The present invention relates to the in vitro use of a group of cell-penetrating conjugate systems or a formulation incorporating the same for transporting e.g. therapeutically active agents, such as chemotherapeutics, insulin and immunosuppressants across the cellular membranes of mammalian cells, including human cells. The invention also relates to an in vitro methods of transporting physiologically active agents, such as therapeutics, across cell-membranes by using the cell-penetrating conjugate systems according to the present invention as well as the cell-penetrating conjugate systems for use in treatment of cancer, diabetes and for use in immunotherapy.

The present invention provides a composition, for preventing or treating an inflammatory disease, comprising, as an active ingredient, a self-hydrolysis extract using a hydrolase in a plant cell from one or more plants selected from Pulsatilla koreana, Pulsatilla chinensis, Pulsatilla cernua, Anemone raddeana, Aralia elata, Akebia quinata, Lonicera species, Adonis amurensis, Hedera helix, Hedera colchica and Patrinia scabiosifolia, and/or additionally an angiogenesis inhibitor.

The present invention provides a composition, for preventing or treating an inflammatory disease, comprising, as an active ingredient, a self-hydrolysis extract using a hydrolase in a plant cell from one or more plants selected from Pulsatilla koreana, Pulsatilla chinensis, Pulsatilla cernua, Anemone raddeana, Aralia elata, Akebia quinata, Lonicera species, Adonis amurensis, Hedera helix, Hedera colchica and Patrinia scabiosifolia, and/or additionally an angiogenesis inhibitor.

A supramolecular nano-drug based on irinotecan and niraparib, and a preparation method and application thereof are provided. The nano-drug is a stable supramolecular nanostructure with a regular geometric appearance, which is formed by self-assembling irinotecan and niraparib through supramolecular acting forces, such as hydrogen bonds, and hydrophobic Van Der Waals force by a dynamic supramolecular self-assembly method. The supramolecular nano-drug formed in the present disclosure is capable of significantly improving the sensitivity of colorectal cells to the irinotecan, and the quantity of DNA damages induced in the colorectal cells is significantly higher than that induced by the irinotecan as a single chemotherapeutic drug. The supramolecular nano-drug of the present disclosure can not only induce death of colorectal cancer cells in vitro, but also play a role in treating the colorectal cancer in vivo after being administrated intravenously.

A supramolecular nano-drug based on irinotecan and niraparib, and a preparation method and application thereof are provided. The nano-drug is a stable supramolecular nanostructure with a regular geometric appearance, which is formed by self-assembling irinotecan and niraparib through supramolecular acting forces, such as hydrogen bonds, and hydrophobic Van Der Waals force by a dynamic supramolecular self-assembly method. The supramolecular nano-drug formed in the present disclosure is capable of significantly improving the sensitivity of colorectal cells to the irinotecan, and the quantity of DNA damages induced in the colorectal cells is significantly higher than that induced by the irinotecan as a single chemotherapeutic drug. The supramolecular nano-drug of the present disclosure can not only induce death of colorectal cancer cells in vitro, but also play a role in treating the colorectal cancer in vivo after being administrated intravenously.

The present application relates to an anti-tumor compound and a preparation method and use thereof, and in particular to a compound or a tautomer, a mesomer, a racemate, an enantiomer or a diastereoisomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, and a preparation method and use thereof.

The present invention relates to therapeutic immunoconjugates comprising SN-38 attached to an antibody or antigen-binding antibody fragment. The antibody may bind to EGP-1 (TROP-2), CEACAM5, CEACAM6, CD74, CD19, CD20, CD22, CSAp, HLA-DR, AFP or MUC5ac and the immunoconjugate may be administered at a dosage of between 4 mg/kg and 24 mg/kg, preferably 4, 6, 8, 9, 10, 12, 16 or 18 mg/kg. When administered at specified dosages and schedules, the immunoconjugate can reduce solid tumors in size, reduce or eliminate metastases and is effective to treat cancers resistant to standard therapies, such as radiation therapy, chemotherapy or immunotherapy.

The present invention relates to therapeutic immunoconjugates comprising SN-38 attached to an antibody or antigen-binding antibody fragment. The antibody may bind to EGP-1 (TROP-2), CEACAM5, CEACAM6, CD74, CD19, CD20, CD22, CSAp, HLA-DR, AFP or MUC5ac and the immunoconjugate may be administered at a dosage of between 4 mg/kg and 24 mg/kg, preferably 4, 6, 8, 9, 10, 12, 16 or 18 mg/kg. When administered at specified dosages and schedules, the immunoconjugate can reduce solid tumors in size, reduce or eliminate metastases and is effective to treat cancers resistant to standard therapies, such as radiation therapy, chemotherapy or immunotherapy.

The present disclosure provides, inter alia, multi-drug Antibody Drug Conjugates (MD-ADCs) and Linking Assembly (LA) Units, that are constructed in a site-specific matter via ‘orthogonal’ deprotection and drug loading. Also provided are, Protected Linking Assembly Units, which allow for ‘orthogonal’ deprotection and construction of MD-ADCs and LA Units of the present disclosure.

The present disclosure provides, inter alia, multi-drug Antibody Drug Conjugates (MD-ADCs) and Linking Assembly (LA) Units, that are constructed in a site-specific matter via ‘orthogonal’ deprotection and drug loading. Also provided are, Protected Linking Assembly Units, which allow for ‘orthogonal’ deprotection and construction of MD-ADCs and LA Units of the present disclosure.