Axitinib (AG-013736) is a selective VEGF antagonist for treatment of solid tumors.  The drug substance is prepared in a convergent synthesis that utilizes a Migita coupling and Heck reaction for the two key bond formations.  Selection of the solid form was challenging in that 5 anhydrous forms were identified, with full characterization occurring later in development.  As a result, early clinical trials were conducted with a metastable form and bridging to a more stable form was required for commercial manufacture.  The presentation will focus on process development using a quality by design approach for process understanding and purity control.  Strategies for controlling residual Pd and other impurities will be a focus in addition to control of solid form.

Commercial route development for axitinib/AG-013736, solid form and control strategy challenges

244th National Meeting (2012)

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