A61K31/337

COMBINATIONS OF LSD1 INHIBITORS FOR USE IN THE TREATMENT OF SOLID TUMORS

The instant invention relates to therapeutic combinations of LSD1 inhibitors and one or more other active pharmaceutical ingredient(s) or pharmaceutically acceptable salts thereof. The combinations are particularly useful for treating neoplastic diseases, such as cancer, particularly small cell lung cancer (SCLC).

CABAZITAXEL WEAKLY- ALKALINE DERIVATIVE AND FORMULATION THEREOF

A cabazitaxel weakly-alkaline derivative, preparation, and synthesis thereof, a liposome preparation containing the cabazitaxel weakly-alkaline derivative and application of the cabazitaxel weakly-alkaline derivative in a drug delivery system are provided. Cabazitaxel is connected with a weakly-alkaline intermediate through an ester bond, the ester bond can be broken under the action of esterase in vivo, and an active drug is released. A connecting group is C.sub.1-C.sub.4 alkyl, C.sub.3-C.sub.6 naphthenic base or phenyl; [N] is an N-methyl piperazinyl group, a piperidinyl group, a 4-(1-piperidinyl) piperidinyl group, a morpholinyl group, a pyrrolidine group or other tertiary amine structures. The cabazitaxel weakly-alkaline derivative can be prepared into the liposome preparation having high drug loading capacity, high encapsulation efficiency, and good stability. The in-vivo circulation time of the drug can be greatly prolonged, the accumulation amount of the drug at a tumor part is increased, and the anti-tumor effect and the tolerance dose are improved.

CABAZITAXEL WEAKLY- ALKALINE DERIVATIVE AND FORMULATION THEREOF

A cabazitaxel weakly-alkaline derivative, preparation, and synthesis thereof, a liposome preparation containing the cabazitaxel weakly-alkaline derivative and application of the cabazitaxel weakly-alkaline derivative in a drug delivery system are provided. Cabazitaxel is connected with a weakly-alkaline intermediate through an ester bond, the ester bond can be broken under the action of esterase in vivo, and an active drug is released. A connecting group is C.sub.1-C.sub.4 alkyl, C.sub.3-C.sub.6 naphthenic base or phenyl; [N] is an N-methyl piperazinyl group, a piperidinyl group, a 4-(1-piperidinyl) piperidinyl group, a morpholinyl group, a pyrrolidine group or other tertiary amine structures. The cabazitaxel weakly-alkaline derivative can be prepared into the liposome preparation having high drug loading capacity, high encapsulation efficiency, and good stability. The in-vivo circulation time of the drug can be greatly prolonged, the accumulation amount of the drug at a tumor part is increased, and the anti-tumor effect and the tolerance dose are improved.

DNA APTAMERS AND USE THEREOF FOR THE TREATMENT OF CANCER

Provided herein are DNA aptamers targeting AXL receptor kinase. The DNA aptamers may comprise a thiophosphate backbone and be chemically modified. Further provided herein are methods of use thereof for the treatment of a disease or disorder, such as cancer.

DNA APTAMERS AND USE THEREOF FOR THE TREATMENT OF CANCER

Provided herein are DNA aptamers targeting AXL receptor kinase. The DNA aptamers may comprise a thiophosphate backbone and be chemically modified. Further provided herein are methods of use thereof for the treatment of a disease or disorder, such as cancer.

DNA APTAMERS AND USE THEREOF FOR THE TREATMENT OF CANCER

Provided herein are DNA aptamers targeting AXL receptor kinase. The DNA aptamers may comprise a thiophosphate backbone and be chemically modified. Further provided herein are methods of use thereof for the treatment of a disease or disorder, such as cancer.

USE OF DKK-1 INHIBITORS FOR TREATING CANCER
20220381786 · 2022-12-01 ·

A method of treating a cancer in a subject, in need thereof, comprising determining a DKK1 expression H-score or % positive in a sample of the subject's cancer; and administering a DKK1 antagonist to the subject determined to have the DKK1 expression H-score or % positive equal to or greater than a predetermined value.

USE OF DKK-1 INHIBITORS FOR TREATING CANCER
20220381786 · 2022-12-01 ·

A method of treating a cancer in a subject, in need thereof, comprising determining a DKK1 expression H-score or % positive in a sample of the subject's cancer; and administering a DKK1 antagonist to the subject determined to have the DKK1 expression H-score or % positive equal to or greater than a predetermined value.

TREATMENT OF PANCREATIC CANCER
20220378692 · 2022-12-01 ·

The present invention relates to ultrasound mediated delivery of therapeutic agents to the pancreas, and particularly for treatment of pancreatic cancer such as pancreatic ductal adenocarcinoma (PDAC). More particularly, the invention provides a cluster composition and a pharmaceutical composition, for use in delivery of therapeutic agents and for treatment of pancreatic cancers, including PDAC.

TREATMENT OF PANCREATIC CANCER
20220378692 · 2022-12-01 ·

The present invention relates to ultrasound mediated delivery of therapeutic agents to the pancreas, and particularly for treatment of pancreatic cancer such as pancreatic ductal adenocarcinoma (PDAC). More particularly, the invention provides a cluster composition and a pharmaceutical composition, for use in delivery of therapeutic agents and for treatment of pancreatic cancers, including PDAC.