Hydrated crystalline form of lazertinib methanesulfonate and methods of making and uses thereof

By preparing hydrate crystal form A of lazertinib mesylate, the problems of insufficient stability and solubility of the existing crystal form I were solved, achieving good drug stability and solubility, which is suitable for drug development and storage.

CN117425651BActive Publication Date: 2026-07-24SOLIPHARMA
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Patent Information

Application Number
CN202280037855.4
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Priority Date
2021-06-01
Filing Date
2022-06-01
Publication Date
2026-07-24
Estimated Expiration
2042-06-01

AI Technical Summary

Technical Problem

The existing lazertinib monomethyl sulfonate crystal form I exhibits discoloration and increased impurities during accelerated stability studies, indicating poor stability, inability to be stored for long periods, and insufficient solubility, which affects drug absorption and bioavailability.

Method used

The hydrate crystal form A of lazertinib methanesulfonate was prepared by a specific preparation method to form a crystal form with good stability, solubility and dissolution rate. This method includes mixing the solution in dichloromethane or trichloromethane and diethyl ether/acetonitrile solvent and then drying it to ensure the characteristic peaks and properties of the crystal form.

Benefits of technology

Crystal form A exhibits good stability under accelerated conditions, with significantly improved solubility and dissolution rate, avoiding degradation and appearance changes during storage, making it suitable for pharmaceutical use and meeting bioavailability requirements.

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Abstract

The application relates to the field of pharmaceutical chemistry. The application relates to a hydrate crystal form of lazertinib monomethanesulfonate and a preparation method and application thereof. The hydrate crystal form of lazertinib monomethanesulfonate provided by the application has at least one of the following advantages: good stability, good solubility, good dissolution, low hygroscopicity, uniform particle size distribution, good morphology, good fluidity, good crystallinity, stable storage, avoidance of degradation, impurity increase, appearance change and crystal transformation during development and storage, simple and reliable preparation method, and great development value.
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