Amorphous nilotinib microparticles and uses thereof
AssigneeFlex Pharma, LLC
InventorsChristian F. Wertz, Tzehaw Chen, Joseph McTarsney
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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.
Claims20
A treatment regimen for treating a proliferative disorder in a patient in need thereof, the regimen comprising:
- (a) administering to the patient a first dose, the first dose comprising a standard dosage of a proton pump inhibitor;
- and
- (b) within 12 hours after the first dose, administering a second dose to the patient, the second dose comprising 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;
- wherein the nilotinib and the hydroxypropyl methylcellulose acetate succinate are present in the amorphous solid dispersion in a w/w ratio of 20:80 to 95:5 (nilotinib:HPMC-AS);
- wherein the amount of nilotinib in the second dose is 50 to 80% less than a dose required for delivering a therapeutically effective amount of nilotinib in the fasted state using a conventional immediate-release crystalline nilotinib formulation;
- and
- wherein the second dose provides a therapeutically relevant exposure of nilotinib to the patient.
Dependencies are inferred from the claim text.