Targeted delivery of tofacitinib citrate to the site of disease to improve efficacy and safety

When delivered to the site of inflammation, liquid drug formulations could result in higher tissue absorption and lower drug exposure.

There is an urgent need to achieve higher rates of clinical response, remission, and mucosal healing in inflammatory bowel disease (IBD). Targeted delivery of drugs directly to the colon may increase local tissue concentration to improve efficacy and reduce system absorption.

To evaluate treatment efficacy, we compared intra-cecal drug delivery of soluble tofacitinib to the standard oral drug delivery in animal models.1

What did we find?

Approximately 10- to 15-fold smaller doses of tofacitinib administered via intra-cecal delivery could achieve equivalent drug concentrations with minimal systemic drug exposure compared to oral delivery.

Soluble tofacitinib formulation increased tissue absorption and coverage via intra-cecal administration.

Intra-cecal delivery of tofacitinib to the inflamed mucosa can potentiate pharmacodynamic effects at a lower dose.

These results indicate that targeted delivery of soluble tofacitinib to the site of inflammation could increase tissue absorption and coverage to achieve maximum efficacy with a lower risk of systemic toxicity.

This research was presented at the virtual Digestive Disease Week on May 21, 2021.

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  1. Lee SN, Stork C, Wahl C, Singh S, Chuang E. Targeted delivery of soluble tofacitinib citrate to the site of inflammation to improve efficacy and safety. Poster presented at Digestive Disease Week virtual conference, May 2021.