Iloperidone for the treatment of schizophrenia

• US 10,441,580 B2
• Filed: 02/17/2016
• Issued: 10/15/2019
• Est. Priority Date: 02/17/2015
• Status: Active Grant

• Current Assignee: Vanda Pharmaceuticals Incorporated
• Original Assignee: Vanda Pharmaceuticals Incorporated
• Inventors: Polymeropoulos, Mihael H., Wolfgang, Curt D.
• Primary Examiner(s): Solola, Taofiq A
• Application Number:
  US15/549,820
• Publication Number:
  US 20180021324A1
• Time in Patent Office: 1,336 Days
• Field of Search: 514326
• CPC Class Codes: A61K 31/454 containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia

Abstract

Aspects of the invention relate generally to the treatment of schizophrenia in an individual and, more specifically, to the treatment of an individual with iloperidone, an iloperidone metabolite, or a pharmaceutically-acceptable salt thereof. In one embodiment, the invention provides a method of preventing schizophrenic relapse in an individual diagnosed with schizophrenia, the method comprising: administering to the individual iloperidone, an iloperidone metabolite, or a pharmaceutically-acceptable salt thereof at a daily dose between about 12 mg and about 16 mg following a period in which the individual'"'"'s schizophrenia was stabilized.

Claims

1. A method of treating schizophrenia or a symptom of schizophrenia in an individual, the method comprising:

administering to the individual a titrated first daily dose of 16-24 mg/day of iloperidone or a pharmaceutically-acceptable salt thereof during an acute treatment phase, wherein the acute treatment phase follows an initial titration of iloperidone,

followed by administering to the individual a second daily dose that is smaller than the titrated first daily dose and is 12-16 mg/day of iloperidone or a pharmaceutically-acceptable salt thereof during a maintenance treatment phase, following completion of the acute treatment phase.

2. The method of claim 1, wherein the titrated first daily dose is 8-12 mg of iloperidone administered orally twice daily, and the second daily dose is 6-8 mg of iloperidone administered orally twice daily.

3. The method of claim 1, wherein the second daily dose is 75% of the first daily dose.

4. The method of claim 1, wherein the titrated first daily dose is 16 mg and the second daily dose is 12 mg.

5. The method of claim 1, wherein the titrated first daily dose is 12 mg and the second daily dose is 8 mg.

6. The method of claim 1, wherein the second daily dose is 50% of the first daily dose.

7. The method of claim 6, wherein the titrated first daily dose is 24 mg and the second daily dose is 12 mg.

8. The method of claim 6, wherein the titrated first daily dose is 16 mg and the second daily dose is 8 mg.

9. The method of claim 6, wherein the titrated first daily dose is 12 mg and the second daily dose is 6 mg.

10. The method of claim 1, wherein the second daily dose is between 12 mg and 16 mg.

11. The method of claim 10, wherein the second daily dose is between 12 mg and 14 mg.

12. A method of continuing the treatment of schizophrenia in an individual who has been receiving a titrated first daily dose of 16-24 mg/day of iloperidone or a pharmaceutically acceptable salt thereof during an acute treatment phase of the schizophrenia, the method comprising:

administering a second daily dose of 12-16 mg/day of iloperidone or the pharmaceutically acceptable salt thereof that is reduced relative to the first daily dose during a subsequent maintenance treatment phase following completion of the acute treatment phase.

13. The method of claim 12, wherein the titrated first daily dose of iloperidone or the pharmaceutically acceptable salt thereof is 8-12 mg administered twice daily, and the second daily dose of iloperidone or the pharmaceutically acceptable salt thereof is 6-8 mg administered twice daily.

14. The method of claim 12, wherein the second daily dose is 75% of the first daily dose.

15. The method of claim 14, wherein the first daily dose is 16 mg and the second daily dose is 12 mg/day.

16. The method of claim 14, wherein the first daily dose is 20 mg and the second daily dose is 15 mg/day.

17. The method of claim 12, wherein the first daily dose is 24 mg and the second daily dose is 16 mg.

18. The method of claim 12, wherein the second daily dose is 50% of the first daily dose.

19. The method of claim 18, wherein the first daily dose is 24 mg and the second daily dose is 12 mg/day.

20. The method of claim 12, wherein the second daily dose is between 12 mg and 14 mg/day.