AXL inhib 
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  • ||||||||||  Journal:  PTBP1-mediated regulation of AXL mRNA stability plays a role in lung tumorigenesis. (Pubmed Central) -  Nov 12, 2020   
    In conclusion, we have identified a molecular mechanism of AXL expression regulation by PTBP1 through controlling the AXL mRNA stability. These findings may represent new thoughts alternative to current approaches that directly inhibit AXL signaling and may eventually help to develop novel therapeutics to avoid cancer metastasis and drug resistance.
  • ||||||||||  ASLAN002 / BMS
    [VIRTUAL] S6K FEEDBACK REGULATION OF THE RECEPTOR TYROSINE KINASE AXL IN PTEN-DEFICIENT GLIOBLASTOMA () -  Nov 10, 2020 - Abstract #SNO2020SNO_1088;    
    Previously we established that combining the LY-2584702 inhibitor of S6K1 with the BMS-777607 inhibitor of the AXL receptor tyrosine kinase (RTK) was selectively cytotoxic for PTEN-deficient GBM...Metabolomic analysis revealed combination effects of S6K and AXL inhibitors in reducing nucleotide precursor metabolic flux. We therefore propose that combination inhibition of S6K and AXL signaling compromises S6K-dependent nucleotide synthesis in PTEN-deficient GBM.
  • ||||||||||  Journal:  AXL Is a Driver of Stemness in Normal Mammary Gland and Breast Cancer. (Pubmed Central) -  Oct 28, 2020   
    An AXL-dependent gene signature is a feature of transcriptomes in basal breast cancers and reduced patient survival irrespective of subtype. Our interpretation is that AXL regulates access to epithelial plasticity programs in MaSCs and, when co-opted, maintains acquired stemness in breast cancer cells.
  • ||||||||||  dubermatinib (TP-0903) / Sumitomo Dainippon, Jakafi oral (ruxolitinib) / Novartis, Incyte
    Journal:  Single-cell Proteomic Profiling Identifies Combined AXL and JAK1 Inhibition as a Novel Therapeutic Strategy for Lung Cancer. (Pubmed Central) -  Oct 22, 2020   
    Patient-derived organoids (PDOs) obtained from tumors with high AXL and JAK1 were sensitive to TP-0903 and ruxolitinib (JAK inhibitor) treatments supporting the CyTOF findings. This study shows that single-cell proteomic profiling of treatment-naïve lung tumors, coupled with ex vivo testing of PDOs, identifies continuous AXL, TGF-β and JAK1-STAT3 signal activation in select tumors that may be targeted by combined AXL-JAK1 inhibition.
  • ||||||||||  SLC-391 / SignalChem Lifesci
    Trial completion date, Trial primary completion date:  Safety Study of SLC-391 in Subjects With Solid Tumors (clinicaltrials.gov) -  Oct 20, 2020   
    P1,  N=50, Recruiting, 
    Novel targeted therapies may be researched that can detect and target these molecules at an earlier stage of pathogenesis of these tumors. Trial completion date: Aug 2020 --> Jun 2021 | Trial primary completion date: Aug 2020 --> Jun 2021
  • ||||||||||  [VIRTUAL] Potent And Selective Inhibition Of AXL Receptor Tyrosine Kinase For The Treatment of Cancer () -  Oct 14, 2020 - Abstract #SITC2020SITC_1538;    
    AXL inhibition reduces the immunosuppressive TME, enables activation of an anti-tumor immune response and renders tumors more susceptible to previously resistant therapies. Highly potent and selective AXL inhibitors have been designed, displaying biological profiles superior to those of less-selective molecules currently advancing through clinical development.
  • ||||||||||  [VIRTUAL] Potent And Selective Inhibition Of AXL Receptor Tyrosine Kinase For The Treatment of Cancer () -  Oct 14, 2020 - Abstract #SITC2020SITC_803;    
    AXL inhibition reduces the immunosuppressive TME, enables activation of an anti-tumor immune response and renders tumors more susceptible to previously resistant therapies. Highly potent and selective AXL inhibitors have been designed, displaying biological profiles superior to those of less-selective molecules currently advancing through clinical development.
  • ||||||||||  Review, Journal:  c-Met expression in renal cell carcinoma with bone metastases. (Pubmed Central) -  Oct 8, 2020   
    However, the efficacy of targeting c-Met in bone metastatic disease, including in RCC, has not been proven. Therefore, further investigation is required focusing the particular role of HGF/c-Met pathway in bone microenvironment (BME) and how to effectively target this pathway in the context of bone metastatic disease.
  • ||||||||||  metformin / Generic mfg., sirolimus / Generic mfg., doxorubicin hydrochloride / Generic mfg.
    Journal:  Metformin suppresses the growth of leukemia cells partly through downregulation of AXL receptor tyrosine kinase. (Pubmed Central) -  Oct 7, 2020   
    Given that metformin also downregulated expression of TYRO3 and phosphorylation of MERTK, these findings indicate that anti-leukemic effects exerted by metformin could be partly due to the inhibition of TAM kinases. Thus, metformin has a clinical potential for patients with leukemia cells positive for AXL and the other TAM proteins as well as activated mTOR.
  • ||||||||||  bemcentinib (BGB324) / BerGenBio
    Journal:  AXL Inactivation Inhibits Mesothelioma Growth and Migration via Regulation of p53 Expression. (Pubmed Central) -  Oct 2, 2020   
    AXL inhibition (shRNA or R428) reduced mesothelioma cell viability, migration, and invasion, whereas TP53 shRNA knockdown attenuated antiproliferative, migration, and invasive effects of AXL silencing or AXL inactivation in these cells. These studies demonstrate a novel feedback regulation loop between AXL and p53, and provide a rationale for mesothelioma therapies targeting AXL/p53 signaling.
  • ||||||||||  Journal:  The crosstalk between AXL and YAP promotes tumor progression through STAT3 activation in head and neck squamous cell carcinoma. (Pubmed Central) -  Sep 16, 2020   
    Mechanistically, Gas6 induced a competitive binding to phosphorylated signal transducers and activators of transcription 3 (STAT3) with large tumor suppressor kinase 1 (LATS1) and inhibited the Hippo pathway. This study revealed a novel non-transcriptional effect of STAT3 in Gas6/AXL-induced YAP activity, suggesting that STAT3 acted as a critical "molecular switch" during the mutual promotion between AXL and YAP, which might be a promising therapeutic target in HNSCC.
  • ||||||||||  bemcentinib (BGB324) / BerGenBio
    Journal:  Long noncoding RNA H19 regulates HIF-1α/AXL signaling through inhibiting miR-20b-5p in endometrial cancer. (Pubmed Central) -  Sep 10, 2020   
    Furthermore, H19 was also verified to stimulate the activity of endometrial cancer with AXL inhibitor BGB324 in vitro and in vivo. To sum up, H19 accelerates the tumor formation of endometrial cancer through the miR-20b-5p/AXL/HIF-1α signaling pathway, thereby providing a novel target for diagnosing and treating endometrial cancer.
  • ||||||||||  [VIRTUAL] Tilvestamab, a novel clinical stage humanized anti-AXL function blocking antibody () -  Sep 7, 2020 - Abstract #AACRNCIEORTC2020AACR_NCI_EORTC_286;    
    P1
    In a non-human primate dose-ranging toxicokinetic study with chronic weekly administration for 26 weeks, tilvestamab was well tolerated during dosing phase, with no abnormal necropsy findings on termination, and with predictable dose-proportional plasma pharmacokinetics, up to the highest studied dose of 25mg/kg. Tilvestamab is currently being evaluated in a Phase I clinical study (BGB149-101; NCT03795142) in healthy volunteers to evaluate safety, tolerability and pharmacokinetics.
  • ||||||||||  [VIRTUAL] Tilvestamab, a novel clinical stage humanized anti-AXL function blocking antibody () -  Sep 7, 2020 - Abstract #AACRNCIEORTC2020AACR_NCI_EORTC_285;    
    P1
    In a non-human primate dose-ranging toxicokinetic study with chronic weekly administration for 26 weeks, tilvestamab was well tolerated during dosing phase, with no abnormal necropsy findings on termination, and with predictable dose-proportional plasma pharmacokinetics, up to the highest studied dose of 25mg/kg. Tilvestamab is currently being evaluated in a Phase I clinical study (BGB149-101; NCT03795142) in healthy volunteers to evaluate safety, tolerability and pharmacokinetics.
  • ||||||||||  Cabometyx (cabozantinib tablet) / Takeda, Exelixis, Ipsen
    [VIRTUAL] XL092, A multi-targeted inhibitor of MET, VEGFR2, AXL and MER with an optimized pharmacokinetic profile (Channel 1) -  Sep 7, 2020 - Abstract #AACRNCIEORTC2020AACR_NCI_EORTC_123;    
    P1
    In preclinical studies XL092 showed potent pharmacodynamic inhibition of MET and VEGFR2 phosphorylation, which was associated with significant anti-tumor activity. PK data from the Phase 1 trial of XL092 shows a significantly shorter terminal half-life compared to cabozantinib, consistent with the desired profile.
  • ||||||||||  Cabometyx (cabozantinib tablet) / Takeda, Exelixis, Ipsen
    [VIRTUAL] Characterization of TKI resistant renal cell carcinoma after sequential application of Cabozantinib (Lecture sessions - available at any time every day) -  Sep 6, 2020 - Abstract #DGU2020DGU_243;    
    However, we could not define a clear correlation between the overexpression of the activated receptor in 786-O / S and 786-O / P and their tolerance towards Cbz. Following Cbz treatment, the activated survival pathway might suggest a signaling synergy resulting in drug tolerance.
  • ||||||||||  Cabometyx (cabozantinib tablet) / Takeda, Exelixis, Ipsen
    Clinical, P2 data, Clinical Trial,Phase II, Journal:  Cabozantinib in patients with platinum-refractory metastatic urothelial carcinoma: an open-label, single-centre, phase 2 trial. (Pubmed Central) -  Aug 22, 2020   
    P2
    Cabozantinib has single-agent clinical activity in patients with heavily pretreated, platinum-refractory metastatic urothelial carcinoma with measurable disease and bone metastases and is generally well tolerated. Cabozantinib has innate and adaptive immunomodulatory properties providing a rationale for combining cabozantinib with immunotherapeutic strategies.
  • ||||||||||  Journal:  Qigesan reduces the motility of esophageal cancer cells via inhibiting Gas6/Axl and NF-κB expression. (Pubmed Central) -  Aug 4, 2020   
    This study is mainly to explore the mechanism that how QGS affect the movement capacity of esophageal cancer cell.QGS incubates ECA109 and TE1 cell lines, and detecting the motility of tumor Cells by different experiments.Growth arrest-specific 6 (Gas6) and Anexelekto(Axl)was co-localized,and then detecting Gas6,Axl signaling pathway and protein expression after QGS intervention.Similarly, Observing the signal localization and protein expression of P-Phosphoinositide3-kinases (PI3K),P-AKT Protein kinase B (AKT),P-Nuclear factor-kappa B(NF-κB),Matrix Metalloproteinase-2(MMP2) and Matrix Metalloproteinase-9(MMP9). The results showed that the concentration of QGS was less than 200 ug/ml, and the cultured cells did not exceed 24 h, that no obvious cytotoxicity was observed.QGS significantly inhibited the mobility of ECA109 and TE1 cell lines in the concentration-dependent manner.In addition, QGS can regulate the Gas6/Axl pathway, inhibit the formation and localization of the Gas6/Axl complex,and reduce the protein activation of PI3K/AKT,NF-κB,MMP2 and MMP9.Experimental innovation shows that QGS can significantly slow down the mobility of EC cells by regulating the Gas6/Axl complex and downstream signaling pathways,and provides a theoretical basis for the pharmacological effects of QGS in the therapy of EC.
  • ||||||||||  bemcentinib (BGB324) / BerGenBio
    [VIRTUAL] Elevated AXL expression following SARS-CoV-2 infection in non-small cell lung cancer (On-Demand) -  Jul 24, 2020 - Abstract #ESMO2020ESMO_2484;    
    Recently, bemcentinib, a highly selective and potent AXL inhibitor with antiviral activity, has been fast-tracked as the first potential treatment for assessment in the United Kingdom’s ACcelerating COVID-19 Research & Development (ACCORD) multicenter, randomized phase II trial...Funding: NIH/NCI CCSG P30-CA016672 (Bioinformatics Shared Resource), NIH/NCI T32 CA009666, ASCO Young Investigator Award (C.M.G.); University of Texas SPORE in Lung Cancer P5-CA070907 (L.A.B. C.M.G.), NIH/NCI R01-CA207295, NIH/NCI U01-CA213273, the Department of Defense (LC170171) (L.A.B.), The LUNGevity foundation (D.G., L.A.B.), through generous philanthropic contributions to The University of Texas MD Anderson Lung Cancer Moon Shot Program (J.V.H., J.W., L.A.B.); an Andrew Sabin Family Fellowship (L.A.B.), and The Rexanna Foundation for Fighting Lung Cancer (J.V.H., L.A.B.).
  • ||||||||||  dubermatinib (TP-0903) / Sumitomo Pharma
    Enrollment closed, Trial completion date, Trial primary completion date, Metastases:  First-in-human Study of Oral TP-0903 (a Novel Inhibitor of AXL Kinase) in Patients With Advanced Solid Tumors (clinicaltrials.gov) -  Jul 9, 2020   
    P1a,  N=177, Active, not recruiting, 
    These results reveal that AXL strongly contributes to the disease progression of glomerular nephritis. Recruiting --> Active, not recruiting | Trial completion date: Sep 2020 --> Dec 2020 | Trial primary completion date: Apr 2020 --> Dec 2020