Meeting Summary Report - 3rd New Perspective in DMPK: The Impact of Drug Design
8-9 February 2016, RSC Burlington House, London
Over one hundred delegates attended the 3rd New Perspectives in DMPK conference at RSC Burlington House on 8-9 February 2016. The meeting was jointly organised by the Royal Society of Chemistry Biological and Medicinal Chemistry Sector (RSC-BMCS), the Drug Metabolism Discussion Group (DMDG), the British Pharmacological Society (BPS), and the Drug Metabolism Group (DMG). The meeting was directly supported by several industrial exhibitors – Agilent Technologies, Biopharma Group, HiChrom, Hypha Discovery, Selcia, XenoGesis – and received additional promotion through Future Science Group / MedChemNet.com.
Keynote speaker Charlotte Allerton (Pfizer Worldwide R&D) started proceedings by provided an excellent framework for discussion through her presentation “Evolution of DMPK sciences and drug design”, ahead of the main conference sessions - each based around a key theme linking aspects of DMPK and drug design.In the theme of “Understanding and exploiting endogenous drug targets”, contributions included those focused on understanding the role of transporters (Scott Summerfield, GSK), selective metabolism for improved targeting of therapies (Klaus Pors, University of Bradford), (Rowan Stringer, Novartis), and chemical aspects of using deutero-substituted compounds for tuned PK and metabolism properties, and compound reactivity for optimising covalent inhibitors (Nicola Colclough, AstraZeneca). Chemical reactivity was also discussed through the different lenses of being included by intention, requiring minimisation, and representing a safety risk – “The Good, The Bad, The Ugly” (Philip MacFaul, RedX Pharma). Rick Schneider (Pfizer Worldwide R&D) concluded the session with a review of the strategies employed to reduce candidate attrition through the identification of reactive metabolite liabilities in the R&D pipeline.
Subsequent sessions turned the focus to exploring the current state of in silico approaches across DMPK and medicinal chemistry drug design. Neil Berry (University of Liverpool) provided an excellent overview of available strategies, and illustrated real world impact that they have had in recent projects (anti-malarial therapy, chronic pain, and filariasis). The wider context for these - and other - tools was provided by Marcel Hop (Genentech), who described how computational methods can potentially inform the lead optimisation process, and help achieve an appropriate balance of the “5Rs” the right target / right patient / right tissue / right safety / right commercial potential.Other contributors to these sessions focused on in silico prediction of metabolism (Robert Glen, Imperial College London / University of Cambridge), and the support that PBPK / PDPK models can make in directly supporting stages in both drug design (Nicolas Frances, Roche) and the prediction of appropriate clinical treatment schedules that can both optimise dose/response profiles, and feed back to chemists to inform compound design for improved pharmacokinetics (Owen Jones, AstraZeneca).
The changing landscape in which DMPK operates was also illustrated by Owen Jones, who commented on the increased interactivity of DMPK scientists within the R&D activities. These comments echoed those by Richard Weaver (XenoGesis) who provided a perspective on how the changes in how R&D knowledge is obtained and used within large pharmaceutical companies have provided opportunities for CRO engagement across multiple research activities, but that continued efforts to highlight the centrality of DMPK are needed to ensure value and impact are demonstrated and appreciated within the wider R&D context.
Awards for best ‘flash’ presentation, was made to Fillipa Antunes (Albumedix) for her elevator pitch of her poster “New pre-clinical model for studying and optimizing the pharmacokinetics of albumin-linked drugs”. Poster prizes were awarded to Peter Bradshaw (ICL) and Amanda Race (University of Bradford), who each received recent DMPK book titles, kindly provided by RSC Publishing.
The Organising Committee wish to thank all those who made platform or poster presentations, exhibitors, and conference delegates for making the conference a success, prompting excellent debate, enabling networking, and fostering collaborative work and knowledge-sharing in this exciting research area.
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For more information on the New Perspectives in DMPK series, please visit the website:
Prizewinners’ presentation with conference organiser and DMDG Chairman Peter Kilford.
(l-r) Pete Bradshaw (Best Student Poster Prize), Amanda Race (Best Poster Prize), Peter Kilford (Organising Committee), Filipa Atunes (Best “Flash” Presentation).
Dr Toby Athersuch (Imperial College London, DMG), on behalf of the Organising Committee:
Steve AlexanderBPS and University of Nottingham
Peter KilfordDMDG and Covance
Graeme ScarfeDMDG and AstraZeneca
Andrew StachulskiRSC and University of Liverpool
Ian WilsonDMG and Imperial College London