ReviewThe AAPS journal2012
Applications of human pharmacokinetic prediction in first-in-human dose estimation.
Review in The AAPS journal, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 50 papers, 2 of them syntheses that pooled it.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
50 citing papers in PubMed, 2 syntheses or guidelines pooled it.
- Utility of physiologically based pharmacokinetic (PBPK) modeling in oncology drug development and its accuracy: a systematic review.European journal of clinical pharmacology · 2018Pooled it
- Determination of the starting dose in the first-in-human clinical trials with monoclonal antibodies: a systematic review of papers published between 1990 and 2013.Drug design, development and therapy · 2016Pooled it
- Trial
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- Predicting Efavirenz Concentrations in the Brain Tissue of HIV-Infected Individuals and Exploring their Relationship to Neurocognitive Impairment.Clinical and translational science · 2019Trial
- Population Pharmacokinetic Modeling of the Enterohepatic Recirculation of Fimasartan in Rats, Dogs, and Humans.The AAPS journal · 2015Trial
- Integrating in vitro aerosol characterization and cross-species PBPK modeling to predict human lung exposure of inhaled therapeutic proteins.International journal of pharmaceutics: X · 2026Article
- Innovative Clinical Pharmacology, Modeling, and Simulation Strategies for Accelerating Rare Disease Drug Development.Journal of clinical pharmacology · 2026Review
- First-in-Human Dose Selection, Pharmacokinetics Prediction, and Clinical Validation of SYHA1805, a Novel FXR Agonist, Using Allometric Scaling and PBPK Modeling.Pharmaceutics · 2026Article
- Beyond Body Weight: A Comprehensive Review of Allometric Scaling in Drug Development for Human Dose Predictions.Pharmaceutics · 2026Review
- Development and Validation of an LC-MS/MS Method for the Quantitation of JNJ-64619178 (JNJ) in Mouse Plasma: Characterization of In Vitro and In Vivo Pharmacokinetic Properties.Molecules (Basel, Switzerland) · 2026Article
- The Cannabinoid CBInternational journal of molecular sciences · 2025Article
- Fraction-based Linear Extrapolation (FLEX) Method for Predicting Human Pharmacokinetic Clearance: Advanced Allometric Scaling Method and Machine Learning Approach.Pharmaceutical research · 2025Article
- A new paradigm for drug discovery in the treatment of complex diseases: drug discovery and optimization.Chinese medicine · 2025Review
- Prediction of first-in-human dose for new composition bee venom based on allometric scaling and pharmacokinetic modeling approach.Translational and clinical pharmacology · 2025Article
- Model-informed drug development for antimicrobials: translational pharmacokinetic-pharmacodynamic modelling of apramycin to facilitate prediction of efficacious dose in complicated urinary tract infections.The Journal of antimicrobial chemotherapy · 2025Article
- Physiological liver microtissue 384-well microplate system for preclinical hepatotoxicity assessment of therapeutic small molecule drugs.Toxicological sciences : an official journal of the Society of Toxicology · 2025Article
- Model-informed drug discovery and development approaches to inform clinical trial design and regulatory decisions: A primer for the MENA region.Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2024Review
- Advances in Physiologically Based Pharmacokinetic (PBPK) Modeling of Nanomaterials.ACS pharmacology & translational science · 2024Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors.
Funding
Abstract
Quantitative estimations of first-in-human (FIH) doses are critical for phase I clinical trials in drug development. Human pharmacokinetic (PK) prediction methods have been developed to project the human clearance (CL) and bioavailability with reasonable accuracy, which facilitates estimation of a safe yet efficacious FIH dose. However, the FIH dose estimation is still very challenging and complex. The aim of this article is to review the common approaches for FIH dose estimation with an emphasis on PK-guided estimation. We discuss 5 methods for FIH dose estimation, 17 approaches for the prediction of human CL, 6 methods for the prediction of bioavailability, and 3 tools for the prediction of PK profiles. This review may serve as a practical protocol for PK- or pharmacokinetic/pharmacodynamic-guided estimation of the FIH dose.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.