Cysteine engineered anti-tenb2 antibodies and antibody drug...

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 16/28 (2006.01) A61K 47/48 (2006.01)

Patent

CA 2698541

Cysteine engineered anti-TENB2 antibodies are engineered by replacing one or more amino acids of a parent anti--TKNB2 antibody with non cross-linked, reactive cysteine amino acids. Methods of design, preparation, screening, and selection of the cysteine engineered anti-TENB2 antibodies are provided. Cysteine engineered anti-TENB2 antibodies (Ab) are conjugated with one or more drug moieties (D) through a linker (L) to form cysteine engineered anti-TENB2 antibody-drug conjugates having Formula I: Ab-(L-D)p I where p is 1 to 4. Diagnostic and therapeutic uses for cysteine engineered antibody drug compounds and compositions are disclosed.

Les anticorps anti-TENB2 de l'invention sont modifiés par des cystéines par remplacement d'un ou de plusieurs acides aminés d'un anticorps anti-TKNB2 parent par des acides aminés cystéine réactifs, non réticulés. Des procédés de conception, préparation, criblage, et sélection d'anticorps anti-TENB2 modifiés par des cystéines sont également décrits. Des anticorps (Ab) anti-TENB2 modifiés par des cystéines sont conjugués avec un ou plusieurs fragments médicament (D) par un élément lieur (L) de manière à former des conjugués anticorps modifiés par des cystéines-médicament répondant à la Formule I : Ab-(L-D)p I où p vaut de 1 à 4. Des utilisations en diagnostic et thérapie des composés et compositions de l'invention sont décrites.

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