Nonclinical Safety Profile of Sotorasib, a KRASG12C-Specific Covalent Inhibitor for the Treatment of KRAS p.G12C-Mutated Cancer

MO01.30 Trial in Progress: A Phase 1b Study of Sotorasib, a KRAS (G12C) Inhibitor, in Combination with other Anticancer Therapies in Patients with Advanced Solid Tumors Harboring KRAS p.G12C Mutation (CodeBreaK101)

(2021) M. Fakih et al.   Journal of Thoracic Oncology

MO01.32 CodeBreaK 200: A Phase 3 Multicenter Study of Sotorasib, a KRAS(G12C) Inhibitor, versus Docetaxel in Patients with Previously Treated Advanced Non-Small Cell Lung Cancer (NSCLC) Harboring KRAS p.G12C Mutation

(2021) M. Reck et al.   Journal of Thoracic Oncology

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

(2021) Jonathan A. Werner et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

Small molecules, big impact: 20 years of targeted therapy in oncology

(2020) Philippe L Bedard et al.   LANCET

Review of embryo-fetal developmental toxicity studies performed for pharmaceuticals approved by FDA in 2018 and 2019

(2020) Paul Barrow et al.   REPRODUCTIVE TOXICOLOGY

KRASG12C Inhibition with Sotorasib in Advanced Solid Tumors

(2020) David S. Hong et al.   NEW ENGLAND JOURNAL OF MEDICINE

Covalent Inhibition in Drug Discovery

(2019) Avick Kumar Ghosh et al.   ChemMedChem

Tyrosine kinase inhibitors and immune checkpoint inhibitors-induced thyroid disorders

(2019) Arnaud Jannin et al.   CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

Discovery of N-(1-Acryloylazetidin-3-yl)-2-(1H-indol-1-yl)acetamides as Covalent Inhibitors of KRASG12C

(2019) Youngsook Shin et al.   ACS Medicinal Chemistry Letters

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

(2019) Jude Canon et al.   NATURE

Cardiovascular Toxicity Induced by Kinase Inhibitors: Mechanisms and Preclinical Approaches

(2019) Sarah D. Lamore et al.   CHEMICAL RESEARCH IN TOXICOLOGY

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

(2019) Brian A. Lanman et al.   JOURNAL OF MEDICINAL CHEMISTRY

KRAS oncogene in non-small cell lung cancer: clinical perspectives on the treatment of an old target

(2018) Marta Román et al.   Molecular Cancer

TargetingBRAF‐Mutant Non‐Small Cell Lung Cancer: From Molecular Profiling to Rationally Designed Therapy

(2017) Christina S. Baik et al.   ONCOLOGIST

Effect of maternal feed restriction on prenatal development in rats and rabbits – A review of published data

(2017) Dana Nitzsche   REGULATORY TOXICOLOGY AND PHARMACOLOGY

Deconvoluting Kinase Inhibitor Induced Cardiotoxicity

(2017) Sarah D. Lamore et al.   TOXICOLOGICAL SCIENCES

AACR Project GENIE: Powering Precision Medicine through an International Consortium

(2017)   Cancer Discovery

Mechanistic Systems Modeling to Improve Understanding and Prediction of Cardiotoxicity Caused by Targeted Cancer Therapeutics

(2017) Jaehee V. Shim et al.   Frontiers in Physiology

Off-Target Effects of BCR-ABL and JAK2 Inhibitors

(2016) Myke R. Green et al.   AMERICAN JOURNAL OF CLINICAL ONCOLOGY-CANCER CLINICAL TRIALS

Nonclinical Evaluations of Small-Molecule Oncology Drugs: Integration into Clinical Dose Optimization and Toxicity Management

(2016) D. M. Dambach et al.   CLINICAL CANCER RESEARCH

Cardio-Oncology

(2015) Andrew M. Bellinger et al.   CIRCULATION

Mechanistic Investigation of Bone Marrow Suppression Associated with Palbociclib and its Differentiation from Cytotoxic Chemotherapies

(2015) W. Hu et al.   CLINICAL CANCER RESEARCH

Understanding Toxicities of Targeted Agents: Implications for Anti-tumor Activity and Management

(2015) Sariah Liu et al.   SEMINARS IN ONCOLOGY

Toxicity of targeted therapy: Implications for response and impact of genetic polymorphisms

(2014) Sariah Liu et al.   CANCER TREATMENT REVIEWS

Understanding, recognizing, and managing toxicities of targeted anticancer therapies

(2013) Grace K. Dy et al.   CA-A CANCER JOURNAL FOR CLINICIANS

Efficacy and Safety of Lersivirine (UK-453,061) Versus Efavirenz in Antiretroviral Treatment–Naive HIV-1–Infected Patients

(2013) Pietro Vernazza et al.   JAIDS-JOURNAL OF ACQUIRED IMMUNE DEFICIENCY SYNDROMES

Effectiveness of CASE Ultra Expert System in Evaluating Adverse Effects of Drugs

(2013) Roustem Saiakhov et al.   Molecular Informatics

K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions

(2013) Jonathan M. Ostrem et al.   NATURE

Effects of Lersivirine on Canine and Rodent Thyroid Function

(2013) Christopher D. Houle et al.   TOXICOLOGIC PATHOLOGY

Optimizing Predictive Performance of CASE Ultra Expert System Models Using the Applicability Domains of Individual Toxicity Alerts

(2012) Suman K. Chakravarti et al.   Journal of Chemical Information and Modeling

Characterization of Xenobiotic-Induced Hepatocellular Enzyme Induction in Rats

(2011) Tanja S. Zabka et al.   TOXICOLOGIC PATHOLOGY

ILSI/HESI maternal toxicity workshop summary: maternal toxicity and its impact on study design and data interpretation

(2010) Bruce K. Beyer et al.   BIRTH DEFECTS RESEARCH PART B-DEVELOPMENTAL AND REPRODUCTIVE TOXICOLOGY

Predictive Toxicology Approaches for Small Molecule Oncology Drugs

(2010) T. Maziasz et al.   TOXICOLOGIC PATHOLOGY

Effects of Hepatic Drug-metabolizing Enzyme Induction on Clinical Pathology Parameters in Animals and Man

(2010) Daniela Ennulat et al.   TOXICOLOGIC PATHOLOGY

Disruption of thyroid hormone homeostasis in Ugt1a-deficient Gunn rats by microsomal enzyme inducers is not due to enhanced thyroxine glucuronidation☆

(2010) Terrilyn A. Richardson et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

Cardiotoxicity induced by tyrosine kinase inhibitors

(2009) George S. Orphanos et al.   ACTA ONCOLOGICA

Gall bladder mucoceles and their association with endocrinopathies in dogs: a retrospective case-control study

(2009) M. L. L. Mesich et al.   JOURNAL OF SMALL ANIMAL PRACTICE

SnapShot: Ras Signaling

(2008) Megan Cully et al.   CELL

A quantitative analysis of kinase inhibitor selectivity

(2008) Mazen W Karaman et al.   NATURE BIOTECHNOLOGY

Ras oncogenes: split personalities

(2008) Antoine E. Karnoub et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

The relationship of maternal and fetal toxicity in developmental toxicology bioassays with notes on the biological significance of the “no observed adverse effect level”

(2008) N. Chernoff et al.   REPRODUCTIVE TOXICOLOGY