Lumakras (sotorasib) / Amgen 
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  • ||||||||||  Lumakras (sotorasib) / Amgen
    LUMAKRAS ! (Twitter) -  May 28, 2021   
  • ||||||||||  adagrasib (MRTX849) / Mirati, Lumakras (sotorasib) / Amgen
    Review, Journal, IO biomarker:  KRAS-Mutant Non-Small Cell Lung Cancer: An Emerging Promisingly Treatable Subgroup. (Pubmed Central) -  May 21, 2021   
    Simultaneously, within the immuno-therapeutic process, immune efficacy has been observed in those patients who have KRAS mutations. In this article, the pathogenesis, treatment status, progress of immunotherapy, and targeted therapy of KRAS-mutant NSCLC are reviewed.
  • ||||||||||  Lumakras (sotorasib) / Amgen
    Journal:  SMALL MOLECULE IMAGING AGENT FOR MUTANT KRAS G12C. (Pubmed Central) -  May 20, 2021   
    Herein, we synthesized and tested a series of fluorescent companion imaging drugs (CID) for KRAS G12C, using two scaffolds, ARS-1323 and AMG-510...We show that this approach can be used to image mutant KRAS G12C directly in cells. Given the current lack of mutant KRAS G12C specific antibodies, these reagents could be useful for specific fluorescence imaging.
  • ||||||||||  adagrasib (MRTX849) / Mirati, Lumakras (sotorasib) / Amgen
    Retrospective data, Journal:  Molecular profile of KRAS G12C-mutant colorectal and non-small-cell lung cancer. (Pubmed Central) -  May 11, 2021   
    KRAS G12C presents in frequencies higher than several other driver mutations, and may represent a large volume of patients in absolute numbers. KRAS testing should be considered in all CRC and NSCLC patients, independently of clinical or demographic characteristics.
  • ||||||||||  Lumakras (sotorasib) / Amgen
    Journal:  Design, synthesis and pharmacological evaluation of bicyclic and tetracyclic pyridopyrimidinone analogues as new KRAS inhibitors. (Pubmed Central) -  May 1, 2021   
    On the basis of the bicyclic pyridopyrimidinone framework of the first-in-class clinical KRAS inhibitor AMG510, a scaffold hopping strategy was conducted including a F-OH cyclization approach and a pyridinyl N-atom working approach leading to new tetracyclic and bicyclic analogues...Molecular docking suggested that the fluorophenol moiety of 26a occupies a hydrophobic pocket region thus forming hydrogen bonding to Arg68. These results will be useful to guide further structural modification.
  • ||||||||||  Lumakras (sotorasib) / Amgen
    [VIRTUAL] Characterization of KRAS mutation variants and prevalence of KRAS-G12C in gastrointestinal malignancies () -  Apr 26, 2021 - Abstract #ESMOGI2021ESMO_GI_63;    
    Background The KRAS G12C inhibitor sotorasib has shown promising anticancer activity in patients with advanced solid tumors harboring the KRAS G12C mutation, holding the potential for transforming clinical management of KRAS mutated solid tumors...G12C was most frequently observed in patients with appendiceal, colorectal, small bowel, biliary, and pancreatic cancers. G12C was not detected in SCC of the esophagus or anal canal.
  • ||||||||||  sotorasib (AMG 510) / Amgen
    Review, Journal, PD(L)-1 Biomarker, IO biomarker:  If Virchow and Ehrlich Had Dreamt Together: What the Future Holds for KRAS-Mutant Lung Cancer. (Pubmed Central) -  Apr 23, 2021   
    Better insights into KRAS structural biochemistry allowed researchers to develop direct KRAS(G12C) inhibitors, which have shown early signs of clinical activity in NSCLC patients and have recently led to an FDA breakthrough designation for AMG-510...This strategy is supported by preclinical models which show that KRAS(G12C) inhibitors can turn some immunologically "cold" tumors into "hot" ones and therefore could benefit patients whose tumors harbor subtype-defining STK11/LKB1 co-mutations. Forty years after the discovery of KRAS as a transforming oncogene, we are on the verge of approval of the first KRAS-targeted drug combinations, thus therapeutically unifying Paul Ehrlich's century-old "magic bullet" vision with Rudolf Virchow's cancer inflammation theory.
  • ||||||||||  zotatifin (eFT226) / eFFECTOR Therap
    Trial primary completion date:  Study of eFT226 in Subjects With Selected Advanced Solid Tumor Malignancies (clinicaltrials.gov) -  Apr 22, 2021   
    P1/2,  N=45, Recruiting, 
    Forty years after the discovery of KRAS as a transforming oncogene, we are on the verge of approval of the first KRAS-targeted drug combinations, thus therapeutically unifying Paul Ehrlich's century-old "magic bullet" vision with Rudolf Virchow's cancer inflammation theory. Trial primary completion date: Apr 2021 --> Oct 2021
  • ||||||||||  Lumakras (sotorasib) / Amgen
    Enrollment change, Metastases:  AMG 510 Ethnic Sensitivity Study (CodeBreaK 105). (clinicaltrials.gov) -  Apr 22, 2021   
    P1,  N=18, Recruiting, 
    Trial primary completion date: Apr 2021 --> Oct 2021 N=12 --> 18