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AssigneeObsEva S.A.
InventorsJean-Pierre GOTTELAND, Ernest LOUMAYE, Oliver POHL
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The present disclosure provides compositions and methods for treating estrogen-dependent disorders, such as disorders of the female reproductive system, including uterine fibroids and endometriosis, among others. Compounds described herein that may be used to treat such indications include gonadotropin-releasing hormone (GnRH) antagonists. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno [3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof, among others. Using the compositions and methods described herein, GnRH antagonists may be periodically administered to a patient, such as one or more times per day, week, or month, in combination with periodic add-back therapy, thereby preventing bone mineral density loss that may otherwise accompany estrogen depletion effectuated by GnRH antagonist activity. Advantageously, using the dosing schedules of the present disclosure, the periodic administration the GnRH antagonist and add-back therapy may commence together, such as on the same day.
A method of treating an estrogen-dependent disease in a human patient in need thereof, the method comprising periodically administering to the patient therapeutically effective amounts of a gonadotropin-releasing hormone (GnRH) antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of reducing the volume of menstrual blood loss a human patient diagnosed as having uterine fibroids, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of inducing amenorrhea in a human patient diagnosed as having uterine fibroids, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of reducing the volume of one or more uterine fibroids in a human patient diagnosed as having uterine fibroids, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of reducing the volume of one or more endometriosis nodes in a human patient diagnosed as having endometriosis, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of reducing pelvic pain in a human patient diagnosed as having endometriosis, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of reducing dysmenorrhea in a human patient diagnosed as having endometriosis, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of reducing dyspareunia in a human patient diagnosed as having endometriosis, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of reducing dyschezia in a human patient diagnosed as having endometriosis, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of reducing uterine bleeding in a human patient diagnosed as having endometriosis, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of inducing amenorrhea in a human patient diagnosed as having endometriosis, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of reducing uterine volume in a human patient diagnosed as having adenomyosis, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of reducing the thickness of the anterior and/or posterior region of the uterine myometrium in a human patient diagnosed as having adenomyosis, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of reducing pelvic pain in a human patient diagnosed as having adenomyosis, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of reducing dysmenorrhea in a human patient diagnosed as having adenomyosis, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of reducing dyspareunia in a human patient diagnosed as having adenomyosis, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of reducing dyschezia in a human patient diagnosed as having adenomyosis, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of reducing uterine tenderness in a human patient diagnosed as having adenomyosis, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of reducing uterine bleeding in a human patient diagnosed as having adenomyosis, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of inducing amenorrhea in a human patient diagnosed as having adenomyosis, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of reducing the volume of one or more rectovaginal endometriosis nodes in a human patient diagnosed as having rectovaginal endometriosis, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of reducing the volume of one or more type III rectovaginal endometriosis nodes in a human patient diagnosed as having rectovaginal endometriosis, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of reducing pelvic pain in a human patient diagnosed as having rectovaginal endometriosis, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of reducing dysmenorrhea in a human patient diagnosed as having rectovaginal endometriosis, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of reducing dyspareunia in a human patient diagnosed as having rectovaginal endometriosis, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of reducing dyschezia in a human patient diagnosed as having rectovaginal endometriosis, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of reducing uterine bleeding in a human patient diagnosed as having rectovaginal endometriosis, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
A method of inducing amenorrhea in a human patient diagnosed as having rectovaginal endometriosis, the method comprising periodically administering to the patient therapeutically effective amounts of a GnRH antagonist and add-back therapy, wherein administration of the GnRH antagonist and administration of the add-back therapy begin on the same day.
Dependencies are inferred from the claim text.