IP Library Granted Patent US 10,751,342
Granted Patent B2
US 10,751,342 · App. 16/748,142 · Granted Aug 25, 2020

Use of inhibitors of Bruton's tyrosine kinase (Btk)

Inventors: Joseph J. Buggy (Mountain View, CA); Gwen Fyfe (San Francisco, CA); Lee Honigberg (San Francisco, CA); David J. Loury (Incline Village, NV)
Assignee: Pharmacyclics LLC
A61K31/519A61K9/007A61K9/0014A61K9/0019A61K9/0031A61K9/0048A61K9/0056A61K9/0078A61K9/06A61K9/4866A61K31/195A61K31/337A61K31/4184A61K31/436A61K31/437A61K31/454A61K31/475A61K31/4745A61K31/573A61K31/606A61K31/664A61K31/675A61K31/69A61K31/704A61K31/7032A61K31/7076A61K39/395A61K39/3955A61K39/39533A61K45/06A61K47/10A61K47/12A61K47/14A61K47/20A61K47/26A61K47/36A61K47/38C07D487/04
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Quick Facts
Patent No.
US 10,751,342
App. No.
16/748,142
Granted
Aug 25, 2020
Kind
B2
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.

Claims (19)

1. A method for treating relapsed or refractory CLL or SLL in an individual comprising orally administering to the individual a dose of 420 mg of an inhibitor of Bruton's tyrosine kinase (Btk) on a continuous once-daily regimen until progression of the CLL or SLL or unacceptable toxicity; and

lymphocytosis is not considered progression of the CLL or SLL,

wherein the inhibitor of Btk has the structure:

wherein the individual achieves a complete response.

2. The method of claim 1 , wherein said administering results in an AUC (0-24) of >about 100 ng*h/ml.

3. The method of claim 1 , wherein said administering results in >90% of the Btk active sites in the peripheral blood mononuclear cells of the individual being occupied by the inhibitor twenty-four hours following said administering.

4. The method of claim 1 , wherein the once-daily regimen is continued for at least 6 months.

5. A method for treating CLL or SLL in an individual comprising orally administering to the individual a dose of 420 mg of an inhibitor of Bruton's tyrosine kinase (Btk) on a continuous once-daily regimen until progression of the CLL or SLL or unacceptable toxicity; and

lymphocytosis is not considered progression of the CLL or SLL,

wherein the inhibitor of Btk has the structure:

wherein the individual achieves a complete response.

6. The method of claim 5 , wherein the individual is treatment nave.

7. The method of claim 5 , wherein said administering results in an AUC (0-24) of >about 100 ng*h/ml.

8. The method of claim 5 , wherein said administering results in >90% of the Btk active sites in the peripheral blood mononuclear cells of the individual being occupied by the inhibitor twenty-four hours following said administering.

9. The method of claim 5 , wherein the once-daily regimen is continued for at least 6 months.

10. The method of claim 1 , wherein the individual has relapsed or refractory CLL.

11. The method of claim 1 , wherein the individual has relapsed or refractory SLL.

12. The method of claim 5 , wherein the individual has relapsed or refractory CLL.

13. The method of claim 5 , wherein the individual has relapsed or refractory SLL.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 15, 2020
From: BUGGY, JOSEPH J.; FYFE, GWEN; LOURY, DAVID J.
To: PHARMACYCLICS, INC.
Reel/Frame 052943/0291 →
MERGER AND CHANGE OF NAME Recorded Jun 15, 2020
From: PHARMACYCLICS, INC.; OXFORD AMHERST LLC; PHARMACYCLICS LLC
To: PHARMACYCLICS LLC
Reel/Frame 052943/0309 →
MERGER Recorded Jun 15, 2020
From: OXFORD AMHERST CORPORATION; PHARMACYCLICS, INC.
To: PHARMACYCLICS, INC.
Reel/Frame 052943/0315 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 15, 2020
From: HONIGBERG, LEE
To: PHARMACYCLICS LLC
Reel/Frame 052943/0356 →