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Development of a Prototype, Once-Daily, Modified-Release Formulation for the Short Half-Life RIPK1 Inhibitor

Debra J Tompson¹, Mark Whitaker², Rennan Pan³

¹Clinical Pharmacology Modelling and Simulation, GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, UK. debra.j.tompson@gsk.com.

Pharmaceutical Research

|June 17, 2021

Summary

Developing a modified-release formulation of GSK2982772 for once-daily dosing showed promise. However, food intake significantly impacted the drug

Keywords:

GSK2982772 modified release once-daily pharmacokinetics short half-life

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Area of Science:

Pharmacology and Drug Development
Biopharmaceutical Sciences
Clinical Pharmacy

Background:

GSK2982772 is a selective inhibitor of receptor-interacting protein kinase-1.
The drug has a short half-life of 2-3 hours, necessitating formulation development for sustained release.
Optimizing dosing regimens is crucial for therapeutic efficacy and patient compliance.

Purpose of the Study:

To evaluate the development of a once-daily modified-release formulation of GSK2982772.
To assess the pharmacokinetic profile of GSK2982772 with different modified-release formulations.
To determine the effect of food on the pharmacokinetics of GSK2982772 formulations.

Main Methods:

Part A: Single-dose pharmacokinetics of matrix minitab (MT-8h, MT-12h) vs immediate release (IR) formulations in fasted state, and MT-12h with a high-fat meal.
Part B: 3-day once-daily MT-12h evaluation at three dose levels.
Part C: Pharmacokinetics of matrix monolithic (MM-12h) formulation at two dose levels in different prandial states.

Main Results:

Modified-release formulations (MT-12h, MM-12h) in the fasted state reduced Cmax and AUC compared to IR, with delayed Tmax.
Co-administration of MT-12h or MM-12h with meals increased Cmax and AUC.
Administering MM-12h one hour before meals minimized food effect on exposure.

Conclusions:

MT-12h and MM-12h formulations achieved a once-daily pharmacokinetic profile in the fasted state.
Food, particularly high-fat meals, disrupted the once-daily pharmacokinetic profile of MT-12h.
The MM-12h formulation demonstrated potential for once-daily dosing with minimal food effect when administered pre-meal.