Company Overview
Lead Discovery Siena (LDS) is a start-up and innovative PMI focused on the research for new drugs, actively participates to national and international projects, with a special attention to local synergies at industrial and academic level within the Life Science area. LDS offers pharmaceutical services for Industry and Academia and has a diversified pipeline of in licensed and proprietary products for oncology and infections therapeutic areas, including rare diseases. Our focus is to foster the design and development of early drug discovery campaigns up to pre-clinical phases.

LDS has developed a wide expertise on Src Family Kinase inhibitors as therapeutic intervention against a number of cancers. In vitro and in vivo studies have been conducted to advance most promising compounds, including PK, tolerability and efficacy in animal models. Current lead compound shows a clear efficacy in intracranial model of glioblastoma multiforme (GBM) in mice. In vivo PK studies confirmed the ability of the compound to cross the BBB. More recently, a novel target, the protein DDX3, became part of the oncology arsenal at LDS. In vitro studies are currently on going to profile a library of DDX3 inhibitors. Moreover, LDS is actively working in the field of Antibody Drug Conjugates (ADC) for tumor targeting and has developed a proprietary ADC technology that comprises some sophisticated linker and conjugation technologies for any kind of highly cytotoxic agent.

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 clinically Gram-negative pathogens. 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.

Our clients take advantage of our knowledge and competences to expedite their drug discovery programmes.
Services can be accessed as standalone projects or may be integrated as a part of a medicinal chemistry optimization programme to build customized solutions to meet drug discovery needs, from hit identi­fication and follow-up, to lead optimization and back-up identi­fication. Competencies include dealing with pharmaco-kinetics and -dynamics, solubility and permeability issues, toxicity and side effects.