Amorphous nilotinib microparticles and uses thereof
AssigneeNanocopoeia, LLC
InventorsChristian F. Wertz, Tzehaw Chen, Joseph McTarsney
Life of this patent
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Abstract
Amorphous solid dispersions and pharmaceutical compositions of the protein kinase inhibitor nilotinib. The pharmaceutical compositions may be used in methods of treating a proliferative disorder such as cancer. In some embodiments, the pharmaceutical compositions can be administered without regard to food consumption. In other embodiments, the pharmaceutical compositions can be administered at a significantly lower dose as compared to a commercially available immediate-release nilotinib formulation, while providing a comparable therapeutic effect.
Claims31
1-30. (canceled)
A pharmaceutical composition comprising an amorphous solid dispersion, the amorphous solid dispersion comprising nilotinib and one or more polymers;
- wherein the one or more polymers comprises a hydroxypropyl methylcellulose acetate succinate that exhibits pH-dependent solubility;
- and
- wherein the nilotinib and the one or more polymers are present in the amorphous solid dispersion in a w/w ratio of 25:75 to 90:10 (nilotinib:polymer).
A method of safely delivering nilotinib to a patient in need of such therapy, the method comprising:
- (a) administering to the patient a therapeutically effective amount of a pharmaceutical composition comprising nilotinib and one or more polymers;
- and
- (b) administering a meal to the patient;
- wherein steps (a) and (b) occur within less than two hours of each other;
- wherein the one or more polymers comprises a hydroxypropyl methylcellulose acetate succinate that exhibits pH-dependent solubility;
- and
- wherein the nilotinib and the one or more polymers are present in the amorphous solid dispersion in a w/w ratio of 25:75 to 90:10 (nilotinib:polymer).
A method of delivering a therapeutically relevant exposure of nilotinib to a subject without regard to whether the subject is in a fasted state or a fed state, comprising administering to the subject a pharmaceutical comprising an amorphous solid dispersion, the amorphous solid dispersion comprising nilotinib and one or more polymers;
- wherein the one or more polymers comprises a hydroxypropyl methylcellulose acetate succinate that exhibits pH-dependent solubility;
- and
- wherein the nilotinib and the one or more polymers are present in the amorphous solid dispersion in a w/w ratio of 25:75 to 90:10 (nilotinib:polymer).
Dependencies are inferred from the claim text.