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1. WO2020093023 - ANTI-TIM-3 ANTIBODIES

Publication Number WO/2020/093023
Publication Date 07.05.2020
International Application No. PCT/US2019/059555
International Filing Date 01.11.2019
IPC
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07K 16/28 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
16Immunoglobulins, e.g. monoclonal or polyclonal antibodies
18against material from animals or humans
28against receptors, cell surface antigens or cell surface determinants
A61K 39/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
39Medicinal preparations containing antigens or antibodies
CPC
A61K 2039/505
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
39Medicinal preparations containing antigens or antibodies
505comprising antibodies
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07K 16/2803
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
16Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
18against material from animals or humans
28against receptors, cell surface antigens or cell surface determinants
2803against the immunoglobulin superfamily
C07K 2317/732
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
2317Immunoglobulins specific features
70characterized by effect upon binding to a cell or to an antigen
73Inducing cell death, e.g. apoptosis, necrosis or inhibition of cell proliferation
732Antibody-dependent cellular cytotoxicity [ADCC]
C07K 2317/76
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
2317Immunoglobulins specific features
70characterized by effect upon binding to a cell or to an antigen
76Antagonist effect on antigen, e.g. neutralization or inhibition of binding
Applicants
  • MERCK PATENT GMBH [DE]/[DE]
  • ZHANG, Dong [US]/[US] (US)
Inventors
  • ZHANG, Dong
  • ZHAO, Xinyan
  • AN, Qi
  • NANNEMANN, David
  • ZAYNAGEDINOV, Rinat
  • SOOD, Vanita
  • IFFLAND, Christel
Agents
  • GUSTAFSON, Megan, A.
  • ARGENTIERI, Steven, R.
  • ASHRAF, Shovon
  • BRODOWSKI, Michael
  • BUCHMAN, Joshua, J.
Priority Data
62/754,38301.11.2018US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) ANTI-TIM-3 ANTIBODIES
(FR) ANTICORPS ANTI-TIM-3
Abstract
(EN)
The invention is based, in part, upon the discovery of a family of antibodies that specifically bind human T Cell Immunoglobulin and Mucin Domain-3 (TIM-3). The antibodies contain TIM-3 binding sites based on the CDRs of the antibodies. The antibodies can be used as therapeutic agents as a monotherapy or in combination with another therapeutic agent. When used as therapeutic agents, the antibodies can be optimized, e.g., affinity-matured, to improve biochemical and/or biophysical properties and/or to reduce or eliminate immunogenicity, when administered to a human patient. The antibodies inhibit TIM-3 from binding to TIM-3 ligands, e.g., galectin-9, phosphatidylserine (PtdSer) and carcinoembryonic antigen-related cell adhesion molecule 1 (CEACAM1). The disclosed antibodies can be used to inhibit the proliferation of tumor cells in vitro or in vivo. When administered to a human cancer patient or an animal model, the antibodies inhibit or reduce tumor growth in the human patient or animal model.
(FR)
L'invention est basée, en partie, sur la découverte d'une famille d'anticorps qui se lient spécifiquement à l'immunoglobuline des lymphocytes T humains et au domaine de la mucine-3 (TIM-3). Les anticorps contiennent des sites de liaison à TIM-3 sur la base des CDR des anticorps. Les anticorps peuvent être utilisés en tant qu'agents thérapeutiques en tant que monothérapie ou en combinaison avec un autre agent thérapeutique. Lorsqu'ils sont utilisés en tant qu'agents thérapeutiques, les anticorps peuvent être optimisés, par exemple, par affinité-maturation, pour améliorer les propriétés biochimiques et/ou biophysiques et/ou pour réduire ou éliminer l'immunogénicité, lorsqu'ils sont administrés à un patient humain. Les anticorps inhibent la liaison de TIM-3 aux ligands TIM-3, par exemple, la galectine-9, la phosphatidylsérine (PtdSer) et la molécule d'adhésion cellulaire liée à l'antigène carcinoembryonnaire 1 (CEACAM1). Les anticorps décrits peuvent être utilisés pour inhiber la prolifération de cellules tumorales in vitro ou in vivo. Lorsqu'ils sont administrés à un patient humain atteint d'un cancer ou à un modèle animal, les anticorps inhibent ou réduisent la croissance tumorale chez le patient humain ou le modèle animal.
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