Lumakras (sotorasib) / Amgen 
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  • ||||||||||  adagrasib (MRTX849) / Mirati, Lumakras (sotorasib) / Amgen
    Review, Journal, IO biomarker:  Molecular Biology and Therapeutic Perspectives for K-Ras Mutant Non-Small Cell Lung Cancers. (Pubmed Central) -  Sep 13, 2022   
    From the description of the biology of KRAS-mutant NSCLC, the present review will focus on the clinical aspects of KRAS mutations in NSCLC, in particular on the emerging efficacy data of Sotorasib and other KRAS inhibitors, including mechanisms of resistance. Finally, the interaction between KRAS mutations and immune checkpoint inhibitors will be discussed.
  • ||||||||||  Lumakras (sotorasib) / Amgen
    SOTORASIB-CAUSING PNEUMONITIS (Convention Center Exhibit Hall: Poster Area) -  Sep 11, 2022 - Abstract #CHEST2022CHEST_3989;    
    CASE PRESENTATION: A 56-year-old male with non small cell lung cancer with spinal metastasis on sotorasib changed from pemetrexed, carboplatin, and pembrolizumab a week before presented with shortness of breath and cough for 2 days. Drug-induced pneumonitis should always be the differential in patients presenting with respiratory distress and radiographic changes.
  • ||||||||||  Lumakras (sotorasib) / Amgen
    Journal:  KSR induces RAS-independent MAPK pathway activation and modulates the efficacy of KRAS inhibitors. (Pubmed Central) -  Sep 10, 2022   
    Mutations in the conserved DFG motif of KSR1 that affect ATP binding impair induction of cell proliferation. We also show that increased expression levels of KSR1 decrease the responsiveness to the KRAS inhibitor sotorasib in human cancer cell lines, thus suggesting that increased levels of expression of KSR may make tumor cells less dependent on KRAS oncogenic signaling.
  • ||||||||||  Lumakras (sotorasib) / Amgen
    Journal:  Strategies of targeting KRAS, challenging drug target. (Pubmed Central) -  Sep 10, 2022   
    The FDA has recently approved sotorasib for the treatement of KRASG12C-mutated advanced non-small cell lung cancer (NSCLC) patients...The structure and function of new insights in RAS have changed this understanding and encouraged the development of many drug candidates. This review provides information about the different strategies of targeting KRAS, a challenging drug target that might be valuable for the scientific community.
  • ||||||||||  Lumakras (sotorasib) / Amgen
    Journal:  Oncogenic KRAS G12C: Kinetic and Redox Characterization of Covalent Inhibition. (Pubmed Central) -  Sep 10, 2022   
    Using a validated fluorescent KRAS variant amenable to stopped-flow spectroscopy, we characterized the kinetics of KRAS fluorescence changes upon addition of ARS-853 or AMG 510, noting that at low temperatures, ARS-853 addition elicited both a rapid first phase of fluorescence change (attributed to binding, K = 36.0 ± 0.7 μM) and a second, slower pH-dependent phase, taken to represent covalent ligation...Moreover, we found that oxidation of the KRAS Cys12 to a sulfinate altered RAS conformation and dynamics to be more similar to KRAS in comparison to the unmodified protein, as assessed by molecular dynamics simulations. Taken together, these findings provide insight for future KRAS drug discovery efforts, as well as identifying the occurrence of G12C oxidation with currently unknown biological ramifications.
  • ||||||||||  Lumakras (sotorasib) / Amgen
    Journal:  KRAS G12C inhibition with sotorasib in metastatic colorectal cancer. (Pubmed Central) -  Sep 10, 2022   
    Taken together, these findings provide insight for future KRAS drug discovery efforts, as well as identifying the occurrence of G12C oxidation with currently unknown biological ramifications. No abstract available
  • ||||||||||  Lumakras (sotorasib) / Amgen
    Microscopic Colitis Induced by KRAS Targeted Therapy, Sotorasib (Crown Ballroom) -  Sep 4, 2022 - Abstract #ACG2022ACG_2228;    
    This is the first case report in the literature, up to our knowledge, that shows an association between microscopic colitis and Sotorasib. Understanding the underlying pathophysiology of diarrhea as a limiting side effect of Sotorasib may help the patients to tolerate such medication.