Polypharmacology in a Single Drug: Multitarget Drugs
M. L. Bolognesi.
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 demand for safer, more effective, and affordable medicines
against the most complex diseases, and by the failures of modern drug discovery to provide these. Polypharmacology
can involve combinations and/or multitarget drugs (MTD). Although not mutually exclusive, my premise is that
MTDs have inherent advantages over combinations. This review article focuses on MTDs from a medicinal chemistry
perspective. I will explore their use in current clinical practice, their likely application in the future, and the challenges to
be overcome to achieve this goal.
Keywords: Multifactorial diseases, Combination therapy, multitarget drug discovery, network pharmacology, multitargetdirected
ligands, designed multiple ligands
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