Drug discovery is an essential part of the drug development process. Researchers test candidates to identify those suitable for regulated animal studies and, ultimately, clinical trials. Bioanalytical discovery involves assessing a compound’s physiochemical properties, screening metabolites, and evaluating bioavailability, toxicity, and pharmacokinetics.

Understanding the Drug Discovery Process

The Role of Drug Discovery

Discovery serves as the critical bridge between early-stage research and the development of commercial therapeutics. By identifying promising drug targets, validating mechanisms of action, and optimizing lead compounds, discovery translates basic scientific insights into candidates ready for preclinical and clinical testing. This stage sets the foundation for safe, effective, and market-ready treatments.

From Concept to Candidate: An Overview

The beginning stage of drug development is a stage of trial and error.  It is generally accepted that for every pharmaceutical drug molecule that makes it to the market, approximately 10,000 or more compounds will need to be tested.

From lead discovery to market approval, a drug can take around 12 years to reach patients. Researchers must determine effective doses, therapeutic thresholds, lethal doses, and pharmacokinetic and pharmacodynamic properties. Answering these questions quickly and reliably is critical to deciding a lead compound’s future.

The Transition from Discovery to Development

Researchers carefully evaluate and optimize early findings from discovery before advancing candidates into preclinical testing, where candidates undergo rigorous studies to assess safety, efficacy, and biological activity. This phase ensures that only the most promising compounds advance toward clinical development.

Drug development involves many twists and turns. Researchers often start with expectations, but data can be surprising. When challenges arise, we provide expert guidance and multiple paths forward to meet timelines and data expectations. We act as an extension of your lab, bringing knowledge, experience, and strategic insight to navigate every twist and turn in the development journey.

Challenges in the Drug Discovery Process

High Attrition Rates

Drug development is a high-risk, high-investment endeavor. Only a small fraction of early candidates ultimately become approved therapies, and the path from discovery to market can take years of focused research, testing, and iteration. Despite the long timelines and low success rates, each step builds critical knowledge that informs the next generation of therapeutics.

Technical and Biological Complexity

Drug development is influenced by technical and biological complexity. Bioavailability and target selectivity play critical roles in determining a candidate’s effectiveness. Reusing methods from prior studies can streamline development without compromising analytical standards. Advanced techniques, such as coupling assays to a UPLC front end, allow us to reach maximum sensitivity for the lowest limit of quantitation and achieve proper separation with the selectivity needed to confidently measure complex biological molecules.

Discovery Tools That Drive Innovation

Analytical Techniques

One of KCAS Bio’s core expertise is using bioanalytical LC-MS/MS to support drug discovery, particularly in assessing bioavailability and pharmacokinetics. Beyond LC-MS/MS, we also offer a full suite of immunoassays and assay support to address complex biological questions, from target engagement to biomarker measurement. We assist with study design, provide guidance on optimal assay selection, and deliver the bioanalytical data needed to conduct thorough pharmacokinetic and pharmacodynamic assessments, helping projects move efficiently from discovery toward development.

Focused Discovery Support

The Discovery team consistently delivers high-quality data with rapid turnaround times and a cost structure designed to maximize value for our sponsors. Our team conducts analyses using acceptance criteria tailored to each sponsor’s experimental design, ensuring relevance and scientific rigor. We can replicate aspects of a regulated (GLP) validation process by performing studies such as benchtop stability, freeze/thaw, and matrix effect assessments, with flexibility to customize the tests performed. By collaborating closely with sponsors, we help design experiments that address critical objectives while minimizing or eliminating non-value-added studies.

Why KCAS Bio Is a Trusted Partner in Drug Discovery

  • Small-Molecule Bioanalysis (LC‑MS/MS) – Quantitation of drugs, metabolites, and biomarkers in discovery / preclinical matrices.

  • Ligand-Binding Assays (LBA) – Including ELISA, MSD (electrochemiluminescence), Luminex; used for soluble/cell-surface biomarkers, PK/TK, PD, and ADA (anti‑drug antibody) detection.

  • Immunogenicity / ADA Testing – Anti‑drug antibody (ADA) and neutralizing antibody (NAb) assays, using acid dissociation, ACE, SPE‑AD to improve drug tolerance, and statistical cut‑point analysis.

  • Flow Cytometry / Immunophenotyping – High-dimensional cellular profiling, immune biomarker discovery, functional screening, cell sorting.

  • Molecular Services – qPCR, ddPCR, biodistribution, PK/PD, cell and gene therapy support.

  • Biomarker Testing – Soluble and cellular biomarkers; assay development / validation tailored to context-of-use, including multiplexed assays.

  • Dose Formulation Analysis – Certificate of Analysis (CoA) and method validation of small molecules, peptides, proteins, siRNA, antibodies, ADCs.

  • Central Lab / Sample Kitting – Biospecimen management, global kitting for clinical and animal studies.

  • ADC Bioanalysis – Quantitation of intact antibody, payload, DAR (drug-to-antibody ratio), stability, immunogenicity (using LBA and hybrid LC-MS).

FAQs

What regulatory requirement is needed?

We use three levels of rigor for quantitative discovery analysis. This approach balances high-quality data with providing actionable results for sponsors.

Where would the in-life portion of the work be done?

KCAS Bio has access to resources and relationships that allow us to offer the full suite of discovery services.

What matrices have you worked on?

Our Discovery team at KCAS Bio is trained in all aspects of bioanalysis including sample extraction, LC-MS analysis, data integration and reporting. We routinely work with plasma samples from rodents, dog, pig and non-human primate. For many drugs, the penetration into tissue is an important factor so we have built extensive experience dealing with tissue and other non-routine matrices.

KCAS Bio’s extensive cross-training program ensures that resources can be available immediately to supplement our core Discovery team when we see a rapid influx of work. We can move forward with your projects at very short notice.