Mersana Therapeutics, Inc.

Dmitry R Gumerov

Timothy B Lowinger

Aleksandr V Yurkovetskiy

Cheri A Stevenson

Mao Yin

Natalya D Bodyak

Patrick R Conlon

Joshua D Thomas

Charles E Hammond

Bingfan Du

Mariya Kozytska

The present disclosure relates generally to antibody-drug conjugates comprising peptide-containing linkers and to methods of using these conjugates as therapeutics and/or diagnostics. Also disclosed herein are peptide-containing scaffolds useful to conjugate with a targeting moiety (e.g., an antibody), a drug, or both to produce the antibody-drug conjugates.

Peptide-containing linkers for antibody-drug conjugates

A drug conjugate is provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -L-D, the protein based recognition-molecule being connected to the polymeric carrier by L. Each occurrence of D is independently a therapeutic agent having a molecular weight&#x2264;5 kDa. Land Lare linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.

Protein-polymer-drug conjugates

Auristatin compounds and conjugates thereof are provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -L-D, the protein based recognition-molecule being connected to the polymeric carrier by L. Each occurrence of D is independently an Auristatin compound. Land Lare linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.

A drug conjugate is provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -L-D, the protein based recognition-molecule being connected to the polymeric carrier by L. Each occurrence of D is independently a therapeutic agent having a molecular weight &#x2266;5 kDa. Land Lare linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.

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Waltham, MA, United States of America

Dmitry R Gumerov