Claims for Patent: 12,280,037

Summary for Patent: 12,280,037

Title:	Method and pharmaceutical composition for treating or preventing trichomoniasis and uses thereof
Abstract:	Method of treating or preventing trichomoniasis or T. vaginalis infection in a subject in need thereof, the method involving administering to the subject a therapeutically effective amount of secnidazole or a pharmaceutically acceptable salt in a microgranule formulation, wherein the microgranule formulation comprises a plurality of microgranules. The subject can also have bacterial vaginosis, is HIV-positive, and/or is suffering with metronidazole-resistant trichomoniasis and/or tinidazole-resistant trichomoniasis. The subject can also be a sexual partner of a person with trichomoniasis. The microgranule formulation can also be administered with paromomycin, tinidazole, metronidazole, boric acid or a combination thereof. Pharmaceutical compositions and uses for treating or preventing trichomoniasis or T. vaginalis infection in a subject in need thereof are also contemplated herein.
Inventor(s):	Helen S. PENTIKIS, David Palling, Carol J. BRAUN, Richard Holl, Gregory Kaufman
Assignee:	Evofem Biosciences Inc
Application Number:	US17/028,838
Patent Claims:	1. A method of treating trichomoniasis in a human in need thereof comprising orally administering to the human a microgranule formulation comprising a therapeutically effective amount of secnidazole or a pharmaceutically acceptable salt thereof that exhibits a maximum plasma concentration (Cmax) of 29.15 μg/ml to 31.05 μg/ml and a time to maximum plasma concentration (Tmax) of 6.6 hours to 24 hours in the human, wherein the microgranule formulation comprises a plurality of microgranules, each microgranule comprises secnidazole and has a particle diameter in the range of 400 micrometers to 841 micrometers, wherein secnidazole or the pharmaceutically acceptable salt thereof is the sole drug in the microgranule formulation. 2. The method of claim 1, wherein the therapeutically effective amount of secnidazole or a pharmaceutically acceptable salt thereof is a total daily dose of 2 grams, 4 grams or 6 grams of secnidazole or a pharmaceutically acceptable salt thereof in a microgranule formulation for a period of 1 day to 14 days. 3. The method of claim 1, wherein the human in need thereof is a sexual partner to a person with trichomoniasis, and the therapeutically effective amount of secnidazole or a pharmaceutically acceptable salt thereof is a total daily dose of 2 grams, 4 grams or 6 grams of secnidazole or a pharmaceutically acceptable salt thereof in a microgranule formulation. 4. The method of claim 1, wherein the microgranule formulation is a taste-masked microgranule formulation. 5. The method of claim 1, wherein each microgranule comprises a sugar core or a microcrystalline cellulose core, and a layer outside of the sugar core or the microcrystalline cellulose core, the layer comprising secnidazole or the pharmaceutically acceptable salt thereof. 6. The method of claim 1, wherein the microgranule formulation further comprises at least one compound selected from the group consisting of sugar spheres, povidone, polyethylene glycol with an average molecular weight of 4000 g/mol, ethyl acrylatemethyl methacrylate copolymer and, talc, or a combination thereof. 7. The method of claim 1, wherein the microgranule formulation is integrated with a food substance prior to administration to the human. 8. The method of claim 7, wherein the food substance is a liquid, semisolid or a soft food. 9. The method of claim 7, wherein the food substance is applesauce, yogurt, or pudding. 10. The method of claim 7, wherein the integration is mixing the microgranule formulation into the food substance. 11. The method of claim 1, wherein the human is a female. 12. The method of claim 1, wherein the human is an adult or child. 13. The method of claim 11, wherein the human is a pregnant female. 14. The method of claim 1, wherein the human is a female who is also suffering from bacterial vaginosis. 15. The method of claim 1, wherein the human is a HIV-positive male or HIV-positive female. 16. The method of claim 1, wherein the human is a HIV-positive female who is also suffering from bacterial vaginosis. 17. The method of claim 1, wherein the human is infected with metronidazole-resistant trichomoniasis or tinidazole-resistant trichomoniasis. 18. The method of claim 1, wherein the human is also HIV-positive, suffering from bacterial vaginosis or a combination thereof. 19. The method of claim 1, wherein the microgranule formulation is administered as a single dose. 20. The method of claim 1, wherein the microgranule formulation is administered with an additional compound selected from ethinyl estradiol (EE2), norethindrone (NET), or a combination thereof. 21. The method of claim 1, wherein the microgranule formulation is administered with paromomycin, tinidazole, metronidazole, boric acid or a combination thereof. 22. The method of claim 20, wherein the additional compound is administered on the same day as the microgranule formulation. 23. The method of claim 20, wherein the additional compound is administered on a different day as the microgranule formulation. 24. The method of claim 1, wherein the microgranule formulation is administered as a single dose and is the only dose required to be administered to the human to achieve a post-treatment clinical outcome by resolution of one or more symptoms of trichomoniasis. 25. The method of claim 1, wherein the therapeutically effective amount of secnidazole or the pharmaceutically acceptable salt thereof is 2 grams. 26. The method of claim 1, wherein the microgranule formulation does not affect the contraceptive efficacy of an additional compound selected from ethinyl estradiol (EE2), norethindrone (NET) or a combination thereof. 27. A method of treating trichomoniasis in a human in need thereof comprising orally administering to the human a therapeutically effective amount of secnidazole or a pharmaceutically acceptable salt thereof in a microgranule formulation, wherein the microgranule formulation comprises a plurality of microgranules, wherein the therapeutically effective amount of secnidazole or the pharmaceutically acceptable salt thereof is an amount of secnidazole or the pharmaceutically acceptable salt thereof that exhibits a maximum plasma concentration (Cmax) of 29.15 μg/ml to 31.05 μg/ml and a time to maximum plasma concentration (Tmax) of 6.6 hours to 24 hours in the human, and wherein secnidazole or the pharmaceutically acceptable salt thereof is the sole drug in the microgranule formulation, wherein the plurality of microgranules has a volume-weighted particle size distribution within a microgranule population, and wherein the volume-weighted particle size distribution as measured by mean diameter using laser diffraction from a representative sample of the microgranule population comprises at least 10% of the microgranule population having a volume-weighted particle size equal to or greater than 470 micrometers. 28. A method of treating trichomoniasis in a human in need thereof, comprising orally administering to the human a therapeutically effective amount of secnidazole or a pharmaceutically acceptable salt thereof in a microgranule formulation, wherein the microgranule formulation comprises a plurality of microgranules, wherein the therapeutically effective amount of secnidazole or the pharmaceutically acceptable salt thereof is an amount of secnidazole or the pharmaceutically acceptable salt thereof that exhibits a maximum plasma concentration (Cmax) of about 29.15 μg/ml to about 31.05 μg/ml and a time to maximum plasma concentration (Tmax) of 6.6 hours to 24 hours in the human, and wherein secnidazole or the pharmaceutically acceptable salt thereof is the sole drug in the microgranule formulation, wherein the plurality of microgranules has a volume-weighted particle size distribution within a microgranule population, and wherein the volume-weighted particle size distribution as measured by mean diameter using laser diffraction from a representative sample of the microgranule population further comprises 50% of the microgranule population having a volume-weighted particle size between about 640 micrometers and about 810 micrometers. 29. A method of treating trichomoniasis in a human in need thereof, comprising orally administering to the human a therapeutically effective amount of secnidazole or a pharmaceutically acceptable salt thereof in a microgranule formulation, wherein the microgranule formulation comprises a plurality of microgranules, wherein the therapeutically effective amount of secnidazole or the pharmaceutically acceptable salt thereof is an amount of secnidazole or the pharmaceutically acceptable salt thereof that exhibits a maximum plasma concentration (Cmax) of about 29.15 μg/ml to about 31.05 μg/ml and a time to maximum plasma concentration (T max) of 6.6 hours to 24 hours in the human, and wherein secnidazole or the pharmaceutically acceptable salt thereof is the sole drug in the microgranule formulation, wherein the plurality of microgranules has a volume-weighted particle size distribution within a microgranule population, and wherein the volume-weighted particle size distribution as measured by mean diameter using laser diffraction from a representative sample of the microgranule population further comprises 90% of the microgranule population having a volume-weighted particle size about no more than 1170 micrometers.