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Drug metabolism in vitro

How can you improve human hepatic drug metabolism predictions?


Drug metabolism is a complex process where drugs are structurally modified to form metabolites. Studying drug metabolism and pharmacokinetics (DMPK) is required to identify lead compounds with optimal PK/PD properties, optimize efficacy, and minimize safety issues.

Standard in vitro drug metabolism and pharmacokinetics studies face various challenges. Many are incompatible with new therapeutic modalities, are inaccurate predictors of human in vivo clearance rates, and fail to identify rare or human-specific metabolites.

Our solution

Liver-, Lung-, and Gut-on-a-chip in vitro models can be used to study metabolism, metabolites, and transporter-mediated uptake and efflux.

Connecting two models related to DMPK offers an improved prediction of in vivo pharmacokinetics and pharmacodynamics. For example, combining liver and gut models allows orally administered drugs to be studied in a multi-organ system. The system can reflect compound permeability through an intestinal barrier, hepatic metabolism, organ–organ interaction, and crosstalk.

PhysioMimix® Drug Metabolism Assays allow the measurement of parent and metabolite concentrations within the intracellular compartment and culture medium, to determine all standard metabolic parameters. They are particularly well suited to measuring slowly metabolized, low clearance drugs where in other systems, such as suspension hepatocytes, compound turnover is not detected.

Our organ-on-a-chip (OOC) models maintain phase I and II metabolism together with transporter function at in vivo-like levels for weeks. The ability to recirculate media around the cultures allows for the decrease in parent or build-up of metabolites to be measured and complete metabolic characterization from a single culture.

Drug metabolism cells

Studying drug metabolism

Limitations with current techniques

  • Low clearance drugs can’t be evaluated with suspension hepatocytes
  • Many systems do not show adequate phase II metabolism
  • Metabolism is not measurable in a ‘single pass’ OOC and spheroids 
  • Some OOC technologies are unsuitable as they use Polydimethylsiloxane (PDMS) which absorbs drugs

Advancements with PhysioMimix OOC

  • Prolonged metabolic competence means low clearance drugs can be evaluated
  • Liver-on-a-chip provides phase I, II, and tertiary metabolism
  • Our models have an optimized cell-to-medium ratio, ensuring measurable metabolism
  • Our systems are made from low-binding non-silicone materials
  • Liver-on-a-chip models typically contain 500K cells, providing material ‘horsepower’ for rare metabolite detection

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Assess first-pass metabolism in vitro


Investigate the combined effects of intestinal absorption and liver metabolism using a multi-organ system, measuring the clearance of parent compound and production of metabolites.

Assessing first-pass metabolism graph
Parent molecule
Assessing first-pass metabolism graph
Primary metabolite

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Predict slowly metabolized drug clearance rates


From slow to fast, a range of in vivo drug clearance rates can be accurately predicted using our metabolically competent, human-relevant in vitro Liver-on-a-chip.

Tsamandouras et al., 2017

Predict slowly metabolized drug clearance rates graph

Access our ADME Service


Get instant access to PhysioMimix Drug Metabolism Assays via our CRO Service. Through a collaborative approach, our experts work with you to plan and execute your study.

Standard and bespoke projects are carried out by our dedicated team of scientists in our CRO facility providing you with actionable data within weeks.

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Add PhysioMimix OOC into your lab


Harness the power of PhysioMimix OOC in your own lab with the purchase of a single- or multi-organ microphysiological system.

With a growing community of users and support from our experts, there has never been a better time to transition into 3D cell culture.

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Featured resources

Scientific publications

Exploration Application Drug Metabolism 2022 Graphic |

Exploration and Application of a Liver-on-a-Chip Device in Combination with Modelling and Simulation for Quantitative Drug Metabolism Studies

Articles

A4 resource mockup Template |

How to Keep Breathing – The Future of Inhaled Medication Testing

Scientific publications

Characterizing Repreducibility MPS 2020 Graphic |

Characterizing the reproducibility in using a liver microphysiological system for assaying drug toxicity, metabolism and accumulation

View all Drug metabolism related resources

Speak to our experts

Speak directly with one of our OOC experts to see how our products and services can support your studies

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Latest news

  • Immune-mediated DILI – Predicting the unpredictable! March 16, 2023
  • CN Bio appoints Deepak Singh as Vice President of Sales and Marketing March 14, 2023
  • CN Bio extends microphysiological system portfolio with PhysioMimix Single-Organ Higher Throughput System   February 27, 2023

Upcoming events

MPS World Summit 2023 June 26-30, 2023

SLAS Europe 2023 May 22-26, 2023

SOT 2023 March 19-23, 2023

WORD 2023 March 22, 2022