Zelboraf (vemurafenib) / Roche 
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 50 Diseases   65 Trials   65 Trials   4287 News 


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  • ||||||||||  Mekinist (trametinib) / Novartis, Erbitux (cetuximab) / Eli Lilly, EMD Serono
    Journal:  Low‑dose trametinib and Bcl‑xL antagonist have a specific antitumor effect in KRAS‑mutated colorectal cancer cells. (Pubmed Central) -  Sep 15, 2021   
    A drug‑screening system (Mix Culture assay) was then applied, revealing that the cells were most sensitive to the MEK inhibitor trametinib among tested drugs, Cetuximab, Panitumumab, Regorafenib, Vemurafenib, BEZ‑235 and Palbociclib...These data suggest that a low dose of trametinib (10 nM), rather than the usual dose of 100 nM, in combination with ABT263 can overcome the resistance to apoptosis induced by Bcl‑xL expression, which occurs concurrently with p‑ERK suppression in KRAS‑mutant cells. This strategy may represent a promising new approach for treating KRAS‑mutant CRC.
  • ||||||||||  Rituxan (rituximab) / Biogen, Zenyaku Kogyo, Roche, Zelboraf (vemurafenib) / Roche
    Journal:  HCL - vemurafenib plus rituximab holds promise. (Pubmed Central) -  Sep 15, 2021   
    This strategy may represent a promising new approach for treating KRAS‑mutant CRC. No abstract available
  • ||||||||||  Zelboraf (vemurafenib) / Roche
    Journal:  The Downregulation of eIF3a Contributes to Vemurafenib Resistance in Melanoma by Activating ERK via PPP2R1B. (Pubmed Central) -  Sep 14, 2021   
    In addition, a positive correlation between eIF3a and PPP2R1B expression was also observed in tumor samples from the Human Protein Atlas and TCGA databases. In conclusion, our studies reveal a previously unknown molecular mechanism of BRAF inhibitor resistance, which may provide a new strategy for predicting vemurafenib responses in clinical treatment.
  • ||||||||||  Opdivo (nivolumab) / BMS, Braftovi (encorafenib) / Pfizer, Mektovi (binimetinib) / Pfizer
    Trial primary completion date:  Adaptive BRAF-MEK Inhibitor Therapy for Advanced BRAF Mutant Melanoma (clinicaltrials.gov) -  Sep 14, 2021   
    P1,  N=20, Recruiting, 
    In conclusion, our studies reveal a previously unknown molecular mechanism of BRAF inhibitor resistance, which may provide a new strategy for predicting vemurafenib responses in clinical treatment. Trial primary completion date: Sep 2021 --> Sep 2022
  • ||||||||||  Zelboraf (vemurafenib) / Roche
    Targeted BRAF Inhibitor Therapy Induces Remission of Unresectable Ampullary Adenocarcinoma (Shoreline Exhibit Hall) -  Sep 8, 2021 - Abstract #ACG2021ACG_2837;    
    He was placed on Vemurafenib, a selective inhibitor of BRAF and V 600 mutations...These mutations are the predominant type in metastatic melanoma for which this drug is used as monotherapy. This case demonstrates the successful treatment of unresectable ampullary adenocarcinoma with targeted chemotherapyFigure: Figure A
  • ||||||||||  Zelboraf (vemurafenib) / Roche
    Journal, PD(L)-1 Biomarker, IO biomarker:  Inhibition of BRAF Sensitizes Thyroid Carcinoma to Immunotherapy by Enhancing TsMHC-II-mediated Immune Recognition. (Pubmed Central) -  Sep 5, 2021   
    Our results suggest that BRAFV600E mutation in PTC impairs the expression of tsMHCII through the TGF-β1/SMAD3 pathway to enhance immune escape. Combined treatment with PLX4032 and anti-PD-1 antibody promotes recognition and elimination of PTC by the immune system in a pre-clinical mouse model, and therefore offers an effective therapeutic strategy for patients with advanced PTC.
  • ||||||||||  Opdivo (nivolumab) / Ono Pharma, BMS
    Clinical, Review, Journal, PD(L)-1 Biomarker, IO biomarker:  First line treatment of BRAF mutated advanced melanoma: Does one size fit all? (Pubmed Central) -  Aug 29, 2021   
    Several immune-checkpoint inhibitors, including pembrolizumab, nivolumab and the combination of nivolumab plus ipilimumab, are also available options for untreated metastatic melanoma patients...Specifically, the triplet of atezolizumab, vemurafenib and cobimetinib has been recently approved by FDA for patients with untreated BRAF-mutant metastatic melanoma...Results from ongoing studies are awaited, to maximise the benefits in survival outcomes and quality of life for patients, balancing adverse events and clinical benefit. The purpose of this review is to summarize the current landscape of standard and experimental treatment strategies for the first line treatment of patients with BRAF-mutated advanced melanoma and discuss the best patient-centered tailored strategies in the first-line setting.
  • ||||||||||  Opdivo (nivolumab) / Ono Pharma, BMS
    Review, Journal, PD(L)-1 Biomarker, IO biomarker:  Treatment of Advanced Metastatic Melanoma. (Pubmed Central) -  Aug 28, 2021   
    As for checkpoint inhibitors, first line immunotherapy is represented by anti-PD1 blockers (nivolumab and pembrolizumab), whilst the anti-CTLA-4 ipilimumab can be used as second line immunotherapy...This review will analyze the current therapeutic tools adopted for the treatment of metastatic melanoma patients. It will then focus on the latest results obtained by novel treatments (checkpoint inhibitors and targeted therapies) which can be used in the clinical daily practice.
  • ||||||||||  imatinib / Generic mfg.
    Journal:  Tyrosine kinase inhibitor therapy and metabolic re-modeling in papillary thyroid cancer. (Pubmed Central) -  Aug 27, 2021   
    In summary, imatinib led to a paradoxical increase of [18F]FDG uptake in xenografts that was reversed through BRAFV600E inhibition. Our data show that metabolic reprogramming in thyroid cancer occurs as a consequence of BRAF-mediated upregulation of HK2 expression that may permit tumour growth with isolated blockade of upstream tyrosine kinase receptors.
  • ||||||||||  Clinical, Retrospective data, Journal:  Sustained Tumor Control With MAPK Inhibition in BRAF V600-Mutant Adult Glial and Glioneuronal Tumors. (Pubmed Central) -  Aug 26, 2021   
    Our data show that metabolic reprogramming in thyroid cancer occurs as a consequence of BRAF-mediated upregulation of HK2 expression that may permit tumour growth with isolated blockade of upstream tyrosine kinase receptors. Our study highlights the clinical benefits of RAFi/MEKi in adult patients with BRAF-mutant GGNT, encourages the systematic screening and rechallenge in responders.
  • ||||||||||  Mekinist (trametinib) / Novartis, Tafinlar (dabrafenib) / Novartis, Zelboraf (vemurafenib) / Roche
    Clinical, Journal, Adverse events:  Ocular side effects of target therapy and immunotherapy in patients with cutaneous malignant melanoma. (Pubmed Central) -  Aug 21, 2021   
    This study highlights the frequency of ocular side effects in patients treated with target therapy and immunotherapy for CMM and shows that symptom resolution can be effectively achieved with proper ophthalmic care. Further research is required to answer whether cessation of these therapies is mandatory during ophthalmic treatment.
  • ||||||||||  cladribine / Generic mfg.
    Review, Journal:  Hairy Cell Leukaemia. (Pubmed Central) -  Aug 20, 2021   
    HCLv has a worse prognosis with median overall survival (OS), only 7-9 years, despite the combination of PNA/rituximab improving front-line response. Moxetumomab or ibrutinib may be a viable treatment but lacks substantial evidence.
  • ||||||||||  Erbitux (cetuximab) / Eli Lilly, Zelboraf (vemurafenib) / Roche
    Trial completion date, Trial primary completion date, Metastases:  Cetuximab and Vemurafenib Plus FOLFIRI for BRAF V600E Mutated Advanced Colorectal Cancer (IMPROVEMENT) (clinicaltrials.gov) -  Aug 19, 2021   
    P2,  N=30, Recruiting, 
    Moxetumomab or ibrutinib may be a viable treatment but lacks substantial evidence. Trial completion date: Dec 2020 --> Dec 2022 | Trial primary completion date: Dec 2020 --> Dec 2021
  • ||||||||||  LY3022855 / Eli Lilly
    Trial completion date, Trial primary completion date:  LY3022855 With BRAF/MEK Inhibition in Patients With Melanoma (clinicaltrials.gov) -  Aug 18, 2021   
    P1/2,  N=5, Active, not recruiting, 
    Trial primary completion date: Jan 2020 --> Oct 2020 Trial completion date: Dec 2022 --> Dec 2023 | Trial primary completion date: Jun 2021 --> Jun 2022
  • ||||||||||  Zelboraf (vemurafenib) / Roche, XL888 / Exelixis, Merck (MSD)
    Trial completion date:  Study of XL888 With Vemurafenib for Patients With Unresectable BRAF Mutated Stage III/IV Melanoma (clinicaltrials.gov) -  Aug 18, 2021   
    P1,  N=21, Active, not recruiting, 
    Trial completion date: Dec 2022 --> Dec 2023 | Trial primary completion date: Jun 2021 --> Jun 2022 Trial completion date: Jul 2021 --> Jul 2022
  • ||||||||||  Zelboraf (vemurafenib) / Roche
    Discovery and development of a MKK-4 inhibitors to increase liver regeneration (Room: Thomas Murphy Ballroom Sections 3 & 4) -  Aug 13, 2021 - Abstract #ACSFall2021ACS_Fall_6438;    
    Further to the observation that the approved BRAFV600E inhibitor vemurafenib shows a high affinity to and moderate functional inhibition potency against MKK4, our hit optimization concept included classical iterative SAR-optimization but also a scaffold-hopping approach by changing the core heterocycle from 1H-pyrrolo[2,3-b]pyridine to 1H-pyrazolo[2,3-b]pyridine...Furthermore, LN3118 demonstrated therapeutic activity in two subchronic animal models. LN3118 reduced alcohol-inducedsteatosis and significantly reversed CCl4-induced liver fibrosis.The latest generation of compounds included highly potent MKK4-inhibitors with a pharmacological,toxicological and pharmacokinetic profile, which meet the specification of a clinical development candidate.
  • ||||||||||  Zelboraf (vemurafenib) / Roche
    Journal:  Design and synthesis of 1H-pyrazolo[3,4-b]pyridines targeting mitogen-activated protein kinase kinase 4 (MKK4) - A promising target for liver regeneration. (Pubmed Central) -  Aug 8, 2021   
    Starting from the approved BRAF inhibitor vemurafenib (8), that showed a high off-target affinity to MKK4 in an initial screening, we followed a scaffold-hopping approach, changing the core heterocycle from 1H-pyrrolo[2,3-b]pyridine to 1H-pyrazolo[2,3-b]pyridine (10)...Further modifications led to 58 and 59 showing high affinity to MKK4 in the low nanomolar range and excellent selectivity profile from mandatory multiparameter-optimization for the essential anti-targets (MKK7, JNK1) and off-targets (BRAF, MAP4K5, ZAK) in the MKK4 pathway. Herein we report the first selective MKK4 inhibitors in this class.
  • ||||||||||  Zelboraf (vemurafenib) / Roche
    Journal:  BRAF and NRAS mutated melanoma: Different Ca responses, Na/Ca exchanger expression, and sensitivity to inhibitors. (Pubmed Central) -  Aug 7, 2021   
    These cells also presented a smaller response to thapsargin and ionomycin regarding the cytosolic Ca levels in relation to SK-MEL-19, which was associated to an increased expression of NCX1, NO basal levels, and sensitivity to NCX inhibitors. These data highlight the differences between B-RAF and NRAS-mutated melanoma cells in response to Ca stimuli and point to the potential combination of clinically used chemotherapeutic drugs, including vemurafenib, with NCX inhibitors as a new therapeutic strategy to the treatment of melanoma.
  • ||||||||||  Opdivo (nivolumab) / Ono Pharma, BMS
    Journal, PD(L)-1 Biomarker, IO biomarker:  Triplet combination of BRAF, MEK and PD-1/PD-L1 blockade in melanoma: the more the better? (Pubmed Central) -  Aug 7, 2021   
    Efficacy can also be increased by combining ICIs with the aim of maintaining a longer response. The possibility to administer three drugs in combination, would allow to induce tumour regression and produce an immune response with a synergistic effect.
  • ||||||||||  Zelboraf (vemurafenib) / Roche
    Journal:  Silencing of CEBPB-AS1 modulates CEBPB expression and resensitizes BRAF-inhibitor resistant melanoma cells to vemurafenib. (Pubmed Central) -  Jul 30, 2021   
    We demonstrated that silencing of CEBPB-AS1 resulted in epigenetic modifications in the CEBPB promoter and in increased CEBPB mRNA and protein levels, inhibited proliferation and partially resensitized BRAF-inhibitor resistant CMM cells to this drug-induced apoptosis. Our data suggest that targeting CEBPB-AS1 may represent a valuable tool to sensitize CMM cells to the BRAF-inhibitor-based therapies.
  • ||||||||||  hydroquinone / Generic mfg.
    Journal:  Molecular insights into the Patched1 drug efflux inhibitory activity of panicein A hydroquinone: a computational study. (Pubmed Central) -  Jul 28, 2021   
    Finally, a blind ensemble docking methodology coupled with the conformational analysis of compounds enabled rationalization of the interaction between PTCH1 and PAH and derivatives in terms of their intrinsic physico-chemical properties. Our results suggest that the Neck pocket is the preferential binding site for PAH analogues on PTCH1, and that compounds assuming an open cylindric-like shape in solution are most likely to be good binders for PTCH1.