SITE SPECIFIC DOSING OF A BTK INHIBITOR
First Claim
Patent Images
1. A solid oral dosage form comprising:
- (i) 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)-pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile(Compound (I)) and/or a pharmaceutically acceptable salt thereof;
(ii) means for release of Compound (I) and/or said pharmaceutically salt thereof in one or more mammalian intestinal sites chosen from the duodenum, jejunum, ileum, and colon; and
(iii) a pharmaceutically acceptable excipient,wherein the average systemic bioavailability of Compound (I) as measured by plasma AUC resulting from administration of said solid oral dosage form is from about 150% to about 4000% of the average systemic bioavailability of Compound (I) as measured by plasma AUC resulting from administration of an immediate release dosage form having an equivalent amount of said Compound (I) and/or said pharmaceutically acceptable salt thereof.
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Accused Products
Abstract
Disclosed herein are formulations and methods of site specific administration of Compound (I) or a pharmaceutically acceptable salt thereof. Compound (I) is a potent BTK inhibitor and hence can be useful for the treatment of diseases such as cancer, autoimmune, and inflammatory diseases.
7 Citations
57 Claims
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1. A solid oral dosage form comprising:
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(i) 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)-pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile (Compound (I)) and/or a pharmaceutically acceptable salt thereof; (ii) means for release of Compound (I) and/or said pharmaceutically salt thereof in one or more mammalian intestinal sites chosen from the duodenum, jejunum, ileum, and colon; and (iii) a pharmaceutically acceptable excipient, wherein the average systemic bioavailability of Compound (I) as measured by plasma AUC resulting from administration of said solid oral dosage form is from about 150% to about 4000% of the average systemic bioavailability of Compound (I) as measured by plasma AUC resulting from administration of an immediate release dosage form having an equivalent amount of said Compound (I) and/or said pharmaceutically acceptable salt thereof. - View Dependent Claims (2, 5, 8, 9, 15, 21, 24, 25, 26, 28, 29, 30, 31, 33, 51, 52, 55, 56)
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3. A solid oral dosage form comprising:
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(i) 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)-pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile (Compound (I)) and/or a pharmaceutically acceptable salt thereof; (ii) means for release of Compound (I) and/or said pharmaceutically salt thereof in one or more mammalian intestinal sites chosen from the jejunum, ileum, and colon; and (iii) a pharmaceutically acceptable excipient, wherein the average systemic bioavailability of Compound (I) as measured by plasma AUC resulting from administration of said solid oral dosage form is from about 125% to about 2000% of the average systemic bioavailability of Compound (I) as measured by plasma AUC resulting from administration of an intraduodenal release dosage form having an equivalent amount of said Compound (I) and/or said pharmaceutically acceptable salt thereof. - View Dependent Claims (4)
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6-7. -7. (canceled)
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10. (canceled)
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11. A solid oral dosage form comprising:
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(i) 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)-pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile (Compound (1)) and/or a pharmaceutically acceptable salt thereof; (ii) an enteric coating which releases Compound (I) and/or said pharmaceutically salt thereof in one or more mammalian intestinal sites chosen from the duodenum, jejunum, ileum, and colon; and (iii) a pharmaceutically acceptable excipient. - View Dependent Claims (12, 36, 42, 43, 44, 45, 46, 47, 48, 49, 50, 53, 54)
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13-14. -14. (canceled)
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16-20. -20. (canceled)
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22-23. -23. (canceled)
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27. (canceled)
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32. (canceled)
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34-35. -35. (canceled)
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37-41. -41. (canceled)
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57. (canceled)
Specification