Modified antibodies and antibody fragments with increased...

Details Modified antibodies and antibody fragments with increased... Modified antibodies and antibody fragments with increased...

C - Chemistry, Metallurgy

07

K

C07K 16/00 (2006.01) C07K 16/28 (2006.01)

Patent

CA 2353082

Modified antibodies with improved pharmacokinetic properties are disclosed. The antibodies bind to one or more human integrin receptors selected from the group consisting of GPIIb/IIIa, .alpha.v.beta.3 and Mac-1, and comprise one to about six organic moieties which are covalently bonded to specific sites on the antibodies. The organic moieties can each independently be a hydrophilic polymeric group, a fatty acid group, a fatty acid ester group, a lipid group or a phospholipid group. Also disclosed is a method of treating a human with a disease or disorder in which cells expressing GPIIb/IIIa,.alpha.v.beta.3 and/or Mac-1 play a pathophysiological role. The method comprises administering an effective amount of one or more antibodies of the invention to a human in need thereof.

L'invention concerne des anticorps modifiés ayant des propriétés pharmacocinétiques améliorées. Les anticorps se fixent à un ou plusieurs récepteurs humains de l'intégrine, sélectionnées dans le groupe des GPIIb/IIIa, .alpha.¿v?.beta.¿3? et Mac-1, et ils comprennent entre un et six fragments organiques liés de manière covalente à des sites spécifiques sur les anticorps. Les fragments organiques peuvent être, de manière indépendante, un groupe polymère hydrophile, un groupe acide gras, un groupe ester d'acide gras, un groupe lipide ou un groupe phospholipide. L'invention concerne également un procédé destiné au traitement de patients atteints d'un état pathologique ou d'un trouble dans lequel les cellules exprimant GPIIb/IIIa, .alpha.¿v?.beta.¿3? et/ou Mac-1, jouent un rôle pathophysiologique. Le procédé concerne l'administration d'une dose efficace d'un ou plusieurs anticorps de cette invention à un être humain le nécessitant.

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