Prioritization of potential targets appropriate for the development of “best-in-class” drugs

Aim of the project:

To evaluate the potential benefits/risks of development of “best-in-class” anti-asthmatic drugs for 2 potential targets: cysteinyl leukotriene receptor 1 (cysLT1R) vs. 5-lipoxygenase (5LO).


A systems pharmacology model describing the effects of Zileuton and Montelukast on FEV1 of asthmatic patients was developed. Zileuton inhibits 5LO, while Montelukast binds with cysLT1R. The model allows us to compare the ability of marketed dosages of the drugs to increase FEV1 – a key clinically measured end-point characterizing the stage and development of asthma. It was found that marketed dosages of Zileuton were more effective than those of Montelukast. The model predicted that cysLT1R was the more appropriate target for the development of “best-in-class” anti-asthmatic drugs.

Initiator of the project:

Institute for Systems Biology

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