Due to the complexity of multifactorial diseases, single-target drugs do not always exhibit
satisfactory efficacy. Recently, increasing evidence indicates that simultaneous modulation …

The development of multitarget-directed ligands (MTDLs) has become a widely focused
research topic, but rational design remains as an enormous challenge. This paper reviews …

The dominant paradigm in drug discovery is to design ligands with maximum selectivity to
act on individual drug targets. With the target-based approach, many new chemical entities …

It has been widely recognised over the recent years that parallel modulation of multiple
biological targets can be beneficial for treatment of diseases with complex etiologies such as …

Polypharmacology offers a model for the way drug discovery must evolve to develop
therapies most suited to treating currently incurable diseases. It is driven by a worldwide …

Drugs designed to act against individual molecular targets cannot usually combat multigenic
diseases such as cancer, or diseases that affect multiple tissues or cell types such as …

It is essential to acknowledge the efforts made thus far to manage or eliminate various
disease burden faced by humankind. However, the rising global trends of the so-called …

For much of the past century, drug discovery relied largely on the use of animal models of
disease as the first-line screens for testing the compounds produced by medicinal chemists …

At present, the legendary magic bullet, ie, a drug with high potency and selectivity toward a
specific biological target, shares the spotlight with an emerging and alternative …

Multitargeting compounds comprising activity on more than a single biological target have
gained remarkable relevance in drug discovery owing to the complexity of multifactorial …