ulixertinib (BVD-523) / BioMed Valley Discoveries 
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  • ||||||||||  ipatasertib (GDC-0068) / Roche
    PK/PD data, Journal:  Pharmacokinetics and bioavailability of ipatasertib in dog plasma by LC/MS/MS. (Pubmed Central) -  Apr 27, 2021   
    The validated assay was further successfully employed to a pharmacokinetic study of ipatasertib after oral and intravenous treatments to dogs. The bioavailability of ipatasertib was determined to be 19.3%.
  • ||||||||||  Ibrance (palbociclib) / Pfizer, ulixertinib (BVD-523) / BioMed Valley Discoveries
    Enrollment change, Combination therapy, Metastases:  Ulixertinib/Palbociclib in Patients With Advanced Pancreatic and Other Solid Tumors (clinicaltrials.gov) -  Apr 14, 2021   
    P1,  N=45, Recruiting, 
    The bioavailability of ipatasertib was determined to be 19.3%. N=30 --> 45
  • ||||||||||  Gilotrif (afatinib) / Boehringer Ingelheim, ulixertinib (BVD-523) / BioMed Valley Discoveries
    [VIRTUAL] Pancreatic cancer musters HER2 signaling through DUSP6 to circumvent therapeutic MAPK inhibition () -  Mar 11, 2021 - Abstract #AACR2021AACR_3690;    
    Combined ERK inhibitor (ulixertinib) and bortezomib was able to prevent DUSP4 and DUSP6 downregulation in vitro but was ineffective in curbing in vivo tumor growth. Our study provided novel mechanisic insight on how PDAC cells evade MAPK inhibition via mustering HER2 signaling, as well as rational therapeutic combinations that can be readily tested in clinical trials.Keys: DUSP6, HER2, KRAS, pancreatic ductal adenocarcinoma, therapeutic resistance
  • ||||||||||  ulixertinib (BVD-523) / BioMed Valley Discoveries, SCH772984 / Otsuka
    [VIRTUAL] EMT and CSC Enrichment Induced by ERK Inhibition in NSCLC () -  Mar 11, 2021 - Abstract #AACR2021AACR_3581;    
    Moreover, in NSCLC cells, we proved ERK knockdown or ERKi treatment can reduce C/EBPα expression, which is believed to be a master epithelial “gatekeeper” whose expression is required to prevent unwarranted mesenchymal transition. Our findings reveal a novel mechanism underlying the tumor relapse after ERKi treatment in NSCLC, and ultimately will help us improve current NSCLC therapeutic methods.
  • ||||||||||  Journal, Combination therapy:  NRAS status determines sensitivity to SHP2 inhibitor combination therapies targeting the RAS-MAPK pathway in neuroblastoma. (Pubmed Central) -  Dec 30, 2020   
    Combinations of SHP2 inhibitors with other RAS pathway inhibitors such as trametinib, vemurafenib, and ulixertinib were synergistic and reversed resistance to SHP2 inhibition in NB in vitro and in vivo. These results suggest for the first time that combination therapies targeting SHP2 and other components of the RAS-MAPK pathway may be effective against conventional therapy-resistant relapsed NB, including those that have acquired NRAS mutations.
  • ||||||||||  ulixertinib (BVD-523) / BioMed Valley Discoveries
    Trial primary completion date, Metastases:  A Phase II Study of BVD-523 in Metastatic Uveal Melanoma (clinicaltrials.gov) -  Jun 16, 2020   
    P2,  N=13, Active, not recruiting, 
    These data highlight the MAPK pathway as a therapeutic target in DIPG, and show the importance of parallel resistance modelling and rational combinatorial treatments likely to be required for meaningful clinical translation. Trial primary completion date: Aug 2021 --> May 2020
  • ||||||||||  ulixertinib (BVD-523) / BioMed Valley Discoveries
    Trial completion date, Trial termination, Metastases:  BVD-523 Plus Nab-paclitaxel and Gemcitabine in Patients With Metastatic Pancreatic Cancer (clinicaltrials.gov) -  Jun 4, 2020   
    P1,  N=18, Terminated, 
    Trial primary completion date: Aug 2021 --> May 2020 Trial completion date: Mar 2021 --> May 2020 | Active, not recruiting --> Terminated; Adverse events
  • ||||||||||  Temporal inhibition of ERK is sufficient for tumor growth inhibition in KRAS-mutant or BRAF-mutant tumors (Virtual Meeting II: E-Posters) -  May 16, 2020 - Abstract #AACRII2020AACR-II_3326;    
    The combination of BRAF and MEK inhibitors have been clinically studied, and three different combinations (dabrafenib plus trametinib, vemurafenib plus cobimetinib and encorafenib plus binimetinib) are approved by the FDA for treatment of melanoma patients with BRAF V600E mutation...We have tested the PK-PD-efficacy of MEK inhibitors trametinib and cobimetinib, as well as ERK inhibitors BVD-523, GDC-0994 and LY3214996 in BRAF V600E or KRAS mutant xenograft models including A375 BRAF V600E melanoma, Colo205 BRAF V600E colorectal carcinoma and HCT116 KRAS G13D colorectal carcinoma...LY3214996 is in Phase 1 clinical development and the preliminary PK profile in patients looks as predicted from preclinical data. Therefore, we believe that the PK profile of LY3214996 offers flexibility with dose and schedule to balance efficacy and safety, and to achieve a better therapeutic index in combination therapy for RAS/MAPK pathway altered cancers.
  • ||||||||||  ulixertinib (BVD-523) / BioMed Valley Discoveries
    Enrollment open, Metastases:  UTAH: Ulixertinib (BVD-523) and Hydroxychloroquine in Patients W Advanced MAPK-Mutated Gastrointestinal Adenocarcinomas (clinicaltrials.gov) -  Apr 7, 2020   
    P1,  N=12, Recruiting, 
    In conclusion, although larger series of patients are needed to corroborate these findings, our results suggest that RAS-BRAF-MAPK-ERK pathway is one of the core cellular processes affected by novel mutations in chronic lymphocytic leukemia, it is associated with adverse clinical features and it could be pharmacologically inhibited. Active, not recruiting --> Recruiting
  • ||||||||||  ulixertinib (BVD-523) / BioMed Valley Discoveries
    BVD-523 (ERK1/2) (STARLIGHT BALLROOM) -  Feb 21, 2020 - Abstract #IASLCLCTT2020IASLC_LCTT_150;    
  • ||||||||||  Review, Journal:  Targeting ERK1/2 protein-serine/threonine kinases in human cancers. (Pubmed Central) -  Feb 16, 2020   
    The best treatments include the combination of B-Raf and MEK inhibitors (dabrafenib and trametinib, encorafenib and binimetinib, vemurafenib and cobimetanib)...Ulixertinib, MK-8353, and GDC-0994 are orally effective, potent, and specific inhibitors of ERK1/2 that are in early clinical trials for the treatment of various advanced/metastatic solid tumors...The decrease in RSK phosphorylation appears to be a result of ERK inhibition and the decrease in ERK1/2 phosphorylation is related to the inability of MEK to catalyze the phosphorylation of the ERK-MK-8353 complex; these decreases characterize the ERK dual mechanism inhibition paradigm. Additional work will be required to determine whether ERK inhibitors will be successful in the clinic and are able to forestall the development of drug resistance of the MAP kinase pathway.
  • ||||||||||  ulixertinib (BVD-523) / BioMed Valley Discoveries
    Enrollment closed, Trial completion date, Trial primary completion date, Metastases:  BVD-523 Plus Nab-paclitaxel and Gemcitabine in Patients With Metastatic Pancreatic Cancer (clinicaltrials.gov) -  Sep 23, 2019   
    P1,  N=25, Active, not recruiting, 
    Suspended --> Recruiting Suspended --> Active, not recruiting | Trial completion date: May 2022 --> Mar 2021 | Trial primary completion date: Aug 2019 --> Mar 2019
  • ||||||||||  ulixertinib (BVD-523) / BioMed Valley Discoveries
    Journal:  Ulixertinib (BVD-523) antagonizes ABCB1- and ABCG2-mediated chemotherapeutic drug resistance. (Pubmed Central) -  Jun 5, 2019   
    Mechanistic investigations revealed that ulixertinib stimulated the ATPase activity of both ABCB1 and ABCG2 in a concentration-dependent manner, and the in silico docking study predicted that ulixertinib could interact with the substrate-binding sites of both ABCB1 and ABCG2. Our finding provides a clue into a novel treatment strategy: a combination of ulixertinib with anticancer drugs to attenuate MDR mediated by ABCB1 or ABCG2 in cancer cells overexpressing these transporters.
  • ||||||||||  ulixertinib (BVD-523) / BioMed Valley Discoveries
    Enrollment closed, Enrollment change, Metastases:  A Phase II Study of BVD-523 in Metastatic Uveal Melanoma (clinicaltrials.gov) -  Apr 29, 2019   
    P2,  N=13, Active, not recruiting, 
    Our finding provides a clue into a novel treatment strategy: a combination of ulixertinib with anticancer drugs to attenuate MDR mediated by ABCB1 or ABCG2 in cancer cells overexpressing these transporters. N=25 --> 13 | Recruiting --> Active, not recruiting
  • ||||||||||  ulixertinib (BVD-523) / BioMed Valley Discoveries
    Trial completion date, Trial primary completion date, Metastases:  BVD-523 Plus Nab-paclitaxel and Gemcitabine in Patients With Metastatic Pancreatic Cancer (clinicaltrials.gov) -  Nov 6, 2018   
    P1,  N=25, Recruiting, 
    N=25 --> 13 | Recruiting --> Active, not recruiting Trial completion date: Dec 2021 --> May 2022 | Trial primary completion date: Dec 2018 --> May 2019
  • ||||||||||  ulixertinib (BVD-523) / BioMed Valley Discoveries
    Enrollment open, Metastases:  A Phase II Study of BVD-523 in Metastatic Uveal Melanoma (clinicaltrials.gov) -  Apr 2, 2018   
    P2,  N=25, Recruiting, 
    Trial completion date: Dec 2021 --> Sep 2027 | Trial primary completion date: Dec 2021 --> Sep 2027 Not yet recruiting --> Recruiting