Seattle Genetics, Inc.

Medimmune Limited

Seagen Inc.

Spirogen Sarl

Patrick J Burke

Scott C Jeffrey

Philip Wilson Howard

Django Sussman

Brian E Toki

Dennis R Benjamin

Stephen C Alley

Peter Senter

Arnaud Charles Tiberghien

Luke Masterson

Maureen Ryan

Travis Biechele

May Kung Sutherland

Joel Courter

Lori Westendorf

Robert Lyon

William Arthur

Andrew Waight

Chris Leiske

Jocelyn Leiske

Robert Kolakowski

Joshua Hunter

Arnaud Tiberghien

Joseph Z Hamilton

The invention provides modified heavy chain constant regions including a cysteine at position 295 by EU numbering and optionally at position 239 by EU numbering. These cysteine residues provide sites for conjugation to a drug or label. When both cysteines are present in a normal heterodimeric antibody format, there are four such sites per molecule of antibody allowing a stoichiometry of one molecule of antibody to four of drug or label. Selection of the cysteine at position 295 with or without cysteine at position 239 is advantageous over cysteines at many other positions due to ease of expression, stability and cytotoxicity.

Cysteine mutated antibodies for conjugation

The invention provides murine, chimeric, and humanized antibodies that specifically bind to GPC3 and conjugates thereof.

Glypican 3 antibodies and conjugates thereof

Compounds and compositions are disclosed in which a quaternized drug unit is linked to a targeting ligand unit from which a tertiary amine-containing drug is released at the targeted site of action. Methods for treating diseases characterized by the targeted abnormal cells, such as cancer or an autoimmune disease using the compounds and compositions of the invention are also disclosed.

Conjugates of quaternized tubulysin compounds

The invention provides methods and compositions for preparing antibodies and antibody derivatives with reduced core fucosylation.

Methods and compositions for making antibodies and antibody derivatives with reduced core fucosylation

The present invention provides Ligand-Drug Conjugates and Drug-Linker Compounds comprising a methylene carbamate unit. The invention provides inter alia, Ligand-Drug Conjugates, wherein the Ligand-Drug Conjugate is comprised of a Self-immolative Assembly Unit having a methylene carbamate unit for conjugation of a drug to a targeting ligand, methods of preparing and using them, and intermediates thereof. The Ligand-Drug Conjugates of the present invention are stable in circulation, yet capable of inflicting cell death once free drug is released from a Conjugate in the vicinity or within tumor cells.

Methylene carbamate linkers for use with targeted-drug conjugates

The present invention provides Ligand-Drug Conjugates comprising a PEG Unit in a parallel orientation to the Drug Unit. The invention provides inter alia, Ligand-Drug Conjugates (LDCs), methods of preparing and using them, and intermediates thereof. The Ligand-Drug Conjugates are stable in circulation, yet capable of inflicting cell death on targeted cells or inhibiting proliferation of targeted cells once its drug cargo is released in the vicinity or within targeted cells. In principle embodiments, an LDC of the present invention is represented by the structure of Formula I.

Pegylated drug-linkers for improved ligand-drug conjugate pharmacokinetics

The invention provides murine, chimeric, and humanized antibodies that specifically hind to CD33. The antibodies are useful for treatment and diagnoses of various cancers as well as detecting CD33.

CD33 antibodies and use of same to treat cancer

Provided are Conjugate comprising PBDs conjugated to a targeting agent and methods of using such PBDs.

Targeted pyrrolobenzodiazapine conjugates

A compound, or a pharmaceutically acceptable salt or solvate thereof, or conjugates thereof, selected from the group consisting of: wherein:(a) Ris H, and Ris OH, OR, where Ris saturated Calkyl;(b) Rand Rform a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are bound; or(c) Ris H and Ris SOM, where z is 2 or 3 and M is a monovalent pharmaceutically acceptable cation, or both M together are a divalent pharmaceutically acceptable cation.

Pyrrolobenzodiazepines and targeted conjugates

This invention relates to pyrrolobenzodiazepines (PBDs), in particular pyrrolobenzodiazepine dimers having a C2-C3 double bond and an aryl group at the C2 position in each monomer unit, and their inclusion in targeted conjugates. The differing substituent groups may offer advantages in the preparation and use of the compounds, particularly in their biological properties and the synthesis of conjugates, and the biological properties of these conjugates.

Pyrrolobenzodiazepine dimers having a C2-C3 double bond and an aryl group at the C2 position on one monomer unit, and a C2-C3 double bond and either a conjugated double or triple bond at the C2 position or an alkyl group at the C2 position on the other monomer unit, and conjugates of these compounds.

Pyrrolobenzodiazepines used to treat proliferative diseases

A compound, or a pharmaceutically acceptable salt or solvate thereof, or conjugates thereof, selected from the group consisting of: wherein:

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Bothell, WA, United States of America

Patrick J Burke