Unexpected Single Crystal Growth Induced by a Wire and New Crystalline Structures of Lapatinib

What is it about?

Lapatinib is a important drug used for treatment of metastatic breast cancer. It is known that pharmaceutical solids can exist in different crystalline structures (polymorphism) that results in changes in chemical and physical properties and may lead to serious consequences in manufacture, stability and efficacy of medicines. Although complex, demanding, and often not possible to achieve, the single crystal growth and structure determination are still fundamental steps to map the crystal space, obtain a standard for powder diffraction and understand the structural aspects of polymorphism phenomena such as solvatation and interconversions. Herein, we report the investigation of new crystalline forms of lapatinib free base and unusual approach to promote single crystal growth of two of these forms.

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Why is it important?

Lapatinib is a highly effective orally administrated drug widely used in the treatment of breast cancer with very limited structure and polymorphism data available. After months of unsuccessful efforts to growth single crystals using classical methods, anhydrous and hydrate crystals were obtained by a new approach on the first attempt. Also, for the first time polymorphism, structure, solvate formation and phase transitions of this important drug were addressed.