Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Concept Videos

Drug Product Performance: In Vitro–In Vivo Correlation01:20

Drug Product Performance: In Vitro–In Vivo Correlation

168
In pharmaceutical development, it's crucial to establish a predictive in vitro–in vivo correlation (IVIVC) for two or more formulations to gain a comprehensive understanding of release properties. IVIVC reduces the need for costly in vivo studies and facilitates the establishment of meaningful dissolution specifications with significant cost savings and decreased regulatory burden. Furthermore, a meaningful IVIVC should predict Cmax and AUC within 20%, aligning with FDA guidance while...
168
Dose-Response Relationship: Potency and Efficacy01:22

Dose-Response Relationship: Potency and Efficacy

6.2K
The potency of a drug is the measure of its ability to produce a biological response and can be compared by looking at the half-maximum effective concentration or EC50 values of different drugs. A lower EC50 value indicates higher potency of the drug. In the dose–response curve of two antihypertensive drugs, candesartan and irbesartan, a significant difference is observed in their EC50 values. A lower EC50 value for candesartan indicates that it is more potent than irbesartan, as it...
6.2K
Clinically Relevant Drug Product Specifications: Methods of Establishment01:29

Clinically Relevant Drug Product Specifications: Methods of Establishment

130
Product specifications define the acceptable quality of a pharmaceutical product by ensuring identity, purity, potency, and strength. These specifications serve as benchmarks during development, manufacturing, and post-approval quality control. Clinically relevant specifications are particularly important because they directly relate to a drug's safety and efficacy in clinical use.Dissolution studies are critical biopharmaceutic tools that link in vitro behavior to in vivo performance. They...
130
In Vitro Drug Release Testing: Overview, Development and Validation01:10

In Vitro Drug Release Testing: Overview, Development and Validation

227
In vitro dissolution and drug release tests assess how quickly and how much of a drug is released from its dosage form into an aqueous medium under standardized laboratory conditions. These tests are essential tools in pharmaceutical development and quality assurance, offering insight into the drug's performance before clinical use.During formulation development, dissolution testing identifies incomplete or inconsistent drug release issues. It also supports decisions on selecting the optimal...
227
In Vitro Drug Dissolution: Compendial Testing Models I01:13

In Vitro Drug Dissolution: Compendial Testing Models I

159
Compendial dissolution methods are standardized procedures defined by pharmacopeias to evaluate the rate at which a drug dissolves in a specific medium. These methods ensure batch-to-batch consistency, enable quality control, and support the prediction of drug bioavailability. They are critical for both immediate and modified-release drug products.The apparatuses used for dissolution testing differ in their design and mechanical function, but all aim to simulate the physiological environment of...
159
In Vitro Drug Dissolution: Compendial Testing Models II01:09

In Vitro Drug Dissolution: Compendial Testing Models II

158
Various dissolution methods are utilized to assess a drug’s dissolution rate, including the flow-through cell, paddle-over-disk, cylinder, and reciprocating disk methods.The flow-through cell apparatus (USP (United States Pharmacopeia) method 4) comprises a reservoir for the dissolution medium and a pump that propels the medium through the cell containing the test sample. This method is crucial for assessing modified-release dosage forms with minimally soluble active ingredients,...
158

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

Application of Virtual Twin PBPK Models in Individuals with Obesity via CYP3A4 Phenotyping Using Endogenous Biomarker Data.

Clinical pharmacology and therapeutics·2026
Same author

Systemic Pharmacokinetic Principles of Therapeutic Peptides.

Clinical pharmacokinetics·2026
Same author

Virtual Twin-PBPK Modelling: A Step Toward Precision Dosing in Patients with Obesity.

The AAPS journal·2026
Same author

Pharmacokinetics of Racemic Eflornithine in Human Plasma and Cerebrospinal Fluid: Clinical Perspectives for L-eflornithine Against Human African Trypanosomiasis.

The AAPS journal·2025
Same author

Cariprazine and clozapine: a systematic review of a promising antipsychotic combination for treatment-resistant schizophrenia.

The international journal of neuropsychopharmacology·2025
Same author

Translational PK/PD: a retrospective analysis of performance and impact from a drug portfolio.

Drug discovery today·2025
Same journal

Symposium Report: Stakeholders' Perspectives on Phase 1 Trials in Japanese Prior to Multi-Regional Clinical Trials and Future Pathways.

Clinical pharmacology and therapeutics·2026
Same journal

Resolving CYP2D6 Structural Complexity with Long-Read Sequencing: Implications for Tamoxifen Precision Dosing in Thai Breast Cancer Patients.

Clinical pharmacology and therapeutics·2026
Same journal

Identification of a Functional CYP2C8 Variant Allele that Alters Splicing, Reduces Protein Expression, and Increases Drug Exposure.

Clinical pharmacology and therapeutics·2026
Same journal

Risk of Hyperkalemia in Patients with Heart Failure Treated with Spironolactone in Combination with Sacubitril/Valsartan vs. Renin-Angiotensin System Inhibitors.

Clinical pharmacology and therapeutics·2026
Same journal

Composite Endpoints in Contemporary Cardiovascular Trials: Trends in Phase 3 Trials and Key Issues in Regulatory Review.

Clinical pharmacology and therapeutics·2026
Same journal

Patient-Specific Determinants of Response to BCMA- and GPRC5D-Targeted CAR T-Cell Therapy in Multiple Myeloma: A QSP Analysis of Clinical Trial and Real-World Data.

Clinical pharmacology and therapeutics·2026
See all related articles

Related Experiment Video

Updated: Dec 24, 2025

Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms
08:46

Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms

Published on: December 9, 2015

11.0K

Does In Vitro Potency Predict Clinically Efficacious Concentrations?

Rasmus Jansson-Löfmark1, Stephan Hjorth2,3, Johan Gabrielsson4

  • 1DMPK, Research and Early Development Cardiovascular, Renal and Metabolism, BioPharmaceuticals R&D, AstraZeneca, Gothenburg, Sweden.

Clinical Pharmacology and Therapeutics
|April 11, 2020
PubMed
Summary
This summary is machine-generated.

In drug discovery, in vitro potency is often predictive of in vivo drug exposure. Most drugs show therapeutic unbound plasma exposure lower than their in vitro potency, with variations by indication and drug properties.

More Related Videos

Broth Microdilution In Vitro Screening: An Easy and Fast Method to Detect New Antifungal Compounds
08:54

Broth Microdilution In Vitro Screening: An Easy and Fast Method to Detect New Antifungal Compounds

Published on: February 14, 2018

19.8K
System for Efficacy and Cytotoxicity Screening of Inhibitors Targeting Intracellular Mycobacterium tuberculosis
09:57

System for Efficacy and Cytotoxicity Screening of Inhibitors Targeting Intracellular Mycobacterium tuberculosis

Published on: April 5, 2017

9.0K

Related Experiment Videos

Last Updated: Dec 24, 2025

Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms
08:46

Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms

Published on: December 9, 2015

11.0K
Broth Microdilution In Vitro Screening: An Easy and Fast Method to Detect New Antifungal Compounds
08:54

Broth Microdilution In Vitro Screening: An Easy and Fast Method to Detect New Antifungal Compounds

Published on: February 14, 2018

19.8K
System for Efficacy and Cytotoxicity Screening of Inhibitors Targeting Intracellular Mycobacterium tuberculosis
09:57

System for Efficacy and Cytotoxicity Screening of Inhibitors Targeting Intracellular Mycobacterium tuberculosis

Published on: April 5, 2017

9.0K

Area of Science:

  • Pharmacology
  • Drug Discovery
  • Medicinal Chemistry

Background:

  • In vitro compound affinity is crucial for drug discovery.
  • Predicting in vivo therapeutic drug exposure from in vitro data remains a challenge.

Purpose of the Study:

  • To assess the relationship between in vitro potency and in vivo efficacious concentrations for marketed small molecule drugs.
  • To identify factors influencing the in vivo-to-in vitro potency ratio.

Main Methods:

  • Analysis of 164 marketed small molecule drugs.
  • Comparison of in vitro potency with clinically efficacious concentrations.
  • Evaluation of differences based on therapeutic indication, mode of action, receptor type, target localization, and active metabolites.

Main Results:

  • Approximately 70% of compounds exhibited therapeutic unbound plasma exposure lower than their in vitro potency.
  • The median ratio of in vivo exposure to in vitro potency was 0.32 (range 0.007–8.7 for 80% of compounds).
  • Significant differences in the in vivo-to-in vitro potency ratio were observed across various drug and target characteristics.

Conclusions:

  • In vitro assay variability is a minor contributor to the observed ratios.
  • In vitro potency, estimated in vivo potency, receptor occupancy, and target turnover are key to understanding the drug exposure-potency link.
  • Understanding these relationships can refine drug development strategies.