The ICESTP™ SafetyOne44 Panel developed by ICE Bioscience is grounded in the strategy of in vitro safety pharmacology profiling, focusing on a comprehensive set of 44 clinically relevant targets, including GPCRs and ion channels. Its design aims at early detection of potential safety concerns by screening compounds against a broad spectrum of biological targets associated with adverse drug reactions. This approach facilitates the efficient optimization of lead compounds, enhancing their safety profiles and reducing the risk of late-stage development failures.
The ICESTP™ SafetyMax90 Panel developed by ICE Bioscience expands the in vitro safety pharmacology profiling with an additional 46 important targets, focusing on critical physiological systems such as the central nervous system, cardiovascular system, metabolism, and immunity. By including these additional targets, ICESTP™ SafetyMax90 Panel aims to enhance early detection of adverse drug reactions and off-target effects, thereby facilitating the development of safer and more effective therapeutic compounds. This extension aims to provide comprehensive data for lead optimization, building robust Structure-Activity Relationship (SAR) models, and driving chemical design. Importantly, it focuses on designing out potential off-target related liabilities based on SAR knowledge. This approach underscores the importance of a wide-ranging and thorough pharmacological assessment in drug development.
Direct Measurement of Functional Activity: Functional assays directly measure the pharmacological effect of a compound on a target, providing more relevant insights into its potential therapeutic and side effect profiles compared to binding assays, which only indicate the ability of a compound to bind to a target.
Better Prediction of Clinical Outcomes: By assessing the actual effect on target activity, functional assays offer a more accurate prediction of a compound's clinical efficacy and safety, enhancing drug development efficiency.
Identification of Agonists and Antagonists: Unlike binding assays, functional assays can distinguish between agonists, antagonists, and inverse agonists based on their effects on target function, crucial for understanding a compound's pharmacodynamics.
Dynamic Range of Response: Functional assays provide a dynamic range of response, allowing for the detection of partial agonists or partial antagonists, which is not possible with binding assays that only provide binary outcomes (bind or not bind).
| Targets | SafetyOne44 | SafetyMAX90 |
|---|---|---|
| GPCR | 24 | 37 |
| Ion Channel | 8 | 15 |
| Enzyme | 7 | 32 |
| Nuclear Receptor | 2 | 3 |
| Transporter | 3 | 3 |
| Total Functional Assays | 74 | 138 |
| TAT | 15 Business Days | 25 Business Days |
A functional safety panel can effectively illustrate the insights gained from agonist and antagonist assays, providing more comprehensive and informative results. As depicted in the figure, the SafetyMAX 90 panel was employed to assess Mivebresib's response in both agonist and antagonist modes. Results surpassing the 50% threshold line indicate a clear functional interaction.
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