药物化学英文版抗肿瘤药

,Medicinal Chemistry Antineoplastic Agents,班级：制药一班学生：张航,Antineoplastic Agents,Tumor formation 1 introduction 2 Basic theoryAntineoplastic Agents 1 Agents Directly Acting on DNA 2 Agents Interfering with DNA Synthesis 3 Antimitotic Agents 4 Agents on Signal Transduction Pathway Mechanism of Tunor(Erlotinib)Tumor prevention 1 Primary prevention of tumor 2 Secondary prevention of tumor 3 Tertiary prevention of tumor,Antineoplastic Agents,Tumor formation 1、Introduction,Antineoplastic Agents,1)Basic characteristics of Tumor cellscellular atypia2)Biological behavior of tumorsheterogeneity,Antineoplastic Agents,Normal cellCarcinogen-induced changeTumor cell variant,Antineoplastic Agents,Tumor formation 2 Basic theory 1)Cancer is a genetic disease 2)Monoclonal expansion of Tumor cells3)Oncogene activation or tumor suppressor gene inactivation4)Long-term, phased, multiple mutations accumulated in the process5)The result of loss of function of immune surveillance,Antineoplastic Agents,Antineoplastic Agents 1)Agents Directly Acting on DNA Alkylating Agents Platinum Complexes Topoisomerase Inhibitors 2)Agents Interfering with DNA Synthesis Antifolates Pyrimidine Antimetabolites Purine Antimetabolites,Antineoplastic Agents,3)Antimitotic Agents Antitumor Agents Having One Binding-Point on TubulinAntitumor Agents Having Two Binding-Point on TubulinAntitumor Agents Acting on the Polymerization State of Microtube4)Agents on Signal Transduction Pathway Mechanism of Tunor Protein Kinase InhibitorsProteasome Inhibitors,Antineoplastic Agents,Erlotinib and Gefitinib,Antineoplastic Agents,Antineoplastic Agents,Erlotinib Tarceva (erlotinib), a once-a-day pill, was one of the first targeted treatments approved by the U.S. Food and Drug Administration (FDA) specifically designed to target the epidermal growth factor receptor (EGFR) pathway. Tarceva has been shown to help some people with advanced NSCLC and advanced pancreatic cancer live longer. NSCLC(Non-small-cell carcinoma ),Antineoplastic Agents,ErlotinibChemical composition,C22H23N3O4氮一(3一乙炔苯)一6，7一二(甲氧己氧)一4一喹唑啉胺,Antineoplastic Agents,ErlotinibMechanism of Action Tarceva is designed to inhibit signaling of the epidermal growth factor receptor (EGFR) pathway. Tarceva works inside the tumor cell by inhibiting the tyrosine kinase activity of the EGFR pathway, which is one of the critical growth factors in NSCLC and pancreatic cancer. By blocking this activity, it is thought that Tarceva may help slow or stop the growth of tumors. The way Tarceva works to treat cancer is not fully known.,Antineoplastic Agents,ErlotinibPharmacodynamicsErlotinib blocks the effectiveness of its tyrosine kinase linearly related to plasma drug concentrations. In the dose of 25200mg/d, the significant reduction in erlotinib Nicole phosphorylation of epidermal growth factor receptor expression, decreased phosphorylation of a free-type EGFR and EGFR ratio, while blocking the EGFR signal transduction downstream access.,Antineoplastic Agents,ErlotinibPharmacokineticsBioavailability of this product is about 60%, after oral administration of 150mg Erlotinib.About 4 hours after administration of plasma peak concentration. With food can make a substantial increase in bioavailability to almost 100%. Absorbed into the bloodstream, the protein binding rate is about 93%.The half-life of the product was 36.2 hours, steady state plasma drug concentration time of 7-8 days.,Antineoplastic Agents,ErlotinibAdverse reactionsSerious side effects (including deaths) in patients taking Tarceva plus gemcitabine were more likely to experience bleeding and clotting problems such as heart attack or stroke. Eye irritation and damage to the cornea have been reported in patients taking Tarceva. Fatigue, rash, nausea, loss of appetite and diarrhea were the most common side effects associated with Tarceva plus gemcitabine therapy in the pancreatic cancer clinical study.,Antineoplastic Agents,Tumor prevention 1 Primary prevention of tumor Promote healthy lifestyles and reduce cancer-causing factors,2 Secondary prevention of tumor Early detection, early diagnosis and early treatment Early signs of cancer