Combinations of Bruton’s tyrosine kinase (Btk) inhibitors, e.g., 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, with CYP3A4 inhibitors are provided. Also provided are methods of treating cancers, and autoimmune disorders by administering combinations of Bruton’s tyrosine kinase (Btk) inhibitors, e.g., 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, and CYP3A4 inhibitors.本發明提供布魯頓氏酪胺酸激酶(Btk)抑制劑(例如,1-((R)-3-(4-胺基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-d]嘧啶-1-基)哌啶-1-基)丙-2-烯-1-酮)與CYP3A4抑制劑之組合。本發明亦提供藉由投與布魯頓氏酪胺酸激酶(Btk)抑制劑(例如1-((R)-3-(4-胺基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-d]嘧啶-1-基)哌啶-1-基)丙-2-烯-1-酮)與CYP3A4抑制劑之組合治療癌症及自體免疫病症之方法。