610786-78-2Relevant academic research and scientific papers
The Development and Scale-Up of an Antibody Drug Conjugate Tubulysin Payload
Parker, Jeremy S.,McCormick, Marc,Anderson, David W.,Maltman, Beatrice A.,Gingipalli, Lakshmaiah,Toader, Dorin
supporting information, p. 1602 - 1609 (2017/10/25)
Significant development and scale-up work was completed on the synthesis of an antibody drug conjugate payload based on the tubulysin natural products. This work included the development of new routes to the tubuvaline and tubuphenylaniline portions of the molecules, as well as extensive optimization of the solid phase peptide synthesis used to assemble the molecule. The initial route (21 steps longest linear sequence, 0.01% overall yield) was improved to a new, more robust route (19 steps longest linear sequence, 2.4% overall yield) affording a 240-fold increase in overall yield and allowing delivery of over 86 g of the required molecule.
BISPECIFIC HER2 ANTIBODIES
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Paragraph 00621, (2015/11/03)
The present invention relates to anti-HER2 binding molecules (e.g., antibodies and antigen binding fragments thereof), derived HER2-binding molecules (e.g., bispecific anti-HER2 antibodies), and antibody-drug conjugates (ADC) that bind the extracellular domain of the HER2 receptor. Also provided are pharmaceutical formulation comprising the disclosed compositions and method for the treating diseases associated with HER2-mediated signal transduction.
ANTIBODIES AND ANTIBODY-DRUG CONJUGATES
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Paragraph 0574, (2015/11/03)
This application provides antibodies and antigen binding fragments thereof which are capable of specifically binding the 5T4 cell surface antigen, antibody-drug conjugates, and antibody-imaging agent conjugates, as well as means and methods for producing and using them.
TUBULYSIN DERIVATIVES
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Page/Page column 23, (2015/11/17)
Novel tubulysin derivatives which may be useful as cytotoxic agents to provide therapeutic benefits in the treatment of various types of cancers, alone or as drug conjugates with antibodies are provided. The tubulysin derivatives consist of a tetrapeptide scaffold comprising methyl and ethyl substituted piperidines. The tubulysin conjugates further comprise monoclonal antibody via succinimide linkers.
