21 results about "Lapatinib" patented technology

The invention discloses an EGFR (epidermal growth factor receptor) dependent micromolecular conjugine-2 as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. The invention discloses an EGFR (epidermal growth factor receptor) dependent micromolecular conjugate. The preparation method comprises the following steps: reacting lapatinib with succinic anhydride to obtain an intermediate compound lapatinib-COOH; and then carrying out an amide condensation reaction on the conjugate and an IDO inhibitor NLG919 to obtain the conjugine-2. The result shows that the compound has a strong inhibition effect on pEGFR (Y1068) protein expression in MDA-MB-231 cells of triple negative breast cancer, and the compound can promote differentiation of CD4 + T cells by inhibiting kynurenine in the MDA-MB-231 cells; and the drug resistance of the lapatinib-mediated MDA-MB-231 cell can be effectively reversed.

The invention belongs to the technical field of chemical medicines, and discloses an oleanolic acid derivative and lapatinib conjugate as well as a preparation method and application thereof. The oleanolic acid derivative and the lapatinib conjugate improve the selectivity and activity of oleanolic acid by modifying the structure of an oleanolic acid mother nucleus, and are connected with lapatinib through a disulfide bond connecting bridge. The oleanolic acid derivative and lapatinib conjugate can be subjected to targeted breakage by glutathione to release free compounds. The invention provides a synthetic route and a purification method of the derivative.

The invention belongs to the field of biological medicines, and particularly relates to application of a compound to preparation of a medicine for treating papilloma of the upper respiratory tract. The invention provides an application of a compound in preparation of a medicine for treating and / or preventing papilloma of the upper respiratory tract, and is characterized in that the compound comprises one or more of asperisib, crizotinib, lapatinib, osimertinib and bortezomib. Experimental results show that the asperisib, crizotinib, lapatinib, osimertinib and bortezomib can realize long-term control on the papilloma of the upper respiratory tract and reduce the recurrence risk of the papilloma of the upper respiratory tract to a certain extent, so that the life quality of patients with the papilloma of the upper respiratory tract can be improved; the invention has important scientific value and clinical application prospect in the field of upper respiratory papilloma treatment.

Described herein are methods useful for the treatment of cancers in a canine subject with a pharmaceutical compositions comprising HDAC inhibitors, Rapamycin, Dasatinib, Lapatinib, Trametinib, Vorinostat, Imatinib, Crizotinib, Sorafenib, and combinations thereof. Also described herein are methods for identification of subjects with cancers that will benefit from administration of the pharmaceutical compositions comprising HIDAC inhibitors, Rapamycin, Dasatinib, Lapatinib, Trametinib, Vorinostat, Imatinib, Crizotinib, Sorafenib, and combinations thereof. In certain aspects, the methods described herein further comprise administering a therapeutically effective amount of at least one additional anti-cancer agent.

The invention belongs to the field of biological medicine, and particularly relates to novel application of an RTKs / RAS / RAF / c-Myc signal channel inhibitor. The invention discloses application of an RTKs / RAS / RAF / c-Myc signal channel inhibitor as a ferroptosis inhibitor. The RTKs signal channel inhibitor comprises BMS-599626, Lapatinib, and Ripretinib, and is characterized in that the RTKs signal channel inhibitor comprises BMS-599626, Lapatinib, and Ripretinib. And the RAS / RAF signal channel inhibitor comprises Lonafarnib and AZ628 (Azosulfuron 628). The c-Myc signal channel inhibitor comprises 10074-G5 and 10058-F4, and the c-Myc signal channel inhibitor comprises 10074-G5 and 10058 The invention provides a new thought for application of the RTKs / RAS / RAF / c-Myc signal channel inhibitor as a novel ferroptosis inhibitor in treatment of injury-related diseases.

The present invention relates to an application of an EGFR inhibitor combined with a PARP inhibitor in the treatment of ovarian cancer, and relates to the technical field of ovarian cancer treatment. The present invention obtains the EGFR inhibitor lapatinib and the PARP inhibitor niraparib by screening the FDA / CFDA approved compound library, and finds that lapatinib and niraparib have a good synergistic anti-ovarian cancer effect. In order to further study the molecular mechanism of the synergistic effect of the two, the present invention also detects the cell death pattern after the combined action of the two by apoptosis and protein immunoblotting. The combination of lapatinib and niraparib effectively inhibits the growth of ovarian cancer in an ovarian cancer animal model, showing good clinical research and application value, and is expected to become a new tool for the treatment of ovarian cancer.

The application discloses application of lapatinib in preparation of a rabies virus resisting medicine, and first discovers the rabies virus resisting activity of lapatinib, breaks the limitation of lapatinib only being used for treating tumors, and first proves the role of lapatinib in inhibiting rabies virus replication through in-vivo and in-vitro experiments, develops the potential application value of lapatinib in early treatment after rabies virus exposure, and provides a new use of lapatinib, i.e., using lapatinib as a candidate medicine for rabies treatment, especially specific treatment in the early stage of rabies virus infection, and fills the blank of specific treatment medicines after rabies virus exposure.

The invention discloses EGFR (epidermal growth factor receptor) dependent micromolecular conjugates 1, 3 and 4 as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. According to the EGFR-dependent micromolecular conjugine-1 disclosed by the invention, an IDO inhibitor D-MT is introduced into a lapatinib structure through reasonable structural modification, so that the target conjugine-1 is obtained. A glutathione S-transferase inhibitor NBDHEX is introduced into the structural fragment of the lapatinib through different connectors, and target conjugates 3 and 4 are obtained. Results show that the conjugate retains the inhibition effect of a parent compound on the activity of EGFR, IDO or GST and the powerful inhibition effect on proliferation of multiple different types of triple-negative breast cancer cells, can effectively reverse drug resistance of lapatinib-mediated triple-negative breast cancer cells, and can be used for preparing antitumor drugs.

The invention relates to the field of biological medicine, in particular to application of a substance specifically combined with STAMBP to preparation of a tumor treatment drug or a tumor treatment drug enhancer. When the STAMBP gene inhibitor is a nucleic acid molecule, the nucleic acid molecule comprises a nucleic acid fragment for coding shRNA (short hairpin Ribonucleic Acid) for knocking down the STAMBP gene; and / or when the STAMBP gene inhibitor is a chemical small molecule substance, the STAMBP gene inhibitor is selected from one or more of the chemical small molecule substances selected from irinotecan hydrochloride, lapatinib disaccharide, emtricitinib, ranolazine or atavalopag. According to the present invention, the STAMBP knockout weakens the aerobic glycolysis in the PC cells, the accompanying PDK1 overexpression reduces the reduction of the capacity and the glycolysis rate, and the irinotecan hydrochloride and the lapatinib disaccharide for the STAMBP significantly enhance the chemosensitivity of the PC cells.

The invention discloses an application of lapatinib in preparation of an anti-rabies virus drug, the anti-rabies virus activity of lapatinib is found for the first time, the limitation that lapatinib is only used for treating tumors is broken through, and the effect of lapatinib in inhibition of rabies virus replication is proved for the first time through in-vivo and in-vitro experiments. The invention develops a potential application value of lapatinib in early treatment after rabies virus exposure, and provides a new application of lapatinib: the lapatinib is applied to a candidate drug for treating rabies, especially specific treatment for early stage of rabies virus infection, and fills the blank of no specific treatment drug after rabies virus exposure.

Described herein are methods useful for the treatment of cancers in a canine subject with a pharmaceutical compositions comprising HD AC inhibitors, Rapamycin, Dasatinib, Lapatinib, Trametinib, Vorinostat, Imatinib, Crizotinib, Sorafenib, and combinations thereof. Also described herein are methods for identification of subjects with cancers that will benefit from administration of the pharmaceutical compositions comprising HD AC inhibitors, Rapamycin, Dasatinib, Lapatinib, Trametinib, Vorinostat, Imatinib, Crizotinib, Sorafenib, and combinations thereof. In certain aspects, the methods described herein further comprise administering a therapeutically effective amount of at least one additional anti-cancer agent.

The invention relates to application of an EGFR (epidermal growth factor receptor) inhibitor and a PARP (poly-ADP-ribose polymerase) inhibitor in treatment of ovarian cancer, and relates to the technical field of ovarian cancer treatment, an EGFR inhibitor lapatinib and a PARP inhibitor niraparib are obtained by screening an FDA / CFDA approved compound library, and it is found that lapatinib and niraparib have a good synergistic ovarian cancer resisting effect. In order to further research the molecular mechanism of the synergistic effect of the two, the cell death mode after the combined effect of the two is detected through apoptosis and western blotting. The combination of lapatinib and niraparib can effectively inhibit the growth of ovarian cancer in an ovarian cancer animal model, shows good clinical research and application values, and is expected to become a new tool for treating ovarian cancer.

The present invention relates to oral pharmaceutical suspension dosage form of Lapatinib and process of manufacturing thereof. The invention relates to providing patient-compliant, economical and technically advanced dosage form over existing dosage form.

This invention relates to the treatment of breast cancer in a subject, and the subject can be either a male or female subject. Including methods of: treating metastatic breast cancer; refractory breast cancer; AR-positive breast cancer; AR-positive refractory breast cancer; AR-positive metastatic breast cancer; AR-positive and ER-positive breast cancer; triple negative breast cancer; advanced breast cancer; breast cancer that has failed selective estrogen receptor modulator (SERM) (tamoxifen, toremifene, raloxifene), gonadotropin-releasing hormone (GnRH) agonist (goserelin), aromatase inhibitor (AI) (letrozole, anastrozole, exemestane), cyclin-dependent kinase 4 / 6 (CDK 4 / 6) inhibitor (palbociclib (Ibrance), ribociclib (Kisqali), lerociclib, abemaciclib (Vorzenio), trilaciclib, lerociclib), mTOR inhibitor (everolimus), trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), alpelisib (Piqray) (an inhibitor of phosphatidylinositol-3-kinase subunit alpha (PI3Kα)), lapatinib, neratinib (Nerlynx), olaparib (Lynparza) (an inhibitor of the enzyme poly ADP ribose polymerase (PARP)), bevacizumab (Avastin), and / or fulvestrant treatments; metastasis in a subject suffering from breast cancer; HER2-positive; treating a subject suffering from ER mutant expressing breast cancer and / or treating breast cancer in a subject, by first determining the 18F-16β-fluoro-5α-dihydrotestosterone (18F-DHT) tumor uptake and identifying said subject as having AR-positive breast cancer based on 18F-DHT tumor uptake, comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound and a cyclin-dependent kinase 4 / 6 (CDK 4 / 6) inhibitor.

The application discloses EGFR-dependent small molecule conjugates-1, 3 and 4, a preparation method and application thereof, and belongs to the technical field of biological medicines. The EGFR-dependent small molecule conjugate-1 disclosed by the application is obtained by introducing an IDO inhibitor D-MT into a lapatinib structure through reasonable structural modification. A glutathione S-transferase inhibitor NBDHEX is introduced into the above structural fragment of the lapatinib through different connectors to obtain target conjugates-3 and 4. The results show that the conjugates all retain the inhibitory effect of the parent compounds on EGFR, IDO or GST enzyme activity, have a strong inhibitory effect on the proliferation of various types of triple-negative breast cancer cells, can effectively reverse the lapatinib-mediated drug resistance of triple-negative breast cancer cells, and can be used for preparing antitumor drugs.

The invention provides a method for the treatment of Ph+ leukemia in a patient comprising administering to the patient (i) a BCR-ABL tyrosine kinase inhibitor, and (ii) an agent which selectively binds to a cell surface receptor expressed on Ph+ leukemic stem cells. The invention further provides for the use of (i) and (ii) in, or in the manufacture of a medicament for, the treatment of Ph+ leukemia in a patient; and a composition for the treatment of Ph+ leukemia in a patient comprising (i) and (ii); and kits comprising (i) and (ii). In some embodiments, the tyrosine kinase inhibitor is or is not imatinib; or is selected from the group consisting of dasatinib, nilotinib, bosutinib, axitinib, cediranib, crizotinib, damnacanthal, gefitinib, lapatinib, lestaurtinib, neratinib, semaxanib, sunitinib, toceranib, tyrphostins, vandetanib, vatalanib, INNO-406, AP24534, XL228, PHA-739358, MK-0457, SGX393 and DC2036; or is selected from the group consisting of dasatinib and nilotinib. In some embodiments, the agent binds to a receptor involved in signalling by at least one of IL-3, G-CSF and GM-CSF. In some embodiments, the agent is a mutein selected from the group consisting of IL-3 muteins, G-CSF muteins and GM-CSF muteins. In some embodiments, the mutein is an IL-3 mutein. In some embodiments, the agent is a soluble receptor which is capable of binding to IL-3.

A breakpoint cluster region-Abelson (Bcr-Abl) inhibitor for use in a method of treating a skin condition or disease, such as keloid disease (KD) or folliculitis keloidalis nuchae (FKN), is provided The Bcr-Abl inhibitor can be GNF-2, GNF-5 or ON012380. Optionally, the Bcr-Abl inhibitor can be administered in combination with one or more 4-anilinoquinazolines, such as dasatinib, nilotinib, bosutinib, axitinib, ponatinib, rociletinib, vemurafenib, dabrafenib, trametinib, cobimetinib, binimetinib, lapatinib, sunitinib, sorafenib or pazopanib. A UDP- glucuronosyltransferase (UGT) inhibitor, such as magnolol, can also be administered in an optional second treatment step, typically about 2 to 4 weeks after the first treatment. One or more 4-anilinoquinazolines can also be administered in the second treatment step. A Bcr-Abl inhibitor and / or one or more 4-anilinoquinazolines can further be administered in an optional third treatment step, typically about 6 weeks after the first treatment. A method of treatment and a kit are also provided.

Disclosed are methods and compositions for repolarizing a macrophage from M2 to M1 comprising administering to a subject in need thereof an effective dose of a compound comprising a dextran backbone and one or more CD206 targeting moieties conjugated thereto. In certain aspects, the compound further comprises a therapeutic agent selected from: paclitaxel, gemcitabine, lapatinib, and doxorubicin. In further aspect, the therapeutic agent comprises a chelator and at least one metal ion. In certain implementations, the at least one metal ion comprises at least one Cu(II) ions.

Methods are provided for treating lung cancer, and more particularly for treating pulmonary adenocarcinoma in a canine subject. The method may comprise assaying a biological sample from the canine subject, such as a tumor sample or a plasma sample, for a mutation in the HER2 gene. The mutation may include HER2 V659E, HER2 A664T, or HER2 K676E. If one or more of the mutations is present in the biological sample, the methods further include treating the canine subject by administering a therapeutically effective amount of an inhibitor of HER2. For example, a HER2 V659E may indicate increase sensitivity to a HER2 inhibitor. The HER2 inhibitor may include a small molecule HER2 inhibitor, such as trastuzumab, neratinib, lapatinib, erlotinib, and pertuzumab.

The application provides doxorubicin and lapatinib in constructing a zebrafish cardiotoxicity damage model and a drug screening method, and belongs to the technical field of biological medicine and animal model construction. The application discloses that doxorubicin and lapatinib can be used in combination to construct a doxorubicin-related zebrafish cardiotoxicity damage model for the first time, and provides a method for establishing a zebrafish cardiotoxicity damage model. The heart index of the application is very comprehensive, and the zebrafish cardiotoxicity damage model constructed by the application can be used to screen drugs of various different action mechanisms which have an improving effect on heart damage.

To provide a method of treating a keratoderma.SOLUTION: The present invention provides a method of treating a keratoderma in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of an EGFR inhibitor. Preferably, the EGFR inhibitor is selected from the group consisting of brigatinib, erlotinib, gefitinib, icotinib, lapatinib, sapitinib, vandetanib, varlitinib, afatinib, canertinib, dacomitinib, neratinib, osimertinib, pelitinib, and rociletinib.SELECTED DRAWING: None