6 results about "Strong inhibitor" patented technology

The application discloses an inhibitor for inhibiting KRAS phase separation to play an anti-tumor role and application, and relates to the fields of tumor molecular biology and targeted therapy.The application aims at solving the problems of limited effect, strong drug resistance and limited application range of KRAS tumor treatment methods, and the inhibitor is a statin.The KRAS protein can form a liquid condensate in cells, and the application discloses the mechanism of the KRAS protein in promoting KRAS protein processing, transportation and downstream signal activation, and further provides a technical scheme for inhibiting tumor growth and enhancing the therapeutic effect of a KRAS inhibitor by inhibiting the formation of KRAS condensates, so as to provide a new target and intervention approach for tumor treatment.

This application discloses the use of artesunate in the preparation of drugs for enhancing the therapeutic effect of PARP inhibitors, belonging to the field of biomedical technology. The artesunate described in this application is a sesquiterpene lactone derivative extracted from the traditional Chinese medicine Artemisia annua. It has an inhibitory effect on the proliferation of BRCA wild-type ovarian cancer cells and low toxicity to normal human ovarian epithelial cells. This application's research found that artesunate can enhance the DNA damage and apoptosis induced by PARP inhibitors (such as olaparib, niraparib, and rucaparib), and improve the sensitivity of PARP inhibitors to BRCA wild-type ovarian cancer.

The application discloses application of TRIM33 and miR-BART8-3p as target points in preparation of a drug for advanced nasopharyngeal carcinoma. The application first discloses that in the advanced nasopharyngeal carcinoma, EBV encoded miR-BART8-3p directly targets and inhibits the expression of TRIM33, up-regulates the expression of PD-L1, and finally promotes the molecular mechanism of immune escape. This discovery is particularly aimed at patients with advanced metastatic nasopharyngeal carcinoma, and fills the blank of the mechanism research of immunotherapy drug resistance of the population. Therefore, by up-regulating TRIM33 or inhibiting miR-BART8-3p, the antitumor immunity of the patient with advanced nasopharyngeal carcinoma can be effectively regulated, and a new strategy for treating advanced nasopharyngeal carcinoma, reversing immunotherapy drug resistance and enhancing the curative effect of a PD-1 inhibitor is formed. The application provides a complete solution from mechanism research to treatment application and precise prediction for the advanced nasopharyngeal carcinoma.

This invention discloses a metformin-enhanced PARP inhibitor, its preparation method, and its application, belonging to the field of biomedical technology. Specifically, it relates to a metformin-enhanced PARP inhibitor comprising metformin and olaparib, with a molar ratio of olaparib to metformin of 1:200-600. This invention reshapes the energy metabolism state of different BRCA1-mutant subtypes of triple-negative breast cancer cells through metformin, significantly enhancing the inhibitory effect of olaparib on these cancer cells under drug-resistant conditions, and effectively promoting apoptosis and inhibiting cell migration, thereby achieving a synergistic enhancement of the efficacy of PARP inhibitors.

This disclosure relates to the administration of the following combinations in certain patient populations: 1) about 100–110 mg, about 104–106 mg, or about 105 mg or less of bupropion hydrochloride or a molar equivalent of the free base form or another salt form of bupropion; and 2) about 40–50 mg, about 44–46 mg, or about 45 mg or less of dextromethorphan hydrobromide or a molar equivalent of the free base form or another salt form of dextromethorphan, in patient populations such as patients with moderate renal impairment, patients receiving a concomitant strong CYP2D6 inhibitor, patients known to be poor CYP2D6 metabolizers, patients requiring an NMDA antagonist that does not cause dissociation, and patients at risk of QT prolongation.

This invention belongs to the field of pharmaceutical technology and discloses a pharmaceutical composition of a USP7 inhibitor and fenofibrate and its antitumor application. The pharmaceutical composition uses a USP7 inhibitor and fenofibrate as the core active ingredients, with a molar ratio of 0.015625 to 0.625. The USP7 inhibitor is selected from at least one of LX04-104 and LML-17-133. This invention is the first to discover that fenofibrate can significantly enhance the antitumor effect of the USP7 inhibitor, and the combination of the two has a synergistic effect. This synergistic effect is cell type specific, particularly significant for nasopharyngeal carcinoma and pancreatic cancer, and the synergistic effect of fenofibrate is independent of the PPARα pathway. This composition can be prepared as an oral or injectable formulation for the treatment of nasopharyngeal carcinoma and pancreatic cancer, and has good prospects for clinical translation.