Mersana Therapeutics, Inc.

Asana Biosciences, LLC

Mersana Therpeutics, Inc.

Mao Yin

Aleksandr V Yurkovetskiy

Timothy B Lowinger

Cheri A Stevenson

Joshua D Thomas

Patrick R Conlon

Charles E Hammond

Natalya D Bodyak

Dmitry R Gumerov

Bingfan Du

Shuyi Tang

Venu Reddy Gurijala

Russell Colyn Petter

Eugene W Kelleher

Roger Astbury Smith

Nitin Krishnaji Damle

Gui Liu

Laura C Akullian

John J Kane

Mariya Kozytska

John Henry Van Duzer

James Rolke

Brian D Jones

Ahmed Hilmy

Dimitry R Gumerov

Emile Farhan

Satyanarayan Reddy Bollu

Carolina B Cabral

Jacques Leblanc

Dennis McGillicuddy

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

The present disclosure relates generally to antibody-drug conjugates comprising pyrrolo[2, 1-c][1, 4]benzodiazepine (PBD) drug moieties. The present disclosure also relates to methods of using these conjugates, e.g., as therapeutics and/or diagnostics.

Pyrrolobenzodiazepine antibody conjugates

A polymeric scaffold useful for conjugating with a protein based recognition-molecule (PBRM) to form a PBRM-polymer-drug conjugate is described herein. The scaffold includes one or more terminal maleimido groups. Also disclosed is a PBRM-polymer-drug conjugate prepared from the scaffold. Compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions are also described.

Protein-polymer-drug conjugates

The disclosure provides methods of synthesis of polymeric scaffolds, e.g., those useful for conjugating with a protein based recognition-molecule (PBRM) to form PBRM-polymer-drug conjugates, and PBRM-polymer-drug conjugates thereof. The methods according to the disclosure allow for large-scale preparation of polymeric scaffolds having a high purity. In some embodiments, the methods according to the disclosure also allow for the preparation of scaffolds and conjugates thereof in better yield than previously used methods for preparing same. Also disclosed are methods of purifying polymeric scaffolds.

Methods of producing drug-carrying polymer scaffolds and protein-polymer-drug conjugates

The present disclosure relates generally to derivatives of pyrrolobenzodiazepines and antibody-drug conjugates thereof and to methods of using these conjugates as therapeutics and/or diagnostics.

Pyrrolobenzodiazepines and conjugates thereof

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.

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.

An auristatin compound 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 an auristatin compound having a molecular weight &#x2264;5 kDa. Land Lare distinct linkers connecting the auristatin compound and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-auristatin compound-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.

Auristatin compounds and conjugates thereof

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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Needham, MA, United States of America

Mao Yin