US 12083103

Patent Summary: US 12,083,103 B2

Title: Tacrolimus for improved treatment of transplant patients

Assignee: Veloxis Pharmaceuticals Inc.

Inventors: Robert D. Gordon, Per Holm, Anne-Marie Lademann, Tomas Norling

Filing Date: August 4, 2021

Issue Date: September 10, 2024

Abstract:
The patent describes an extended-release oral dosage form of tacrolimus, an immunosuppressive drug used in transplant patients. The formulation is designed for once-daily administration and aims to provide improved bioavailability and a better pharmacokinetic profile compared to conventional tacrolimus formulations. This is achieved by releasing the active substance over a prolonged period, which is intended to reduce the variability in drug absorption and metabolism often seen with immediate-release versions. The goal is to offer a more stable and predictable drug concentration in the blood, enhancing the safety and efficacy of the treatment for preventing organ rejection.

Overview of Independent Claims

The independent claims of US patent 12,083,103 B2 define the core inventive aspects of the extended-release tacrolimus formulation. A plain-language summary of each is provided below.

Claim 1: This claim protects a method for the immunosuppressive treatment of a transplant patient. The method involves administering, on a once-daily basis, a solid oral dosage form of tacrolimus. The key feature of this dosage form is its specific in vitro dissolution profile: when tested using a standard USP paddle or basket method at 50 rpm in a pH 4.5 medium containing 0.005% hydroxypropylcellulose, it releases no more than 63.5% of its tacrolimus content within 12 hours. This slow release is intended to provide a stable and extended therapeutic effect over a 24-hour period.

Claim 11: This claim focuses on a method for converting a transplant patient's treatment regimen from a twice-daily immediate-release tacrolimus product (like Prograf®) to the once-daily extended-release formulation described in the patent. The conversion involves administering a total daily dose of the new formulation that is reduced by 20-34% compared to the previous total daily dose of the immediate-release product. This reduction is possible due to the improved bioavailability of the extended-release formulation.

Claim 15: This claim covers a method of treating a de novo transplant patient, meaning a patient who has just received a transplant and is starting oral tacrolimus treatment for the first time. The method involves initiating treatment with the once-daily extended-release tacrolimus formulation. The formulation must provide a systemic drug exposure (measured as Area Under the Curve, or AUC) on the first day of treatment that is at least 70% of the exposure that would be achieved with the same total daily dose of an immediate-release tacrolimus formulation administered twice a day. This ensures that therapeutic drug levels are reached quickly and effectively in these critical early-stage patients.

Note on Litigation: My search of the CAFC 2026 dockets did not yield any specific results for US patent 12,083,103. However, information available through Google Patents indicates that the patent family is associated with litigation in the Delaware District Court. The provided information does not specify the details or the current status of these legal proceedings.