US2023145356A1PendingUtilityA1

Use of fak inhibitor in preparation of drug for treating tumors having nras mutation

Assignee: INXMED NANJING CO LTDPriority: Nov 18, 2019Filed: Nov 17, 2020Published: May 11, 2023
Est. expiryNov 18, 2039(~13.3 yrs left)· nominal 20-yr term from priority
A61K 31/444A61P 35/00A61K 45/06A61K 31/506A61P 1/00A61K 31/4439A61P 17/00A61P 19/04A61K 31/5377A61K 31/337
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Claims

Abstract

A use of a FAK inhibitor in the preparation of a drug for preventing and/or treating tumors having an NRAS mutation. A method for treating tumors that have experienced an NRAS mutation, which comprises administering an effective dose of a FAK inhibitor to an individual. A FAK inhibitor for treating tumors having an NRAS mutation. The FAK inhibitor is BI853520, defactinib, GSK2256098, PF-00562271, VS-4718 or a pharmaceutically acceptable salt thereof.

Claims

exact text as granted — not AI-modified
1 - 7 . (canceled) 
     
     
         8 . A method of treating tumors having an NRAS mutation comprising administering to an individual an effective amount of a FAK inhibitor. 
     
     
         9 . The method of  claim 8 , wherein the FAK inhibitor is BI853520, defactinib, GSK2256098, PF-00562271, VS-4718 or a pharmaceutically acceptable salt thereof, alternatively, the FAK inhibitor is BI853520 or a pharmaceutically acceptable salt thereof, especially BI853520 tartrate. 
     
     
         10 . The method of  claim 8 , further comprising administering to the individual an effective amount of a second therapeutic agent. 
     
     
         11 . The method of  claim 8 , further comprising radiotherapy or cell therapy. 
     
     
         12 . The method of  claim 8 , wherein the tumor is Hodgkin's lymphoma, non-Hodgkin's lymphoma, non-small cell lung cancer, small cell lung cancer, hepatocellular carcinoma, cholangiocarcinoma, myelodysplastic syndrome, acute lymphoblastic leukemia, acute myeloid leukemia, chronic myeloid leukemia, thyroid cancer, glioma, colon cancer, rectal cancer, colorectal cancer, ovarian cancer, bladder cancer, prostate cancer, breast cancer, liposarcoma, fibrosarcoma, rhabdomyosarcoma, leiomyosarcoma, angiosarcoma, neuroblastoma, renal cell carcinoma, head and neck cancer, stomach cancer, esophageal cancer, gastroesophageal junction cancer, thymic cancer, pancreatic cancer, endometrial cancer, cervical cancer, melanoma, skin cancer, germ cell carcinoma, nasopharyngeal carcinoma, oropharyngeal carcinoma or laryngeal carcinoma. 
     
     
         13 . The method of  claim 10 , wherein the second therapeutic agent is one or more selected from chemotherapeutic agents, targeted therapeutic agents and immunotherapeutic agents. 
     
     
         14 . The method of  claim 10 , wherein the second therapeutic agent is one or more selected from the group consisting of nimustine, carmustine, lomustine, temozolomide, cyclophosphamide, isocyclophosphamide, glyfosfin, doxifluridine, Furtulon, fluorouraeil, mercaptopurine, azathioprine, tioguanine, floxuridine, tegafur, gemcitabine, decitabine, carmofur, hydroxyurea, methotrexate, UFT, capecitabine, ancitabine, thiotepa, actinomycin D, adriamycin, liposomal doxorubicin, daunorubicin, epirubicin, mitomycin, pingyangmycin, pirarubicin, valrubicin, idarubicin, irinotecan, harringtonine, camptothecin, hydroxycamptothecine, topotecan, vinorelbine (navelbine), taxol, taxotere, hycamtin, vinblastine, vincristine, vindesine, vindesine sulfate, vincaleukoblastine, teniposide, etoposide, elemene, atamestane, anastrozole, aminoglutethimide, letrozole, formestane, megestrol, tamoxifen, asparaginase, carboplatin, cisplatin, dacarbazine, oxaliplatin, eloxatin, mitoxantrone, procarbazine, docetaxel, gefitinib, erlotinib, icotinib, afatinib, osimertinib, crizotinib, ceritinib, alectinib, lapatinib, everolimus, palbociclib, ribociclib, apatinib, regorafenib, sorafenib, sunitinib, temsirolimus, lenvatinib, pazopanib, axitinib, cabozantinib, trametinib, binimetinib, vemurafenib, dabrafenib, Cobimetinib, vandetanib, bortezomib, palbociclib, lenalidomide, ixazomib, imatinib, dasatinib, bosutinib, ponatinib, ibrutinib, idelalisib, belinostat, romidepsin, vorinostat, olaparib, niraparib, denosumab, vismodegib, sonidegib, rucaparib, brigatinib, bicalutamide, enzalutamide, abiraterone, abemaciclib, apalutamide, aflibercept, azacitidine, bleomycin, chlorambucil, cytarabine, epothilone, fludarabine, flutamide, mechlorethamine, paclitaxel, pemetrexed, raltitrexed, necitumumab, bevacizumab, ramucirumab, Ado-trastuzumab, pertuzumab, cetuximab, panitumumab, alirocumab, durvalumab, nimotuzumab, daratumumab, atezolizumab, sintilimab, toripalimab, camrelizumab, tislelizumab, durvalumab, nivolumab, and pembrolizumab. 
     
     
         15 . The method of  claim 10 , wherein the FAK inhibitor and the second therapeutic agent are administered simultaneously, alternately or sequentially. 
     
     
         16 . The method of  claim 11 , wherein the FAK inhibitor and radiotherapy or cell therapy are performed simultaneously, alternately or sequentially. 
     
     
         17 - 23 . (canceled) 
     
     
         24 . The method of  claim 12 , wherein the tumor is acute myeloid leukemia, melanoma, thyroid carcinoma, colorectal carcinoma, esophageal carcinoma, hepatocellular carcinoma, ovarian carcinoma, fibrosarcoma or cholangiocarcinoma. 
     
     
         25 . The method of  claim 14 , wherein the second therapeutic agent is selected from decitabine, gemcitabine, cisplatin, carboplatin, oxaliplatin, adriamycin, liposomal doxorubicin, taxol, docetaxel, trametinib, binimetinib, cobimetinib, durvalumab, atezolizumab, sintilimab, toripalimab, camrelizumab, tislelizumab, nivolumab, or pembrolizumab. 
     
     
         26 . The method of  claim 25 , wherein the second therapeutic agent is selected from docetaxel, liposomal doxorubicin, cobimetinib, pembrolizumab, or decitabine. 
     
     
         27 . The method of  claim 26 , wherein the second therapeutic agent is cobimetinib.

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