Monoclonal antibodies: what are the pharmacokinetic and pharmacodynamic considerations for drug development?
Abstract
INTRODUCTION: The number of monoclonal antibodies available for clinical use and under development has dramatically increased in the last 10 years. Understanding their pharmacokinetics and pharmacodynamics is essential for selecting the right clinical candidate, correct dose and regimen for a target indication. AREAS COVERED: This article reviews the existing literature and knowledge of monoclonal antibodies. Specifically, the authors discuss monoclonal antibodies with respect to their pharmacokinetics (including absorption, distribution and elimination) and their pharmacodynamics. The authors also look at the pharmacokinetic/pharmacodynamic relationship, scaling from preclinical to clinical studies and selection of the first-in-human dose. EXPERT OPINION: Monoclonal antibodies have complex pharmacokinetic and pharmacodynamic characteristics that are dependent on several factors. Therefore, it is important to improve our understanding of the pharmacokinetics and pharmacodynamics of monoclonal antibodies from a basic research standpoint. It is also equally important to apply mechanistic pharmacokinetic/pharmacodynamic models to interpret the experimental results and facilitate efforts to predict the safety and efficacy of monoclonal antibodies.
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Factors influencing mAbs distribution to individual organs or tissues include drug-specific features such as binding affinity to target antigens, target internalization rate, mAb hydrophilicity, and charge, and tissue-specific features such as membrane structure and blood flow.
“Additional factors influencing mAbs distribution to individual organs or tissues include: drug‐specific features such as their binding affinity to specific target antigens, targets internalization rate,24 mAb hydrophilicity, charge,25 and tissue‐specific features such as membrane structure and blood flow.26”
From Tutorial on monoclonal antibody pharmacokinetics and its considerations in early development (2018) · cites this paper as [26]
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Self-citation
- Authors
- Deng, R., Jin, F., Prabhu, S., & Iyer, S.
- Affiliations
- Genentech (US)
- Merck & Co., Inc., Rahway, NJ, USA (United States) (US)
- Venue
- Expert Opinion on Drug Metabolism & Toxicology
- Publisher
- Informa UK Limited
- Published
- 2012-01-17
- Volume
- 8
- Issue
- 2
- Pages
- 141-160
- ISSN
- 1742-5255 (ISSN-L)
- 1744-7607
- OpenAlex
- W1969671154
- Cited by
- 126
- References
- 109
- Citations by year
- 2026: 4 · 2025: 5 · 2024: 5 · 2023: 7 · 2022: 8 · 2021: 7 · 2020: 6 · 2019: 10 · 2018: 11 · 2017: 13 · 2016: 9 · 2015: 19 · 2014: 6 · 2013: 13 · 2012: 3
- FWCI
- 1.76
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Expert Opinion on Drug Metabolism & Toxicology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Monoclonal and Polyclonal Antibodies Research
- Life Sciences › Immunology and Microbiology › Immunology › Biosimilars and Bioanalytical Methods
- Life Sciences › Immunology and Microbiology › Immunology › Immunotoxicology and immune responses
- Keywords
- monoclonal antibodies, pharmacokinetics, pharmacodynamics, pharmacokinetic-pharmacodynamic relationship, first-in-human dose selection, drug development
- MeSH terms
- Antibodies, Monoclonal, Humans, Drug Discovery
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
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