US 10864199

Here is a concise summary of US Patent 10864199, including information from the USPTO and CAFC dockets.

US Patent 10864199 Summary

• Title: Tacrolimus for improved treatment of transplant patients
• Current Assignee: Veloxis Pharmaceuticals Inc.
• Original Assignee: Veloxis Pharmaceuticals AS
• Inventors: Robert D. Gordon, Per Holm, Anne-Marie Lademann, Tomas Norling
• Filing Date: 2016-02-11
• Issue Date: 2020-12-15
• Abstract: An extended release oral dosage form comprising tacrolimus or a pharmaceutically active analogue thereof for once-daily immunosuppressive treatment of transplant patients. This dosage form releases the active substance over a very extended period, providing high bioavailability and an improved pharmacokinetic profile compared to conventional dosage forms.

Plain-Language Overview of Independent Claims:

• Claim 1: This claim describes an extended-release oral dosage form containing tacrolimus (or a similar active drug) for once-daily immunosuppressive treatment. The key feature is its slow release profile: when tested in a specific lab setup (USP II paddle or USP I basket test at pH 4.5 with 0.005% hydroxypropylcellulose and 50 rpm rotation), no more than 63.5% of the drug is released after 12 hours.
• Claim 26: This claim covers a pharmaceutical composition in particulate form (like a powder or granules) that contains tacrolimus (or a similar drug) and other standard pharmaceutical ingredients. When given orally, this composition results in an Area Under the Curve (AUC) in the body that is at least 1.3 times higher than that of Prograf® (a commercially available tacrolimus product) under similar conditions, indicating improved drug absorption.
• Claim 27: This claim describes a pharmaceutical composition in particulate form with tacrolimus and other ingredients that, when taken orally, releases tacrolimus in a controlled way. This controlled release leads to a maximum drug concentration (Cmax) in the body that is no more than about 80% of the Cmax achieved with Prograf® tablets.
• Claim 37: This claim focuses on a pharmaceutical composition in particulate form containing tacrolimus (or an analogue) and other ingredients. When administered orally, this composition releases the drug in a controlled manner and reduces side effects compared to Prograf® when both provide an equivalent therapeutic effect.
• Claim 49: This claim describes the extended-release oral dosage form of Claim 1 for use in an immunosuppressive treatment method. This method involves once-daily administration and provides one or more improved pharmacokinetic outcomes such as a lower maximum concentration (Cmax), reduced "swing" (fluctuation between max and min concentrations), increased total drug exposure (AUC), longer mean residence time (MRT), later time to maximum concentration (Tmax), or a higher minimum concentration (Cmin).
• Claim 50: This claim describes a method of providing once-daily immunosuppressive treatment using the extended-release formulation. A key aspect is that the minimum drug concentration (Cmin) in the blood highly correlates with the overall drug availability (bioavailability), with a correlation factor of at least 0.75 (and preferably higher).
• Claim 51: This claim describes a method of providing once-daily immunosuppressive treatment using the extended-release formulation, where the bioavailability of the drug is largely unaffected by the time of day it is taken. This allows for flexible dosing, including at bedtime or in the evening.
• Claim 52: This claim describes a method for converting a patient from an immediate-release tacrolimus regimen (like Prograf®) to the once-daily extended-release regimen. The method involves reducing the daily tacrolimus dosage by 25% to 50% (preferably around 33%) during this conversion.
• Claim 53: This claim describes a method for converting a patient from an Advagraf® regimen to the once-daily extended-release regimen. The conversion ratio from Advagraf® to the new formulation is between 1:0.30 and 1:0.75, depending on available dosage strengths (0.5 mg, 1 mg, 2 mg, and 5 mg).
• Claim 54: This claim describes a method of providing once-daily immunosuppressive treatment using the extended-release formulation specifically to reduce side effects related to high peak drug concentrations, such as neurological side effects like tremor and headache.
• Claim 55: This claim describes a method for treating patients at risk of organ toxicity from tacrolimus, specifically targeting organs known to accumulate the drug, including the adrenal gland, lung, heart, liver, gastrointestinal tract, and kidney.
• Claim 58: This claim describes a method for the initial treatment of a new liver transplant patient with tacrolimus. It involves administering the once-daily extended-release oral dosage form which, in an in vitro dissolution test (FDA method for Prograf®), releases less than 50% of tacrolimus after 10 hours. This dosage form must provide a systemic drug exposure on day 1 that is at least 50% of the exposure obtained on day 1 from an immediate-release tacrolimus form given twice a day.
• Claim 59: This claim describes a method for the initial treatment of a new kidney transplant patient with tacrolimus. It involves administering the once-daily extended-release oral dosage form which, in an in vitro dissolution test (FDA method for Prograf®), releases less than 50% of tacrolimus after 10 hours. This dosage form must provide a systemic drug exposure on day 1 that is at least 70% of the exposure obtained on day 1 from an immediate-release tacrolimus form given twice a day.
• Claim 60: This claim describes a method for the initial treatment of a new liver transplant patient with tacrolimus. It involves administering the once-daily extended-release oral dosage form which, in an in vitro dissolution test (FDA method for Prograf®), releases less than 50% of tacrolimus after 10 hours. This dosage form must provide a systemic drug exposure on day 1 that is at least 100% of the exposure obtained on day 1 from an extended-release oral dosage form that releases more than 30% of tacrolimus within 5 hours.
• Claim 61: This claim describes a method for the initial treatment of a new kidney transplant patient with tacrolimus. It involves administering the once-daily extended-release oral dosage form which, in an in vitro dissolution test (FDA method for Prograf®), releases less than 50% of tacrolimus after 10 hours. This dosage form must provide a systemic drug exposure on day 1 that is at least 100% of the exposure obtained on day 1 from an extended-release oral dosage form that releases more than 30% of tacrolimus within 5 hours.

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