Decoding DMPK Frontiers for Novel Therapeutics: WuXi AppTec DMPK’s New Book Release

Advances in the pharmaceutical industry and the rise of novel drug modalities have presented new challenges and opportunities for drug development, driving continuous innovation and progress in DMPK research. In July 2025, WuXi AppTec DMPK published a book, “Drug Metabolism and Pharmacokinetics: Frontiers, Strategies, and Applications” with a leading academic publisher, Wiley, that addresses this need. Edited by Dr. Liang Shen and authored by over 100 scientists from WuXi AppTec DMPK, this book compiles 68 chapters that merge two decades of research with practical strategies to tackle complex DMPK challenges in novel therapeutics.

Beyond Theory: Best DMPK Practices for Novel Drug Modalities

Conventional approaches for small molecules often fall short in the rapidly evolving landscape of novel drug modalities, where regulatory guidance is also limited. Leveraging WuXi AppTec DMPK’s extensive experience, this book delivers actionable strategies for today’s most transformative modalities. Representative chapters include:

• Antibody-Drug Conjugates (ADCs): DMPK characteristics and overall strategy, in vitro stability, biotransformation, and drug-to-antibody ratio (DAR) value determination, and identification of payload-related metabolites.

• Oligonucleotide (OLIGO) Drugs: Modification and delivery systems, integrated bioanalytical platforms (LC-MS, qPCR, LBA, fluorescence), metabolite identification, and characteristics of approved siRNA and ASO drugs.

• Peptide Drugs: ADME properties of approved peptide drugs, metabolic pathways, radiolabeling techniques, and their applications, overcoming bioanalytical complexities such as nonspecific binding and stability.

• Proteolysis-Targeting Chimeras (PROTACs): Strategies to enhance oral bioavailability, defining soft spots and metabolites, and de-risking DDI potential.

Identifying Distinctive DMPK Challenges in Targeted Therapeutic Areas

With an aging population and an increasing number of patients with chronic diseases, there is a growing demand for drug development in disease areas. Specific preclinical study models or methods need to be developed to address the characteristics resulting from different pathogeneses and modes of action, such as:

• Ophthalmic Drugs: Administration across multiple biological barriers (BBB), in vitro drug-melanin binding study, analytical challenges and strategies, and intricate experimental operations with in vivo samples.

• Central Nervous System Drugs: Techniques to enhance blood-brain barrier penetration (microdialysis, intrathecal injection), in vitro BBB permeability evaluation, and measurement      of free-drug concentration in brain tissues and plasma.

• Transdermal and Topical Drugs and Respiratory Drugs: In vitro permeation tests (IVPT), topical formulations, bioanalysis, inhalation devices, and preclinical PK strategies.

Discovering Toolbox: Front-Edge DMPK Methods and Strategies

With experience from over 1,700 IND/NDA filings, we formed mature methodologies and specifically established front-edge DMPK methods and strategies for challenging research. Massive validation studies were included in the book, substantiating the precision and reproducibility of methods.

• In Vitro ADME: RP-HPLC lipophilicity assessment, flux dialysis method for high protein-binding drugs, metabolic clearance of slowly metabolized compounds, transporter, and CYP and non-CYP metabolism.

• In Vivo Pharmacokinetics: Rodent and large animal studies, vehicle screening for higher exposure, and surgical models including liver biopsy and SPIP.

• Metabolite Identification: Metabolite profiling and identification, soft spots, reactive metabolites, and metabolite biosynthesis.

• Radiolabeled ADME: Quantitative whole-body autoradiography (QWBA), human mass balance, placental transfer, and milk excretion.

• Bioanalysis: High-throughput bioanalysis, high-resolution mass spectrometry, biomarkers, and bioanalytical strategies for intact proteins and nanobodies.

Concluding Remarks

Drug Metabolism and Pharmacokinetics: Frontiers, Strategies, and Applications represents more than academic knowledge—it equips researchers with actionable insights, innovative strategies, and time-saving methodologies. Whether tackling small molecules, biologics, or novel modalities, this guide serves to accelerate R&D from bench to bedside.

Interested in getting a free sample chapter on PROTAC or a discount code for purchasing this book from Wiley? Click to access more.

Talk to a WuXi AppTec expert today to get the support you need to achieve your drug development goals.

Committed to accelerating drug discovery and development, we offer a full range of discovery screening, preclinical development, clinical drug metabolism, and pharmacokinetic (DMPK) platforms and services. With research facilities in the United States (New Jersey) and China (Shanghai, Suzhou, Nanjing, and Nantong), 1,000+ scientists, and over fifteen years of experience in Investigational New Drug (IND) application, our DMPK team at WuXi AppTec are serving 1,600+ global clients, and have successfully supported 1,700+ IND applications.