IP Library Granted Patent US 10,912,771
Granted Patent B1
US 10,912,771 · App. 17/073,304 · Granted Feb 9, 2021

Methods for the administration of certain VMAT2 inhibitors

Inventors: Christopher F. O'Brien (San Diego, CA); Haig P. Bozigian (San Diego, CA)
Assignee: Neurocrine Biosciences, Inc.
A61K31/4745
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Quick Facts
Patent No.
US 10,912,771
App. No.
17/073,304
Granted
Feb 9, 2021
Kind
B1
Abstract

Provided are methods of administering a vesicular monoamine transport 2 (VMAT2) inhibitor chosen from valbenazine and (+)-α-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-ol, or a pharmaceutically acceptable salt and/or isotopic variant thereof to a patient in need thereof wherein the patient is being treated with a strong cytochrome P450 3A4 (CYP3A4) inducer.

Claims (17)

1. A method of treating a patient with a hyperkinetic movement disorder, wherein the patient is being administered a strong cytochrome P450 3A4 (CYP3A4) inducer, comprising:

discontinuing treatment of the strong CYP3A4 inducer, and then

orally administering once daily to the patient a therapeutically effective amount of a vesicular monoamine transporter 2 (VMAT2) inhibitor chosen from (S)-2-amino-3-methyl-butyric acid (2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-yl ester and a pharmaceutically acceptable salt thereof, thereby avoiding the concomitant use of the VMAT2 inhibitor with the strong CYP3A4 inducer.

2. The method of claim 1 , wherein the strong CYP3A4 inducer is chosen from nevirapine, pentobarbital, phenytoin, lumacaftor, rifabutin, rifampicin, carbamazepine, fosphenytoin, phenobarbital, primidone, enzalutamide, mitotane, and St. John's Wort.

3. The method of claim 1 , wherein the strong CYP3A4 inducer is chosen from rifampicin, carbamazepine, phenytoin, and St. John's Wort.

4. The method of claim 1 , wherein the strong CYP3A4 inducer is rifampicin.

5. The method of claim 1 , wherein the VMAT2 inhibitor is administered in the form of a capsule.

6. The method of claim 1 , wherein the hyperkinetic movement disorder is tardive dyskinesia.

7. The method of claim 1 , wherein the hyperkinetic movement disorder is chorea.

8. The method of claim 1 , wherein the hyperkinetic movement disorder is chorea associated with Huntington's disease.

9. The method of claim 1 , wherein the VMAT2 inhibitor is a pharmaceutically acceptable salt of (S)-2-amino-3-methyl-butyric acid (2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-yl ester.

10. The method of claim 1 , wherein the VMAT2 inhibitor is a ditosylate salt of (S)-2-amino-3-methyl-butyric acid (2R,3R, 11bR)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-yl ester.

11. The method of claim 1 , wherein the ditosylate salt of (S)-2-amino-3-methyl-butyric acid (2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-yl ester is in polymorphic Form I.

12. The method of claim 1 , wherein the therapeutically effective amount is an amount equivalent to about 40 mg as measured by (S)-2-amino-3-methyl-butyric acid (2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-yl ester free base once daily for one week, and an amount equivalent to about 80 mg as measured by (S)-2-amino-3-methyl-butyric acid (2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-yl ester free base once daily after one week.

13. The method of claim 1 , wherein the therapeutically effective amount is an amount equivalent to about 40 mg as measured by (S)-2-amino-3-methyl-butyric acid (2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-yl ester free base once daily.

14. The method of claim 1 , wherein the therapeutically effective amount is an amount equivalent to about 60 mg as measured by (S)-2-amino-3-methyl-butyric acid (2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-yl ester free base once daily.

15. The method of claim 1 , wherein the therapeutically effective amount is an amount equivalent to about 80 mg as measured by (S)-2-amino-3-methyl-butyric acid (2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-yl ester free base once daily.

Assignments (2)
CONFIRMATORY GRANT OF SECURITY INTEREST IN UNITED STATES PATENTS Recorded May 26, 2026
From: NEUROCRINE BIOSCIENCES, INC.
To: JPMORGAN CHASE BANK, N.A.
Reel/Frame 075670/0001 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 12, 2020
From: O'BRIEN, CHRISTOPHER F.; BOZIGIAN, HAIG P.
To: NEUROCRINE BIOSCIENCES, INC.
Reel/Frame 054349/0110 →
Continuity (2)
Continuation 16481033
Provisional Application 62451605 · Jan 27, 2017