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Wednesday, March 15 • 14:00 - 16:00
Industry-academia research collaborations

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It is well recognised that pharma industry is changing, especially in the field of early drug discovery. The concept of open innovation is embraced and collaborations between academia and industry are setup to fill the emerging gap in drug discovery. On the one hand, academia is moving into the field of screening and compound management, on the other hand, industry is making their compound collections available to a wider scientific community. This session will show how these developments impact compound management and how industry and academia are making progress in combining the best of both worlds.

14.00 Yoichi Kurebayashi
Mission and Strategy of Japan Agency for Medical Research and Development for Boosting Drug Discovery in Japan

Slow development in clinical application and commercialization of outcomes from basic researches has been a long standing issue in Japan. In this context, a new funding agency, Japan Agency for Medical Research and Development (AMED), was established in 2015 to accelerate and innovate the medical research and development in Japan. In AMED, the department of innovative Drug Discovery and Development (iD3) is taking the initiative in drug discovery and development domain. The missions of iD3 include 1) accelerating translation of promising basic researches into innovative medicines, 2) promoting development of innovative translational sciences enabling more efficient drug discovery and development, and 3) creating and expanding precompetitive collaboration space in Japan. In this session, iD3’s new national projects for boosting collaborative drug discovery, i.e., iD3 Booster, Drug Discovery Support Network and Joint Pharma-compound Library initiative, will be presented.

14.30 Constantin Radu
The NTD Drug Discovery Booster: A Disruptive Approach to Chemical Screening

Small molecule screening has developed over the years from the early 1940’s, testing small molecules in test tubes, to technological breakthroughs leading to high throughput screening (HTS) in the 1990’s, in the efforts to discover pharmacological active molecules and subsequently leading to a lead molecule. The Drugs for Neglected Diseases initiative (DNDi), in conjunction with several consortium partners, have developed a disruptive approach to drug discovery, the NTD Drug Discovery Booster, to effectively maximise the Structure-Activity Relationship (SAR) space around new chemical hits and leads targeting Leishmania donovani and Trypanosoma cruzi, the kinetoplastid parasites responsible for visceral leishmaniasis and Chagas disease respectively. Institut Pasteur Korea (IPK) was selected as the screening hub for sample preparation and screening of small molecules distributed by the NTD Booster consortium members, where each member mines their own chemical library based on lead chemical series and ships it to IPK for process. The IPK Automation & Logistics Management (ALM) group is accountable for the logistical framework of importing the small molecules from various global locations and implementing good sample management practices with a strategic approach, taking into consideration compound stability and integrity. The objective of this presentation will be to show the logistical effort that is needed to import and manage small molecules as part of a multi-nations consortium and identifying a lead candidate.The NTD Drug Discovery Booster consortium currently consists of AstraZeneca plc., Celgene Corporation, Eisai Co, Ltd., Shionogi & Co, Ltd., Takeda Pharmaceutical Ltd., the Drugs for Neglected Diseases initiative and Institut Pasteur Korea.

15.00 Dr Kristian Birchall

Key Considerations in Compound Collection Composition and Quality – Seeding Success in Hit Follow Up

The adage “garbage in, garbage out” is painfully true in HTS. Attrition at the stage of hit triage is a frustrating waste of resource, especially given the repeated deployment of a screening collection, the difficulty of removing troublesome compounds and the consequences of following up poor quality hits. Thankfully there is an increasing awareness of the factors associated with poor prognosis, including physicochemical property profiles (e.g. QED score) and sub-structural flags (e.g. PAINS). However, many more subtle combinations of factors such as the location and frequency of undesirable groups alongside synthetic tractability can also diminish the prospects of a compound in hit follow up. Whilst it can be difficult to develop a set of rules that cover all possible scenarios, undesirable compounds can easily be spotted by experienced medicinal chemists. We describe a “wisdom of crowds” approach used as the final step when building our compound collection.

Other examples of strategies employed to improve the chance of success will be described including; the use of upfront experimental data to steer compound selection away from off-target liabilities, the use of target-focussed sets to improve hit rates and the use of knowledge-annotated and index sets to expedite hit follow up.

15.45: Closing remarks 



Moderators
avatar for Steven Van Helden

Steven Van Helden

Business Development & Account Management, Pivot Park Screening Centre
Steven van Helden studied chemistry at Utrecht University and, after obtaining his Ph.D. , worked for 20 years in various roles in pharmaceutical industry. Since 2003 he has been responsible for High Throughput Screening (HTS) operations and strategy at Organon/MSD. After the  closure of  those research facilities he developed a business plan for continuation of the screening activities in Oss, The Netherlands. This led to the formation... Read More →

Speakers
avatar for Kristian Birchall

Kristian Birchall

Senior Scientist (Modelling and Informatics), MRC Technology
Kristian gained his first taste of the challenges encountered in drug discovery doing QSAR and microarray data analysis during industrial placements whilst studying for a masters in biochemistry at the University of Bath. He undertook a CASE studentship between the University of Sheffield and GSK Stevenage, working on molecular similarity multi-objective optimisation algorithms. Enjoying pharmaceutical research at the interface between industry... Read More →
avatar for Yoichi Kurebyashi

Yoichi Kurebyashi

Senior Director, Japan Agency for Medical Research and Development (AMED)
In 1979, Yoichi Kurebayashi started his industry career at Daiichi Pharmaceutical Co. Ltd as a medicinal biologist. Later he served as Head of the Institute of Allergy at Bayer’s Research Center Kyoto and Vice President of Discovery Research Japan at Pfizer Global Research and Development, during which time he led multiple global project teams for drug discovery and development. In 2007, taking advantage of the long industry experience, he... Read More →
avatar for Constantin Radu

Constantin Radu

Group Head, Institut Pasteur Korea
Constantin Radu is the Head of the Automation and Logistics Management group at the Institut Pasteur Korea (IPK), in Seoul, South Korea, since January 2015. His group is responsible for supporting screening campaigns for infectious and neglected diseases, using dynamic robotic platforms and high content microscopy, as well as the management of the chemical and RNAi libraries and logistics management for the institute. Prior to joining IPK, he has... Read More →


Wednesday March 15, 2017 14:00 - 16:00
Music Hall 1