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LEAD DISCOVERY SIENA

Lead Discovery Siena (LDS) is a SME focused on the research for new drugs and providing services in drug discovery. LDS actively participates to national and international projects, with a special attention to local synergies at industrial and academic level within the Life Science area.
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DISCOVERY SERVICES

Lead Discovery Siena offers: Integrated medicinal chemistry services / A wide range of biological services / Specific expertise in anticancer agent bioconjugation with antibodies
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TRANSLATING SCIENCE INTO DRUGS

A multi facet approach for an efficient drug discovery process

Lead Discovery Siena is a SME providing tools and expertise to develop drug discovery programs. 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.

COMPANY OVERVIEW

LDS was founded as a spin-off of the University of Siena in 2012 by combining the scientific background and the entrepreneurship of its management to offer specific competences and solutions in drug discovery

MISSION STATEMENT

Lead Discovery Siena mission is to contribute to human health by fostering progress in both basic and applied research for new effective medicines in specific therapeutic areas. Find out more about our mission.

PORTFOLIO

LDS offers products and expertise in a wide range of therapeutic areas ranging from oncology to infections. LDS is looking for suitable opportunities to combine experience and resources with other organisations.

THERAPEUTIC AREAS

LDS offers products and expertise in a wide range of therapeutic areas ranging from oncology to infections.

LDS is looking for suitable opportunities to combine experience and resources with other organisations where specific projects may benefit in the form either of collaborations at various phases during the life of a program or through out-licensing of specific small molecules or classes.

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 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.

DISCOVERY SERVICES

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.

Integrated medicinal chemistry services, including computational chemistry, synthesis, ADME/PK and biological testing to guide and support the design and development of a new potential drug up to pre-clinical phase, through small molecule rational design, pharmacological and physico-chemical profiling.

A wide range of biological services to support drug discovery and optimization programmes including protein production and purification, assay development and validation, target-based and whole-cell HTS and compound profiling, optimization of biologicals (therapeutic proteins) and protein engineering.

Specific expertise in anticancer agent bioconjugation with antibodies, including development of conjugation techniques with custom antibodies, development of attaching mode of custom toxins to antibodies, development of proprietary antibodies bioconjugated with innovative mode of action.

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