Fulvestrant formulations suitable for intramuscular injection at concentration in excess of 40 mg/ml in the absence of castor oil and castor oil derivatives are disclosed.

The present invention relates to a vaginal drug delivery device configured to safely and effectively deliver a therapeutic formulation in the vagina at or near a desired target area for a specified time period.

Methods for treating uterine fibroids, endometriosis, adenomyosis, or heavy menstrual bleeding in a subject, which include administering to the subject from 10 mg to 60 mg per day of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, and from 0.01 mg to 5 mg per day of a hormone replacement medicament. The present disclosure has methods for reducing menstrual bleeding in a subject, reducing bone mineral density loss in a subject caused by administering a GnRH antagonist to the subject, suppressing sex hormones in a subject, reducing vasomotor symptoms or hot flashes in a subject, and reducing symptoms of decreased libido in a subject having uterine fibroids, endometriosis, or adenomyosis. Further provided are methods of maintaining blood glucose profile, maintaining lipid profile, and/or maintaining bone mineral density in a pre-menopausal woman being treated for one or more conditions or symptoms of endometriosis, adenomyosis, uterine fibroids, or heavy menstrual bleeding; and methods of contraception and treating infertility.

Methods for treating uterine fibroids, endometriosis, adenomyosis, or heavy menstrual bleeding in a subject, which include administering to the subject from 10 mg to 60 mg per day of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, and from 0.01 mg to 5 mg per day of a hormone replacement medicament. The present disclosure has methods for reducing menstrual bleeding in a subject, reducing bone mineral density loss in a subject caused by administering a GnRH antagonist to the subject, suppressing sex hormones in a subject, reducing vasomotor symptoms or hot flashes in a subject, and reducing symptoms of decreased libido in a subject having uterine fibroids, endometriosis, or adenomyosis. Further provided are methods of maintaining blood glucose profile, maintaining lipid profile, and/or maintaining bone mineral density in a pre-menopausal woman being treated for one or more conditions or symptoms of endometriosis, adenomyosis, uterine fibroids, or heavy menstrual bleeding; and methods of contraception and treating infertility.

Methods, compositions and systems are presented to deliver estradiol benzoate to prevent and/or inhibit boar taint and/or male aggression as compared to animal that has not been administered estradiol.

Methods, compositions and systems are presented to deliver estradiol benzoate to prevent and/or inhibit boar taint and/or male aggression as compared to animal that has not been administered estradiol.

A fulvestrant pharmaceutical composition, a preparation method therefor, and an application thereof are provided. The fulvestrant pharmaceutical composition contains fulvestrant solid particles. The particle size of the fulvestrant solid particles satisfies that Dv(10) is selected from 0.400 micrometers to 6.000 micrometers, Dv(50) is selected from 0.700 micrometers to 6.000 micrometers, and Dv(90) is selected from 1.000 micrometers to 6.000 micrometers, provided that Dv(10) is not 0.400 micrometers, Dv(50) is not 0.700 micrometers, and Dv(90) is not 1.000 micrometers. The fulvestrant pharmaceutical composition has a long-acting sustained release.

The present invention relates a microcapsule that comprises an active pharmaceutical ingredient and a polymeric shell comprised of polymeric materials such as polyether, polyester, polyamine, polyamide, polyurea, polyurethane, polythiocarbamate, and polythiocarbonate. The outer surface of shell comprises surface functional groups such as hydroxide, primary amine, carboxylic acid, or protected forms thereof. These surface functional groups may be reacted further with reactants to place specific organic groups on the surface of the microcapsule. Such microcapsules are prepared by a modified interfacial condensation polymerization.

The present invention relates a microcapsule that comprises an active pharmaceutical ingredient and a polymeric shell comprised of polymeric materials such as polyether, polyester, polyamine, polyamide, polyurea, polyurethane, polythiocarbamate, and polythiocarbonate. The outer surface of shell comprises surface functional groups such as hydroxide, primary amine, carboxylic acid, or protected forms thereof. These surface functional groups may be reacted further with reactants to place specific organic groups on the surface of the microcapsule. Such microcapsules are prepared by a modified interfacial condensation polymerization.

The present invention concerns methods to identify RIPK1 modulators capable of modulating RIPK1 activity, RIPK1 interacting molecules that modulate RIPK1 activity and pharmaceutical compositions comprising RIPK1 modulators.