Drug Repurposing

Drug repurposing is the search for new indications or molecular targets distinct from a drug’s putative activity, pharmacological effect, or binding specificities. It involves establishing new therapeutic uses for already known drugs, including approved, discontinued, abandoned, and experimental drugs. This new approach to drug repositioning is likely to be adopted by traditional drug discovery programs by reducing high cost, longer development time, and increased risk of failure. With the increasing rate of drug termination in clinical trials, drug repositioning has become one of the effective ways to against the risk of drug failure.

Approaches of Drug Repurposing

Systematic repurposing approaches can be largely divided into experimental screening approaches and in silico approaches.

Experimental screening approaches are used as a source of hits for both drug discovery and drug repurposing, with notable differences in their application and outcomes. Experimental screening approaches are used as a source of hits for drug discovery and drug repurposing, and they vary significantly in application and results. Repurposing programs focus on known molecules that are either approved or not, but have some knowledge of their safety or MoA, through in-depth screening, and use smaller libraries of compounds. Another key difference between drug discovery and repurposing is the fate of the hits. For a repurposing screen, a compelling hit is a drug molecule that is a candidate to be advanced into development. For drug discovery screens, an efficient assay must be simple and fast to manage the number of potential compounds for review, whereas for repurposing screens, the limited scale allows a broader range of complexity of assay types. The ability of multiple independent screens to identify similar classes of a compound and the potential to advance repurposing hits rapidly into clinical development effectively highlight the potential of repurposing screens.

In silico repurposing approaches apply sophisticated analytical methods to existing data identifying new potential associations between drug and disease. Approaches can be broadly divided into two categories: (i) molecular approaches, which are based on the understanding of drug activity and disease pathophysiology and are often powered by large-scale molecular data, and (ii) RWD approaches, focusing on identification of unknown, and at times unexpected, relationships between drugs and diseases or their symptoms.

Approaches of drug repositioning. Fig.1 Approaches of drug repositioning. (Mithun, 2020)

Opportunities and Challenges

On contrary to traditional drug discovery programs (a complex and time-consuming process with a high cost of development and risk of failure), drug repositioning reduces the time and cost of drug development. Drug repositioning is also a low-risk strategy. The computational or machine learning approach has significantly improved the performance of drug repositioning. In recent years computational approaches are usually combined with the experimental approaches to identify new indications for old drugs, called mixed approaches. Drug repositioning offers an opportunity for many pharmaceutical companies to develop drugs with lower investments. With the advent of technologies such as genomics, proteomics, transcriptomics, metabolomics, etc., and the availability of huge databases resources including drug omics data, disease omics data, etc., there are plenty of opportunities to discover drugs by drug repositioning in a collective and integrated effort of all the above methods/approaches mentioned above. In recent years, drug repurposing has emerged as a viable strategy to increase the overall productivity of drug discovery.

Drug repurposing can be successfully utilized in the discovery and development of new drugs with novel and effective therapeutic indications for human diseases. Creative Biolabs is a biotechnology company. We specialize in drug discovery and development. Our goal is to simply provide the highest quality pharmaceutical services to our customers. Years of experience and knowledge flood our labs and facility to ensure the best processes and practices. Please feel free to contact us for details.


  1. Mithun, R.; et al. Drug Repurposing (DR): An Emerging Approach in Drug Discovery, Drug Repurposing - Hypothesis, Molecular Aspects and Therapeutic Applications. IntechOpen. July 13th 2020.
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