Disclosed is a method for preparing high-load oral paclitaxel capsule for a slow release in colon, belonging to the field of porous starch drug loading. The preparation method of the present disclosure includes the following steps: (1) dripping an ethanol solution of paclitaxel into a water phase and drying the solution to obtain an amorphous paclitaxel microsphere; (2) redissolving the paclitaxel microsphere prepared in step (1) in the ethanol solution, dispersing porous starch in the ethanol solution for adsorption, volatilizing a solvent in an oven, washing the porous starch with the ethanol solution to remove unadsorbed paclitaxel, and centrifuging same to obtain a precipitate, namely the porous starch loaded with paclitaxel; and (3) dispersing the porous starch loaded with paclitaxel prepared in step (2) in a chitosan solution, dropwise adding the solution into a phytic acid solution, and stirring the solution for 4 hours to obtain a coated capsule.

Disclosed is a method for preparing high-load oral paclitaxel capsule for a slow release in colon, belonging to the field of porous starch drug loading. The preparation method of the present disclosure includes the following steps: (1) dripping an ethanol solution of paclitaxel into a water phase and drying the solution to obtain an amorphous paclitaxel microsphere; (2) redissolving the paclitaxel microsphere prepared in step (1) in the ethanol solution, dispersing porous starch in the ethanol solution for adsorption, volatilizing a solvent in an oven, washing the porous starch with the ethanol solution to remove unadsorbed paclitaxel, and centrifuging same to obtain a precipitate, namely the porous starch loaded with paclitaxel; and (3) dispersing the porous starch loaded with paclitaxel prepared in step (2) in a chitosan solution, dropwise adding the solution into a phytic acid solution, and stirring the solution for 4 hours to obtain a coated capsule.

The present invention concerns improved methods and compositions for preparing SN-38 conjugates of proteins or peptides, preferably immunoconjugates of antibodies or antigen-binding antibody fragments. More preferably, the SN-38 is attached to the antibody or antibody fragment using a CL2A linker, with 1-12, more preferably 6-8, alternatively 1-5 SN-38 moieties per antibody or antibody fragment. Most preferably, the immunoconjugate is prepared in large scale batches, with various modifications to the reaction scheme disclosed herein to optimize yield and recovery in large scale. Other embodiments concern optimized dosages and/or schedules of administration of immunoconjugate to maximize efficacy for disease treatment and minimize side effects of administration.

The present invention concerns improved methods and compositions for preparing SN-38 conjugates of proteins or peptides, preferably immunoconjugates of antibodies or antigen-binding antibody fragments. More preferably, the SN-38 is attached to the antibody or antibody fragment using a CL2A linker, with 1-12, more preferably 6-8, alternatively 1-5 SN-38 moieties per antibody or antibody fragment. Most preferably, the immunoconjugate is prepared in large scale batches, with various modifications to the reaction scheme disclosed herein to optimize yield and recovery in large scale. Other embodiments concern optimized dosages and/or schedules of administration of immunoconjugate to maximize efficacy for disease treatment and minimize side effects of administration.

Provided herein are substituted biaryl sulfonamide compounds, pharmaceutical compositions comprising the compounds, methods of their preparation, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or amelioration of various disorders, including cancer and proliferative disorders. In one embodiment, the compounds provided herein modulate initiation of protein translation. In one embodiment, the compounds provided herein are used in combination with surgery, radiation therapy, immuno therapy and/or one or more additional anticancer drugs for the treatment, prevention, and/or amelioration of cancer and proliferative disorders.

Provided herein are substituted biaryl sulfonamide compounds, pharmaceutical compositions comprising the compounds, methods of their preparation, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or amelioration of various disorders, including cancer and proliferative disorders. In one embodiment, the compounds provided herein modulate initiation of protein translation. In one embodiment, the compounds provided herein are used in combination with surgery, radiation therapy, immuno therapy and/or one or more additional anticancer drugs for the treatment, prevention, and/or amelioration of cancer and proliferative disorders.

Compositions and methods for treating ovarian cancer are provided. Methods include combined treatment with chemotherapeutic agents and anti-STn antibodies. Chemotherapy resistant ovarian cancer cells may be reduced. Chemotherapy resistant ovarian cancer cells may include cancer stem cells.

Compositions and methods for treating ovarian cancer are provided. Methods include combined treatment with chemotherapeutic agents and anti-STn antibodies. Chemotherapy resistant ovarian cancer cells may be reduced. Chemotherapy resistant ovarian cancer cells may include cancer stem cells.

Compositions and methods for treating ovarian cancer are provided. Methods include combined treatment with chemotherapeutic agents and anti-STn antibodies. Chemotherapy resistant ovarian cancer cells may be reduced. Chemotherapy resistant ovarian cancer cells may include cancer stem cells.

The present disclosure is directed to use of MrgprX2 antagonists in the treatment of inflammatory disorders, e.g., inflammatory disorders of the skin. This invention is also directed to pharmaceutical compositions comprising a MrgprX2 antagonist and a pharmaceutically or orally acceptable carrier for administration.