ABCB1 limits brain exposure of the KRASG12C inhibitor sotorasib, whereas ABCB1, CYP3A, and possibly OATP1a/1b restrict its oral availability

Mercapturate pathway metabolites of sotorasib, a covalent inhibitor of KRASG12C, are associated with renal toxicity in the Sprague Dawley rat

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Quantification of KRAS inhibitor sotorasib in mouse plasma and tissue homogenates using liquid chromatography-tandem mass spectrometry

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On target: Rational approaches to KRAS inhibition for treatment of non-small cell lung carcinoma

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Quantitative Proteomics of Clinically Relevant Drug-Metabolizing Enzymes and Drug Transporters and Their Inter-correlations in the Human Small Intestine

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Rapid non-uniform adaptation to conformation-specific KRAS(G12C) inhibition

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The impact of ABCB1 gene polymorphism and its expression on non-small-cell lung cancer development, progression and therapy – preliminary report

(2020) Izabela Zawadzka et al.   Scientific Reports

KRASG12C Inhibition with Sotorasib in Advanced Solid Tumors

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Validated HPLC‐MS/MS method for quantitation of AMG 510, a KRAS G12C inhibitor, in mouse plasma and its application to a pharmacokinetic study in mice

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Vertical pathway inhibition overcomes adaptive feedback resistance to KRASG12C inhibition

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The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity

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Protein Expression and Functional Relevance of Efflux and Uptake Drug Transporters at the Blood–Brain Barrier of Human Brain and Glioblastoma

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Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors

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Differential Regulation of CYP3A4 and CYP3A5 and its Implication in Drug Discovery

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Relevance of breast cancer resistance protein to brain distribution and central acting drugs: a pharmacokinetic perspective

(2018) Joana Goncalves et al.   CURRENT DRUG METABOLISM

P-glycoprotein and Breast Cancer Resistance Protein restrict brigatinib brain accumulation and toxicity, and, alongside CYP3A, limit its oral availability

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Therapeutic Potential and Utility of Elacridar with Respect to P-glycoprotein Inhibition: An Insight from the Published In Vitro, Preclinical and Clinical Studies

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The mutational spectrum of HRAS, KRAS, NRAS and FGFR3 genes in bladder cancer

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The potential utility of re-mining results of somatic mutation testing: KRAS status in lung adenocarcinoma

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Drugging the undruggable RAS: Mission Possible?

(2014) Adrienne D. Cox et al.   NATURE REVIEWS DRUG DISCOVERY

Cytochrome P450 enzymes in drug metabolism: Regulation of gene expression, enzyme activities, and impact of genetic variation

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A Comprehensive Survey of Ras Mutations in Cancer

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A comprehensive study of polymorphisms inABCB1, ABCC2andABCG2and lung cancer chemotherapy response and prognosis

(2012) Daniele Campa et al.   INTERNATIONAL JOURNAL OF CANCER

Double-Transduced MDCKII Cells To Study Human P-Glycoprotein (ABCB1) and Breast Cancer Resistance Protein (ABCG2) Interplay in Drug Transport across the Blood−Brain Barrier

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Membrane transporters in drug development

(2010)   NATURE REVIEWS DRUG DISCOVERY

Impact of OATP transporters on pharmacokinetics

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A Gene Expression Signature Associated with “K-Ras Addiction” Reveals Regulators of EMT and Tumor Cell Survival

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Importance of knowledge on drug metabolism for the safe use of drugs in humans

(2009) Franz Oesch   DRUG METABOLISM REVIEWS

Frequency and type of KRAS mutations in routine diagnostic analysis of metastatic colorectal cancer

(2009) Jens Neumann et al.   PATHOLOGY RESEARCH AND PRACTICE

The role of ABC transporters in drug absorption, distribution, metabolism, excretion and toxicity (ADME–Tox)

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