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

Fundamental & clinical pharmacology

Barré J, Riant P, Tillement JP.
PMID: 2093625
Fundam Clin Pharmacol. 1990;4:141s-150s. doi: 10.1111/j.1472-8206.1990.tb00072.x.

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...

The influence of food on the absorption and metabolism of drugs: an update.

European journal of drug metabolism and pharmacokinetics

Williams L, Hill DP, Davis JA, Lowenthal DT.
PMID: 8980916
Eur J Drug Metab Pharmacokinet. 1996 Jul-Sep;21(3):201-11. doi: 10.1007/BF03189714.

Food-drug interactions can lead to a loss of therapeutic efficacy or toxic effects of drug therapy. Generally, the effect of food on drugs results in a reduction in the drug's bioavailability; however, food can also alter drug clearance. The...

For medicinal purposes.


Petsko GA.
PMID: 8895592
Nature. 1996 Nov 07;384(6604):7-9. doi: 10.1038/384007a0.

Developments in techniques of pharmaceutical chemistry are poised to revolutionize the design of drugs beyond previous expectations. But what are our current expectations and what does the future hold?

Early ADME in support of drug discovery: the role of metabolic stability studies.

Current drug metabolism

Thompson TN.
PMID: 11465046
Curr Drug Metab. 2000 Nov;1(3):215-41. doi: 10.2174/1389200003339018.

The area of Drug Discovery has undergone an amazing evolution in the past decade. This evolution is typified by the development of automated combinatorial synthesis and high throughput pharmacological testing. This, in turn, has lead to the ability to...

Metabolism profiling, and cytochrome P450 inhibition & induction in drug discovery.

Current topics in medicinal chemistry

Yan Z, Caldwell GW.
PMID: 11899105
Curr Top Med Chem. 2001 Nov;1(5):403-25. doi: 10.2174/1568026013395001.

To reduce the high attrition rates of NCEs in preclinical and clinical development uncovering pharmacokinetics, toxicokinetics, drug metabolism, and drug-drug interactions early in drug discovery would be highly valuable. There have been many in vitro screens developed for these...

The long, hard road: drug metabolism in the lifetime of the DMDG.

Xenobiotica; the fate of foreign compounds in biological systems

Smith DA.
PMID: 11569522
Xenobiotica. 2001 Aug-Sep;31(8):459-67. doi: 10.1080/00498250110052742.

No abstract available.

Do drug metabolism and pharmacokinetic departments make any contribution to drug discovery?.

Clinical pharmacokinetics

Smith D, Schmid E, Jones B.
PMID: 12403640
Clin Pharmacokinet. 2002;41(13):1005-19. doi: 10.2165/00003088-200241130-00001.

The alignment of drug metabolism and pharmacokinetic departments with drug discovery has not produced a radical improvement in the pharmacokinetic properties of new chemical entities. The reason for this is complex, reflecting in part the difficulty of combining potency,...

Drug metabolism and pharmacokinetics in drug discovery.

Current opinion in drug discovery & development

Roberts SA.
PMID: 12613278
Curr Opin Drug Discov Devel. 2003 Jan;6(1):66-80.

The discovery and development of new drugs seems to be an inefficient process, since too few new chemical entities (NCEs) successfully make it to the market. Because one of the main reasons for failure in development is thought to...

In Silico and Ex silico ADME approaches for drug discovery.

Current topics in medicinal chemistry

Darvas F, Keseru G, Papp A, Dormán G, Urge L, Krajcsi P.
PMID: 12470281
Curr Top Med Chem. 2002 Dec;2(12):1287-304. doi: 10.2174/1568026023392841.

The high attrition rate of drug candidates during clinical trials for poor pharmacokinetic and metabolic properties has created a need to do these studies as early as it is possible during the drug discovery process. In addition the most...

Computational approaches to the understanding of ADMET properties and problems.

Drug discovery today

Modi S.
PMID: 12867147
Drug Discov Today. 2003 Jul 15;8(14):621-3. doi: 10.1016/s1359-6446(03)02739-9.

No abstract available.

Rho Chi lecture. Pharmaceutical sciences in the next millennium.

The Annals of pharmacotherapy

Triggle DJ.
PMID: 10084422
Ann Pharmacother. 1999 Feb;33(2):241-6. doi: 10.1345/aph.18337.

Even a cursory survey of this article suggests that the pharmaceutical sciences are being rapidly transformed under the influence of both the new technologies and sciences and the economic imperatives. Of particular importance are scientific and technological advances that...

Applications of protein arrays for small molecule drug discovery and characterization.

Biotechnology & genetic engineering reviews

Michaud GA, Salcius M, Zhou F, Papov VV, Merkel J, Murtha M, Predki P, Schweitzer B.
PMID: 18476332
Biotechnol Genet Eng Rev. 2006;22:197-211. doi: 10.1080/02648725.2006.10648071.

No abstract available.

Showing 1 to 12 of 132 entries