1、,Medicinal Chemistry Antineoplastic Agents,班级：制药一班 学生：张航,Antineoplastic Agents,Tumor formation1 introduction2 Basic theory Antineoplastic Agents1 Agents Directly Acting on DNA2 Agents Interfering with DNA Synthesis3 Antimitotic Agents 4 Agents on Signal Transduction PathwayMechanism of Tunor(Erlotin
2、ib) Tumor prevention1 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 cells cellular atypia2)Biological behavior of tumors heterogeneity,Antineoplast
3、ic Agents,Normal cellCarcinogen-induced changeTumor cell variant,Antineoplastic Agents,Tumor formation2 Basic theory1)Cancer is a genetic disease2)Monoclonal expansion of Tumor cells3)Oncogene activation or tumor suppressor gene inactivation4)Long-term, phased, multiple mutations accumulated in the
4、process5)The result of loss of function of immune surveillance,Antineoplastic Agents,Antineoplastic Agents1)Agents Directly Acting on DNAAlkylating Agents Platinum Complexes Topoisomerase Inhibitors2)Agents Interfering with DNA Synthesis Antifolates Pyrimidine Antimetabolites Purine Antimetabolites,
5、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 Microtube4)Agents on Signal Transduction Pathway Mechanism of Tunor Protein Kinase Inhibitors Pr
6、oteasome Inhibitors,Antineoplastic Agents,Erlotinib and Gefitinib,Antineoplastic Agents,Antineoplastic Agents,ErlotinibTarceva (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 epiderma
7、l 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,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,Erlot
8、inib Mechanism of ActionTarceva 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 b
9、locking 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 concentra
10、tions. 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
11、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
12、 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
13、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 cl
14、inical study.,Antineoplastic Agents,Tumor prevention1 Primary prevention of tumorPromote healthy lifestyles and reduce cancer-causing factors,2 Secondary prevention of tumorEarly detection, early diagnosis and early treatment Early signs of cancerA swelling or small palpable massUnexplained bleedingPersistent indigestion,Antineoplastic Agents,Antineoplastic Agents,3 Tertiary prevention of tumor Active medical treatment, for best effect,Thank you,班级：制药一班 学生：张航,
