ArticleClinical pharmacology and therapeutics2020
Does In Vitro Potency Predict Clinically Efficacious Concentrations?
Article in Clinical pharmacology and therapeutics, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 40 papers.
What it found
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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.
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Who cites it
40 citing papers in PubMed.
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- An organoid-guided roadmap for precision delivery of epigallocatechin gallate in oral submucous fibrosis.Frontiers in bioengineering and biotechnology · 2026Review
- Drug Discovery and Repurposing forJournal of fungi (Basel, Switzerland) · 2025Review
- Investigating of harmane, harmine, and norharman as inhibitors of MDR1 and MRP1 to overcome chemotherapy resistance in cancer cells.Scientific reports · 2025Article
- Pharmacoepigenomic effects of anti-hypertensive drugs on DNA methylation and its implication to drug response and side effects.Epigenomics · 2025Article
- Preclinical Animal Models to Investigate the Role of NaLife (Basel, Switzerland) · 2025Review
- Antioxidant and neuroprotective effects of nutriosomes and grape pomace phytochemicals in a cell model of oxidative stress and mouse model of Parkinson disease.Scientific reports · 2025Article
- Characterization of trazodone metabolic pathways and species-specific profiles.Frontiers in pharmacology · 2025Article
- Trends of in vitro pharmacological potency and in vivo pharmacokinetics parameters of modern drugs: Can the therapeutic/subtherapeutic dose be estimated from in vitro KClinical and translational science · 2024Article
Corrections and comments
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Authors and funding
3 authors.
Funding
Abstract
The in vitro affinity of a compound for its target is an important feature in drug discovery, but what remains is how predictive in vitro properties are of in vivo therapeutic drug exposure. We assessed the relationship between in vitro potency and clinically efficacious concentrations for marketed small molecule drugs (n = 164) and how they may differ depending on therapeutic indication, mode of action, receptor type, target localization, and function. Approximately 70% of compounds had a therapeutic unbound plasma exposure lower than in vitro potency; the median ratio of exposure in relation to in vitro potency was 0.32, and 80% had ratios within the range of 0.007 to 8.7. We identified differences in the in vivo-to-in vitro potency ratio between indications, mode of action, target type, and matrix localization, and whether or not the drugs had active metabolites. The in vitro-assay variability contributions appeared to be the smallest; within the same drug target and mode of action the within-variability was slightly broader; but both were substantially less compared with the overall distribution of ratios. These data suggest that in vitro potency conditions, estimated in vivo potency, required level of receptor occupancy, and target turnover are key components for further understanding the link between clinical drug exposure and in vitro potency.
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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.