Overview of the Approaches and Challenges in Drug-Repurposing for New Therapeutics Development
Charlene Pillay, Ravikant Ranjan · 2026
Traditional drug development is a lengthy, costly, and high-risk process underscoring the need for a more efficient alternative. Drug repurposing (or drug repositioning) has emerged as an alternative drug development tool and promising strategy by identifying and exploiting new therapeutic uses for numerous compounds already approved for clinical use. This approach enables the discovery and development of drug molecules with novel pharmacological and therapeutic potential in a more efficient, cost-effective, and time-saving manner. Drug repurposing complements traditional drug design and development particularly for rare diseases. The advent of analytical methods of pharmacological compounds in terms of molecular, genomic, and phenotypic data has led to the emergence of computational drug repurposing through experimental and in silico approaches. The three main categories involved in drug repurposing are drug-oriented, target-oriented, and disease or therapy-oriented, related to the physico-chemical, biological, pharmacological, toxicological, and pharmacokinetic properties of drug molecules. This chapter explores the various strategies employed in drug repurposing, and highlights the major challenges and the future perspectives for its continued role in therapeutic innovation.