Pharmaceutical compositions comprising a JAK inhibitor
Inventors
Alonzo, David • Li, Bei • Stefanidis, Dimitrios
Assignees
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Publication Number
US-12502394-B2
Publication Date
2025-12-23
Expiration Date
Abstract
Pharmaceutical compositions comprising filgotinib maleate Form I, further comprising citric acid, and characterized by an XRPD pattern substantially the same as shown in FIG. 1 and uses thereof are described herein.
Core Innovation
The invention relates to a pharmaceutical composition comprising a therapeutically effective amount of filgotinib maleate Form I together with citric acid, where the filgotinib maleate Form I is characterized by an XRPD pattern substantially the same as shown in FIG. 1. The XRPD characterization is presented using a diffractometer and Cu-Kα radiation, and the pattern is described through matching XRPD peak positions and patterns.
The disclosed solid form characterization of filgotinib maleate Form I is further supported by thermogravimetric analysis (TGA) thermograms substantially the same as shown in FIG. 2 and a 1H NMR proton nuclear magnetic resonance spectrum substantially the same as shown in FIG. 3. These analytical characterizations are used to define and verify the identity of filgotinib maleate Form I in the pharmaceutical composition.
The document also discloses formulations in which citric acid is used alongside other optional acids and common tablet excipients, and it provides example evidence based on XRPD peak sets and comparative pharmacokinetic outcomes. The pharmacokinetic comparison indicates increased exposure with concurrent use of fumaric acid/citric acid versus formulations lacking those acids, alongside human bioavailability comparisons using a test versus reference formulation (WO 2015/117980).
Claims Coverage
The independent claim coverage centers on a pharmaceutical composition that combines filgotinib maleate Form I with citric acid, with Form I defined by an XRPD pattern substantially the same as FIG. 1. The dependent claims add further inventive features to define Form I by additional characterization methods and to specify formulation and therapeutic use for JAK-mediated inflammatory diseases.
Filgotinib maleate Form I defined by an XRPD pattern with citric acid
A pharmaceutical composition comprising a therapeutically effective amount of filgotinib maleate Form I and citric acid, wherein the filgotinib maleate Form I is characterized by an XRPD pattern substantially the same as shown in FIG. 1.
Specific XRPD peak set for Form I on a Cu-Kα diffractometer
A pharmaceutical composition in which filgotinib maleate Form I is defined by an XRPD pattern comprising peaks at 28.9, 16.4, 8.2, 18.9, 20.0, 11.9, 14.9, 18.1, 20.5, and 22.6° 2θ (±10.2° 2θ), as determined on a diffractometer using Cu-Kα radiation.
Form I defined by a TGA thermogram substantially the same as FIG. 2
A pharmaceutical composition where filgotinib maleate Form I is characterized by a thermogravimetric analysis (TGA) thermogram substantially the same as that in FIG. 2.
Form I defined by a 1H NMR spectrum substantially the same as FIG. 3
A pharmaceutical composition in which filgotinib maleate Form I has a 1H NMR proton nuclear magnetic resonance spectrum substantially the same as shown in FIG. 3.
Quantitative formulation ranges for active and excipients
A pharmaceutical composition defined by weight-percentage ranges of filgotinib maleate Form I, microcrystalline cellulose, lactose monohydrate, pregelatinized starch, colloidal silicon dioxide, and magnesium stearate.
Treatment of a JAK-mediated inflammatory disease by administering the composition
A method treats a JAK-mediated inflammatory disease by administering a pharmaceutical composition to a patient, where the disease is selected from the listed inflammatory disorders.
Overall, the claims cover a composition containing filgotinib maleate Form I and citric acid, with Form I identity verified by an XRPD pattern substantially the same as FIG. 1, and further refined by additional characterization, formulation constraints, and treatment of JAK-mediated inflammatory diseases.
Stated Advantages
Increased exposure with concurrent use of fumaric acid/citric acid versus formulations lacking those acids.
Human bioavailability comparisons using a test versus reference formulation (WO 2015/117980).
Documented Applications
Treatment of a JAK-mediated inflammatory disease by administering a pharmaceutical composition to a patient, with disease selected from rheumatoid arthritis, Crohn's disease, ulcerative colitis, alopecia areata, uveitis, acute graft-versus-host disease, cutaneous lupus nephritis, membranous lupus nephritis, atopic dermatitis, psoriasis, ankylosing spondylitis, and psoriatic arthritis.
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