- |||||||||| Lumakras (sotorasib) / Amgen
LUMAKRAS ! (Twitter) - May 28, 2021
- |||||||||| Lumakras (sotorasib) / Amgen
Trial primary completion date, Combination therapy, Monotherapy, Metastases: A Phase 1/2, Study Evaluating the Safety, Tolerability, PK, and Efficacy of Sotorasib (AMG 510) in Subjects With Solid Tumors With a Specific KRAS Mutation (CodeBreaK 100) (clinicaltrials.gov) - May 27, 2021 P1/2, N=733, Recruiting, Trial primary completion date: Jan 2023 --> Apr 2023
- |||||||||| 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
Enrollment change, Trial completion date, Trial primary completion date, Combination therapy, Monotherapy, Metastases: A Phase 1/2, Study Evaluating the Safety, Tolerability, PK, and Efficacy of Sotorasib (AMG 510) in Subjects With Solid Tumors With a Specific KRAS Mutation (CodeBreaK 100) (clinicaltrials.gov) - May 11, 2021 P1/2, N=733, Recruiting, KRAS testing should be considered in all CRC and NSCLC patients, independently of clinical or demographic characteristics. N=533 --> 733 | Trial completion date: Feb 2024 --> Feb 2025 | Trial primary completion date: Nov 2021 --> Jan 2023
- |||||||||| 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.
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[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
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