Microdosing offers a technique to augment drug development by commencing human studies earlier to Phase 1 studies. A systematic search for articles in the PubMed was performed MedLine up to August 2012. The rationale is to support in the go versus no-go decision-making process and to reject early non-promising molecules from the drug pipeline. Selection of several probable frontrunners can be accomplished at the clinical stage instead of in preclinical studies. The microdosing technique can be easily utilized for a molecularly targeted promising drug compound with a known mechanism of action. It offers beneficial data concerning accessibility and biodistribution that can be used in many assessments furthering the development of the molecule. However, the use of microdose pharmacokinetic studies as a vital tool in drug development is still to catch on. While this methodology assures probable expenditure reductions and a significant increase in productivities of the drug development practice, foremost obstacles still must be overcome before the procedure becomes routine practice. Clear guidelines in Europe and the USA have had a supporting effect. The dearth of permitting requirements for microdosing studies in Indian regulation, in spite of low-risk and obvious application for the local drug development industry, is inconsistent with the nation's hopes to be among the bests in pharmaceutical research.