Designing safer oral drugs.

ABSTRACT: Designing an oral drug such that its estimated dose to humans is both efficacious and safe is challenging. During the early design stage, where in vitro or preclinical species in vivo safety data are limited, heuristic-based criteria often related to physicochemical properties are used for guidance. The causal relationship between a compound's log P and its human in vivo toxicity is considered. With respect to designing efficacious oral drugs that potentially have reduced toxicity liabilities, an alternative heuristic-based criterion is proposed based on the amount of compound in the body at steady state. In humans, a threshold for the amount of compound in the body at steady state of 0.5 mg kg^-1 is suggested. The criterion is based on the minimum tox

SUBMITTER: Wenlock MC 

PROVIDER: S-EPMC6072361 | biostudies-literature | 2017 Mar

REPOSITORIES: biostudies-literature