In LDS, particular attention is placed on the infections area.
Lead Discovery Siena is contributing to the discovery and development of multiple anti-infective agents including pre-clinical candidates.
The escalating trend of invasive fungal infections and the emerging drug resistance and poor patient outcome, clearly tell us that there is a meaningful and growing unmet need for new antifungal agents. At LDS, we are working on novel macrocyclic amidinourea derivatives with antifungal activity against azole-resistant Candida and Aspergillus strains in vitro and in vivo.
The emergence of multi-drug, extremely-drug, or even pan-drug resistant bacteria have revealed that therapeutic options in this area are strongly limited. LDS is developing a library of compounds active against various bacterial strains including XDR/PDR clinically - relevant Gram-negative pathogens (Linear guanidine derivatives, methods of preparation and uses thereof. WO 2016/055644 A1). Moreover, LDS is involved in microbiota-focused projects (collaborations) to prevent antibiotic-associated disorders (AAD, IBS, C. difficile infections) which has led to 4 patent applications
LDS is working on small molecule inhibitors of human protein DDX3 for the development of broad spectrum antivirals. The most advanced compound shows multiple antiviral activities and no cellular toxicity. PK and toxicity studies in rats confirmed a good safety profile and bioavailability of the compounds.
New biological targets and inhibitors for treating asthma are among the key challenges of the pharmaceutical research. We recently start a target-based drug discovery project looking for chitinase inhibitors to be used for the treatment of asthma.