# Intestinal Drug Transporters in Veterinary Animals

> **NIH FDA R43** · APRICITY THERAPEUTICS, INC. · 2022 · $168,400

## Abstract

Intestinal Drug Transporters in Veterinary Animals
Intestinal transporters in the ATP Binding Cassette Family (ABC) reduce the absorption of many xenobiotics
including prescription drugs. ABCG2 encodes BCRP, an important transporter that is highly expressed in the
intestine as well as other barrier tissues such as the Blood Brain Barrier. BCRP limits the oral bioavailability of
its substrates and therefore candidate drugs that are found to highly interact with BCRP are often discarded
during drug development. Only those with limited or no interactions with BCRP are selected for further
development. However, for veterinary drug development, cell lines expressing the appropriate species
orthologs of BCRP are not available. Since species differences in the substrate and inhibitor selectivity of
transporters are likely to occur, the lack of cell lines expressing species orthologs of transporters represents an
enormous gap for veterinary drug development. The goals of this Phase I SBIR research are to create and
characterize cell lines and yeast strains stably expressing veterinary animal BCRP from dog, cat,
sheep and pig. The cell lines and yeast strains will serve as resources for drug developers, and will represent
innovative “alternative methods, in support of replacement/reduction/refinement for activities involving animal
research.” In studies under aim 1, we will create stable cell lines and yeast strains expressing the species
orthologs of BCRP. In aim 2, we will create robust assays and use model substrates and inhibitors of BCRP to
characterize species differences in the substrate and inhibitor specificity of the transporter. Methods used in
the proposed studies include technologies for creation of cell lines stably expressing the transporter orthologs,
and isotopic uptake and flux assays in cells. Yeast transformation procedures and cytotoxicity assays will also
be applied. Collectively these studies will enable veterinary drug development by providing much needed cell
lines for predicting drug absorption. The cell lines will reduce the reliance on trial-and-error experimental
approaches in animals.

## Key facts

- **NIH application ID:** 10544701
- **Project number:** 1R43FD007586-01
- **Recipient organization:** APRICITY THERAPEUTICS, INC.
- **Principal Investigator:** Claire Brett
- **Activity code:** R43 (R01, R21, SBIR, etc.)
- **Funding institute:** FDA
- **Fiscal year:** 2022
- **Award amount:** $168,400
- **Award type:** 1
- **Project period:** 2022-09-20 → 2023-08-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10544701

## Citation

> US National Institutes of Health, RePORTER application 10544701, Intestinal Drug Transporters in Veterinary Animals (1R43FD007586-01). Retrieved via AI Analytics 2026-05-23 from https://api.ai-analytics.org/grant/nih/10544701. Licensed CC0.

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