Drug Discovery

The OICR Drug Discovery Program is one of the largest programs of its kind in Canada. Our mission is to help efficiently translate discoveries made in Ontario’s labs into novel oncology therapies. The team is comprised of more than 25 researchers whose collective expertise spans the entire drug discovery process from target identification and validation to clinical candidate selection. The group has extensive drug discovery experience within pharma and biotech environments and combines the disciplines of biology, ADME/PK, analytical, medicinal and computational chemistry expertise along with state-of-the-art infrastructure necessary to successfully conduct drug discovery projects.

Principal Investigator

Dr. Rima Al-awar
Director and Senior Principal Investigator, Drug Discovery

Program expertise and capabilities

OICR’s Drug Discovery Team has the infrastructure and expertise to help drive small molecule drug discovery projects. We can aid in target validation, assay design and optimization, hit identification, hit triaging, hit to lead and lead optimization Structure-Activity Relationship (SAR) activities.

Additionally, a range of in vitro and in vivo experiments can be performed at OICR to fully characterize the ADME PK profile of hits, leads and candidate molecules.

Projects

  • Protein-protein interaction inhibitor projects in collaboration with pharma, biotech and Ontario’s research community;

  • Epigenetic modulators and chemical probes in collaboration with the Structural Genomics Consortium (SGC);

  • Novel kinase targets  

OICR is making its technology infrastructure, expertise and resources available to the Ontario cancer research community through cost-sharing arrangements.

Collaborative Research Resources

OICR enables research by providing expertise, advice and access to research services on a cost-recovery basis. Researchers can benefit from high-end technology infrastructure, world-leading research knowledge, high-quality services and support at each stage of the project development process.

OICR’s Drug Discovery program, supports the synthesis of small molecules, low to medium throughput screening, SAR analysis and hit triaging, a range of in vitro and in vivo assays to fully characterize ADME, pharmacokinetic profiles and maximum tolerated dose of candidates, including help with biochemical or cell based assay development and optimization for profiling and screening small molecule libraries.

Services available:

  • Plasma or blood stability – single time point.
  • Microsomal stability – single time point or time course and half-life determination.
  • Microsomal stability – metabolite ID.
  • Primary hepatocyte stability – single time point or time course and half-life determination.
  • Caco-2 permeability – bi-directional (papp and efflux ratio).
  • Caco-2 permeability – efflux transporter (P-gp MRP2 etc.) inhibition.
  • CYP450 inhibition – P450 inhibition percent inhibition one concentration -1 isoform.
  • Plasma or protein binding – single time point.
  • MTD determination – IV, PO or IP (three dose, two time point study) – mouse, rat or only sample analysis.
  • PK study – IV, PO or IP (single dose, nine time points) – mouse, rat or only sample analysis.
  • PK study – IV plus one other route (for F% determination) – mouse, rat or only sample analysis.
  • Prep HPLC use – purify compounds.
  • 500 MHz NMR use – analyze compounds.
  • Assay development and optimization (guidance and execution).
  • Low to medium through put screening.
  • Expertise with state-of-the-art equipment (SPR/ HP dispenser/FACS etc)
  • Medicinal chemistry and synthetic expertise.
  • SAR analysis and hit triaging.
  • Surface plasmon resonance (SPR) use.

To learn how Drug Discovery can help further your project please contact Jeff O’Meara, Senior Program Manager, Drug DiscoveryJeff.omeara@oicr.on.ca.

News

To find out more about what’s happening in Drug Discovery, visit OICR News.

Contact

Jeff O’Meara
Senior Program Manager, Drug Discovery
Jeff.omeara@oicr.on.ca

Dr. Rima Al-awar
Director and Senior Principal Investigator, Drug Discovery
Rima.AlAwar@oicr.on.ca