Claims for Patent: 12,102,638

Summary for Patent: 12,102,638

Title:	Use of vibegron to treat overactive bladder
Abstract:	The present disclosure is directed to a method of treating overactive bladder comprising orally administering to a subject in need thereof an amount of from about 60 mg to about 90 mg (e.g., about 75 mg) of vibegron per day. The present disclosure is also directed to a pharmaceutical unit dosage composition comprising from about 60 mg to about 90 mg (e.g., about 75 mg) of vibegron for oral administration.
Inventor(s):	Stephen C. PISCITELLI, Paul Mudd
Assignee:	Urovant Sciences GmbH
Application Number:	US16/620,179
Patent Claims:	1. A method of treating overactive bladder in a human subject in need thereof, the method comprising administering to the subject about 75 mg per day of vibegron or a pharmaceutically acceptable salt thereof. 2. The method of claim 1, wherein treating overactive bladder comprises treating one or more symptoms selected from urge urinary incontinence (UUI), urinary urgency, urinary frequency, nocturia, or a combination thereof. 3. The method of claim 1, wherein the overactive bladder comprises symptoms of urge urinary incontinence (UUI), urinary urgency, and urinary frequency. 4. The method of claim 3, wherein vibegron is administered once per day. 5. The method of claim 4, wherein vibegron is administered with a meal. 6. The method of claim 4, wherein vibegron is administered without a meal. 7. The method of claim 4, wherein vibegron is administered as a tablet. 8. The method of claim 7, wherein the tablet is crushed before administration. 9. The method of claim 1, wherein after administration vibegron is effective in treating overactive bladder in about 4 weeks, about 3 weeks, or about 2 weeks. 10. The method of claim 9, wherein after administration vibegron is effective in treating overactive bladder in about 2 weeks. 11. The method of claim 1, wherein the subject is a female. 12. The method of claim 1, wherein the subject is a male. 13. The method of claim 1, wherein the subject suffers from severe renal impairment. 14. The method of claim 1, wherein the subject suffers from moderate renal impairment. 15. The method of claim 1, wherein the subject is concomitantly receiving a CYP3A/P-glycoprotein inhibitor. 16. The method of claim 1, wherein the subject is concomitantly receiving a CYP2D6 substrate, a CYP2C9 substrate, a CYP3A inhibitor, a P-glycoprotein inhibitor, an oral contraceptive, or a combination thereof. 17. The method of claim 1, wherein a pharmaceutically acceptable salt of vibegron is administered. 18. The method of claim 1, wherein the subject experiences a mean change of systolic blood pressure from baseline over a treatment period, wherein the mean change is less than 1 mm/Hg from that of a subject taking a placebo. 19. The method of claim 18, wherein the treatment period is selected from the group consisting of about 2, 4, 6, 8, 12, and 52 weeks. 20. The method of claim 1, wherein the percent of subjects that experience a mean change of systolic blood pressure from baseline of ≥15 mm/Hg over a treatment period is about 1.3%. 21. The method of claim 1, wherein the subject experiences a mean change of diastolic blood pressure from baseline over a treatment period, wherein the mean change is less than 1 mm/Hg from that of a subject taking a placebo. 22. The method of claim 1, wherein the subject experiences a mean change of diastolic blood pressure from baseline of less than 5 mm/Hg over a treatment period. 23. The method of claim 1, wherein the subject experiences a change in average number of micturitions per 24 hours from baseline of from about −1.5 to about −2.1 over a treatment period. 24. The method of claim 1, wherein the subject experiences a difference from placebo in average number of micturitions per 24 hours of from about −0.4 to about −0.8 over a treatment period. 25. The method of claim 1, wherein the subject has an average of ≥1 urge urinary incontinence (UUI) episodes per day prior to treatment and experiences a change in average number of UUI episodes from baseline of from about −1.8 to about −2.3 over a treatment period. 26. The method of claim 1, wherein the subject has an average of >1 urge urinary incontinence (UUI) episodes per day prior to treatment and experiences a difference from placebo in average number of UUI episodes of from about −0.3 to about −0.9 over a treatment period. 27. The method of claim 1, wherein the subject experiences a change in average number of urgency episodes from baseline of from about −2.3 to about −3.0 over a treatment period. 28. The method of claim 1, wherein the subject experiences a change in average number of total incontinence episodes from baseline of from about −2.0 to about −2.3 over a treatment period. 29. The method of claim 1, wherein the subject experiences a difference from placebo in increased volume voided per micturition of from about 20 mL to about 28 mL over a treatment period. 30. The method of claim 1, wherein treating overactive bladder comprises treating one or more symptoms of nocturia. 31. A method of treating overactive bladder in a human subject in need thereof, the method comprising administering to the subject about 75 mg of vibegron per day, wherein the pharmacokinetic profile of vibegron following a single dose has an area under the curve (AUC) of about 1140 ng-hr/mL±476 ng-hr/mL. 32. The method of claim 31, wherein the subject suffers from severe renal impairment. 33. The method of claim 31, wherein the subject suffers from moderate renal impairment. 34. The method of claim 31, wherein the subject is concomitantly receiving a CYP3A/P-glycoprotein inhibitor. 35. The method of claim 31, wherein the subject is concomitantly receiving a CYP2D6 substrate, a CYP2C9 substrate, a CYP3A inhibitor, a P-glycoprotein inhibitor, an oral contraceptive, or a combination thereof. 36. The method of claim 31, wherein the subject experiences a mean change of diastolic blood pressure from baseline of less than 5 mm/Hg over a treatment period. 37. A method of treating overactive bladder in a human subject in need thereof, the method comprising administering to the subject about 75 mg of vibegron per day, wherein the pharmacokinetic profile of vibegron following a single dose has a Cmax of about 120 ng/mL±74.7 ng/mL. 38. The method of claim 37, wherein the subject suffers from severe renal impairment. 39. The method of claim 37, wherein the subject suffers from moderate renal impairment. 40. The method of claim 37, wherein the subject is concomitantly receiving a CYP3A/P-glycoprotein inhibitor. 41. The method of claim 37, wherein the subject is concomitantly receiving a CYP2D6 substrate, a CYP2C9 substrate, a CYP3A inhibitor, a P-glycoprotein inhibitor, an oral contraceptive, or a combination thereof. 42. The method of claim 37, wherein the subject experiences a mean change of diastolic blood pressure from baseline of less than 5 mm/Hg over a treatment period. 43. A method of reducing the average number of micturitions per 24 hours in a human subject, the method comprising administering to the subject about 75 mg of vibegron per day, wherein the vibegron reduces the average number of micturitions to treat overactive bladder. 44. The method of claim 43, wherein the average number of micturitions per 24 hours is reduced from baseline by about −1.5 to about −2.1 over a treatment period. 45. The method of claim 43, wherein the difference from placebo in average number of micturitions per 24 hours is about −0.4 to about −0.8 over a treatment period. 46. A method of reducing the average number of UUI episodes per day in a human subject, the method comprising administering to the subject about 75 mg of vibegron per day, wherein the vibegron reduces the average number of UUI episodes to treat overactive bladder. 47. The method of claim 46, wherein the average number of UUI episodes per day is reduced from baseline by about −1.8 to about −2.3 over a treatment period. 48. The method of claim 46, wherein the difference from placebo in average number of UUI episodes is from about −0.3 to about −0.9 over a treatment period. 49. A method of reducing the average number of urgency episodes per day in a human subject, the method comprising administering to the subject about 75 mg of vibegron per day, wherein the vibegron reduces the average number of urgency episodes to treat overactive bladder. 50. The method of claim 49, wherein the average number of urgency episodes per day is reduced from baseline by at least 50% over a treatment period. 51. A method of reducing the average number of total incontinence episodes per day in a human subject, the method comprising administering to the subject about 75 mg of vibegron per day, wherein the vibegron reduces the average number of total incontinence episodes to treat overactive bladder. 52. The method of claim 51, wherein the average number of total incontinence episodes per day is reduced from baseline by about −2.0 to about −2.3 over a treatment period. 53. A method of increasing the volume voided (mL) per micturition in a human subject, the method comprising administering to the subject about 75 mg of vibegron per day, wherein the vibegron increases volume voided per micturition to treat overactive bladder. 54. The method of claim 53, wherein the increase in volume voided (mL) per micturition is increased from placebo from about 20 mL to about 28 mL over a treatment period.