The drug discovery and development industry is constantly striving to achieve success with new approaches such as personalized vaccines, CRISPR-based therapies, and microbiome therapies. The therapies are expected to provide effective treatment solutions for various diseases and illnesses including cancer. Small molecules are intrinsic to most successful therapeutic drugs, which amount to 90% of the currently available therapeutics in the market.

A well-known fact - 9 of 10 drugs sold or prescribed in the US market are small molecule drugs which include pain killers, blood pressure medicines, etc. Hence, the bioanalysis of small molecules is an important procedure in drug discovery and development. Correct analysis and tests meeting the regulatory guidelines of the FDA ensure safety and efficacy of the drugs for human consumption and use. 

In this article, we will discuss some key factors about small molecular bioanalysis.

What Are Small Molecule Drugs?
Small molecules have a molecular weight of 900 Daltons or less. These molecules are derived from natural products produced by plants, fungi, bacteria, etc. For example, Penicillium fungi is the main source of the antibiotic penicillin, amphotericin B is an antifungal isolated from Streptomyces nodosus, and the anti-cancer drug paclitaxel is derived from the Pacific yew tree.

Small Molecule Bioanalysis
Bioanalysis of small molecules is essential to understand how the chemical composition will act on the cause of the disease as it progresses and to know the prognosis if used during the course of treatment. Thus, the chemical analysis of drug compounds inside a biological matrix during the drug discovery and development process are essential to assess a drug compound within a biological matrix such as plasma or serum.

Below are some of the common small molecule bioanalysis processes.

PK Bioanalysis

Pharmacokinetic studies are crucial in bioanalysis as these studies offer a clear understanding of a drug’s movement in the body. Quantitative and exploratory studies allow scientists to reveal various essential discovery variables. These variables include a drug’s half-life, exposure, bioavailability, bioequivalence (in case of a generic drug), clearance, distribution, and metabolism. These variables determine the differentiating factors that lead to the success or failure of a small molecule drug product.

In Vivo PD, PK, And TK Studies

In vivo pharmacokinetic, pharmacodynamic, and toxicokinetic studies have a high significance in drug discovery and development. These studies help the scientists to evaluate the human equivalent doses (HED), no effect levels (NOEL), and other PK or PD drivers. PK studies, in particular, allow identification of distribution volume, half-life, AUC, Cmax, Cmin, etc.

Further, toxicokinetic studies help in identifying the toxic impact of the drug compound on the human body. Based on this analysis, scientists define the effective drug dosage that can be consumed without harming the body.

Biomarker Analysis
A bioanalytical laboratory will use biomarkers to identify the normal biological, pharmacological, and pathological processes in the human body. It is important to analyze these markers to understand disease progression and verify the safety of a drug compound and its efficacy for treating a particular condition. The biomarkers are essential in clinical studies as these often form the primary endpoints of the experimentation.

Reliable bioanalytical results at various stages of drug development, starting from lead discovery to optimization are necessary and require experts to help with the condition. Correct and efficient execution of bioanalytical processes additionally ensure potent and sensitive drug products.