Dasatinib Co-crystals and Solvate Forms
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current forms of dasatinib, such as those described in existing patents, do not include an ethyl formate solvate or co-crystals with specific second compounds like butyl paraben, propyl paraben, and ethyl vanillin, limiting the therapeutic options for treating Philadelphia chromosome-positive chronic myeloid leukemia and acute lymphoblastic leukemia.
Innovation Solution
Development of dasatinib co-crystals and solvate forms, specifically ethyl formate solvate, in combination with butyl paraben, propyl paraben, and ethyl vanillin, along with processes for their preparation, to create pharmaceutical compositions for treating diseases like Philadelphia chromosome-positive chronic myeloid leukemia and acute lymphoblastic leukemia.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Adaptability or versatility
If existing forms of dasatinib are used, then the treatment options for Philadelphia chromosome-positive chronic myeloid leukemia and acute lymphoblastic leukemia are limited, but developing new co-crystal and solvate forms requires additional research and development time
Solution Approach 1:
The patent applies parameter changes by creating different crystalline forms of dasatinib with varying physical and chemical properties. Specifically, it describes Form I (anhydrous), Form II (monohydrate), and various solvate forms (ethyl formate, butyl paraben, propyl paraben, ethyl vanillin). Each form represents a different parameter state of the same compound, enabling diverse therapeutic applications while maintaining the core medicinal activity of dasatinib against Philadelphia chromosome-positive leukemias.
2Reliability
If multiple co-crystal and solvate forms of dasatinib are developed, then therapeutic efficacy and stability are enhanced, but the complexity of the pharmaceutical composition increases
Solution Approach 1:
The patent employs composite materials by forming co-crystals and solvates that combine dasatinib with other compounds. Examples include dasatinib co-crystals with butyl paraben, propyl paraben, and ethyl vanillin, as well as ethyl formate solvate forms. These composite structures integrate multiple components into a single crystalline phase, enhancing therapeutic properties while maintaining compositional integrity through defined stoichiometric ratios and crystalline ordering.
Data Source
AI summary
The present disclosure relates to a dasatinib co-crystal form comprising dasatinib and a second compound, also referred to as a co-crystal former, wherein the second compound is selected from butyl paraben, propyl paraben and ethyl vanillin. The present disclosure is also related to an ethyl formate solvate form of dasatinib. The present disclosure is also related to processes for the preparation of the dasatinib co-crystal and solvate forms of dasatinib. Further, the present disclosure also relates to pharmaceutical compositions comprising the dasatinib co-crystal and solvate forms of dasatinib and methods for treating disease using the dasatinib co-crystal and solvate forms of dasatinib.