GPX4 inhibitor in combination with anticancer agent for treating proliferative disease
AssigneeEubulus Biotherapeutics Inc.
InventorSheldon Cao
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Abstract
Provided herein is a method of treating, preventing, or ameliorating one or more symptoms of a GPX4-mediated disorder, disease, or condition in a subject with a GPX4 inhibitor and an anticancer agent. Also provided herein are methods of inducing ferroptosis in a cell or inhibiting the growth of a cell with a GPX4 inhibitor and an anticancer agent.
Claims17
A method of abrogating or alleviating cancer in a subject, comprising administering to the subject in need thereof a therapeutically effective amount of a glutathione peroxidase 4 inhibitor and a therapeutically effective amount or a subtherapeutically effective amount of an anticancer agent;
- wherein the cancer is colorectal adenocarcinoma, hepatocellular carcinoma, or ovarian adenocarcinoma;
- wherein the glutathione peroxidase 4 inhibitor is methyl 4-((3R)-3-(hydroxymethyl)-2-propioloyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)benzoate or N-(1-(4-aminophenyl)-2-(tert-butylamino)-2-oxoethyl)-N-(3-chloro-4-methoxyphenyl)-propiolamide;
- or an enantiomer, a mixture of enantiomers, a diastereomer, a mixture of two or more diastereomers, a tautomer, a mixture of two or more tautomers, or an isotopic variant thereof;
- or a pharmaceutically acceptable salt, solvate, or hydrate thereof;
- and wherein the anticancer agent is neratinib, regorafenib, or sorafenib.
A method of inhibiting the growth of a cancerous cell or inducing ferroptosis in a cancerous cell, comprising contacting the cell with an effective amount of a GPX4 inhibitor and an effective amount or a subeffective amount of an anticancer agent;
- wherein the glutathione peroxidase 4 inhibitor is methyl 4-((3R)-3-(hydroxymethyl)-2-propioloyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)benzoate or N-(1-(4-aminophenyl)-2-(tert-butylamino)-2-oxoethyl)-N-(3-chloro-4-methoxyphenyl)-propiolamide;
- or an enantiomer, a mixture of enantiomers, a diastereomer, a mixture of two or more diastereomers, a tautomer, a mixture of two or more tautomers, or an isotopic variant thereof;
- or a pharmaceutically acceptable salt, solvate, or hydrate thereof;
- and wherein the anticancer agent is neratinib, regorafenib, or sorafenib.
Dependencies are inferred from the claim text.