Abstract
The Biopharmaceutics Drug Disposition Classification system (BDDCS) is a four-class approach based on water solubility and extent of metabolism/permeability rate. Based on the BDDCS class to which a drug is assigned, it is possible to predict the role of metabolic enzymes and transporters on the drug disposition of a new molecular entity (NME) prior to its administration to animals or humans. Here, we report a total of 1475 drugs and active metabolites to which the BDDCS is applied. Of these, 379 are new entries, and 1096 are revisions of former classification studies with the addition of references for the approved maximum dose strength, extent of the systemically available drug excreted unchanged in the urine, and lowest solubility over the pH range 1.0–6.8 when such information is available in the literature. We detail revised class assignments of previously misclassified drugs and the literature analyses to classify new drugs. We review the process of solubility assessment for NMEs prior to drug dosing in humans and approved dose classification, as well as the comparison of Biopharmaceutics Classification System (BCS) versus BDDCS assignment. We detail the uses of BDDCS in predicting, prior to dosing animals or humans, disposition characteristics, potential brain penetration, food effect, and drug-induced liver injury (DILI) potential. This work provides an update on the current status of the BDDCS and its uses in the drug development process.Graphical abstract
Highlights
The Biopharmaceutics Drug Disposition Classification System (BDDCS), based on rate of membrane permeability/ extent of metabolism and solubility characteristics, was proposed by Wu and Benet (1) as a methodology to predict drug disposition properties
System (BCS) assignments with BDDCS assignments when the former are available; and review uses/insights that BDDCS classification provides in early drug development before a new molecular entity (NME) is dosed to animals or humans
It is worth noting that the Biopharmaceutics Classification System (BCS) class 4 drugs azathioprine, loperamide, meclizine, ribociclib, and selumetinib, utilizing the BDDCS classification based on the solubility values referenced here, would have made them eligible for a biowaiver
Summary
The Biopharmaceutics Drug Disposition Classification System (BDDCS), based on rate of membrane permeability/ extent of metabolism and solubility characteristics, was proposed by Wu and Benet (1) as a methodology to predict drug disposition properties. Almost all of these 257 drugs were assigned their BCS class based on the previous MDS solubility criterion, not the revised highest therapeutic dose criterion (3); in this compilation, we continue to use MDS in the BDDCS classification.
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
