医学ppt药物化学英文版抗肿瘤药

LOGO Medicinal Chemistry Antineoplastic Agents n班级：制药一班 n学生：张航 Antineoplastic Agents u Tumor formation 1 introduction 2 Basic theory u Antineoplastic 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) u Tumor prevention 1 Primary prevention of tumor 2 Secondary prevention of tumor 3 Tertiary prevention of tumor Antineoplastic Agents Tumor Tumor formation formation 1 1、IntroductionIntroduction Antineoplastic Agents 1)Basic characteristics of Tumor cells cellular atypia 2)Biological behavior of tumors heterogeneity Antineoplastic Agents Normal cellNormal cell Carcinogen-induced Carcinogen-induced changechange Tumor cell variantTumor cell variant Antineoplastic Agents uTumor formation 2 Basic theory 1)Cancer is a genetic disease 2)Monoclonal expansion of Tumor cells 3)Oncogene activation or tumor suppressor gene inactivation 4)Long-term, phased, multiple mutations accumulated in the process 5)The result of loss of function of immune surveillance Antineoplastic Agents uAntineoplastic 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 Tubulin Antitumor Agents Having Two Binding-Point on Tubulin Antitumor Agents Acting on the Polymerization State of Microtube 4)Agents on Signal Transduction Pathway Mechanism of Tunor Protein Kinase Inhibitors Proteasome 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 Erlotinib Chemical composition C C22 22 H H 2323 N N3 3O O4 4 氮氮一一(3(3一乙一乙炔苯炔苯) )一一6 6，7 7一二一二( (甲甲氧氧己己氧氧) )一一 4 4一一喹唑喹唑啉胺啉胺 Antineoplastic Agents Erlotinib u Mechanism 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 Erlotinib Pharmacodynamics Erlotinib 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 Erlotinib Pharmacokinetics Bioavailability 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 Erlotinib Adverse reactions Serious 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 uTumor 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 cance