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Updated: Jan 1, 2026
Production, Crystallization, and Structure Determination of the IKK-binding Domain of NEMO
Published on: December 28, 2019
Cediranib Maleate-From Crystal Structure Toward Materials Control
Simon N Black1, Helen P Wheatcroft2, Ron Roberts3
1Chemical Development, Pharmaceutical Technology & Development, AstraZeneca, Macclesfield Campus, Macclesfield SK10 2NA, UK; School of Chemical Engineering and Analytical Sciences, University of Manchester, Manchester M13 9PL, UK.
Cediranib maleate development involved controlling crystal structure to prevent unwanted forms and ensure consistent particle size. Insights from crystal structure analysis guided API performance control, leading to a robust development process.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Chemical Engineering
Background:
- Cediranib maleate, an active pharmaceutical ingredient (API) in oncology development.
- Robust salt form selection is critical for drug development.
- Controlling solid-state properties impacts API performance.
Purpose of the Study:
- To analyze and control the crystal structure of cediranib maleate.
- To avoid metastable polymorphs and solvates during API development.
- To establish a method for building API performance from crystal structure.
Main Methods:
- Crystal structure analysis
- Polymorph screening and characterization
- Particle size analysis
- Process redesign for salt formation
Main Results:
- The selected salt form of cediranib maleate was confirmed as robust.
- An unwanted metastable polymorph was successfully avoided through process redesign.
- A challenging solvate was identified and mitigated using crystal structure insights.
- Differences in aspect ratios correlated with crystal interaction strength.
- Acceptable particle size variability was defined and managed.
Conclusions:
- Understanding and controlling crystal structure is essential for robust API development.
- Crystal structure insights enable the avoidance of problematic solid-state forms.
- The 'Matwall' approach facilitates performance control from the molecular level upward.
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