Why Use Cytotoxicity Testing in Small Molecule Drug Development and Testing?

Cytotoxicity references the toxicity of a cell that leads to cell damage or death. In the field of drug development and research, a cytotoxicity test helps scientists and researchers measure how a particular compound or molecule can impact cell health, leading to cell death.

Since living organisms are made up of cells, the unexplained death of a cell can lead to diseases. Through cytotoxicity studies, researchers are looking to identify the safety of a drug compound for human consumption.

The simple fact is that all molecules, big and small, require stringent testing to understand how they will react with an analyte or protein in the human body. In the field of biochemistry, small and big are not classified for size alone. Factors such as composition, suitability for different drug forms, behavior patterns, and mode of transportation are also considered. Since most research is based on small molecules, it is but obvious, that it is essential to test their effect on living, healthy as well as unhealthy cells. For example, the unstoppable proliferation of cells in a cancer patient requires cytotoxic compounds that allow the human body to maintain cell balance.

 Let’s look at the role and importance of a cytotoxicity assay on drug development and research:

Did you know that the cost of developing a new drug today stands at around USD 1 billion? Given the rising expenses and the need to follow GLP and FDA protocols, using cells and plant molecules allows for quicker testing. 

Every new drug compound undergoes a series of tests to measure precisely how much damage it can cause. Since a small molecule will travel from the point of intake to the site of action, it is necessary to carry out detailed studies of interactions with cells on-route. For example, a drug compound that is necessary for killing cancer cells may require direct application to the site of action to limit damage to the affected area.

A cytotoxicity assay is combined with in vivo testing of the ADME properties of a drug to achieve a safety profile. Absorption or permeability, metabolic stability during metabolism, and interaction to membrane transport systems during distribution are essential aspects that validate behavior and possible outcomes.

In small molecules testing, especially, qualitative and quantitative assays are used to create markers for biocompatibility. For example, if a compound is highly toxic, small molecule testing will undertake studies to identify the pathways that can mitigate the toxic effects of the compound on the cells.

One of the most important things to remember while undertaking a cytotoxicity assay is choosing the right assay. Additionally, it is equally important to remember that using a single test or kit is not enough to provide accuracy.