Drug selection is one of the important steps in new drug development. There are multiple factors that contribute to new drug formulation. Biopharmaceutical considerations along with physiological and pharmaceutical parameters are more helpful in defining the process. Various GIT restrictive barriers are challenges for many new drug developments. New drug formulation advantages over the traditional molecules should be cost-effective, therapeutically superior and compliant as compared to previously used active agents. Drug selection compromises multiple steps including preliminary studies in the lab (screening) to the formulation of the dosage form to in-vitro studies along with in-vivo studies. These led to the clinical trials after the selection had been made. Wide drug selection techniques are employed to save costs along with adverse drug effect profiles. It also includes safety for animal studies and in humans.