1057314-02-9Relevant articles and documents
Synthesis and biological evaluations of a monomethylauristatin E glucuronide prodrug for selective cancer chemotherapy
Legigan, Thibaut,Clarhaut, Jonathan,Renoux, Brigitte,Tranoy-Opalinski, Isabelle,Monvoisin, Arnaud,Jayle, Christophe,Alsarraf, Jerome,Thomas, Mikael,Papot, Sebastien
, p. 75 - 80 (2013)
We developed a glucuronide prodrug of the potent monomethylauristatin E (MMAE). This prodrug is signi ficantly less toxic than the parent drug. However, in the presence of b-glucuronidase the prodrug leads to the efficient release of MMAE thereby triggering a subnanomolar cytotoxic activity against several cancer cell lines. Preliminary in vivo experiments conducted in C57BL/6 mice bearing a subcutaneous murine Lewis Lung Carcinoma (LLC) demonstrated the potential of this targeting system for the selective treatment of solid tumors.
EFFICIENT PREPARATION OF DOLASTATIN AND AURISTATIN ANALOGS THROUGH A COMMON INTERMEDIATE
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, (2021/09/17)
Methods for making a dolastatin, auristatin or related compounds comprising the steps of providing a universal dolastatin core of Formula (I) reacting the C-terminal carboxylic acid group with an amine (A) to form an amide bond and reacting the N-terminal amine with a carboxylic acid (CA) to form an amide bond, wherein the steps can be performed in either order. Also provided are an isolated salt of the universal dolastatin core for use in preparation of dolastatins, auristatins and related compounds. Also provided are a number of intermediates and process steps which are useful for the preparation of high purity dolastatin core and high purity dolastatin and auristatin compounds.
NOVEL BINDER-DRUG CONJUGATES (ADCs) AND USE OF SAME
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, (2015/10/05)
The present patent application relates to novel binder-drug conjugates (ADCs) of N,N-dialkylauristatins directed against the target epidermal growth factor receptor (EGFR, gene ID 1956), effective metabolites of these ADCs, methods for producing these ADCs, use of these ADCs for treatment and or prevention of diseases as well as the use of these ADCs to produce pharmaceutical drugs for treatment and/or prevention of diseases, in particular hyperproliferative and/or angiogenic diseases such as cancer, for example. Such treatments may be administered as monotherapy or in combination with other pharmaceutical drugs or other therapeutic measures.