US 11110081

US Patent 11110081: Summary and Claim Analysis

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: 2020-10-30

Issue Date: 2021-09-07

Abstract: The patent describes an extended-release oral dosage form containing tacrolimus or a pharmaceutically active analogue for once-daily immunosuppressive treatment of transplant patients. This dosage form is designed to release the active substance over a very extended period, providing high bioavailability and an improved pharmacokinetic profile compared to conventional formulations.

---

Plain-Language Overview of Independent Claims:

US Patent 11110081 contains several independent claims, each defining a distinct aspect of the invention.

Independent Claim 1:
This claim describes an extended-release oral dosage form for once-daily immunosuppressive treatment using tacrolimus or a similar active substance. The key features are its extended release over time, defined by specific in vitro dissolution criteria: no more than 63.5% of the active substance is released after 12 hours when tested using USP II (paddle) or USP I (basket) dissolution methods in a pH 4.5 medium containing 0.005% hydroxypropylcellulose at 50 rpm. Additionally, the dosage form must release at least 8% at 4 hours and/or at least 15% at 8 hours to ensure continuous release.

Independent Claim 13:
This claim focuses on a method for providing immunosuppressive treatment to a patient using the extended-release oral dosage form of claim 1. The method involves administering this dosage form once daily to achieve one or more improved pharmacokinetic parameters compared to conventional treatments. These improvements include decreased maximal concentration (Cmax), decreased "swing" (Cmax-Cmin/Cmin), decreased fluctuation (Cmax-Cmin/Caverage), increased overall drug exposure (AUC), increased mean residence time (MRT), a longer time to reach maximal concentration (Tmax), and a higher minimum concentration (Cmin).

Independent Claim 14:
This claim describes a method for converting a patient from a twice-daily tacrolimus immediate-release regimen (like Prograf®) to a once-daily regimen using the extended-release oral dosage form of claim 1. The conversion involves decreasing the total daily dose of tacrolimus by 25% to 50% (preferably 30% to 40%, most preferably approximately 33%) when switching to the extended-release formulation. This reduction is adjusted based on available tablet strengths (0.5 mg, 1 mg, 2 mg, 5 mg) for the extended-release product, resulting in a conversion ratio of 1:0.66 to 0.80.

Independent Claim 15:
This claim details a method for converting a patient from a once-daily tacrolimus extended-release regimen (like Advagraf®) to a once-daily regimen using the extended-release oral dosage form of claim 1. The conversion ratio for the daily dose of tacrolimus is between 1:0.30 and 0.75 (such as 1:0.33 to 0.7), again dependent on the available strengths of the inventive extended-release formulation (0.5 mg, 1 mg, 2 mg, 5 mg).

Independent Claim 16:
This claim outlines a method for treating a de novo liver transplant patient with tacrolimus. It involves administering the once-daily extended-release oral dosage form described in claim 1. The critical aspects are its in vitro release profile (less than 50% of tacrolimus released after 10 hours according to the FDA dissolution method for Prograf®) and its ability to provide a systemic exposure on Day 1 that is at least 50% of the exposure obtained on Day 1 from the same daily dose administered as a twice-daily immediate-release formulation.

Independent Claim 17:
Similar to Claim 16, this claim describes a method for treating a de novo kidney transplant patient with tacrolimus using the once-daily extended-release oral dosage form of claim 1. The in vitro release profile is the same (less than 50% of tacrolimus released after 10 hours by the FDA Prograf® method), but the systemic exposure on Day 1 must be at least 70% of the exposure obtained from the same daily dose administered as a twice-daily immediate-release formulation.

---

CAFC 2026 Dockets:

As of April 26, 2026, a direct search of publicly available CAFC 2026 dockets specifically referencing US patent 11110081 did not yield authoritative case numbers or detailed litigation information. While Google Patents indicates that the patent family has ongoing litigation, including multiple US cases filed in the Delaware District Court (e.g., 1:26-cv-00467, 1:25-cv-00458, 1:24-cv-00784, 1:24-cv-00726, 1:22-cv-00909), and notes a "First worldwide family litigation filed" via Darts-ip, specific CAFC dockets for 2026 for this patent were not directly identifiable through the performed searches. Further investigation, potentially through subscription-based legal databases like Darts-ip or PACER (which typically requires specific case information for effective searching), would be necessary to confirm any active CAFC proceedings related to US11110081 in 2026.