Drug Summary for Exam

4 Pages

Course Code
Pharmacology 4360A/B
Moshmi Bhattacharya

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Drug  Name   Type  of  Drug   Target   Mechanism  of  Action   Farnesyltransferase     Small  GTPases   Prevents  the  post-­‐ Inhibitors   translational   modification  farnesyl   group   Gemcitabine   Nucleoside   DNA   Replaces  cytadine  during   Analog   DNA  replication  leading   to  arrest  of  tumor   growth   Sorafenib   Monoclonal   Raf  inhibitor     Antibody   Avastin   Monoclonal   VEGF   Binds  VEGF  and  blocks   Antibody   the  activation  of   angiogenesis   PI3K  Inhibitor     PI3K   Inhibits  the  production   of  PIP3  and  activation  of   PI3K/Akt  signaling   pathway   Mek  Inhibitor         Akt  Inhibitor         Vitaxin  2     Human  alpha  v   Inhibits  angiogenesis   beta  3  integrin   Combrestatin     Beta  subunit  of   Binds  the  beta  subunit  of   tubulin   tubulin,  inhibits  tubulin   polymerization/prevents   cancer  from  producing   MTs   Iressa       Tyrosine     kinsases   Leuprolide/   GnRH   GnRH  receptor   AA  6/10  are   Goserelin/Buserlin     Superagonist   SUBSTITUTED  in   superagonists  to  extend   half  lives  (resistant  to   enzymatic  degradation)   and  200x  more  potent   then  GnRH       GnRH     Can  get  serious  allergic   Antagonist   reactions   Abarelix   GnRH   GnRH  receptor   Prostate  cancer   Antagonist   treatment  –  blocks  the   GnRH  receptor  at  the   pituitary,  has  the  first   three  amino  acids   changed  to  d-­‐amino   acids.       Sustained  release   formulation   Plerixafor   Antagonist   CXCR4     Cytotoxic  GnRH         Analog  with   doxorubicin   Cyclophosphamide     Alkylating  Agent   DNA  replication   Metabolized  in  the  liver   by  P450  to   aldophosphamide  which   forms  phosphoramide   mustard  (has  two  groups   to  grab  on  to  two   guanines)  and  acrolein   (give  mesna  with   acrolein  to  prevent   bladder  damage).     Mercaptopurine   Antipurine   Metabolite  -­‐   Inhibits  purine  synthesis   purine   by  being  incorporated   into  DNA  and  interfering   with  DNA  replication   5’-­‐Fluorouracil   Antipyramidine   Enzyme-­‐specific   Inhibits  DNA  synthesis   by  inhibiting  the  enzyme   involved  in  the  synthesis   of  cytosine  and  thymine,   incorporate  into  RNA   instead  of  uracil  (inhibits   RNA  synthesis)   Methotrexate     Folate   Enzyme  specific   Inhibits  dihydrofolate   Anatagonist     reductase  (DHFR),  as   essential  enzyme  in   folate  metabolism.   Prevents  the  generation   of  tetrahydrofolate,   interferes  with   thymidylate  synthesis   Cytarabine   Arabinoside   DNA   False  nucl
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