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NZ739493B2 - Pd-1-binding molecules and methods of use thereof - Google Patents
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NZ739493B2 - Pd-1-binding molecules and methods of use thereof - Google Patents

Pd-1-binding molecules and methods of use thereof Download PDF

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Publication number
NZ739493B2
NZ739493B2 NZ739493A NZ73949316A NZ739493B2 NZ 739493 B2 NZ739493 B2 NZ 739493B2 NZ 739493 A NZ739493 A NZ 739493A NZ 73949316 A NZ73949316 A NZ 73949316A NZ 739493 B2 NZ739493 B2 NZ 739493B2
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Prior art keywords
cancer
domain
human
pdbinding
seq
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NZ739493A
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NZ739493A (en
Inventor
Ezio Bonvini
Leslie S Johnson
Scott Koenig
Motte Mohs Ross La
Paul A Moore
Kalpana Shah
Douglas H Smith
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Macrogenics Inc
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Publication date
Application filed by Macrogenics Inc filed Critical Macrogenics Inc
Priority to NZ778489A priority Critical patent/NZ778489B2/en
Priority to NZ778490A priority patent/NZ778490A/en
Priority claimed from PCT/US2016/044430 external-priority patent/WO2017019846A1/en
Publication of NZ739493A publication Critical patent/NZ739493A/en
Publication of NZ739493B2 publication Critical patent/NZ739493B2/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
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    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A61P31/04Antibacterial agents
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    • A61P31/10Antimycotics
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
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    • A61P37/02Immunomodulators
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    • A61P5/18Drugs for disorders of the endocrine system of the parathyroid hormones
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    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • 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
    • 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
    • C07K2317/20Immunoglobulins specific features characterized by taxonomic origin
    • C07K2317/24Immunoglobulins specific features characterized by taxonomic origin containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/30Immunoglobulins specific features characterized by aspects of specificity or valency
    • C07K2317/31Immunoglobulins specific features characterized by aspects of specificity or valency multispecific
    • 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
    • C07K2317/52Constant or Fc region; Isotype
    • 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
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/90Immunoglobulins specific features characterized by (pharmaco)kinetic aspects or by stability of the immunoglobulin
    • C07K2317/94Stability, e.g. half-life, pH, temperature or enzyme-resistance
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/705Assays involving receptors, cell surface antigens or cell surface determinants
    • G01N2333/70503Immunoglobulin superfamily, e.g. VCAMs, PECAM, LFA-3
    • G01N2333/70521CD28, CD152
    • G01N33/574
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/577Immunoassay; Biospecific binding assay; Materials therefor involving monoclonal antibodies binding reaction mechanisms characterised by the use of monoclonal antibodies
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/68Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
    • G01N33/6872Intracellular protein regulatory factors and their receptors, e.g. including ion channels

Abstract

The present invention is directed to selected anti-PD-1 antibodies capable of binding to both cynomolgus monkey PD-1 and to human PD-1 : PD-1 mAb 1, PD-1 mAb 2, PD-1 mAb 3, PD-1 mAb 4, PD-1 mAb 5, PD-1 mAb 6, PD-1 mAb 7, PD-1 mAb 8, PD-1 mAb 9, PD-1 mAb 10, PD-1 mAb 11, PD-1 mAb 12, PD-1 mAb 13, PD-1 mAb 14, or PD-1 mAb 15, and to humanized and chimeric versions of such antibodies. The invention additionally pertains to PD-1 -binding molecules that comprise PD-1 binding fragments of such anti-PD-1 antibodies, immunocongugates, and to bispecific molecules, including diabodies, BiTEs, bispecific antibodies, etc., that comprise (i) such PD-1 -binding fragments, and (ii) a domain capable of binding an epitope of a molecule involved in regulating an immune check point present on the surface of an immune cells. The present invention also pertains to methods of using molecules that bind PD-1 for stimulating immune responses, as well as methods of detecting PD-1.

Claims (30)

What Is Claimed Is:
1. An anti-human PDbinding monospecific monoclonal antibody that comprises a Variable Heavy Chain Domain and a Variable Light Chain Domain, wherein: said Variable Heavy Chain Domain comprises a CDRH1 , a CDRH2 Domain and a CDRH3 Domain, and said Variable Light Chain Domain comprises a CDRL1 Domain, a CDRL2 Domain, and a CDRL3 Domain, wherein: (1) the CDRH1 Domain, CDRH2 Domain, and CDRH3 Domain are the Heavy Chain CDRs of hPD-1 mAb 7(1.2), and respectively comprise the amino acid sequences: SEQ ID NO:139, SEQ ID , and SEQ ID NO:141; and (2) the CDRL1 Domain, CDRL2 Domain, and CDRL3 Domain are the Light Chain CDRs of hPD-1 mAb 7(1.2), and respectively comprise the amino acid sequences: SEQ ID NO:157, SEQ ID NO:145, and SEQ ID NO:146.
2. The anti-human PDbinding monospecific monoclonal dy of claim 1, wherein said antibody comprises a Heavy Chain Variable Domain that comprises the amino acid ce of SEQ ID NO:147 or SEQ ID NO:149.
3. The anti-human PDbinding monospecific monoclonal antibody of any one of claims 1 or 2, wherein said antibody comprises a Light Chain Variable Domain that comprises the amino acid ce of SEQ ID .
4. The anti-human PDbinding monospecific monoclonal dy of any one of claims 1- 3, wherein said antibody comprises a Heavy Chain Variable Domain that comprises the amino acid sequence of SEQ ID NO:147.
5. The anti-human PDantibody of any one of claims 1-3, wherein said antibody comprises a Heavy Chain Variable Domain having the amino acid sequence of SEQ ID NO:147, and wherein said antibody comprises a Light Chain Variable Domain having the amino acid sequence of SEQ ID NO:153.
6. The anti-human PDbinding monospecific monoclonal dy of any one of claims 1- 5, wherein said antibody comprises an Fc Region.
7. The anti-human inding monospecific onal dy of claim 6, n said Fc Region, is of the IgG1, IgG2, IgG3, or IgG4 isotype.
8. The anti-human PDbinding monospecific monoclonal antibody of claim 7, wherein said antibody further comprises a Hinge Domain.
9. The anti-human PDbinding monospecific monoclonal antibody of claim 8, wherein said Fc Region and said Hinge Doman are of the IgG4 isotype, and wherein said Hinge Domain ses a stabilizing mutation.
10. The anti-human PDbinding monospecific monoclonal antibody of any one of claims 6- 8, wherein said antibody comprises SEQ ID NOs: 264 and 265.
11. The anti-human PDbinding monospecific monoclonal antibody of any one of claims 6- 8, wherein said dy comprises SEQ ID NOs: 264 and 266.
12. The anti-human PDbinding monospecific monoclonal antibody of any one of claims 6- 9, wherein said Fc Region is a variant Fc Region that comprises: (a) one or more amino acid modifications that reduces the affinity of the variant Fc Region for an Fc?R; and/or (b) one or more amino acid modifications that enhances the serum half-life of the variant Fc Region.
13. The anti-human PDbinding monospecific monoclonal dy of claim 12, wherein said modifications that reduce the affinity of the variant Fc Region for an Fc?R comprise the substitution of L234A; L235A; or L234A and L235A, n said numbering is that of the EU index as in Kabat.
14. The anti-human PDbinding monospecific monoclonal antibody of claims 12 or 13, wherein said modifications that that enhance the serum ife of the variant Fc Region comprise the substitution of M252Y; M252Y and S254T; M252Y and T256E; M252Y, S254T and T256E; or K288D and H435K, wherein said numbering is that of the EU index as in Kabat.
15. The anti-human PDbinding monospecific monoclonal antibody of any one of claims 1- 14, wherein said antibody is detectably labeled and is used in the ion of PD-1.
16. A composition comprising the anti-human PDbinding monospecific monoclonal antibody of any one of claims 1-14 and a pharmaceutically acceptable r.
17. Use of the anti-human PDbinding monospecific monoclonal antibody of any one of claims 1-14 or the composition of claim 16 for the manufacture of a ment for the treatment of a .
18. The use of claim 17, wherein said cancer is characterized by the presence of a cancer cell selected from the group consisting of a cell of: an adrenal gland tumor, an AIDS-associated cancer, an alveolar soft part sarcoma, an astrocytic tumor, bladder cancer, bone cancer, a brain and spinal cord cancer, a metastatic brain tumor, a breast cancer, a carotid body tumors, a cervical cancer, a chondrosarcoma, a chordoma, a chromophobe renal cell carcinoma, a clear cell carcinoma, a colon cancer, a colorectal cancer, a cutaneous benign fibrous histiocytoma, a desmoplastic small round cell tumor, an ependymoma, a Ewing’s tumor, an extraskeletal myxoid chondrosarcoma, a fibrogenesis imperfecta ossium, a fibrous dysplasia of the bone, a gallbladder or bile duct cancer, gastric cancer, a gestational trophoblastic disease, a germ cell tumor, a head and neck cancer, hepatocellular carcinoma, an islet cell tumor, a Kaposi’s Sarcoma, a kidney cancer, a leukemia, a /benign tous tumor, a liposarcoma/malignant tous tumor, a liver cancer, a lymphoma, a lung cancer, a medulloblastoma, a ma, a meningioma, a multiple endocrine sia, a multiple myeloma, a ysplastic syndrome, a neuroblastoma, a neuroendocrine tumors, an ovarian cancer, a pancreatic cancer, a ary thyroid carcinoma, a parathyroid tumor, a pediatric cancer, a peripheral nerve sheath tumor, a phaeochromocytoma, a pituitary tumor, a prostate cancer, a posterious uveal melanoma, a rare hematologic er, a renal metastatic cancer, a rhabdoid tumor, a rhabdomyosarcoma, a sarcoma, a skin cancer, a soft-tissue sarcoma, a us cell cancer, a stomach cancer, a synovial sarcoma, a testicular cancer, a thymic carcinoma, a thymoma, a thyroid metastatic cancer, and a uterine cancer.
19. The use of claim 17, wherein the cancer is a e .
20. The use of claim 17, wherein the cancer is a squamous cell cancer.
21. The use of claim 17, wherein the cancer is glioma.
22. The use of claim 17, wherein the cancer is a cervical .
23. The use of claim 17, wherein the cancer is kidney cancer.
24. The use of claim 17, wherein the cancer is a lung cancer.
25. The use of claim 17, wherein the cancer is non-small cell lung cancer.
26. The use of claim 17, wherein the cancer is a head and neck cancer.
27. The use of claim 17, wherein the cancer is a renal metastatic cancer.
28. The use of claim 17, wherein the cancer is a chromophobe renal cell carcinoma.
29. The use of claim 17, wherein the cancer is a skin cancer.
30. A nucleic acid expression vector encoding the anti-human PDbinding monospecific monoclonal antibody of any one of claims 1-14. W0 20172’019846 K—coil {or E-coii} Poiypeptide Chain 1 cool-1Wc Linker 12 Linker 2 Poiypeptide Chain 2 COOH WWI: C"1' (or ) Assembled Diabody W0 019846 Polypeptide Chain 1 \
NZ739493A 2015-07-30 2016-07-28 Pd-1-binding molecules and methods of use thereof NZ739493B2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
NZ778489A NZ778489B2 (en) 2016-07-28 PD-1-binding molecules and methods of use thereof
NZ778490A NZ778490A (en) 2015-07-30 2016-07-28 Pd-1-binding molecules and methods of use thereof

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201562198867P 2015-07-30 2015-07-30
US201562239559P 2015-10-09 2015-10-09
US201562255140P 2015-11-13 2015-11-13
US201662322974P 2016-04-15 2016-04-15
PCT/US2016/044430 WO2017019846A1 (en) 2015-07-30 2016-07-28 Pd-1-binding molecules and methods use thereof

Publications (2)

Publication Number Publication Date
NZ739493A NZ739493A (en) 2024-12-20
NZ739493B2 true NZ739493B2 (en) 2025-03-21

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