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1. WO2018152634 - EGFR-BINDING AGENTS AND USES THEREOF

Publication Number WO/2018/152634
Publication Date 30.08.2018
International Application No. PCT/CA2018/050202
International Filing Date 22.02.2018
IPC
C07K 16/28 2006.1
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 47/68 2017.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
68the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 49/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
49Preparations for testing in vivo
A61P 35/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
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
A61K 2039/507
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
39Medicinal preparations containing antigens or antibodies
505comprising antibodies
507Comprising a combination of two or more separate antibodies
A61K 47/6849
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
68the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
6835the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
6849the antibody targeting a receptor, a cell surface antigen or a cell surface determinant
A61K 49/0032
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
49Preparations for testing in vivo
001Preparation for luminescence or biological staining
0013Luminescence
0017Fluorescence in vivo
0019characterised by the fluorescent group
0021the fluorescent group being a small organic molecule
0032Methine dyes, e.g. cyanine dyes
A61K 49/0058
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
49Preparations for testing in vivo
001Preparation for luminescence or biological staining
0013Luminescence
0017Fluorescence in vivo
005characterised by the carrier molecule carrying the fluorescent agent
0058Antibodies
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
Applicants
  • UNIVERSITY OF SASKATCHEWAN [CA]/[CA]
  • THE GOVERNING COUNCIL OF THE UNIVERSITY OF TORONTO [CA]/[CA]
Inventors
  • SIDHU, Sachdev
  • MIERSCH, Shane
  • GEYER, Clarence
Agents
  • BERESKIN & PARR LLP/S.E.N.C.R.L., S.R.L.
Priority Data
62/462,17522.02.2017US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) EGFR-BINDING AGENTS AND USES THEREOF
(FR) AGENTS DE LIAISON À L'EGFR ET LEURS UTILISATIONS
Abstract
(EN) An Epidermal Growth Factor Receptor (EGFR, HER1, ErbB1)-binding agent has a heavy chain and a light chain, wherein the dimerization loop from EGFR's Domain II is grafted within complementarity determining region 3 (CDR3) of the heavy chain, and the binding agent is affinity matured. The graft directs the binding agent to bind EGFR at its dimerization region, to thereby inhibit EGFR dimerization and activation. In another embodiment, an EGFR-binding agent is panned out of Library F, a Fab library. The binding agents are for detecting and/or quantifying EGFR expression, for targeting EGFR-expressing cells, and for decreasing levels of EGFR in EGFR-expressing cells.
(FR) La présente invention concerne un agent de liaison au récepteur du facteur de croissance épidermique (EGFR, HER1, ErbB1) présentant une chaîne lourde et une chaîne légère, la boucle de dimérisation du domaine II de l'EGFR étant greffée dans la région 3 déterminant la complémentarité (CDR3) de la chaîne lourde, et l'agent de liaison étant à maturation par affinité. Selon l'invention, la greffe dirige l'agent de liaison pour se lier à l'EGFR au niveau de sa région de dimérisation, pour ainsi inhiber la dimérisation et l'activation de l'EGFR. Selon un autre mode de réalisation de l'invention, un agent de liaison à l'EGFR est extrait de la banque F, une banque Fab. Les agents de liaison de l'invention sont destinés à détecter et/ou à quantifier l'expression d'EGFR, à cibler des cellules exprimant EGFR, et à diminuer les taux d'EGFR dans des cellules exprimant l'EGFR.
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