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12 results about "Carfilzomib" patented technology
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Carfilzomib (marketed under the trade name Kyprolis, developed by Onyx Pharmaceuticals) is an anti-cancer drug acting as a selective proteasome inhibitor. Chemically, it is a tetrapeptide epoxyketone and an analog of epoxomicin.
The invention discloses application of carfilzomib in preparation of a medicine for preventing and treating Nipah virus, and belongs to the technical field of medicine. The method mainly aims at ubiquitination modification of nipah virus M protein, the carfilzomib is used for inhibiting a host proteasome path, free ubiquitination factors in cells are depleted to achieve the effect of inhibiting ubiquitination of the M protein, then nucleoplasm shuttle of the M protein is inhibited, replication of the nipah virus is inhibited, and the effect is good. At present, most of research and development of virus medicines and vaccines are designed or modified aiming at viruses, a new thought is provided for research and development of medicines and vaccines in the future, and a new application is also provided for Carfilzomib.
To provide a stable modified carfilzomib formulation. [Solution] The present invention provides a stable pharmaceutical composition of a PEGylated carfilzomib compound, a method for preparing the composition, and the use of the composition for treating cancer, including vascular malignancies such as multiple myeloma. The composition can be stored in a frozen form or lyophilized in a dry solid form.
The invention discloses a method for detecting N-methyl pyrrolidone in a carfilzomib intermediate, which comprises the following steps: adopting a high performance liquid chromatography, using a ZORBAX Eclipse C18 ball porous filler chromatographic column to realize reverse phase separation, and using a diode array detector to perform quantitative analysis. Chromatographic conditions are as follows: a mobile phase A is water; a mobile phase B is methanol, and carrying out gradient elution on the phase A and the phase B; the flow velocity is 0.8 to 1.0 ml / min; the column temperature is 25-40 DEG C; the detection wavelength is 205 to 220 nm; the sample size is 10-20 [mu] l; and the diluent is a 50-70% methanolaqueous solution. The N-methyl pyrrolidone disclosed by the invention is relatively high in response, high in detection sensitivity, good in peak pattern and accurate and reliable in detection result; the high performance liquid chromatography is adopted, instruments, solvents and chromatographic columns used for detection are conventional and easy to obtain, samples and reference substances are easy to prepare and operate, and the method can be widely applied to detection of N-methyl pyrrolidone.
The invention relates to application of retinol compounds and carfilzomib in preparation of drugs for treating multiple myeloma, and belongs to the technical field of antitumor drugs. Aiming at the problem of drug resistance in treatment of multiple myeloma, the invention provides a technical scheme of drug combination. The retinol compound is preferably synthetic retinol WYC-209, the retinol compound can enhance the sensitivity of carfilzomib for treating multiple myeloma, and the action mechanism is that WYC-209 aggravates endoplasmic reticulum stress of multiple myeloma cells and destroys an endoplasmic reticulum structure. The combined treatment scheme can inhibit proliferation of multiple myeloma cells, induce cellapoptosis, reduce tumor load, inhibit bone marrow infiltration of tumor cells and improve the long-term survival rate of mice. The invention further provides a pharmaceutical composition containing WYC-209 and carfilzomib, the mass ratio of WYC-209 to carfilzomib is (0.01-3000): 1, and the pharmaceutical composition can be prepared into a solution or suspension and is suitable for treating first-diagnosis high-risk multiple myeloma or recurrent / refractory multiple myeloma.