Focal adhesion kinase inhibitor as a therapeutic agent in diabetes
View Patent ↗It is disclosed herein that a FAK inhibitor induces conversion of acinar cells into beta cells. Methods are provided for increasing beta cell proliferation by administering an effective amount of a FAK inhibitor to a subject in need thereof. Methods are also provided for treating a subject with diabetes or at risk of developing diabetes, comprising administering to the subject a therapeutically effective amount of a FAK inhibitor.
1 . A method for treating a subject with type 2 diabetes, comprising:
administering to the subject a therapeutically effective amount of a focal adhesion kinase (FAK) inhibitor, wherein the FAK inhibitor is PF-562271, thereby treating the type 2 diabetes in the subject.
2 . The method of claim 1 , further comprising selecting the subject with type 2 diabetes for treatment with the FAK inhibitor.
3 . The method of claim 2 , wherein the therapeutically effective amount of the FAK inhibitor converts acinar cells into beta cells in the subject.
4 . The method of claim 2 , wherein treating the type 2 diabetes does not require administration of the FAK inhibitor after blood glucose is normalized.
5 . The method of claim 1 , wherein the FAK inhibitor is administered in a dose of 75 mg, 100 mg, or 125 mg, given once or twice daily.
6 . The method of claim 1 , further comprising measuring beta cell function of the subject.
7 . The method of claim 1 , further comprising measuring glucose tolerance, insulin resistance, plasma glucose levels, plasma insulin levels, serum triglycerides, free fatty acids, and/or HbA1c levels in a sample from the subject.
8 . The method of claim 1 , wherein the therapeutically effective amount of the FAK inhibitor increases a number of beta cells in the subject.
9 . The method of claim 1 , wherein the therapeutically effective amount of the FAK inhibitor converts acinar cells into beta cells in the subject.
10 . The method of claim 1 , wherein the therapeutically effective amount of the FAK inhibitor increases a number of insulin-secreting cells in the islets of Langerhans of the subject.
11 . The method of claim 1 , wherein the subject is human.
12 . The method of claim 1 , wherein the therapeutically effective amount of the FAK inhibitor reduces plasma glucose levels in the subject.
13 . The method of claim 1 , wherein the therapeutically effective amount of the FAK inhibitor increases plasma insulin levels in the subject.
14 . The method of claim 1 , further comprising measuring plasma glucose levels in a sample from the subject.
15 . The method of claim 1 , wherein treating the type 2 diabetes does not require administration of the FAK inhibitor after blood glucose is normalized.
16 . The method of claim 1 , further comprising detecting acinar-derived beta cells in the subject.
17 . The method of claim 1 , wherein a single dose of the FAK inhibitor is administered to the subject.
18 . The method of claim 1 , wherein the FAK inhibitor is not administered in combination with another diabetes medication or treatment.
19 . A method for treating a subject with type 2 diabetes, comprising:
selecting the subject with type 2 diabetes for treatment,
administering to the subject a therapeutically effective amount of PF-562271, and
subsequently detecting acinar-derived beta cells in the subject,
thereby treating the type 2 diabetes in the subject.
20 . The method of claim 19 , wherein the FAK inhibitor is not administered in combination with another diabetes medication or treatment.
21 . The method of claim 19 , wherein blood glucose level of the subject remains normalized one month after treatment with PF-562271 ceases.
22 . A method for treating a subject with type 2 diabetes, comprising:
selecting the subject with type 2 diabetes for treatment, and
increasing an amount of acinar-derived beta cells in the subject by administering a therapeutically effective amount of PF-562271 to the subject,
thereby treating the type 2 diabetes in the subject.