In Vitro DMPK & ADME

In Vitro DMPK and ADME on Human Gut Tissue.

RepliGut® Planar brings human intestinal biology to your ADME studies. Measure permeability, transport, and metabolism on real human tissue, across regions and donors, and catch the failures Caco-2 misses.

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Why it matters

Why intestinal biology decides drug fate

Strong in vitro DMPK and ADME data early keeps weak candidates from failing late. The gut sets the pace. It decides how much drug gets absorbed, how fast enzymes clear it, and which transporters push it back out.

Caco-2 has long been the default screen. Yet it comes from a single colon tumor and misses much of that biology. It underexpresses key metabolic enzymes and carries the wrong transporter and esterase profile. So its predictions can mislead, and regulators now favor human-relevant alternative testing methods.

RepliGut® vs Caco-2

A human alternative to Caco-2

RepliGut® Planar grows from human adult donor stem cells into a polarized epithelial monolayer, in the same 96-well transwell format labs already use. You keep the workflow and gain the biology.

FeatureCaco-2RepliGut® Planar
Cell sourceOne colon cancer cell line, single donor genetics.Human adult donor stem cells, from many donors.
Regional identityColon tumor origin only, no regional range.Duodenum, jejunum, ileum, and colon, each retained.
Phase I and II metabolismLow CYP3A4 and patchy conjugation.Functional CYP3A4, UGT, and SULT turnover.
Efflux transportersAltered expression, limited efflux.Active P-gp and BCRP, efflux ratio above 2.
CarboxylesteraseHigh CES1, unlike the human small intestine.CES1 absent, matching human gut.
Mucus layerNone, so it can overpredict absorption.MUC2 goblet cells and a real mucus layer.
6
Gut regions, from duodenum to descending colon, each with its own biology.
Phase I + II
Functional CYP3A4, UGT, and SULT metabolism, the intestinal clearance Caco-2 underrepresents.
ER > 2
Active P-gp and BCRP efflux, confirmed with transporter inhibitors.
The Caco-2 trap

Caco-2 cells express high CES1, an enzyme barely present in the human small intestine. So they over-metabolize prodrugs like temocapril and overpredict clearance. RepliGut® Jejunum lacks CES1, just like real gut, so the read stays true to human biology.

Capabilities

Four in vitro DMPK and ADME assays on one platform

Each assay answers a different question about how a candidate moves through the gut. Run one, or combine them into a full disposition package on the same human tissue.

Permeability & BCS

Measure permeability and BCS class

Run Papp and efflux ratios in a 96-well transwell with apical and basal access. Atenolol and propranolol anchor the low and high controls, and TEER confirms the barrier holds.

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Transporters

Profile P-gp and BCRP efflux

Confirm active efflux with efflux ratios above 2. Add tariquidar or Ko143 to pin transport to a specific carrier.

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Metabolism

Quantify intestinal first-pass

Track CYP3A4, UGT, and SULT turnover on human tissue. Catch the Phase I and Phase II clearance that Caco-2 misses.

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Drug-drug interaction

Flag intestinal DDI risk

Profile PXR, AhR, and VDR induction in the gut. The intestinal response differs from liver, so gut DDI risk gets its own read.

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Each assay runs as a standalone study or as part of a full disposition package. Explore full-service options or talk to our team.

Validation
In vitro DMPK and ADME permeability data: RepliGut Planar Jejunum Papp versus human fraction absorbed

Permeability that tracks human absorption

RepliGut® Planar Jejunum tells high and low permeability compounds apart, and the Papp readout follows the human fraction absorbed. You run it in the same transwell format you already use, aligned to ICH M9 guidance.

That gives you a reliable early read on how well a candidate will be taken up in the gut, before it reaches the clinic.

See the publications
Gene expression heatmap comparing RepliGut Planar Jejunum and Caco-2 across ADME, Phase I, and Phase II metabolism genes

Enzyme and transporter expression Caco-2 cannot match

RNAseq shows RepliGut® Jejunum expressing critical ADME genes well above Caco-2. That spans Phase I oxidation, Phase II conjugation, and the P-gp and BCRP efflux transporters.

Because the enzymes and carriers are present and active, first-pass predictions reflect the real gut instead of a tumor line.

Why the data holds up

Built to reflect the human gut

Real human biology

Grown from human adult donor stem cells, across regions of the small intestine and colon.

Apical and basal access

The planar transwell format opens both surfaces for dosing and sampling, unlike spherical organoids.

Region and donor range

Compare metabolism and transport across gut regions and demographically diverse donors.

TEER barrier control

Automated TEER confirms a tight, intact barrier before and after every incubation.

Get started

Run it in your lab or have us run it

RepliGut® Kits

Run RepliGut® Planar in your own lab. Kits ship in 12-well and 96-well formats, complete with cells, plates, media, and technical support.

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Full-service DMPK

Have our scientists design and run the study. We deliver Papp, efflux, metabolism, and gene expression data, ready for your model.

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Working on gut safety instead? See StemTox GI toxicity screening, or explore the full RepliGut® platform.

Ready to run DMPK on human tissue?

Tell us the candidate and the question. We will design the right in vitro DMPK and ADME study on RepliGut® Planar.

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