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Published in 2024 at "Clinical Pharmacology in Drug Development"
DOI: 10.1002/cpdd.1452
Abstract: Sotorasib is a small molecule drug that specifically and irreversibly inhibits the KRAS p.G12C mutant protein. This analysis investigated the impact of a high‐calorie high‐fat meal on the pharmacokinetics, safety, and tolerability of sotorasib in…
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Keywords:
meal pharmacokinetics;
impact high;
fat meal;
kras g12c ... See more keywords
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Published in 2025 at "Molecular Carcinogenesis"
DOI: 10.1002/mc.23908
Abstract: KRAS is the most frequently mutated oncogene. In epithelial malignancies such as lung, colorectal, and pancreatic tumors, KRAS is mutated in 25 to above 90% cases. KRAS was considered undruggable for over three decades until…
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Keywords:
resistance;
kras targeted;
resistance kras;
response ... See more keywords
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Published in 2024 at "Targeted Oncology"
DOI: 10.1007/s11523-024-01055-y
Abstract: Kristen Rat Sarcoma viral oncogene (KRAS) mutations are one of the most common oncogenic drivers found in 12–14% of non-small cell lung cancer (NSCLC) and 4% of colorectal cancer tumors. Although previously difficult to target,…
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Keywords:
divarasib evolving;
kras g12c;
evolving landscape;
landscape kras ... See more keywords
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Published in 2025 at "Advances in Therapy"
DOI: 10.1007/s12325-025-03259-8
Abstract: Sotorasib and adagrasib are the only treatments approved in the USA and Europe for advanced/metastatic KRAS G12C-mutated non-small cell lung cancer (NSCLC). In the absence of head-to-head trials, a matching-adjusted indirect comparison (MAIC) was conducted…
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Keywords:
non small;
cancer;
cell lung;
sotorasib ... See more keywords
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Published in 2020 at "Cell"
DOI: 10.1016/j.cell.2020.09.044
Abstract: KRAS mutations are among the most common genetic alterations in lung, colorectal, and pancreatic cancers. Direct inhibition of KRAS oncoproteins has been a long-standing pursuit in precision oncology, one established shortly after the discovery of…
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Keywords:
inhibitory mechanism;
g12c inhibitory;
targeting kras;
mechanism modulation ... See more keywords
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Published in 2021 at "ESMO Open"
DOI: 10.1016/j.esmoop.2021.100279
Abstract: Background KRAS is mutated in ∼30% of non-small-cell lung cancer (NSCLC) but it has also been identified as one of the mechanisms underlying resistance to tyrosine kinase inhibitors (TKIs) in EGFR-positive NSCLC patients. Novel KRAS…
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Keywords:
nsclc;
first line;
g12c mutation;
kras g12c ... See more keywords
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Published in 2023 at "Analytical chemistry"
DOI: 10.1021/acs.analchem.2c04417
Abstract: The growing opportunities recognized for covalent drug inhibitors, like KRAS G12C inhibitors, are driving the need for mass spectrometry methods that can quickly and robustly measure therapeutic drug activity in vivo for drug discovery research…
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Keywords:
mass spectrometry;
kras g12c;
drug;
activity ... See more keywords
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Published in 2025 at "Analytical chemistry"
DOI: 10.1021/acs.analchem.5c02696
Abstract: Understanding the target engagement of covalent inhibitors, such as KRAS G12C inhibitors, is essential for evaluating their mechanisms of action and efficacy, particularly given the KRAS G12C mutation's significant role in cancer progression. We previously…
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Keywords:
formalin fixed;
kras g12c;
fixed paraffin;
target engagement ... See more keywords
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Published in 2019 at "Nature Reviews Clinical Oncology"
DOI: 10.1038/s41571-019-0304-3
Abstract: Nature reviews | CliniCal OnCOlOgy Attempts to therapeutically target the products of the RAS oncogenes, frequently mutated in cancer, have had disappointing results thus far. The small molecules MRTX849 and AMG 510, from two independent…
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Keywords:
kras g12c;
treatment;
amg 510;
oncology ... See more keywords
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Published in 2025 at "Journal of chemotherapy"
DOI: 10.1080/1120009x.2025.2503052
Abstract: Mutations in the KRAS gene are the most common gain-of-function mutations found in lung adenocarcinomas. The most prevalent mutation, KRAS G12C, occurs in 13% of lung adenocarcinomas. Sotorasib is an irreversible small molecule inhibitor that…
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Keywords:
combination therapy;
lung;
sotorasib;
kras g12c ... See more keywords
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Published in 2023 at "Expert Opinion on Investigational Drugs"
DOI: 10.1080/13543784.2023.2178419
Abstract: ABSTRACT Introduction KRAS G12C targeted covalent inhibitors for cancer therapy are revolutionary. However, resistance to KRAS G12C inhibitors in clinical trials is a proven fact. Areas covered The authors focus on providing coverage and emphasizing…
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Keywords:
kras g12c;
inhibitor resistance;
therapy;
resistance ... See more keywords