Modern drug discovery involves the identification of screening hits, medicinal chemistry, and optimization of those hits to increase the affinity, selectivity, efficacy/potency, metabolic stability, and bioavailability. This process is time-consuming, costly, and risky. Nuclear receptors are ideal targets for drug discovery. They control a variety of biological and disease processes through the expression of specific genes. Nuclear receptors do this by binding to lipophilic substances known as ligands.

Pharmacotherapy is based on the interplay of pharmacokinetics and pharmacodynamics, which allows scientists to understand the effect drugs have on the human body and helps researchers develop drugs that are safe and effective. These two concepts explain how the body impacts drugs (pharmacokinetics) and how those drugs can then impact the body (pharmacodynamics).

Biliary excretion is the crucial process of removing drugs from the human body and it plays an important role in drug processing. Researchers and drug development teams frequently examine this active process relative to differences in drug responses and challenges with drug toxicity.

Utilizing the human multidrug resistance protein 1 is a core component of modern drug development as it aids the assessment of drug-drug interaction. Learn more about MDR1 through a brief overview of its function in the human body and its role in public health and safety.

Through further examination of enzyme induction and its relationship to drug-drug interaction, we can better understand the effects of certain drugs and develop safer solutions for diseases and conditions.

From research available to us today, we know that there are many environmental chemicals that carry the potential to greatly impact the endocrine system. These are known as endocrine disrupting chemicals (EDCs), which are compounds that can alter drug and xenobiotic metabolic processes and interfere with the production, release, metabolism, and elimination of naturally occurring hormones.

Liver toxicity is a major cause of drug failure in clinical trials and often leads to the complete market withdrawal of many approved drugs today. Due to inherent differences in drug metabolism between species, it’s also difficult to extrapolate results obtained from preclinical animal models for human use. But new research on upcyte^® hepatocytes suggests that they may be an effective solution for reducing attrition due to metabolism-mediated toxicity and the key to improving the safety of new drug candidates.

The drug discovery process is time-consuming, costly, and risky. Here is a quick look at some of the risks and challenges associated with drug discovery, as well as solutions that can be utilized to streamline the process to increase return-on-investment and mitigate risk.