Novel heterodimer antibiotics: a review of recent patent literature

There is a clear and urgent need for novel antibacterial agents that can address the concerns of growing resistance. This article details recent patent activity within the antibiotic field based on the emerging strategy of a multivalent approach to drug discovery. A range of heterodimer antibiotics are discussed, which consist of two antibacterial chemical classes covalently linked to afford compounds with the potential to engage multiple mechanisms of action. The possible benefits of such compounds include activity against drug-resistant bacteria, enhanced efficacy and duration, an expanded spectrum of activity and reduced potential for generating bacterial resistance. This exciting approach towards novel heterodimer antibiotics holds significant promise, but must overcome a range of challenges before yielding a successful medicine. Progress to date is encouraging and has resulted in three compounds entering clinical trials.