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Review
. 2016 Jun 1:101:89-98.
doi: 10.1016/j.addr.2016.05.007. Epub 2016 May 13.

BDDCS, the Rule of 5 and drugability

Leslie Z Benet  1 , Chelsea M Hosey  1 , Oleg Ursu  2 , Tudor I Oprea  2
Affiliations
Review

BDDCS, the Rule of 5 and drugability

Leslie Z Benet et al. Adv Drug Deliv Rev. .

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.

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

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Figures

Figure 1
Figure 1
BDDCS Classes for Orally Dosed Drugs, Percentage of Drugs in Each Class and Prediction of Transporter Effects [16]
See this image and copyright information in PMC

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