Use of inhibitors of bruton's tyrosine kinase (Btk)
AssigneePharmacyclics, Inc.
InventorsLee Honigberg, David J. Loury
Life of this patent
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Abstract
Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.
Claims17
A method of inhibiting proliferation and survival of activated B-cells in a human subject suffering from a B-cell proliferative disorder, comprising:
- orally administering to the human subject suffering from a B-cell proliferative disorder a therapeutically effective amount of 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (Compound 13), on a continuous once-daily regimen until progression of the disorder or unacceptable toxicity,
- wherein said administration of the therapeutically effective amount results in an AUC(0-24) of >about 100 ng*h/ml;
- and
- wherein said administration of the therapeutically effective amount results in >90% of the Btk active sites in the peripheral blood mononuclear cells of the human subject being occupied by Compound 13 twenty-four hours following said administration.
A method of inhibiting proliferation and survival of activated B-cells in a human subject suffering from a B-cell proliferative disorder, comprising:
- orally administering to the human subject suffering from a B-cell proliferative disorder a therapeutically effective amount of 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (Compound 13),
- wherein the therapeutically effective amount of Compound 13 is an amount that results in >90% of the Btk active sites in the peripheral blood mononuclear cells of the human subject being occupied by Compound 13 twenty-four hours following said administration, and
- wherein proliferation and survival of the activated B-cells in the human are inhibited.
Dependencies are inferred from the claim text.