17 results about "Antimetabolite" patented technology

Compositions and methods for inducing pterygium regression from visual axis / central cornea, stabilizing pterygium, treating hyperemia and symptoms in pterygium patients, and treating pterygium recurrence following pterygiectomy are disclosed. The methods include administration of a multikinase inhibitor, an antimetabolite or a combination thereof to patients in need thereof.

Compositions and methods for inducing pterygium regression from visual axis / central cornea, stabilizing pterygium, treating hyperemia and symptoms in pterygium patients, and treating pterygium recurrence following pterygiectomy are disclosed. The methods include administration of a multikinase inhibitor, an antimetabolite or a combination thereof to patients in need thereof.

To provide a method for treating the target cancer. [Solution] A method for treating a target cancer, comprising administering a bispecific antibody having binding specificity to EGFR and HER3 and a therapeutic agent to the target, wherein the therapeutic agent includes a tyrosine kinase inhibitor (TKI), an alkylating agent, an antimetabolite, a microtubule inhibitor, an anti-cancer antibiotic, a topoisomerase inhibitor, a chemoprotective agent, or a combination thereof.

Dengue virus (DENV) is a mosquito-borne flavivirus responsible for dengue fever. Studies have shown that DENV interacts with metabolic pathways, in particular the glycolysis is increased in DENV-infected cells. However, the dependence of DENV on this pathway has not been investigated in details. The inventors identified an interaction between the non-structural protein 3 (NS3) of DENV and GCKR, a host protein that regulates the liver-specific hexokinase GCK. NS3 expression alone was found to increase glucose consumption and lactate secretion in an hepatic cell line expressing GCK. The inventors observed that GCKR interaction with GCK decreases DENV replication, supporting the role of NS3 as an inhibitor of GCKR function. By targeting NAD(H) biosynthesis with the antimetabolite 6-Amino-Nicotinamide (6-AN), the inventors decreased cellular glycolytic activity and inhibited DENV replication in hepatic cell. The present invention thus relates to the use of inhibitors of NAD biosynthesis for the treatment of dengue virus infections.

To provide a gamma-polyglutamate oxidase folate antagonist composition that can overcome pharmacological challenges related to dose-limiting toxicity and therapeutic resistance associated with folate antagonist therapy. [Solution] A liposome composition (Lp-γPANTIFOL composition) containing a gamma polyglutamine oxidized folate antimetabolitic agent, wherein the gamma polyglutamine oxidized folate antimetabolitic agent contains 2 to 15 glutamyl groups, and the liposomes are pegylated.

The present application provides an antibody-drug conjugate, a method for preparing same, and use thereof. The antibody-drug conjugate has a structure of formula I. The drug is selected from a topoisomerase inhibitor, a DNA-damaging agent, a microtubule inhibitor, an RNA polymerase inhibitor, and an antimetabolite. The prepared antibody-drug conjugate has an optimized drug-to-antibody ratio and targeted killing effects against breast cancer, gastric cancer, lung cancer, and colorectal cancer.

To provide an alpha polyglutamated antifolate composition capable of overcoming pharmacological challenges associated with dose-limiting toxicity and treatment resistance related to antifolate therapy.SOLUTION: There is provided a liposomal composition comprising a liposome encapsulating an alpha polyglutamated antifolate, wherein the alpha polyglutamated antifolate comprises 2 to 15 glutamyl groups linked via alpha-carboxyl group bonds, wherein the liposome is pegylated, and comprises a targeting moiety having specific affinity for a surface antigen of a desired target cell.SELECTED DRAWING: None

The present invention provides methods, devices, and kits related to treatment of urothelial carcinomas of the lower tract with antimetabolite (such as gemcitabine). In some aspects the methods, devices and kits relate to treatment of urothelial carcinomas of the lower tract with an antimetabolite (such as gemcitabine) and an immunomodulating agent.

An object of the present invention is to provide a new combination of antitumor agents, which can significantly reduce tumors through synergistic antitumor effects while minimizing the increase of side effects. The present invention provides an antitumor composition, which comprises the following compound (B) or a salt thereof used in combination with the following antitumor agent (A): (A) at least one antitumor agent selected from alkylating agents, CD20 recognition molecules, DNA methylation inhibitors, pyrimidine antimetabolites, purine antimetabolites, antifolate agents, Bcl-2 inhibitors and tyrosine kinase inhibitors; (B) a compound represented by the following formula (1) or a salt thereof: wherein R 1 represents a halogen atom, an aryl group, an aryloxy group or a lower alkyl group optionally substituted by one or more halogen atoms; R 2 represents a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group; m represents an integer from 1 to 3, provided that when m represents 2 or 3, R 1 Same or different.

To provide gamma polyglutamated antifolate compositions to overcome pharmacological challenges associated with antifolate therapy, the dose-limiting toxicities and treatment resistance.SOLUTION: Disclosed is a liposome composition comprising a gamma polyglutamated antifolate (Lp-γPANTIFOL composition), where the gamma polyglutamated antifolate comprises 2-10 glutamyl groups, the liposome is PEGylated, and the liposome composition comprises a targeting moiety that has a specific affinity to a surface antigen on a target cell of interest.SELECTED DRAWING: None

Providing pharmaceutical compositions for the treatment of melanoma. [Solution] A pharmaceutical composition comprising (a) an LXRβ agonist selected from the following compounds 1, 2, 12, and 25, and / or a salt thereof, and (b) an antiproliferative compound selected from immunomodulators, topoisomerase inhibitors, antimetabolites, angiogenesis inhibitors, tyrosine kinase inhibitors, alkylating agents, and mitotic inhibitors. TIFF2026062949000078.tif110166

Provided is use of a monophosphate deoxyribose fluorouracil nucleoside prodrug in the preparation of a drug for preventing and / or treating tumors. The monophosphate deoxyribose fluorouracil nucleoside prodrug is a derivative formed by substituting at least one thymine in nucleolin aptamer AS1411 with fluorouracil. The tumors include at least one of lung cancer, breast cancer, prostate cancer, pancreatic cancer, kidney cancer, cervical cancer, leukemia and lymphoma, melanoma, glioblastoma, neuroblastoma, sarcoma, and gastric cancer. The monophosphate deoxyribose fluorouracil nucleoside prodrug binds to the nucleolin protein and selectively enters tumor cells under the action of the nucleolin protein, and release an antimetabolite to inhibit thymine nucleotide synthase, thereby achieving an anti-tumor effect.

A method of treating hematological cancer comprising administering to a patient in need thereof a therapeutically effective amount of a phosphatidylinositol 3-kinase gamma (PI3Kg) inhibitor and an antimetabolite, optionally a therapeutically effective amount of a BCL-2 inhibitor. A method of identifying hematological cancer patients susceptible to treatment with a PI3Kg inhibitor. A method of treating hematological cancer, the method comprising administering to a patient in need thereof a therapeutically effective amount of a p-21 activated kinase 1 (PAK-1) inhibitor, optionally a therapeutically effective amount of a BCL-2 inhibitor.

To provide an ophthalmic composition and a method for treating primary and recurrent pterygium.SOLUTION: Compositions and methods for inducing pterygium regression from the visual axis / central cornea, for stabilizing pterygium, for treating hyperemia and symptoms in pterygium patients, and for treating pterygium recurrence after pterygiectomy are disclosed. The methods include administering a multikinase inhibitor, an antimetabolite, or a combination thereof to a patient in need of the method.SELECTED DRAWING: None

A pharmaceutical which exhibits sufficient anticancer effects by using an antibody which binds to a mutant CALR protein and another anticancer agent in combination. A pharmaceutical for preventing and / or treating a cancer, including an antibody which specifically binds to a mutant calreticulin protein or a functional fragment thereof and a drug selected from the group consisting of an alkylating agent, a platinum preparation, an antimetabolite, a ribonucleotide reductase inhibitor, a nucleotide analog, a topoisomerase inhibitor, a microtubule polymerization inhibitor, an antitumor antibiotic, an interferon, a cytokine preparation, a molecular targeting drug, a nucleic acid synthesis inhibitor, a jak inhibitor, and a cancer immunotherapeutic agent in combination.

Disclosed are compositions and methods for inducing pterygium regression from the visual axis / corneal center, stabilizing pterygium, treating hyperemia and symptoms in pterygium patients, and treating pterygium recurrence after pterygium resection. The method comprises administering a multi-kinase inhibitor, an antimetabolite, or a combination thereof to a patient requiring the method.

The present invention provides compositions and methods for inducing pterygium regression from the visual axis / corneal center, stabilizing pterygium, treating hyperemia and symptoms in pterygium patients, and treating pterygium recurrence after pterygium excision. [Solution] A method for inducing pterygium regression from the visual axis / corneal center, comprising administering a therapeutically effective amount of (1) a multikinase inhibitor; (2) an antimetabolite that inhibits epithelial cell proliferation and fibroblast proliferation; or (3) a combination thereof to the affected eye of a subject requiring treatment.