Compositions and methods for treating anemia
Inventors
Smith, Alexander • Chandorkar, Gurudatt Ajay • Ette, Ene Ikpong • Maroni, Bradley John • Hartman, Charlotte Suzanne • Farzaneh-Far, Ramin • Inrig, Jula Kern
Assignees
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Publication Number
US-11324734-B2
Publication Date
2022-05-10
Expiration Date
Abstract
Provided herein are specific doses of, and dosing regimens for, using a HIF prolyl hydroxylase inhibitor in treating or preventing anemia, such as anemia secondary to or associated with chronic kidney disease, anemia secondary to or associated with non-dialysis dependent chronic kidney disease anemia associated with or resulting from chemotherapy, or anemia associated with AIDS.
Core Innovation
The invention relates to a tablet formulation comprising an intra-granular component, an extra-granular component, and a film coating component. The intra-granular component comprises about 60% to about 70% by weight of {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid or a pharmaceutically acceptable salt thereof, about 20% to about 30% by weight of microcrystalline cellulose, about 2.5% to about 3.5% by weight of sodium starch glycolate, and about 2.3% to about 3.3% by weight of hydroxypropyl methylcellulose. The extra-granular component comprises about 2.5% to about 3.5% by weight of sodium starch glycolate, about 0.2% to about 0.3% by weight of colloidal silicon dioxide, and about 0.55% to about 0.95% by weight of magnesium stearate, and the film coating component comprises about 1.0% to about 8% by weight of a tablet coating.
The document also describes HIF-alpha stabilizers, including pharmaceutically acceptable salts, solvates, and hydrates, and related metabolites such as phenolic glucuronides and acyl-glucuronides. It provides tablet formulation concepts that include the same three-part architecture and specifies excipients and weight-percentage ranges for the intra-granular and extra-granular regions. The film coating amount is further defined as about 1.0% to about 8% by weight of a tablet coating.
From the provided document content, the formulation is associated with clinical use of HIF prolyl hydroxylase inhibitors/HIF-alpha stabilizers to treat anemia in non-dialysis-dependent chronic kidney disease and other conditions associated with HIF prolyl hydroxylase modulation. The stated use also includes promoting wound healing, revascularization/vascularization of ischemic tissue, and guided tissue regeneration/skin graft replacement. The document further describes hemoglobin monitoring and hemoglobin increase/decrease adjustment, including dosing schedules, daily dose ranges, and combination approaches with iron and ESA.
Claims Coverage
The document content includes independent claims directed to a tablet formulation architecture, with inventive features centered on a three-part tablet composition and specified weight-percentage ranges for the intra-granular, extra-granular, and film coating components.
Three-part tablet formulation with intra-granular, extra-granular, and film coating components
A tablet formulation comprising an intra-granular component, an extra-granular component, and a film coating component, wherein the intra-granular component and extra-granular component each have specified weight-percentage ranges for designated excipients, and the film coating component comprises about 1.0% to about 8% by weight of a tablet coating.
Intra-granular composition with specified active and excipient ranges
The intra-granular component comprises about 60% to about 70% by weight of {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid or a pharmaceutically acceptable salt thereof, about 20% to about 30% by weight of microcrystalline cellulose, about 2.5% to about 3.5% by weight of sodium starch glycolate, and about 2.3% to about 3.3% by weight of hydroxypropyl methylcellulose.
Extra-granular composition with specified excipient ranges
The extra-granular component comprises about 2.5% to about 3.5% by weight of sodium starch glycolate, about 0.2% to about 0.3% by weight of colloidal silicon dioxide, and about 0.55% to about 0.95% by weight of magnesium stearate.
Overall, the claims define a tablet formulation with a three-region architecture and use quantitative, weight-based constraints to specify the active and excipient composition of the intra-granular and extra-granular components and the proportion of film coating.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Anemia treatment in non-dialysis-dependent chronic kidney disease, including patient selection criteria and hemoglobin monitoring-based dose adjustment.
Use with combination approaches including iron and ESA (erythropoiesis-stimulating agent/rhEPO) as described in the document.
Promoting wound healing.
Revascularization/vascularization of ischemic tissue.
Guided tissue regeneration/skin graft replacement.
Broader disease indications tied to HIF prolyl hydroxylase modulation.
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