12 results about "Osimertinib" patented technology

Disclosed herein are methods of determining whether a subject suffering from non-small cell lung cancer (NSCLC) is sensitive to treatment with osimertinib. In some embodiments, the method comprises obtaining an experimental matrix comprising a mutation status of at least one gene in an experimental sample associated with the subject, applying the obtained experimental matrix to a model, the model being based on a partitioning matrix comprising, for a plurality of reference samples, a mutation status of at least one gene and a sensitivity label for each of the plurality of reference samples indicating whether a corresponding reference subject is sensitive to osimertinib, wherein the at least one gene of the partitioning matrix corresponds to the at least one gene of the experimental matrix, and determining the subject as sensitive to treatment with osimertinib based on a result of the applied model.

Bispecific antibody against EGFR and c-Met. The heterodimeric interaction between the EGFR binding arm and the c-Met binding arm of the bispecific antibody is stronger than the interaction of each in the source homodimer by modifying the Fc segment amino acid sequence of the binding arm, so that it can be assembled into a heterodimer in vitro; its effect on inhibiting the proliferation of EGFR and c-Met double-positive tumor cells is stronger than the combination of EGFR monoclonal antibody and c-Met monoclonal antibody, mediates antibody-dependent cellular cytotoxicity (ADCC), promotes target protein internalization and inhibits the proliferation of osimertinib acquired resistant cell lines. Since the prepared bispecific antibody is simple to prepare, stable in structure, and can obtain a pure bispecific antibody by in vitro assembly, it is expected to better meet the clinical treatment needs, and therefore has a good market prospect.

UQCC2-based computer-assisted method, system, and device for diagnosing osimertinib-resistant lung cancer, predicting drug treatment effects, and screening drugs targeted for osimertinib-resistant lung cancer are provided. The method includes receiving input data, the input data including expression level data of UQCC2 in a patient with lung cancer; generating, based on the input data, an indication of whether the patient with lung cancer is a patient with osimertinib-resistant lung cancer through a machine learning model, a lung cancer including non-small cell lung cancer. The disclosure first discovers the significant overexpression of UQCC2 in the osimertinib-resistant lung cancer and the functional interaction between UQCC2 and METTL3, and provides an efficient and rapid method for diagnosing the patient with osimertinib-resistant lung cancer, predicting the drug treatment effect on the patient with osimertinib-resistant lung cancer, and screening drugs based on targeting UQCC2 and METTL3, demonstrating critical research significance for related disease prevention and treatment.

This invention belongs to the field of medical and pharmaceutical technology, and specifically relates to an antibacterial composition and its application. It comprises osimertinib mesylate and polymyxin. This invention is the first to demonstrate the novel pharmaceutical use of osimertinib mesylate as a synergistic antibacterial adjuvant for polymyxin. Experimental results show that osimertinib mesylate can significantly enhance the antibacterial activity of polymyxin against multidrug-resistant Gram-negative bacteria, effectively reduce the minimum inhibitory concentration of polymyxin, thereby reducing the clinical dosage of polymyxin and lowering the risk of its inherent nephrotoxicity and neurotoxicity. Furthermore, this invention reveals that the combined use of osimertinib mesylate and polymyxin can delay or reverse bacterial resistance to polymyxin, improve the survival rate of infected animal models, and broaden the antibacterial spectrum.

The application relates to application of osimertinib and a pharmaceutical composition thereof in preparation of a medicine for treating leukemia, and relates to the technical field of biological medicines. The application proves for the first time that a tyrosine kinase inhibitor targeting EGFR, osimertinib, exhibits significant anti-leukemia activity in T-ALL, and through combination of osimertinib and a nuclear export protein XPO1 inhibitor selinexor, T-ALL cell proliferation can be synergistically inhibited and apoptosis can be induced, so that the anti-tumor effect is significantly improved, and the defect that the curative effect of a single drug is limited is effectively overcome, the synergistic effect is verified in an in-vitro cell line model, T-ALL patient primary cells and an in-vivo mouse xenograft model, and a new way is provided for developing a high-efficiency and low-toxicity T-ALL treatment scheme.

The osimertinib-containing tablet of the present disclosure comprises 40% by mass or more of osimertinib or a pharmaceutically acceptable salt thereof, and is a direct compression tablet.

The application discloses a method for determining the concentration of sofosbuvir in blood plasma and screening a non-isotope labeled internal standard, wherein anlotinib, imatinib, olaparib, osimertinib and pralsetinib are used as internal standards, quantitative analysis is performed by combining LC-MS / MS with protein precipitation pretreatment. The internal standard screening method is screened from candidate compounds by systematically evaluating four dimensions of protein precipitation compatibility, matrix effect, detection stability and extraction recovery, and an internal standard consistent with the behavior of the measured substance is screened. The application solves the problem of the lack of commercial isotope internal standards for sofosbuvir, and provides a reliable and efficient detection and internal standard screening scheme.

The application belongs to the technical field of medicines, and provides a pyrimidine derivative containing a cyclopropane sulfonamide group, a pharmaceutically acceptable salt thereof, a preparation method and application thereof. The pyrimidine derivative containing a cyclopropane sulfonamide group has a structure shown in formula I. The pyrimidine derivative containing a cyclopropane sulfonamide group has a cyclopropane sulfonamide group substituted in the A ring and no alkoxy group substituted in the C ring. The active molecules can not only effectively inhibit the drug resistance of the third generation targeted drug Osimertinib after EGFR C797S mutation, but also can significantly inhibit EGFR single mutation or double mutation (L858R, del 19, T790M). The preparation method of the pyrimidine derivative containing a cyclopropane sulfonamide group and the pharmaceutically acceptable salt thereof has the advantages of simple synthesis process and low cost.

Provided are a cyclic 2-aminopyrimidine compound having a structure as shown in formula (I), or a pharmaceutically acceptable salt, stereoisomer or prodrug molecule thereof, and a use thereof. The compound can effectively inhibit the activity of EGFR protein kinase drug-resistant mutants (such as EGFRT790M and EGFR19del / T790M / C797S), and can overcome the clinical drug resistance of patients suffering from tumors such as non-small cell lung cancer induced by existing third-generation selective EGFRT790M small molecule inhibitors Osimertinib (AZD9291), Olmutinib (HM6171), Rociletinib (CO-1686) and the like.

This invention discloses the application of polyphosphates in the preparation of sensitizing drugs for osimertinib-resistant non-small cell lung cancer, belonging to the field of targeted sensitization technology. This invention is particularly applicable to the treatment of EGFR-mutant osimertinib-resistant non-small cell lung cancer, significantly enhancing the killing effect of osimertinib on resistant tumor cells. By using polyphosphates in combination with osimertinib, or by using polyphosphates alone as a sensitizer, osimertinib resistance can be improved, significantly enhancing the therapeutic effect. This invention demonstrates the potential of polyphosphates to inhibit the progression of PC9 OR cells in vitro and in vivo, clarifies the mechanism of action of polyphosphates on PC9 OR cells, and confirms that polyphosphates achieve their inhibitory effect on PC9 OR cells by regulating the expression of circPDE8A, providing a basis for using polyphosphates in the preparation of therapeutic drugs for PC9 OR cell-related diseases.

This invention discloses a pharmaceutical composition comprising osimertinib and carboxytriazole, a solid dispersion prepared from the two compounds and a dissolution enhancer, a pharmaceutical formulation prepared using the solid dispersion, and its antitumor use. By preparing carboxytriazole and osimertinib into a solid dispersion, the tablets prepared by this invention exhibit significantly better dissolution than ordinary tablets. Furthermore, bioavailability results show that the AUC of the osimertinib mesylate and carboxytriazole composition tablets prepared by this method is significantly higher than that of the comparative example and the original osimertinib mesylate formulation. Simultaneously, it demonstrates high stability and can achieve a synergistic effect.