--- title: | ADME/DMPK (3) description: ADME/DMPK | (3) --- [![Cyprotex | The Leading ADME-Tox Specialist](https://news.cyprotex.com/hs-fs/hubfs/cyprotex%20logo.png?width=224&height=62&name=cyprotex%20logo.png "Cyprotex | The Leading ADME-Tox Specialist")](https://www.cyprotex.com/) # Science Pool ## [A Focus on Drug Transporters Webinar Series - Hayley Atkinson, Cyprotex](https://news.cyprotex.com/sciencepool/a-focus-on-drug-transporters) Posted by [Evotec](https://news.cyprotex.com/sciencepool/author/evotec) on Jan 18, 2022 1:31:43 PM ### **Quantitative Prediction of Drug-Drug Interactions with Common Statin Co-meds: A Framework for Decision-making within Drug Discovery/Development** The first webinar in this series on drug transporters was presented by Hayley Atkinson from Cyprotex.   --- ### About the Webinar   Due to polypharmacy, drug-drug interactions (DDIs) continue to account for 5% of UK hospital admissions and as such remain a major regulatory concern. This is particularly true for common co-meds such as statins which due to their prescribing prevalence in patients with co-morbidities have high potential for DDI. Within Drug Discovery and Development we are moving away from relatively simple hazard identification of DDI potential using basic static equations detailed in regulatory guidance to actual risk analysis and mitigation using quantitative prediction of DDI. Using mechanistic static equations we can predict the AUC change of each statin due to inhibition of its critical enzyme/transporter pathway(s) so that the clinical team can make a decision on whether any potential DDI is simply a pharmacokinetic DDI or a clinically significant DDI requiring intervention. The statin mechanistic equation model requires very few* in vitro* input parameters and can be utilised towards aiding preclinical development candidate selection and towards reducing unexpected clinical findings in patients providing a useful tool in Drug Discovery and Early Development.   --- ### About the Speaker   | ![Hayley Atkinson](https://news.cyprotex.com/hs-fs/hubfs/Hayley%20Atkinson.png?width=254&name=Hayley%20Atkinson.png) | **Hayley Atkinson PhD ***Associate Principal Scientist \| Cyprotex * Hayley Atkinson is an Associate Principal Scientist in the permeability and drug transporter team at Cyprotex, UK where she acts as deputy scientific lead for drug transporter studies.  Her research interests include prediction of transporter mediated drug-drug interactions with improved *in vitro* assays.  Prior to joining Cyprotex in 2013, Hayley received her PhD from the University of Liverpool under Prof. Munir Pirmohamed where she conducted research on anti-epileptic drug transporters at the blood-brain barrier in the context of drug resistance. | | --- | --- | Watch the webinar to learn more! [hs-form id="e52f470e-0e88-41ac-99f1-349b2316ef8a" show="hide on login" url="https://news.evotecsciencepool.com/hubfs/Sciencepool/Videos%20and%20Webinars/Cyprotex%20webinars%20and%20videos/focus-on-drug-transporters-webinar-series-hayley-atkinson-cyprotex-sept2020.m4v"] 0 Comments [Click here to read/write comments](https://news.cyprotex.com/sciencepool/a-focus-on-drug-transporters#comments-listing) Tags: [Videos & Webinars](https://news.cyprotex.com/sciencepool/tag/videos-webinars), [ADME/DMPK](https://news.cyprotex.com/sciencepool/tag/adme-dmpk) ## [Discovery of Novel UDP-N-Acetylglucosamine Acyltransferase (LpxA) Inhibitors](https://news.cyprotex.com/sciencepool/discovery-of-novel-udp-n-acetylglucosamine-acyltransferase-lpxa-inhibitors-with-activity-against-pseudomonas-aeruginosa) Posted by [Evotec](https://news.cyprotex.com/sciencepool/author/evotec) on Sep 30, 2021 7:41:42 PM *Alastair Parkes, Ph.D, Group Leader, Discovery Chemistry, Evotec UK* As part of our ongoing efforts at Evotec to tackle AMR through the design of novel antibiotics we have been working with Boston-based X-Biotix in a collaboration focussed on targeting priority Gram-negative pathogens. We are now able to share the story of our work on inhibitors of UDP-N-Acetylglucosamine Acyltransferase (LpxA), a key enzyme in the biosynthetic pathway of the outer membrane lipopolysaccharide of Gram-negative bacteria. Building on hit-finding work at X-Biotix we put together a multi-disciplinary team including Medicinal Chemistry, Computational Chemistry, Structural Biology and DMPK at our Abingdon UK site, *in vitro *and *in vivo *Microbiology and PK at our Alderley Park UK site, and *in vitro* Biology at our site in Hamburg, Germany. Through structure and property-based optimisation we were able to design highly potent inhibitors of *Pseudomonas aeruginosa *LpxA that were active against multi-drug resistant clinical isolates. To our knowledge, this is the first reported LpxA inhibitor series with selective activity against *P. aeruginosa *bacteria. In our paper in the Journal of Medicinal Chemistry we share the optimisation story, along with a significant quantity of activity data that we hope will be useful for other teams working on small molecule strategies to tackle *P. aeruginosa *and other Gram-negative bacteria. [LEARN MORE](https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.1c00888) 0 Comments [Click here to read/write comments](https://news.cyprotex.com/sciencepool/discovery-of-novel-udp-n-acetylglucosamine-acyltransferase-lpxa-inhibitors-with-activity-against-pseudomonas-aeruginosa#comments-listing) Tags: [Antibacterial](https://news.cyprotex.com/sciencepool/tag/antibacterial), [Medicinal Chemistry](https://news.cyprotex.com/sciencepool/tag/medicinal-chemistry), [Articles & Whitepapers](https://news.cyprotex.com/sciencepool/tag/articles-whitepapers), [ADME/DMPK](https://news.cyprotex.com/sciencepool/tag/adme-dmpk), [In vitro Biology](https://news.cyprotex.com/sciencepool/tag/in-vitro-biology), [In vivo Pharmacology](https://news.cyprotex.com/sciencepool/tag/in-vivo-pharmacology), [Anti-Infectives](https://news.cyprotex.com/sciencepool/tag/anti-infectives), [Antimicrobial resistance](https://news.cyprotex.com/sciencepool/tag/antimicrobial-resistance) ## [Pharmacokinetic Prediction Fact Sheet](https://news.cyprotex.com/sciencepool/pk-prediction) Posted by [Evotec](https://news.cyprotex.com/sciencepool/author/evotec) on Sep 9, 2021 5:52:45 PM Learn more about human pharmacokinetic prediction including: - background information on the predictive model - *in vitro* ADME data and structural data requirements for PK prediction - data delivered for the PK prediction - validation data for the predictive model [DOWNLOAD](https://news.cyprotex.com/hubfs/Sciencepool/Fact%20sheets/Cyprotex%20Facts%20Sheets/cyprotex-pk-prediction-using-adme-data-fact-sheet-2.pdf) 0 Comments [Click here to read/write comments](https://news.cyprotex.com/sciencepool/pk-prediction#comments-listing) Tags: [Fact Sheets](https://news.cyprotex.com/sciencepool/tag/fact-sheets), [ADME/DMPK](https://news.cyprotex.com/sciencepool/tag/adme-dmpk), [Modelling and Simulation](https://news.cyprotex.com/sciencepool/tag/modelling-and-simulation) ## [Brain Tissue Binding Fact Sheet](https://news.cyprotex.com/sciencepool/blood-tissue-binding-fact-sheet) Posted by [Evotec](https://news.cyprotex.com/sciencepool/author/evotec) on Sep 1, 2021 3:17:35 PM Learn more about the brain tissue binding assay including: - Background information - Assay details and protocol summary - Data generated in the brain tissue binding assay [DOWNLOAD](https://news.cyprotex.com/hubfs/Sciencepool/Fact%20sheets/Cyprotex%20Facts%20Sheets/cyprotex-brain-tissue-binding-fact-sheet-2021.pdf) 0 Comments [Click here to read/write comments](https://news.cyprotex.com/sciencepool/blood-tissue-binding-fact-sheet#comments-listing) Tags: [Fact Sheets](https://news.cyprotex.com/sciencepool/tag/fact-sheets), [ADME/DMPK](https://news.cyprotex.com/sciencepool/tag/adme-dmpk) ## [Cytochrome P450 Time Dependent Inhibition (IC50 Shift) Fact Sheet](https://news.cyprotex.com/sciencepool/cytochrome-p450-time-dependent-inhibition-ic50-shift-fact-sheet) Posted by [Evotec](https://news.cyprotex.com/sciencepool/author/evotec) on Sep 1, 2021 3:13:19 PM Learn more about the cytochrome P450 time dependent inhibition (CYP TDI) IC50 shift assay including: - Background information - Assay details and protocol summary - Data generated in the CYP TDI IC50 shift assay [DOWNLOAD](https://news.cyprotex.com/hubfs/Sciencepool/Fact%20sheets/Cyprotex%20Facts%20Sheets/cyprotex-cytochrome-p450-time-dependent-inhibition-ic50-shift-fact-sheet-2021.pdf) 0 Comments [Click here to read/write comments](https://news.cyprotex.com/sciencepool/cytochrome-p450-time-dependent-inhibition-ic50-shift-fact-sheet#comments-listing) Tags: [Fact Sheets](https://news.cyprotex.com/sciencepool/tag/fact-sheets), [ADME/DMPK](https://news.cyprotex.com/sciencepool/tag/adme-dmpk) ## [Blood Binding Fact Sheet](https://news.cyprotex.com/sciencepool/blood-binding-fact-sheet) Posted by [Evotec](https://news.cyprotex.com/sciencepool/author/evotec) on Sep 1, 2021 3:09:22 PM Learn more about the whole blood binding assay including: - Background information - Assay details and protocol summary - Data generated in the whole blood binding assay [DOWNLOAD](https://news.cyprotex.com/hubfs/Sciencepool/Fact%20sheets/Cyprotex%20Facts%20Sheets/cyprotex-blood-binding-fact-sheet-2021.pdf) 0 Comments [Click here to read/write comments](https://news.cyprotex.com/sciencepool/blood-binding-fact-sheet#comments-listing) Tags: [Fact Sheets](https://news.cyprotex.com/sciencepool/tag/fact-sheets), [ADME/DMPK](https://news.cyprotex.com/sciencepool/tag/adme-dmpk) ## [Hepatic Uptake Fact Sheet](https://news.cyprotex.com/sciencepool/hepatic-uptake-fact-sheet) Posted by [Evotec](https://news.cyprotex.com/sciencepool/author/evotec) on Sep 1, 2021 2:58:00 PM Learn more about the hepatic uptake assay including: - Background information - Assay details and protocol summary - Data generated in the hepatic uptake assay [DOWNLOAD](https://news.cyprotex.com/hubfs/Sciencepool/Fact%20sheets/Cyprotex%20Facts%20Sheets/cyprotex-hepatic-uptake-fact-sheet-2021.pdf) 0 Comments [Click here to read/write comments](https://news.cyprotex.com/sciencepool/hepatic-uptake-fact-sheet#comments-listing) Tags: [Fact Sheets](https://news.cyprotex.com/sciencepool/tag/fact-sheets), [ADME/DMPK](https://news.cyprotex.com/sciencepool/tag/adme-dmpk) ## [Log D Shake Flask Fact Sheet](https://news.cyprotex.com/sciencepool/logd-fact-sheet) Posted by [Evotec](https://news.cyprotex.com/sciencepool/author/evotec) on Sep 1, 2021 2:54:33 PM Learn more about the Log D shake flask assay including: - Background information - Assay details and protocol summary - Data generated in the Log D shake flask assay [DOWNLOAD](https://news.cyprotex.com/hubfs/Sciencepool/Fact%20sheets/Cyprotex%20Facts%20Sheets/cyprotex-logD-shake-flask-fact-sheet-2021.pdf) 0 Comments [Click here to read/write comments](https://news.cyprotex.com/sciencepool/logd-fact-sheet#comments-listing) Tags: [Fact Sheets](https://news.cyprotex.com/sciencepool/tag/fact-sheets), [ADME/DMPK](https://news.cyprotex.com/sciencepool/tag/adme-dmpk) ## [Parallel Artificial Membrane Permeation Assay Fact Sheet](https://news.cyprotex.com/sciencepool/parallel-artificial-membrane-permeation-assay-fact-sheet) Posted by [Evotec](https://news.cyprotex.com/sciencepool/author/evotec) on Sep 1, 2021 2:49:30 PM Learn more about parallel artificial membrane permeation assay (PAMPA) including: - Background information - Assay details and protocol summary - Data generated in PAMPA [DOWNLOAD](https://news.cyprotex.com/hubfs/Sciencepool/Fact%20sheets/Cyprotex%20Facts%20Sheets/cyprotex-pampa-fact-sheet-2021.pdf) 0 Comments [Click here to read/write comments](https://news.cyprotex.com/sciencepool/parallel-artificial-membrane-permeation-assay-fact-sheet#comments-listing) Tags: [Fact Sheets](https://news.cyprotex.com/sciencepool/tag/fact-sheets), [ADME/DMPK](https://news.cyprotex.com/sciencepool/tag/adme-dmpk) ## [pKa and LogP Fact Sheet](https://news.cyprotex.com/sciencepool/pka-logp-fact-sheet) Posted by [Evotec](https://news.cyprotex.com/sciencepool/author/evotec) on Sep 1, 2021 2:44:30 PM Learn more about pKa and LogP determination including: - Background information - Assay details and protocol summary - Data generated for pKa and LogP [DOWNLOAD](https://news.cyprotex.com/hubfs/Sciencepool/Fact%20sheets/Cyprotex%20Facts%20Sheets/cyprotex-pka-and-logp-fact-sheet-2021.pdf) 0 Comments [Click here to read/write comments](https://news.cyprotex.com/sciencepool/pka-logp-fact-sheet#comments-listing) Tags: [Fact Sheets](https://news.cyprotex.com/sciencepool/tag/fact-sheets), [ADME/DMPK](https://news.cyprotex.com/sciencepool/tag/adme-dmpk) [Previous](https://news.cyprotex.com/sciencepool/tag/adme-dmpk/page/2) [All posts](https://news.cyprotex.com/sciencepool/all) [Next](https://news.cyprotex.com/sciencepool/tag/adme-dmpk/page/4)