: 23; a heavy chain variable region CDR2 of SEQ ID NO: 24; a heavy chain variable region CDR3 of SEQ ID NO: 25; a light chain variable region CDR1 of SEQ ID NO: 33; a light chain variable region CDR2 of SEQ ID NO: 34; and a light chain le region CDR3 of SEQ ID NO: 35; ii. a heavy chain variable region CDR1 of SEQ ID NO: 26; a heavy chain variable region CDR2 of SEQ ID NO: 27; a heavy chain variable region CDR3 of SEQ ID NO: 28; a light chain variable region CDR1 of SEQ ID NO: 36; a light chain variable region CDR2 of SEQ ID NO: 37; and a light chain variable region CDR3 of SEQ ID NO: 38; iii. a heavy chain variable region CDR1 of SEQ ID NO: 43; a heavy chain variable region CDR2 of SEQ ID NO: 44; a heavy chain variable region CDR3 of SEQ ID NO: 45; a light chain variable region CDR1 of SEQ ID NO: 47; a light chain variable region CDR2 of SEQ ID NO: 37; and a light chain variable region CDR3 of SEQ ID NO: 15; or iv. a heavy chain variable region CDR1 of SEQ ID NO: 46; a heavy chain variable region CDR2 of SEQ ID NO: 4; a heavy chain variable region CDR3 of SEQ ID NO: 5; a light chain variable region CDR1 of SEQ ID NO: 33; a light chain variable region CDR2 of SEQ ID NO: 14; and a light chain variable region CDR3 of SEQ ID NO: 15.
2. The use of claim 1, wherein: (i) the antibody or antigen-binding fragment thereof comprises a variable region heavy chain of SEQ ID NO: 9 and a variable region light chain ce of SEQ ID NO: (ii) the dy or antigen-binding nt thereof comprises a variable region heavy chain of SEQ ID NO: 29 and a variable region light chain sequence of SEQ ID NO: (iii) the antibody comprises a heavy chain sing the amino acid sequence of SEQ ID NO: 31 and a light chain comprising the amino acid sequence of SEQ ID NO: 41; (iv) the antibody comprises a heavy chain comprising the amino acid sequence of SEQ ID NO: 11 and a light chain comprising the amino acid sequence of SEQ ID NO: 21.
3. The use of claim 2, wherein the dy comprises D265A and P329A substitutions in the Fc domain.
4. The use of any one of claims 1-3, wherein the subject is afflicted with or at risk of developing a thromboembolic disorder ed from the group consisting of: venous thromboembolism, paroxysmal atrial fibrillation or atrial r, stroke associated with atrial fibrillation or atrial flutter, deep vein thrombosis (DVT), cancer, transient ischemic attack, severe protein S deficiency, thromboembolic stroke, ischemic stroke, systemic embolism, and myocardial infarction.
5. The use of any one of claims 1-4, wherein the subject is afflicted with one or more of stroke associated with atrial lation and deep vein thrombosis.
6. The use of any one of claims 1-5, wherein the subject is afflicted with stroke associated with atrial fibrillation or atrial flutter.
7. The use of claim 6, wherein the atrial fibrillation or atrial flutter is paroxysmal atrial fibrillation (PAF).
8. The use of any one of claims 1-4, wherein the subject is afflicted with or at risk of developing venous thromboembolism.
9. The use of any one of claims 1-5, n the subject is afflicted with or at risk of developing deep vein thrombosis (DVT).
10. The use of claim 8 or 9, the treatment further comprising measuring efficacy by incidence of DVT occurrence.
11. The use of any one of claims 1-10, wherein the subject is at high risk for bleeding.
12. The use of any one of claims 1-4 or 8-11, wherein the subject has undergone a medical procedure ed from the group ting of knee replacement surgery, hip replacement y, orthopedic surgery, ker installation, catheter installation, thoracic surgery, and abdominal surgery.
13. The use of claim 12, wherein the medical procedure is knee replacement surgery.
14. The use of any one of claims 1-7, wherein the subject at risk is ted with one or more of hypertension, congestive heart failure, left ventricular hypertrophy, and diabetes mellitus.
15. The use of any one of claims 1-14, the treatment further comprising evaluating efficacy of the antibody or antigen-binding fragment f by one or more biomarkers selected from the group consisting of free Factor XI, total Factor XI, Factor XI coagulation ty, ted l thromboplastin time, and D-dimer.
16. The use of any one of claims 1-15, the treatment further comprising evaluating adverse events to the antibody or n-binding fragment thereof by measuring bleeding events and/or the presence of rug antibodies.
17. The use of claim 16, the treatment further comprising applying one or more of the following to the t experiencing an adverse event, wherein the adverse event is a bleeding event: (i) fluid replacement using colloids, crystalloids, human plasma, or plasma proteins, such as albumin; (ii) transfusion with packed red blood or whole blood; or (iii) administration of fresh frozen plasma (FFP), prothrombin complex trates (PCC), or activated PCC (APCC), such as factor VIII inhibitor and/or recombinant activated factor VII.
18. The use of any one of claims 1-17, the treatment further comprising administration to the subject afflicted with or at risk of developing a thromboembolic disorder an effective amount of a statin therapy.
19. The use of any one of claims 1-18, wherein a dose of about 150 mg of the antibody or antigen-binding fragment thereof is to be administered to the subject.
20. The use of any one of claims 1-19, wherein the antibody or antigen-binding fragment thereof is to be stered to the subject subcutaneously or intravenously.
21. The use of any one of claims 1-20, wherein the antibody or antigen-binding fragment thereof is to be administered to the subject once a month.
22. The use of any one of claims 1-21, n the dy or antigen-binding fragment thereof is to be administered to the subject in a pharmaceutical composition further comprising sucrose, a polysorbate, L-histidine, and histidine HCl monohydrate.
23. The use of claim 22, wherein the pharmaceutical ition is at a pH of about 5.5.
24. The use of any one of claims 1-23, wherein the antibody or antigen-binding fragment thereof is an anti-Factor XI (FXI) and/or anti-activated Factor XI (FXIa) antibody or antigen-binding fragment thereof.
25. The use of claim 1, substantially as herein described with nce to any one of the examples and/or
NZ777273A 2016-06-24 Factor XI antibodies and methods of use NZ777273B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562184955P 2015-06-26 2015-06-26
US201662341568P 2016-05-25 2016-05-25
NZ738480A NZ738480B2 (en) 2016-06-24 Factor xi antibodies and methods of use

Publications (2)

Publication Number Publication Date
NZ777273A NZ777273A (en) 2025-05-30
NZ777273B2 true NZ777273B2 (en) 2025-09-02

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