AMG-510 Solid State Forms for Stability and Bioavailability
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Solution Overview
Problem
There is a need for additional solid state forms of AMG-510, including crystalline polymorphs and cocrystals, to improve processing properties, stability, and bioavailability for effective treatment of non-small cell lung and colorectal cancers.
Innovation Solution
The development of various solid state forms of AMG-510, such as crystalline polymorphs and cocrystals, including specific forms characterized by X-ray powder diffraction patterns, which can be used to prepare pharmaceutical compositions and formulations for cancer treatment.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If additional solid state forms of AMG-510 are developed, then stability and bioavailability are improved, but manufacturing complexity increases
Solution Approach 1:
The patent applies parameter changes by developing multiple solid state forms (polymorphs, solvates, cocrystals) of AMG-510 with different physical and chemical parameters. Each form has distinct crystal structures, melting points, solubility profiles, and stability characteristics. By systematically varying these parameters through controlled crystallization processes, the patent creates a portfolio of forms that optimize stability and bioavailability while managing manufacturing complexity through standardized preparation methods.
2Ease of manufacture
If multiple solid state forms are prepared, then processing characteristics and bioavailability are enhanced, but process complexity increases
Solution Approach 1:
The patent applies segmentation by dividing the solid state forms into distinct categories (polymorphs, monosolvates, hydrates, cocrystals) with specific preparation methods for each type. This segmentation allows systematic development and optimization of processing characteristics for each form while managing overall process complexity through standardized classification and preparation protocols. Each segment can be independently optimized for specific therapeutic applications.
3Reliability
If new solid state forms are discovered, then bioavailability and shelf-life are improved, but development time increases
Solution Approach 1:
The patent applies preliminary action by systematically exploring and characterizing multiple solid state forms early in the development process. Through preliminary crystallization studies, polymorph screening, and stability assessments, the patent identifies promising forms before final formulation selection. This preliminary exploration enables optimization of shelf-life and bioavailability characteristics while managing development time through efficient screening methodologies and prioritization of clinically relevant forms.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
These solid state forms enhance the stability, bioavailability, and processing characteristics of AMG-510, providing improved therapeutic options for non-small cell lung and colorectal cancers.
Implementation Method 1
One or more of these techniques may be used to distinguish different polymorphic forms of a compound... a single molecule may give rise to a variety of polymorphs having distinct crystal structures... X-ray diffraction (XRD) pattern
Data Source
AI summary
The present disclosure encompasses solid state forms of AMG-510 (Sotorasib), in embodiments crystalline polymorphs of AMG-510, processes for preparation thereof, and pharmaceutical compositions thereof.