Anti-Cancer Drugs design课件.ppt

Anti-Cancer Drugs 2007,12 million，annual dead over 7 million sales ： (15% annual) 2004, 240 billion 2007, 396 billion 2008, 480 billion 2009, 550 billion 2012, 800 billion annual increase rate 15%， 1997~2008， Targeted-drug: about 15个！ 1997,Rituxan 1998, Herceptin (1.6 billion) The time of targeted-drug is coming 2001: Gleevec (small molecule ) 2004: Avastin (antibody, 1.3 billion） Blockbuster Target is factor of signal transduction pathway。 2006: Vectibix （monoclonal antibody）, Sutent（美国历史上首次批准的一个药物同时拥有两 个适应症） 2006: Vectibix（monoclonal antibody） Sprycel,Sutent (small molecule ) 2007: lapatinib, nilotinib (small molecule ) temsirolimus , ixabepilone (nature materials) cervical cancer vaccine Cervarix ,vaccine for brain cancer 2008: Degarelix (nature materials) vitespen (vaccine) all are Targeted-drug except vaccine or antibody   Chemistry drugs 1) Targeted-drug: kinase inhibitor. recognize and attack the particular tumor cell, not damage normal cell 2)Cellulotoxic: tumor cell splinter faster, sensitive to DNA damage Oxaliplatin 3) Hormone:Tamoxifen 4) Aromatase inhibitor (Anti-hormone) : anastrozole(阿那曲唑)、 letrozole(来曲唑) 5) Nature-drug: Taxol (1992), Epothilones Biology drugs 1) Monoclonal antibody: mechanism is activated and enhanced immune system to defense tumor cell. Target is better and side effect is small. 2) Vaccine 3) Antisense oligonucleotide(反义寡核苷酸） Chemistry durgs: about 2 thousend Peptide and vaccine: dozens added indications : 230 Introduction of protein kinases: family 1）catalyze phosphorylation 2）signal transduction pathway 3）deregulation is implicated some diseases 4)targeted inhibition ??doubt thether inhibit the kinas