10 results about "Regorafenib" patented technology

This invention discloses the application of regorafenib in the preparation of drugs to reverse gemcitabine resistance in pancreatic cancer. This invention is the first to discover that the protein FBLN3 plays a key regulatory role in gemcitabine-resistant pancreatic cancer cells; its downregulation significantly reduces the half-maximal inhibitory concentration (IC50) of gemcitabine. Furthermore, this invention clarifies that FBLN3 specifically interacts with EGFR, and identifies the key binding region between the two. This invention is also the first to discover that regorafenib can effectively block the interaction between FBLN3 and EGFR, and that the combination of regorafenib and sativa shows significantly better anti-tumor effects than monotherapy, effectively reversing gemcitabine resistance in pancreatic cancer.

A pharmaceutical composition for prevention or treatment of a disease or disorder characterized by chronic inflammation, associated with angiogenesis and fibrosis. The pharmaceutical composition includes a multi-target inhibitor, multi-phase modulator, or multi-kinase inhibitor, such as axitinib, nintedanib, pirfenidone, riociguat, sorafenib, sunitinib, lenvatinib, regorafenib, ponatinib, or pazopanib.

A process for preparing regorafenib using N,N'-bis[(2R)-1,1,1-trifluoropropan-2-yl] triamidodicarbonic acid diamide hydrochloride.

The invention relates to application of a proteasome inhibitor in preparation of a medicine for treating tumors resistant to a tyrosine kinase inhibitor, and in the application, a plurality of strains of liver cancer cells with drug resistance to lenvatinib or regorafenib are constructed by utilizing a plurality of human liver cancer cell lines with different genetic backgrounds; a high-throughput CRISPR (clustered regularly interspaced short palindromic repeats) gene knockout screening technology and a patent medicine gene CRISPR library are utilized, and gene targets of which the gene knockout or inactivation can better kill drug-resistant cells are specifically identified from thousands of patent medicine genes. Wherein the function inactivation of a plurality of genes in the proteasome family shows more obvious cell killing activity in a plurality of drug-resistant cell models compared with non-drug-resistant cells. The invention discovers and verifies that the proteasome inhibitor has a specific killing effect on tyrosine kinase inhibitor drug-resistant liver cancer for the first time.

The invention relates to an oligonucleotide lung targeting delivery system and application thereof in treatment of lung diseases, and relates to the technical field of biological medicines and nano-medicines. The invention designs a high-efficiency lung targeting oligonucleotide delivery drug, which comprises lipid nanoparticles, the lipid nanoparticles contain oligonucleotide and lipid components, and the lipid components are composed of 4-(N, N-dimethylamino) butyric acid (dilinoleyl) methyl ester, (2, 4-dimethylamino) butyric acid (dilinoleyl) methyl ester, (2, 4-dimethylamino) butyric acid (2, 4-dimethylamino) butyric acid (2, 4-dimethylamino) butyric acid (2, 4-dimethylamino) butyric acid (2, 4-dimethylamino) butyric acid The composition is composed of 1, 3-dioleoyl-propyl)-trimethylamine, dipalmitoyl phosphatidylcholine and pegylated lipid. A breakthrough of a nucleic acid medicine lung delivery technology is realized, in-vivo experiment verification results show that the lung aggregation efficiency is improved by about 2-4 times compared with that of traditional lipid nanoparticles, the lipid nanoparticles have remarkable lung metastatic tumor resisting activity, in-vivo experiments show that the lipid nanoparticles can inhibit growth of colorectal cancer lung metastatic tumors and prolong the survival time of mice, and the lipid nanoparticles have good application prospects. And the effect is better than that of 5-fluorouracil and regorafenib.

The application belongs to the field of colorectal cancer treatment, and particularly relates to application of dihydroartemisinin in preparation of colorectal cancer liver metastasis drugs. The application research finds that dihydroartemisinin (DHA) can inhibit expression of mutant KRAS, reshape tumor immune microenvironment, thereby enhancing therapeutic effect of regorafenib combined with PD-1 inhibitor. These findings provide new insights for overcoming drug resistance in KRAS mutant colorectal cancer liver metastasis (CRCLM), and support further development of DHA as an adjuvant drug for combination therapy to improve patient prognosis.

The invention provides a regorafenib-entrapped albumin preparation, a pharmaceutical composition and a preparation method and application of the regorafenib-entrapped albumin preparation, the regorafenib-entrapped albumin preparation is prepared from regorafenib into an albumin nano preparation, the solubility of REG is enhanced, side effects are relieved, the biological half-life period is prolonged, long-acting circulation is achieved, and the regorafenib-entrapped albumin preparation has a good application prospect. And the curative effect is enhanced by increasing the tumor tissue drug accumulation amount. In addition, according to the pharmaceutical composition, the regorafenib component is added into the albumin paclitaxel preparation, so that the pharmaceutical composition has the capability of synergistically reprogramming macrophages. Cell experiments prove that the combined use of PTX and REG under certain proportion conditions can enhance the M1 type polarization of macrophages.

To provide combination pharmaceuticals for treating, preventing or managing diseases and conditions including hyperproliferative disorders such as cancer in humans and other mammals.SOLUTION: Disclosed is a combination pharmaceutical comprising regorafenib or its hydrate, solvate, metabolite or pharmaceutically acceptable salt or a polymorph thereof and a PD-1 / PD-L1(2) inhibitor.SELECTED DRAWING: None

The invention relates to the technical field of tumor treatment, in particular to a VEGFR-2 / BRD4 double-target inhibitor and application thereof. The structural general formula of the VEGFR-2 / BRD4 double-target inhibitor is as shown in a formula I in the specification. The tetrahydropteridine compound containing the aryl amide or aryl urea structure, disclosed by the invention, has relatively strong inhibitory activity on VEGFR-2 / BRD4 activity; according to the present invention, the VEGFR-2 / BRD4 double-target inhibitor has good anti-proliferative activity on tumor cells, the compound I-5 shows the optimal activity, and the activity is far superior to the positive control Sorafenib, ReGrafenib and JQ-1, the effect of the ReGrafenib and the effect of the combination of the Sorafenib and the JQ-1 respectively, and the target treatment drug for leukemia, gastrointestinal stromal tumor, liver cancer, kidney cancer, thyroid cancer, non-small cell lung cancer, colorectal cancer and the like can be prepared, and the compound I-5 can be used for the preparation of the target treatment drug for treating leukemia, gastrointestinal stromal tumor, liver cancer, kidney cancer, thyroid cancer, non-small cell lung cancer, colorectal cancer and the like.