Psma antibody-drug conjugates

A - Human Necessities – 61 – K

Patent

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Details

A61K 47/48 (2006.01)

Patent

CA 2612762

This invention relates generally to antibody-drag conjugates (ADCs). In particular,the invention relates to ADCs which comprise an antibody or antigen- binding fragmentthereof which binds to prostate-specific membrane antigen (PSMA) and is conjugated tomonomethylauristatin norephedrine or monomethylauristatin phenylalanine. The antibody- drug conjugate has a PC-3~ cell to C4-2 or LNCaP~ cell selectivity of at least 250. Theinvention also relates, in part, to compositions of and methods of using the ADCs. Themethods provided include, for example, methods for treating a PSMA-mediated disease.

L'invention se rapporte de manière générale à des conjugués anticorps-médicaments (ADC: antibody-drug conjugates), et plus particulièrement à des ADC qui contiennent un anticorps ou un fragment de liaison de l'antigène de celui-ci, qui se lie avec l'antigène de membrane spécifique de la prostate (PSMA), conjugués avec de la monométhylauristatine noréphédrine ou de la monométhylauristatine phénylalanine. Ce conjugué anticorps-médicament présente une sélectivité des cellules PC-3~ pour les cellules C4-2 ou LNCaP~ d'au moins 250. L'invention se rapporte également, en partie, à des compositions de conjugués ADC et à des méthodes d'utilisation de ceux-ci. Les méthodes décrites comprennent par exemple des méthodes permettant de traiter les maladies dans lesquelles l'antigène PSMA agit comme médiateur.

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