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Intro; Preface; Contents; 1 Erlotinib; Abstract; 1 Introduction; 2 Mechanism of Action; 3 Non-small Cell Lung Cancer; 4 Pancreatic Adenocarcinoma; 5 Hepatocellular Carcinoma; 6 Other Tumour Entities; References; 2 Lapatinib; Abstract; 1 Introduction; 1.1 The Epidermal Growth Factor Receptor Family of Tyrosine Kinases; 1.2 Human Epidermal Growth Factor Receptors and Their Inhibition in Cancer; 2 Structure and Mechanism of Action; 3 Clinical Application; 3.1 Pharmacology; 4 Results from Clinical Trials; 4.1 Efficacy in Breast Cancer
4.1.1 Second-Line Treatment and Beyond in Advanced Breast Cancer4.1.2 First-Line Treatment in Advanced Breast Cancer; 4.1.3 Neoadjuvant Treatment in Early Breast Cancer; 4.1.4 Adjuvant Treatment in Early Breast Cancer; 4.2 Efficacy in Gastrointestinal Cancer; 4.3 Tolerability; 5 Biomarkers; 6 Conclusion and Future Perspectives; References; 3 Regorafenib; Abstract; 1 Structure, Mechanism of Action, and Pharmacokinetics; 1.1 Mechanism of Action; 1.2 Pharmacokinetics and Elimination; 1.3 Regorafenib in Renal or Hepatic Impairment; 2 Preclinical Data; 3 Clinical Data
3.1 Regorafenib in Metastatic Colorectal Cancer (mCRC)3.2 Regorafenib in Metastatic Gastrointestinal Stromal Tumors (mGIST); 3.3 Regorafenib in Hepatocellular Carcinoma (HCC); 3.4 Regorafenib in Metastatic Renal Cell Carcinoma (RCC); 3.5 Regorafenib in Soft-Tissue Sarcoma (STS); 4 Detailed Analysis of Toxicity; 4.1 Dermatological Toxicity; 4.2 Hypertension, Cardiac Ischemia, and Infarction; 4.3 Hepatotoxicity; 4.4 Gastrointestinal Perforation or Fistula; 4.5 Hemorrhage; 4.6 Embryo-Fetal Toxicity; 5 Drug Interactions; 5.1 Effect of Strong CYP3A4 Inducers; 5.2 Effect of Strong CYP3A4 Inhibitors
5.3 Effect of Regorafenib on UGT1A1 Substrates6 Biomarkers; 7 Summary and Perspectives; References; 4 Crizotinib; Abstract; 1 Structure and Mechanism of Action; 2 Preclinical Data; 3 Clinical Data; 3.1 NSCLC; 3.2 Other Entities; 4 Toxicity; 5 Drug Interactions; 6 Biomarkers; 7 Summary and Perspectives; References; 5 Cabozantinib: Multi-kinase Inhibitor of MET, AXL, RET, and VEGFR2; Abstract; 1 Introduction; 2 Preclinical Properties and Pharmacokinetics; 3 Clinical Trials; 3.1 Phase I; 3.2 Phase III EXAM Trial; 3.3 Phase III Trials in Renal Cell Cancer (METEOR and CABOSUN)
4 Cabozantinib Combination with Immuno-oncology5 Discussion; References; 6 Vemurafenib; Abstract; 1 Introduction; 2 Structure and Mechanism of Action; 3 Preclinical Data; 3.1 Pharmacokinetics and Drug Interactions; 3.2 Vemurafenib in Melanoma; 3.3 Toxicity; 3.4 Vemurafenib in Colorectal Cancer; 4 Vemurafenib in Papillary Thyroid Cancer; 4.1 Vemurafenib in Non-small-Cell Lung Cancer (NSCLC); 4.2 Vemurafenib in Hairy Cell Leukaemia; 4.3 Vemurafenib in Other Cancers; 4.4 Biomarkers and Monitoring of Vemurafenib Treatment; 5 Summary and Perspectives; References; 7 Trametinib (GSK1120212)
4.1.1 Second-Line Treatment and Beyond in Advanced Breast Cancer4.1.2 First-Line Treatment in Advanced Breast Cancer; 4.1.3 Neoadjuvant Treatment in Early Breast Cancer; 4.1.4 Adjuvant Treatment in Early Breast Cancer; 4.2 Efficacy in Gastrointestinal Cancer; 4.3 Tolerability; 5 Biomarkers; 6 Conclusion and Future Perspectives; References; 3 Regorafenib; Abstract; 1 Structure, Mechanism of Action, and Pharmacokinetics; 1.1 Mechanism of Action; 1.2 Pharmacokinetics and Elimination; 1.3 Regorafenib in Renal or Hepatic Impairment; 2 Preclinical Data; 3 Clinical Data
3.1 Regorafenib in Metastatic Colorectal Cancer (mCRC)3.2 Regorafenib in Metastatic Gastrointestinal Stromal Tumors (mGIST); 3.3 Regorafenib in Hepatocellular Carcinoma (HCC); 3.4 Regorafenib in Metastatic Renal Cell Carcinoma (RCC); 3.5 Regorafenib in Soft-Tissue Sarcoma (STS); 4 Detailed Analysis of Toxicity; 4.1 Dermatological Toxicity; 4.2 Hypertension, Cardiac Ischemia, and Infarction; 4.3 Hepatotoxicity; 4.4 Gastrointestinal Perforation or Fistula; 4.5 Hemorrhage; 4.6 Embryo-Fetal Toxicity; 5 Drug Interactions; 5.1 Effect of Strong CYP3A4 Inducers; 5.2 Effect of Strong CYP3A4 Inhibitors
5.3 Effect of Regorafenib on UGT1A1 Substrates6 Biomarkers; 7 Summary and Perspectives; References; 4 Crizotinib; Abstract; 1 Structure and Mechanism of Action; 2 Preclinical Data; 3 Clinical Data; 3.1 NSCLC; 3.2 Other Entities; 4 Toxicity; 5 Drug Interactions; 6 Biomarkers; 7 Summary and Perspectives; References; 5 Cabozantinib: Multi-kinase Inhibitor of MET, AXL, RET, and VEGFR2; Abstract; 1 Introduction; 2 Preclinical Properties and Pharmacokinetics; 3 Clinical Trials; 3.1 Phase I; 3.2 Phase III EXAM Trial; 3.3 Phase III Trials in Renal Cell Cancer (METEOR and CABOSUN)
4 Cabozantinib Combination with Immuno-oncology5 Discussion; References; 6 Vemurafenib; Abstract; 1 Introduction; 2 Structure and Mechanism of Action; 3 Preclinical Data; 3.1 Pharmacokinetics and Drug Interactions; 3.2 Vemurafenib in Melanoma; 3.3 Toxicity; 3.4 Vemurafenib in Colorectal Cancer; 4 Vemurafenib in Papillary Thyroid Cancer; 4.1 Vemurafenib in Non-small-Cell Lung Cancer (NSCLC); 4.2 Vemurafenib in Hairy Cell Leukaemia; 4.3 Vemurafenib in Other Cancers; 4.4 Biomarkers and Monitoring of Vemurafenib Treatment; 5 Summary and Perspectives; References; 7 Trametinib (GSK1120212)