Polymorphism can cause quality deviations during the production of medicines and can influence their effectiveness. Therefore, an understanding of this phenomenon and its implications opens a wide field of possibilities to be explored in the pharmaceutical field, including the emergence of new paradigms and tools for the quality assurance of medicines. Small molecule tyrosine kinase inhibitors (TKIs) represent an extremely promising and rapidly expanding group of antitumor drugs given orally. Although some polymorphism information of these compounds is included in the patents, the basic structural and thermodynamic data are poor in terms of quality of the measurements and differences and misconceptions between the crystals forms reported are evident. Additionally, polymorphism is an important factor that can impact the bioavailability and, consequently, clinical efficacy of those compounds, since most of them have low solubility in water. This project falls within this scope and focuses on: (i) preparation of polymorphs, solvates, or co-crystals of TKIs; (ii) their characterization in terms of structure and thermodynamic stability; (iii) their evaluation in terms of biopharmaceutical performance.
News published in Agência FAPESP Newsletter about the scholarship: