Use of Flibanserin for the Treatment of Sexual Disorders in Females

• US 20090318469A1
• Filed: 07/11/2007
• Published: 12/24/2009
• Est. Priority Date: 07/14/2006
• Status: Abandoned Application

• Current Assignee: Sprout Pharmaceuticals, Inc. (Sprout2, Inc.)
• Original Assignee: Boehringer Ingelheim International GmbH (C.H. Boehringer Sohn AG & Co. KG)
• Inventors: Pyke, Robert
• Application Number:
  US12/306,945
• Publication Number:
  US 20090318469A1
• Time in Patent Office: Days
• US Class Current: 514/254.60
• CPC Class Codes: A61K 31/496 Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/08 for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis

Abstract

The invention is directed to the use of flibanserin or a pharmacologically acceptable derivative thereof, for the preparation of a medical composition for the treatment of Sexual Disorder in females whereby the medication of a patient is selected to achieve a significant change (with administration of a therapeutically effective amount of flibanserin) starting from a baseline (without administration of flibanserin), the significant change being achieved within at least one primary criteria for efficacy and optionally within at least one secondary criteria of efficacy.

Claims

1. A method for treating a sexual disorder in a female patient comprising administering a medication comprising flibanserin or a pharmacologically acceptable derivative thereof whereby the medication of the female patient is selected to achieve a significant change (with administration of a therapeutically effective amount of flibanserin) starting from a baseline (without administration of flibanserin),

wherein the significant change is within at least one primary criteria for efficacy, the primary criteria for efficacy being selected from the group consisting of criteria a) and criteria b),

wherein:

criteria a) is the number of satisfying sexual events determined with the following algorithm;

total monthly events=28×

(sum of the number of events)/(sum of number of days entered);

 

and

criteria b) is the level of sexual desire collected daily determined with the following algorithm;

Desire days=28×

(number of entries with moderate or strong desire)/(number of entries),

 

wherein the significant change determined by comparing the algorithm of criteria a) with and without administration of flibanserin is represented by a satisfying sexual events increase of at least two per month; and

the significant change determined by comparing the algorithm of criteria b) with and without administration of flibanserin is represented by a desire days increase of at least four per month.

2. The method for treating a sexual disorder in a female patient according to claim 1, whereby the medication of the female patient is selected to achieve a significant change (with administration of a therapeutically effective amount of flibanserin) starting from a baseline (without administration of flibanserin), wherein the significant change is within at least one secondary criteria for efficacy,

whereby the secondary criteria for efficacy are criteria c), criteria d) criteria e), and criteria f),

wherein:

criteria c) is the Female Sexual Distress Scale (FSDS) or the Female Sexual Distress Scale-Revised (FSDS-R) test;

criteria d) is the Female Sexual Functioning Index (FSFI);

criteria e) is the Patient Global Impression (PGI) of Improvement; and

criteria f) is the Patient Benefit Evaluation,

wherein the significant change determined by comparing at least one of the criteria c) to f) with and without administration of flibanserin, respectively, is represented by

in criteria c), a PGI of Improvement of at least ‘

1’

, preferably at least ‘

2’

; and

in criteria d), an improvement of the result(s) of the test performed; and

in criteria e), an improvement of the result(s) of the test performed; and

in criteria f), an improvement of the result(s) of the test performed.

3. The method for treating a sexual disorder in a female patient according to claim 1, wherein the significant change of at least one primary criteria for efficacy is determined over a period of time of one month or longer.

4. The method for treating a sexual disorder in a female patient according to claim 1, wherein the medication to be administered to the female patient is adjusted to have a significant change in at least one of criteria a) or b) to achieve the therapeutic most effective dose and/or most effective administration mode of the medication.

6. A method for treating a sexual disorder in a female patient according to claim 1, wherein the dose is administered in the morning and the evening.

7. The method for treating a sexual disorder in a female patient according to claim 1, wherein the first dose of a beginning therapy is administered in the evening.

8. The method for treating a sexual disorder in a female patient according to claim 1, wherein the dose is administered in an amount of 1 to 100 mg.

9. The method for treating a sexual disorder in a female patient according to claim 8, the dose is 10 to 90 mg and is administered once daily or twice daily.

10. The method for treating a sexual disorder in a female patient according to claim 1, wherein the dose is administered once daily every evening.

12. The method for treating a sexual disorder in a female patient according to claim 1, wherein the sexual disorder is selected from the group consisting of Sexual Desire Disorders (such as Hypoactive Sexual Desire Disorders, Sexual Aversion Disorders, and Sexual Arousal Disorders), Orgasmic Disorders, Sexual Pain Disorders, Sexual Dysfunction due to a General Medical Condition, Substance-Induced Sexual Dysfunction, and Sexual Dysfunction not otherwise specified.

13. The method for treating a sexual disorder in a female patient according to claim 1, wherein the sexual disorder is Dyspareunia, Vaginismus, Noncoital Sexual Pain Disorder, Sexual Pain Disorder due to General Medical Condition, or Substance-induced Sexual Pain Disorder.

14. The method for treating a sexual disorder in a female patient according to claim 1, wherein the sexual disorder is Sexual Desire Disorder, Hypoactive Sexual Desire Disorder (HSDD), Sexual Aversion Disorder, loss of sexual desire, lack of sexual desire, decreased sexual desire, inhibited sexual desire, loss of libido, libido disturbance, or frigidity.

15. The method for treating a sexual disorder in a female patient according to claim 1, wherein the sexual disorder is Hypoactive Sexual Desire Disorder and loss of sexual desire.

16. The method for treating a sexual disorder in a female patient according to claim 1, wherein the sexual disorder is selected from the group consisting of acquired Hypoactive Sexual Desire Disorder, acquired Sexual Aversion Disorder, acquired loss of sexual desire, acquired lack of sexual desire, acquired decreased sexual desire, acquired inhibited sexual desire, acquired loss of libido, acquired libido disturbance, and acquired frigidity.

17. The method for treating a sexual disorder in a female patient according to claim 1, wherein the sexual disorder is a post- or pre-menopausal Sexual Desire Disorder.

18. The method for treating a sexual disorder in a female patient according to claim 1, wherein the sexual disorder is Premenstrual Dysphoria, Premenstrual Syndrome, or Premenstrual Dysphoric Disorder.

19. The method for treating a sexual disorder in a female patient according to claim 1, wherein the medication is suitable for oral, rectal, or parenteral administration, or for nasal inhalation.

20. The method for treating a sexual disorder in a female patient according to claim 1, wherein the flibanserin derivative is a pharmacologically acceptable acid addition salt, hydrate, or solvate of flibanserin.

21. The method for treating a sexual disorder in a female patient according to claim 1, wherein the medication comprises flibanserin.

22. The method for treating a sexual disorder in a female patient according to claim 21, wherein the medication comprises flibanserin as polymorph A of the free base, having a melting point of about 161°

C. as measured using DSC.

23. The method for treating a sexual disorder in a female patient according to claim 1, wherein the pharmaceutically acceptable acid addition salt is selected from the salts formed by the acids selected from succinic acid, hydrobromic acid, acetic acid, fumaric acid, maleic acid, methanesulphonic acid, lactic acid, phosphoric acid, hydrochloric acid, sulphuric acid, tartaric acid, citric acid, and mixtures thereof.

24. The method for treating sexual disorder in a female patient according to claim 2, wherein the significant change of at least one primary criteria for efficacy and at least one secondary criteria for efficacy is determined over a period of time of one month or longer.

25. The method for treating sexual disorder in a female patient according to claim 2, wherein the medication to be administered to the female patient is adjusted to have a significant change in at least one of criteria a) or b), and at least one of criteria c), d), e), or f), to achieve the therapeutic most effective dose and/or most effective administration mode of the medication.

26. The method for treating sexual disorder in a female patient according to claim 3, wherein the medication to be administered to the female patient is adjusted to have a significant change in at least one of criteria a) or b), and at least one of criteria c), d), e), or f), to achieve the therapeutic most effective dose and/or most effective administration mode of the medication.

27. The method for treating a sexual disorder in a female patient according to claim 8, wherein the dose is administered in an amount of 1 to 40 mg.

28. The method for treating a sexual disorder in a female patient according to claim 8, wherein the dose is administered in an amount of 41 to 60 mg.

29. The method for treating a sexual disorder in a female patient according to claim 8, wherein the dose is administered in an amount of 61 to 90 mg.

30. The method for treating a sexual disorder in a female patient according to claim 8, wherein the dose is administered in an amount of 91 to 100 mg.

5. A method for treating a sexual disorder in a female patient comprising administering a medication comprising flibanserin or a pharmacologically acceptable derivative thereof, wherein the dose is administered once daily consecutively over a period of time.

11. (canceled)