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1. WO2022135200 - ANTIBODY CONJUGATE AND METHOD FOR ENHANCING IMMUNE EFFECT FUNCTION OF ANTIBODY MOLECULE

Publication Number WO/2022/135200
Publication Date 30.06.2022
International Application No. PCT/CN2021/137352
International Filing Date 13.12.2021
IPC
A61K 47/60 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
56the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
59obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
60the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61K 47/54 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
54the modifying agent being an organic compound
A61K 39/44 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
39Medicinal preparations containing antigens or antibodies
395Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
44Antibodies bound to carriers
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 39/44
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
39Medicinal preparations containing antigens or antibodies
395Antibodies
44Antibodies bound to carriers
A61K 47/545
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
54the modifying agent being an organic compound
545Heterocyclic compounds
A61K 47/549
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
54the modifying agent being an organic compound
549Sugars, nucleosides, nucleotides or nucleic acids
A61K 47/60
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
56the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
59obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
60the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
Applicants
  • 江南大学 JIANGNAN UNIVERSITY [CN]/[CN]
Inventors
  • 吴志猛 WU, Zhimeng
  • 洪皓飞 HONG, Haofei
  • 周坤 ZHOU, Kun
  • 周志昉 ZHOU, Zhifang
Agents
  • 无锡承果知识产权代理有限公司 CHENGGUO INTELLECTUAL PROPERTY AGENCY CO., LTD
Priority Data
202011516850.921.12.2020CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) ANTIBODY CONJUGATE AND METHOD FOR ENHANCING IMMUNE EFFECT FUNCTION OF ANTIBODY MOLECULE
(FR) CONJUGUÉ D'ANTICORPS ET PROCÉDÉ D'AMÉLIORATION DE LA FONCTION D'EFFET IMMUNITAIRE DE MOLÉCULE D'ANTICORPS
(ZH) 一种抗体缀合物、增强抗体分子免疫效应功能的方法
Abstract
(EN) An antibody conjugate and a method for enhancing the immune effect function of an antibody molecule. The antibody conjugate is obtained by modifying an antibody molecule with a hapten derivative molecule, and the hapten derivative consists of a hapten, a connecting arm and a coupling domain. According to the invention, the antibody molecule is modified with the hapten derivative by means of a mild, simple and convenient method, such that the obtained antibody conjugate not only retains an excellent affinity level of the original antibody, but can also recruit a corresponding specific natural antibody to tumor cells so as to achieve the purpose of significantly improving the immune effect function of antibodies ADCC, CDC, etc. In addition, the hapten derivative SMCC-PEG 3-Rha is obtained by optimizing the length of the connecting arm. Compared with other reported antibody molecules, the SMCC-PEG 3-Rha modified antibody has a more prominent immune effect function.
(FR) Conjugué d'anticorps et procédé d'amélioration de la fonction d'effet immunitaire d'une molécule d'anticorps. Le conjugué d'anticorps est obtenu par modification d'une molécule d'anticorps avec une molécule de dérivé d'haptène, et le dérivé d'haptène est constitué d'un haptène, d'un bras de liaison et d'un domaine de couplage. Selon l'invention, la molécule d'anticorps est modifiée avec le dérivé d'haptène au moyen d'un procédé peu contraignant, simple et pratique, de sorte que le conjugué d'anticorps obtenu conserve non seulement un excellent niveau d'affinité de l'anticorps d'origine, mais peut également recruter un anticorps naturel spécifique correspondant à des cellules tumorales de façon à atteindre l'objectif d'amélioration significative de la fonction d'effet immunitaire des anticorps ADCC, CDC, etc. En outre, le dérivé d'haptène SMCC-PEG 3-Rha est obtenu par optimisation de la longueur du bras de liaison. Par comparaison avec d'autres molécules d'anticorps rapportées, l'anticorps modifié SMCC-PEG 3-Rha a une fonction d'effet immunitaire plus importante.
(ZH) 一种抗体缀合物、增强抗体分子免疫效应功能的方法。所述抗体缀合物由抗体分子经半抗原衍生物分子修饰所得,所述半抗原衍生物由半抗原、连接臂和耦合域组成。通过温和简便的方法将半抗原衍生物修饰在抗体分子上,所获得的抗体缀合物不仅保留了原有抗体的优良亲和水平,还可以招募相应的特异性天然抗体至肿瘤细胞上,从而达到显著提高抗体ADCC和CDC等免疫效应功能的目的。此外,还通过对连接臂长度的优化,优化得到了SMCC-PEG 3-Rha这一半抗原衍生物。相比于其它已报道的抗体分子,SMCC-PEG 3-Rha修饰的抗体,具备更加突出的免疫效应功能。
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