Abstract: The present invention provides a class of fulvestrant ester derivatives and preparation method thereof. Such a compound is an aliphatic ester formed by esterifying the —OH at positions C-3 and C-17 of fulvestrant, having a structure of the following formula: In the formula, substituent R is H, alkanoyl or alkenoyl having 2 to 22 carbon atoms or stereoisomers thereof; substituent R? can be H, alkanoyl or alkenoyl having 2 to 4 carbon atoms or stereoisomers thereof; such an aliphatic ester compound being used as a pro-drug can improve the stability of a compound, meanwhile the decrease of polarity can enable them to be easily made into preparations like lipid emulsion, microsphere etc., and avoid the degradation of the compound caused by factors like high temperature etc. and the use of an organic solution during preparation process.

Abstract: The present invention provides the use of a compound of Formula A for the manufacture of a medicament in the treatment of tumor necrosis factor (TNF)-related diseases, and a method for treating a TNF-related disease, said method comprising administering to a subject in need a therapeutically effective amount of a compound of Formula A.

Abstract: Fulvestrant nanosphere/microsphere and preparation method and use thereof are provided in the present invention. The carrier material of the fulvestrant nanosphere/microsphere is methoxy ended polyethylene glycol-polylactic acid block copolymer. The nanosphere/microsphere is prepared by solvent-nonsolvent method, in-liquid drying method and/or spray drying method, and has the features of high drug loading and high encapsulation efficiency, controllable release of medicine and no irritant to application site or blood vessel. The fulvestrant nanosphere/microsphere can be used to treat metastatic advanced breast cancer in post-menopausal woman.

Abstract: Fulvestrant nanosphere/microsphere and preparation method and use thereof are provided in the present invention. The carrier material of the fulvestrant nanosphere/microsphere is methoxy ended polyethylene glycol-polylactic acid block copolymer. The nanosphere/microsphere is prepared by solvent-nonsolvent method, in-liquid drying method and/or spray drying method, and has the features of high drug loading and high encapsulation efficiency, controllable release of medicine and no irritant to application site or blood vessel. The fulvestrant nanosphere/microsphere can be used to treat metastatic advanced breast cancer in post-menopausal woman.

Abstract: Fulvestrant nanosphere/microsphere and preparation method and use thereof are provided in the present invention. The carrier material of the fulvestrant nanosphere/microsphere is methoxy ended polyethylene glycol-polylactic acid block copolymer. The nanosphere/microsphere is prepared by solvent-nonsolvent method, in-liquid drying method and/or spray drying method, and has the features of high drug loading and high encapsulation efficiency, controllable release of medicine and no irritant to application site or blood vessel. The fulvestrant nanosphere/microsphere can be used to treat metastatic advanced breast cancer in post-menopausal woman.

Abstract: A nanosphere or microsphere drug carrier, formulations comprising the drug carrier and the preparation method of the formulations and the use of the carrier are disclosed. The carrier comprises a biodegradable methoxy end-capped polyethylene glycol-polylactide block copolymersor a derivative thereof represented by formula (I) as the main carrier material: CH3O—[CH2—CH2—O]m—[C(O)—CH(CH3)—O]n—R (I).

Abstract: A nanosphere or microsphere drug carrier, formulations comprising the drug carrier and the preparation method of the formulations and the use of the carrier are disclosed. The carrier comprises a biodegradable methoxy end-capped polyethylene glycol-polylactide block copolymersor a derivative thereof represented by formula (I) as the main carrier material: CH3O—[CH2—CH2—O]m—[C(O)—CH(CH3)—O]n—R (I).

Abstract: Fulvestrant nanosphere/microsphere and preparation method and use thereof are provided in the present invention. The carrier material of the fulvestrant nanosphere/microsphere is methoxy ended polyethylene glycol-polylactic acid block copolymer. The nanosphere/microsphere is prepared by solvent-nonsolvent method, in-liquid drying method and/or spray drying method, and has the features of high drug loading and high encapsulation efficiency, controllable release of medicine and no irritant to application site or blood vessel. The fulvestrant nanosphere/microsphere can be used to treat metastatic advanced breast cancer in post-menopausal woman.