Chemotherputics

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  1. Mephalan
    • Nitrogen mustard -> causes alkylation of DNA primarily at N-7 of G which leads to misreading, depurination, and double strand breaks
    • Stable enough for oral administration
  2. Chlorambucil
    • Nitrogen mustard -> causes alkylation of DNA primarily at N-7 of G which leads to misreading, depurination, and double strand breaks
    • Stable enough for oral administration
  3. Cyclophosphamide
    • Nitrogen mustard -> causes alkylation of DNA primarily at N-7 of G which leads to misreading, depurination, and double strand breaks
    • Must be activated by hepatic cytochrome p450
    • No hepatotoxicity because converted to inactive metabolite in the liver
    • Toxicities: pulmonary fibrosis, cystitis
  4. Lomustine
    • Nitrosourea -> heterobifunctional compound that causes alkylation, DNA crosslinking, and carbamoylation of protiens
    • Cross readily into CNS -> Tx for malignant glioma
    • Toxicity: Delayed but severe hematopoietic depression
  5. Carmustine
    • Nitrosourea -> heterobifunctional compound that causes alkylation, DNA crosslinking, and carbamoylation of protiens
    • Cross readily into CNS -> Tx for malignant glioma
    • Toxicity: Delayed but severe hematopoietic depression
  6. Cisplatin
    • Platinum coordination complex -> potent alkylating activity that causes a variety of cross links
    • Toxicities: myelosuppression, nephrotoxicity, ototoxicity
    • Administer with amifostin (free radical scavenger) to attenuate nephrotoxicity
  7. Oxaliplatin
    • Cisplatin analog that is not crss-resistant
    • Platinum coordination complex -> potent alkylating activity that causes a variety of cross links
    • Toxicities: myelosuppression, nephrotoxicity, ototoxicity
    • Administer with amifostin (free radical scavenger) to attenuate nephrotoxicity
  8. Carboplatin
    • Platinum coordination complex -> potent alkylating activity that causes a variety of cross links
    • Toxicities: myelosuppression, nephrotoxicity, ototoxicity
    • Substantially less renal toxicity than cisplatin or oxaliplatin
  9. Procarbazine
    • Nonspecific alkylator (DNA, RNA, protien)
    • Metabolized to active form by hepatic enzymes
    • Toxicities: Myelosuppression, MAO inhibitor, carcinogenicity
  10. Vincristine
    • Vinca alkaloid -> depolymerizes microtubules -> inihbits movement and mitosis
    • Toxicities: Neurotoxicity, stimulation fo ADH release
    • Resistance: MDR
  11. Vinblastine
    • Vinca alkaloid -> depolymerizes microtubules -> inihbits movement and mitosis
    • Toxicities: myelosuppression, mucositis
    • Resistance: MDR
  12. Paclitaxel
    • Taxane -> stabalizes the assembly of microtubules by inhibiting disassembly
    • Toxicities: Neutropenia, mucositis, cardiac arrythmia in pnts who have recieved other cardiotoxic drugs
    • Derived from the bark of the western yew tree
  13. Docetaxel
    • Semisynthetic analogue of paclitaxel
    • Taxane -> stabalizes the assembly of microtubules by inhibiting disassembly
  14. Ixabepilone
    • Epothilone -> binds directly to beta-tubulin and promotes polymerization and stabalizes microtubule, arresting cells in G2/M
    • Toxicities: neutropenia, cardiotoxicity, peripheral neuropathy
  15. Etoposide
    • Epipodophyllotoxins -> Inhibition of topoisomerase II
    • Toxicities: leukopenia, thrombocytopenia
    • Resistance: MDR
    • Semisynthetic derivatives derived from mandrake plant
  16. Teniposide
    • Epipodophyllotoxins -> Inhibition of topoisomerase II
    • Toxicities: leukopenia, thrombocytopenia
    • Resistance: MDR
    • Semisynthetic derivatives derived from mandrake plant
  17. Irinotecan
    • Camptothecin derivatives -> Inhibition of topoisomerase I
    • Prodrug
    • Effective in metastatic colorectal cancer
    • Toxicities: neutropenia, diarrhea
    • Resistance: MDR
  18. Topotecan
    • Camptothecin derivatives -> Inhibition of topoisomerase I
    • Effective in ovarian and small cell CA of lung
    • Toxicities: neutropenia, diarrhea
    • Resistance: MDR
  19. Daunorubicin
    • Antibiotic
    • Mechanism: DNA intercalation, introduction of single stranded breaks
    • Toxicities: Cumulative cardiotoxicity that can manifest as arrythmias or digitalis unresponsive heart failure. Reduce cardiac damage by giving with Dexrazoxane
  20. Doxorubicin
    • Antibiotic
    • Mechanism: DNA intercalation, introduction of single stranded breaks
    • Toxicities: Cumulative cardiotoxicity that can manifest as arrythmias or digitalis unresponsive heart failure.
    • Reduce cardiac damage by giving with Dexrazoxane
  21. Dexrazoxane
    • Iron chelator that inhibits free radical formation and can be used to reduce cardiac damage, as well as to minimize extravasation reactions
    • Given with daunorubicin and doxorubicin to minimize cardiotoxicity
  22. Bleomycin
    • Antibiotic
    • Mechanism: Depurination and depyrimidation; both single and double stranded breaks are introduced
    • Toxicities: Subacute or chronic pneumonitis, lesions of the skin
    • Resistance: Over expression of bleomycin hydrolase
  23. Methotrexate
    • Folic acid analog that is a competitive inhibitor of dihydrofolate reductase
    • Cells in S phase cannot synthesize DNA
    • Toxicities: fatal myelosuppression; renal, hepatic and neuro toxicity; teratogenicity
    • Resistance: Increased DHFR activity
  24. Leucovorin
    • Used to abort MTX toxicity by supplying reduced folate to cells, thus bypassing the inhibited reductase.
    • Can also be used to potentiate the activity of 5-FU
  25. 5-fluorouracil
    • Potent suicide inhibitor of thymidylate synthase
    • Toxicities: myelosuppress, GI distress, acute or chronic conjunctivitis
    • Resistance: Overexpression of TS
  26. Capecitabine
    5-FU prodrug whose final step of activation is catalyzed by thymidine phosphorylase, an enzyme elevated in certain tumors
  27. Cytosine arabinoside (Cytarabine)
    • Recognized as deoxycytidine by cytosine kinase, phosphorylated, and becomes a potent inhibitor of DNA polymerase and when incorporated into DNA causes defective ligation and premature chain termination
    • Toxicities: Myelosuppression, nausea, vomiting, GI ulceration, and seizures
    • Resistance: decreased cytosine kinase activity, increased cytosine deaminase activity
  28. Gemcitabine
    • 2'-2'-difluorodeoxycytidine
    • Similar to cytosine arabinoside
    • Good activity in advanced breast cancer, non-small-cell lung cancer, pancreatic adenocarcinoma, and ovarian carcinoma
  29. Azacitidine
    • Inhibits DNA methyltransferase resulting in hypomethylation; incorporated into RNA
    • Good for Tx of myelodysplastic syndrome
  30. 6-mercaptopurine
    • Purine analog
    • Converted by hypoxanthine-granine-phosphoribosyl transferase to monophosphates:
    • Feedback inhibit de novo purine synthesis; competitively inhibit biosynthetic reactions, converted to triphosphates that are incorporated into DNA and RNA
    • Toxicity: myelosuppression, hepatotoxicity
    • Resistance: HPRT mutations, overexpression of thiopurine methyltransferase
  31. Asparaginase
    • Catalyzes the conversion of asparagine to aspartate
    • In some cancer cells asparagine is an essential amino acid (lack of asparagine synthetase)
    • Pegylated form has longer t1/2
    • Toxicities: reduction in concentration of secreted protiens, hypersensitivity, hepatotoxicity
  32. Imantinib mesylate
    • Competitively blocks the ATP-binding site of c-abl tyrosine kinase
    • Tx for CML
    • Toxicities: congestive heart failure, myelosuppression
  33. Erlotinib
    • Inhibitor of EGF receptor-associated tyrosine kinase
    • Tx for non-small cell lung cancer and pancreatic cancer
    • Toxicity: congestive heart failure
  34. Gefitinib
    • Inhibitor of EGF receptor-associated tyrosine kinase
    • Tx for non-small cell lung cancer and pancreatic cancer
    • Toxicity: congestive heart failure
  35. Vemurafenib
    • Inhibitor of BRAF serine-threonine kinase
    • Good for Tx of melanoma
  36. Cetuximab
    • Chimeric monoclonal Ab directed against the EGFR
    • For use in head and neck and metastatic colorectal cancer
  37. Trastuzumab (herceptin)
    • Induces antibody-dependent cell-mediated cytotoxicity
    • For the tx of p185-HER2 overexpressing breast cancer
    • Toxicity: cardiotoxicity, especially when used with or after anthracyclines
  38. Bevacizumab
    • Humanized monoclonal Ab directed against VEGF
    • designed to inhibit angiogenesis
    • effective in tx of lung, colon, and kidney cancer
    • use associated with increased risk of thromboembolic events
  39. Rituximab
    • Recombinant anti-CD20 monoclonal Ab that promotes complement mediated lysis of malignant B-cells
    • Use can result in HBV reactivation
  40. Gemtuzumab ozogamicin
    Recombinant monoclonal Ab directed against myeloid cell surface Ag CD33
  41. Vorinostat
    • Histone deacetylase inhibitor
    • Used to tx cutaneous T cell lymphoma
  42. Bortezomib
    Proteosome inhibitor used for tx of multiple myeloma and mantle cell lymphoma
  43. All-trans-retinoic acid
    First line therapy for promyelocytic leukemia
  44. Tamoxifen
    • Selective estrogen receptor modulator
    • Competitive partial agonist inhibitor
    • In breast tissue acts like an antagonist, in endometrial tissue acts like an agonist
    • Must be activated by CYP2D6
    • Use in postmenopausal women with estrogen receptor positive breast cancer
    • Only use for 5 years
    • Adverse effects: Endometrial CA, thromboembolic events
  45. Raloxifene
    • SERM
    • As effective as tamoxifen
    • Lower incidence of uterine cancer and fewer blood clots
  46. Fulvestrant
    • Pure estrogen receptor antagonist
    • Given once a month IM
    • Geven to postmenopausal women whose cancer has progressed on tamoxifen or other anti-estrogen
  47. Anastrozole
    • Selective and irreversible inhibitors of aromatase
    • Used only for postmenopausal women
    • Continue to be effective beyond 5 years
    • No risk of endometrial cancer or thromboembolic event
    • Approved as first line therapy or as an alternative to tamoxifen
  48. Letrozole
    • Selective and irreversible inhibitors of aromatase
    • Used only for postmenopausal women
    • Continue to be effective beyond 5 years
    • No risk of endometrial cancer or thromboembolic event
    • Approved as first line therapy or as an alternative to tamoxifen
  49. Exemestane
    • Selective and irreversible inhibitors of aromatase
    • Used only for postmenopausal women
    • Continue to be effective beyond 5 years
    • No risk of endometrial cancer or thromboembolic event
    • Approved as first line therapy or as an alternative to tamoxifen
  50. Trastuzumab
    • Humanized monoclonal Ab against HER2/erbB-2 receptor
    • Side effects: cardiomyopathy when combined with anthracyclines
  51. Lapatinib
    • Orally active tyrosine kinase inhibitor that targets both erbB receptors
    • Used for the tx of advanced breast cancer expressing high levels of HER-2 that no longer respond to trastuzumab
  52. Leuprolide
    • GnRH analog
    • For use in prostate cancer - equivalent to surgical castration or diethylstilbestrol tx
    • Initial surge of LH and FSH compensated by administering biclutamide
  53. Goserelin
    • GnRH analog
    • For use in prostate cancer - equivalent to surgical castration or diethylstilbestrol tx
    • Initial surge of LH and FSH compensated by administering biclutamide
  54. Abarelix
    • GnRH antagonist
    • Will inhibit LH and FSH release and testosterone production without a flare
  55. Flutamide
    • Pure androgen antagonist
    • Prevents binding of endogenous androgens to the androgen receptor
    • No intrinsic steroidal activity
    • Side effects: diarrhea, gynecomastia, hepatotoxicity (rare)
  56. Biclutamide
    • Newer nonsteroidal antiandrogen
    • Could be more effective than flutamide
    • Less side effects than flutamide
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151452
Card Set
Chemotherputics
Description
Meds we have to know from cancer chemotherapy I, II and III along with hormonal agents
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