PMID: 2093625Jan 1, 1990Paper

Measurement of free drug in phase I: is it useful?

Fundamental & Clinical Pharmacology
J BarréJ P Tillement

Abstract

Early investigation of protein binding of a new drug is mandatory. The following questions have to be answered: is unbound fraction constant over tested concentrations? Which proteins are involved? What are the binding parameters? Can the drug compete with other therapeutic agents for the binding sites or in other words can drug displacements be predicted? What is the interindividual variability in protein binding? Is the binding stereoselective? All this information is necessary in predicting the pharmacokinetic behaviour of the drug and in assisting in the design of future pharmacokinetic protocols in phases II and III. The use of free drug concentration should also be considered when comparing the bioavailability of regular vs sustained release dosage forms of drugs exhibiting concentration-dependent binding and when studying concentration-effect relationships.

References

Sep 1, 1989·Journal of Pharmaceutical Sciences·F JamaliF M Pasutto
Jan 1, 1988·Therapeutic Drug Monitoring·J BarreJ P Tillement
Nov 1, 1986·Clinical Pharmacokinetics·C K SvenssonD Lalka
Feb 1, 1987·Journal of Pharmacokinetics and Biopharmaceutics·M YasuharaC Kawai
Jul 1, 1986·Clinical Pharmacology and Therapeutics·C H KleinbloesemD D Breimer
Aug 1, 1986·Journal of Pharmacokinetics and Biopharmaceutics·R A Upton, R L Williams
Jan 1, 1984·Pharmacology·E AlbengresJ P Tillement
Dec 1, 1984·Journal of Pharmacokinetics and Biopharmaceutics·M ThibonnierR L Williams
Aug 1, 1982·Clinical Pharmacology and Therapeutics·E Pike, B Skuterud

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Citations

Jun 4, 2011·Expert Opinion on Drug Metabolism & Toxicology·Mario PellegattiDimitri Colato
Dec 29, 2005·Journal of Clinical Oncology : Official Journal of the American Society of Clinical Oncology·David M GoldenbergJean-François Chatal

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