US 12403095

Analysis of U.S. Patent 12,403,095: Stabilized Tacrolimus Composition

Date of Analysis: May 1, 2026

A detailed review of U.S. Patent 12,403,095 has been conducted. This document, titled "Stabilized tacrolimus composition," was issued on September 2, 2025, and is assigned to Veloxis Pharmaceuticals Inc. The inventors are listed as Nikolaj Skak and Per Holm. The patent application was filed on July 5, 2022.

No litigation concerning this patent has been identified in the CAFC dockets for 2026.

Abstract:

The invention relates to a stable pharmaceutical composition comprising a solid dispersion of tacrolimus in a vehicle. The composition further includes a stabilizing agent capable of providing a pH below 7 in the composition, as measured after re-dispersion in water. This stabilization is aimed at preventing or reducing the formation of major degradation products of tacrolimus, particularly 8-epitacrolimus, upon storage.

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Summary of Independent Claims:

The patent asserts two independent claims, which are foundational to the intellectual property protection sought.

Independent Claim 1:

This claim defines a pharmaceutical composition that is a solid dispersion of the immunosuppressive drug tacrolimus. Key limitations of this claim are:

• Active Ingredient: Tacrolimus is the sole active ingredient.
• Formulation: It is a solid dispersion in a mixture of a vehicle and a stabilizing agent.
• Stabilizing Agent: The agent must be a metal chelating agent and must result in a pH below 7 for the composition.
• Tacrolimus Concentration: The composition must contain between approximately 0.5% and 5% of tacrolimus by total weight.
• Stability Requirement: When stored at 40°C and 75% relative humidity for 5 weeks, the amount of the degradation product 8-epitacrolimus must not increase by more than 0.5% of the total weight of tacrolimus.
• Vehicle Exclusion: The vehicle used in the formulation cannot include a cyclo-dextrin.

In essence, this claim protects a specific formulation of tacrolimus that is stabilized against degradation under defined stress conditions, with particular compositional and functional requirements.

Independent Claim 11:

Similar to the first independent claim, this claim also describes a stabilized solid dispersion of tacrolimus where it is the only active ingredient and the vehicle does not contain a cyclo-dextrin. The primary distinctions and key features are:

• Active Ingredient & Formulation: Tacrolimus is the sole active ingredient in a solid dispersion with a vehicle and a metal-chelating stabilizing agent that provides a pH below 7.
• Tacrolimus Concentration: The concentration of tacrolimus is also set between approximately 0.5% and 5% by total weight.
• Stability Requirement: This claim sets a different stability standard. After storage at 25°C and 60% relative humidity for 5 weeks, the amount of 8-epitacrolimus should not increase by more than 0.2% of the total tacrolimus weight.

This claim provides protection for a tacrolimus formulation that demonstrates stability under more standard storage conditions, with a stricter limit on the formation of the specified degradation product.