Spanish National Cancer Research Centre (CNIO) / Experimental Therapeutics

Therapeutic Approaches: Small Molecules

Therapeutic Areas of Expertise: Oncology

Center/Program Highlights: The Experimental Therapeutics Programme (ETP) within the CNIO (Spanish National Cancer Centre) was established in 2006 to foster translation of scientific breakthroughs into novel and more effective ways of prevent, diagnose and treat cancer. Its main role is to translate fundamental understanding of cancer into novel drugs.

For the past ten years, the ETP was completely focused on delivering balanced and optimized lead compounds (activity, off-target selectivity and ADME-Tox properties) with demonstrated in vivo proof-of-concept (PoC) after oral administration (mechanism of action and efficacy in tumor models).

Our multidisciplinary team of medicinal chemists, biologists, pharmacologists, crystallographers, etc. has proven skills in early drug discovery ranging from High-Throughput Screening (HTS) assay development (library of 50K chemically diverse compounds), medicinal chemistry for hit generation, hit-to-lead and lead optimization, to in vivo pharmacokinetics and PoC studies in animal models of human cancer.

By working closely with CNIO and other external basic research scientists, several lead compounds for PIM, PI3K and ATR kinases were progressed into preclinical phases, which have triggered licensing agreements with companies such as Inflection Biosciences and Merck-Serono.

The current ETP-CNIO pipeline encompasses targeted projects directed towards the discovery of novel inhibitors for CDK8 (Lead Optimization), HASPIN and MASTL kinases (Hit Generation phase) and projects based on phenotypic screenings such as the identification of TRF1 (shelterin) modulators and novel targets and inhibitors to erradicate Cancer Stem Cells (CSCs). In addition to classical drug discovery approaches for targeted projects, our team apply target deconvolution techniques for phenotypic projects, including the design of affinity and imaging chemical probes to help in the identification of molecular targets responsible for a given phenotype.

Sources of Funding: Federal/State, Industry Partnerships, Revenue

Website

Institutional Affiliation(s):

Address:
Melchor Fernandez Almagro, 3
Madrid
Madrid, 28029
Spain

Center/Program Start Date: 2006

Number of Employees: 400/23