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NZ766604B2 - Pd-1 agonist antibodies and uses thereof - Google Patents
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NZ766604B2 - Pd-1 agonist antibodies and uses thereof - Google Patents

Pd-1 agonist antibodies and uses thereof Download PDF

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Publication number
NZ766604B2
NZ766604B2 NZ766604A NZ76660419A NZ766604B2 NZ 766604 B2 NZ766604 B2 NZ 766604B2 NZ 766604 A NZ766604 A NZ 766604A NZ 76660419 A NZ76660419 A NZ 76660419A NZ 766604 B2 NZ766604 B2 NZ 766604B2
Authority
NZ
New Zealand
Prior art keywords
antibody
disease
seq
amino acid
acid sequence
Prior art date
Application number
NZ766604A
Other versions
NZ766604A (en
Inventor
Qing Chai
Yiqing Feng
Kristin Paige Newburn
Stephanie Marie Truhlar
Petra Verdino
Pia Pauliina Yachi
Original Assignee
Eli Lilly And Company
Filing date
Publication date
Application filed by Eli Lilly And Company filed Critical Eli Lilly And Company
Priority claimed from PCT/US2019/019076 external-priority patent/WO2019168745A1/en
Publication of NZ766604A publication Critical patent/NZ766604A/en
Publication of NZ766604B2 publication Critical patent/NZ766604B2/en

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    • 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
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or 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
    • 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
    • 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
    • A61K39/39558Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against tumor tissues, cells, antigens
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
    • C07K16/2818Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against CD28 or CD152
    • 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
    • C07K2317/50Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/51Complete heavy chain or Fd fragment, i.e. VH + CH1
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/50Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/515Complete light chain, i.e. VL + CL
    • 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
    • C07K2317/71Decreased effector function due to an Fc-modification
    • 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
    • C07K2317/75Agonist effect on antigen
    • 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

Abstract

The present invention relates to anti-human PD-1 agonist antibodies, and uses thereof for treating autoimmune disorders such as rheumatoid arthritis or for decreasing rejection of transplanted cells and/or tissues. wherein the antibody is defined by 6 CDRS: - HCDR1: KVSGYSLSKYDMS - HCDR2: IIYTSGYTDYAQKFQG - HCDR3: ATGNPYYTNGFNS - LCDR1: QASQSPNNLLA - LCDR2: YGASDLPS - LCDR3: QNNYYVGPVSYA"

Claims (26)

WE CLAIM:
1. An antibody that binds human PD-1, comprising: 1) a heavy chain variable region (HCVR); and 2) a light chain variable region (LCVR), wherein the HCVR 5 comprises a HCDR1, HCDR2, and HCDR3, and the LCVR comprises a LCDR1, LCDR2, and LCDR3, wherein the amino acid sequence of the HCDR1 is SEQ ID NO:5, the amino acid sequence of the HCDR2 is SEQ ID NO:6, and the amino acid sequence of the HCDR3 is SEQ ID NO:7, the amino acid sequence of the LCDR1 is SEQ ID NO:8, the amino acid sequence of the LCDR2 is SEQ ID 10 NO:9, and the amino acid sequence of the LCDR3 is SEQ ID NO:10.
2. The antibody of Claim 1, wherein the antibody is a human PD-1 agonist.
3. The antibody of Claim 1 or Claim 2, wherein the antibody binds to the Fc-gamma receptor (Fc?R) family.
4. The antibody of any one of Claims 1-3, wherein the antibody is an IgG1. 15
5. The antibody of any one of Claims 1-4, wherein the amino acid sequence of the HCVR is SEQ ID NO:3 and the amino acid sequence of the LCVR is SEQ ID NO:4.
6. The antibody of Claim 5 comprising: 1) a HC; and 2) a LC, wherein the amino acid sequence of the HC is SEQ ID NO:1, and the amino acid sequence of the LC 20 is SEQ ID NO:2.
7. The antibody of Claim 6 comprising two HCs and two LCs, wherein the amino acid sequence of each of the HCs is SEQ ID NO:1, and the amino acid sequence of each of the LCs is SEQ ID NO:2.
8. The antibody of any one of Claims 1-7, wherein the antibody is an agonist of 25 human PD-1 as determined in an in vivo model of an autoimmune disorder or transplant rejection.
9. The antibody of Claim 8 wherein the in vivo model is a model for GVHD, solid organ transplantation rejection, vasculitis, SLE, T1DM, MS, GCA, PsO, PsA, RA,
10. IBD, UC, AS, SjS, autoimmune hepatitis, or scleroderma. 30 10. The antibody of Claim 8 wherein the in vivo model is a mouse model for GVHD and/or lupus nephritis.
11. A pharmaceutical composition comprising the antibody of any one of Claims 1- 10, and one or more pharmaceutically acceptable carriers, diluents, or excipients.
12. Use of the antibody of any one of Claims 1-10 in the manufacture of a medicament for the treatment of an autoimmune disease. 5
13. The use of Claim 12, wherein the autoimmune disease is GVHD, solid organ transplantation rejection, vasculitis, lupus nephritis, SLE, T1DM, MS, GCA, PsO, PsA, RA, IBD, UC, AS, SjS, autoimmune hepatitis, scleroderma, celiac disease, Addison's disease, Hashimoto's disease, Graves’ disease, atrophic gastritis/pernicious anemia, acquired hypogonadism/infertility, 10 hypoparathyroidism, Coombs positive-hemolytic anemia, chronic allergic diseases, Crohn’s disease, male or female infertility, Behcet’s, Wegener’s granulomatosis, myocarditis, myositis, PMR, spontaneous abortion, vitiligo, atherosclerosis, autoimmune pancreatitis, bullous pemphigoid, chronic viral infections, or myasthenia gravis. 15
14. The use of Claim 13, wherein the autoimmune disease is GVHD, solid organ transplantation rejection, vasculitis, lupus nephritis, SLE, T1DM, MS, GCA, PsO, PsA, RA, IBD, UC, AS, SjS, autoimmune hepatitis, or scleroderma.
15. The use according to Claim 13, wherein the chronic allergic disease is asthma, hay fever or allergic rhinitis. 20
16. The use of any one of Claims 12-15, wherein the antibody is to be administered in simultaneous, separate, or sequential combination with another therapeutic agent effective for the treatment of an autoimmune disease.
17. The antibody of any one of Claims 1-10, for use in therapy.
18. The antibody of any one of Claims 1-10, for use in treating an autoimmune 25 disease.
19. The antibody for use of Claim 18, wherein the autoimmune disease is GVHD, solid organ transplantation rejection, vasculitis, lupus nephritis, SLE, T1DM, MS, GCA, PsO, PsA, RA, IBD, UC, AS, SjS, autoimmune hepatitis, scleroderma, celiac disease, Addison's disease, Hashimoto's disease, Graves’ disease, atrophic 30 gastritis/pernicious anemia, acquired hypogonadism/infertility, hypoparathyroidism, Coombs positive-hemolytic anemia, chronic allergic diseases, Crohn’s disease, male or female infertility, Behcet’s, Wegener’s granulomatosis, myocarditis, myositis, PMR, spontaneous abortion, vitiligo, atherosclerosis, autoimmune pancreatitis, bullous pemphigoid, chronic viral infections, or myasthenia gravis. 5
20. The antibody for use of Claim 18 wherein the autoimmune disease is GVHD, solid organ transplantation rejection, vasculitis, lupus nephritis, SLE, T1DM, MS, GCA, PsO, PsA, RA, IBD, UC, AS, SjS, autoimmune hepatitis, or scleroderma.
21. The antibody for use of Claim 18, wherein the chronic allergic disease is asthma, hay fever or allergic rhinitis. 10
22. The antibody for use of any one of Claims 18-21 wherein the antibody is to be administered in simultaneous, separate, or sequential combination with another therapeutic agent effective for the treatment of an autoimmune disease.
23. The antibody of any one of Claims 1-10 substantially as herein described and with reference to any example thereof and with or without reference to the figures. 15
24. The pharmaceutical composition of Claim 11 substantially as herein described and with reference to any example thereof and with or without reference to the figures.
25. The use of any one of Claims 12-16 substantially as herein described and with reference to any example thereof and with or without reference to the figures.
26. The antibody for use of any one of Claims 17-22 substantially as herein described 20 and with reference to any example thereof and with or without reference to the figures.
NZ766604A 2019-02-22 Pd-1 agonist antibodies and uses thereof NZ766604B2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862637643P 2018-03-02 2018-03-02
PCT/US2019/019076 WO2019168745A1 (en) 2018-03-02 2019-02-22 Pd-1 agonist antibodies and uses thereof

Publications (2)

Publication Number Publication Date
NZ766604A NZ766604A (en) 2024-10-25
NZ766604B2 true NZ766604B2 (en) 2025-01-28

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