Combination of a btk inhibitor and a checkpoint inhibitor for treating cancers
AssigneesGilead Sciences, Inc., Ono Pharmaceutical Co., Ltd.
InventorsSriram Venkataraman, Daniel B. Tumas, Kohei Tanaka, Tomoko Yasuhiro, Toshio Yoshizawa
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Abstract
Provided herein are methods relating to a therapeutic strategy for treatment of cancer, including hematological malignancies. In particular, the methods include administration of a Btk inhibitor and a checkpoint inhibitor, including combinations in which the Btk inhibitor is 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one, or a pharmaceutically acceptable salt thereof, and the checkpoint inhibitor is selected from inhibitors of PD-1, PD-L1, and CTLA-4.
Claims23
A method for a treating cancer in a human in need thereof, comprising administering to the human a therapeutically effective amount of a Btk inhibitor and a therapeutically effective amount of a checkpoint inhibitor, wherein the Btk inhibitor has the chemical structure:
- or a pharmaceutically acceptable salt or hydrate thereof.
An article of manufacture comprising:
- (i) a unit dosage form of a Btk inhibitor, wherein the Btk inhibitor is 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one, or a pharmaceutically acceptable salt or hydrate thereof;
- and
- (ii) a unit dosage form of a checkpoint inhibitor;
- and
- (iii) a label containing instructions for use of the Btk inhibitor and the checkpoint inhibitor in treating cancer.
The article of manufacture wherein the checkpoint inhibitor is an inhibitor of a checkpoint protein selected from the group of PD-1, PD-L1, CTLA-4, PD-L2, LAG3, Tim3, 2B4, A2aR, ID02, B7-H3, B7-H4, BTLA, CD2, CD20, CD27, CD28, CD30, CD33, CD40, CD52, CD70, CD80, CD86, CD112, CD137, CD160, CD226, CD276, DR3, OX-40, GAL9, GITR, HVEM, IDO1, ICOS, KIR, LAIR, LIGHT, MARCO, PS, SLAM, TIGIT, VISTA, VTCN1 and combinations thereof
A kit comprising:
- (i) a pharmaceutical composition comprising a Btk inhibitor, wherein the Btk inhibitor is has the structure
- or a pharmaceutically acceptable salt or hydrate thereof;
- (ii) a pharmaceutical composition comprising a checkpoint inhibitor.
A method for sensitizing a human who is (i) refractory to at least one chemotherapy treatment, or (ii) in relapse after treatment with chemotherapy, or both (i) and (ii), wherein the method comprises administering a Btk inhibitor in combination with a checkpoint inhibitor to the human.
Dependencies are inferred from the claim text.