Literature DB >> 27182629

BDDCS, the Rule of 5 and drugability.

Leslie Z Benet1, Chelsea M Hosey1, Oleg Ursu2, Tudor I Oprea2.   

Abstract

The Rule of 5 methodology appears to be as useful today in defining drugability as when it was proposed, but recognizing that the database that we used includes only drugs that successfully reached the market. We do not view additional criteria necessary nor did we find significant deficiencies in the four Rule of 5 criteria originally proposed by Lipinski and coworkers. BDDCS builds upon the Rule of 5 and can quite successfully predict drug disposition characteristics for drugs both meeting and not meeting Rule of 5 criteria. More recent expansions of classification systems have been proposed and do provide useful qualitative and quantitative predictions for clearance relationships. However, the broad range of applicability of BDDCS beyond just clearance predictions gives a great deal of further usefulness for the combined Rule of 5/BDDCS system.
Copyright © 2016 Elsevier B.V. All rights reserved.

Entities:  

Keywords:  BCS; BDDCS; Biliary elimination; Drug-likeness; Metabolism; Renal elimination; Rule of 5

Mesh:

Substances:

Year:  2016        PMID: 27182629      PMCID: PMC4910824          DOI: 10.1016/j.addr.2016.05.007

Source DB:  PubMed          Journal:  Adv Drug Deliv Rev        ISSN: 0169-409X            Impact factor:   15.470


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