Chemo Drugs

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What's the characteristic of Class 1 Chemo Agents?

Kill cells regardless of state of proliferation
What's the characteristic of Class 2 chemo agents?

Kill cells in a specific phase of cell cycle; plateau proportional to fraction not at stage
What's the characteristic of Class 3 chemo drugs?
- Non-cycle specific
- More effective against proliferating cells
What are chemo drugs' effectiveness dependent on?

Concentration and time of exposure
What chemo class are Alkylating agents?

Class III (no specific phase)
What's the mechanism of alkylating agents?

Induce DNA damage or p53 mediated apoptosis
What's the specific mechanism of action of Nitrogen Mustards?
- Alkylation of DNA at N-7 position of guanine
- Misreading of DNA replication
What is Mechlorethamine?

Nitrogen Mustard Alkylating Agent
What is Melphalan?
- Nitrogen Mustart Alylating agent
- Oral stable
What's Chlorambucil?

Nitrogen Mustard Alkylating Agent
What's Cyclophosphamide?
- Nitrogen Mustard Alkylating Agent
- CYP450 Activation
What SE come from Cyclophosphamide?
- Hepatotoxicity
- Pulmonary Fibrosis
What's Busulfran? (MoA & SE)
- Alkylsulfonate Alkylating Agent
- Granulocytopenia
What's Carmustine? (MoA & SE)
- Nitrosourea Alkylating Agent
- Lipid soluble -> CNS & delayed/severe BM&pulmonary fibrosis
What's Cisplatin? (MoA & SE)
- Platinum Complex Alkylating Agent
- MoA: Covalent bonds to plasma proteins
- SE: Nephrotoxicity
What's Oxaliplatin? (MoA & SE)
- Cisplatin analogue (AA)
- SE: not cross resistant
What's Carboplatin? (MoA & SE)
- Cisplatin Analogue (AA)
- Less renal toxicity
What's vincristine?
- Vinca Alkaloid
- MoA: inhibit spindle fiber mitosis/cytoskeletal movement
- SE: Neurotoxicity
What's vinblastine?
- Vinca Alkaloid
- MoA: inhibit spindle fiber mitosis/cytoskeletal movement
- SE: less neurotoxicity; granulocytopenia
What's Paclitaxel?
- Taxane
- MoA: inhibits dissasembly of microtubules during mitosis
- SE: cardiotoxic
What's Docetaxel?
- Paclitaxel Analogue
- MoA: inhibits dissasembly of microtubules during mitosis
- SE: cardiotoxic
What's etoposide?
- Epipodophyllotoxin
- Inhibition of topoisomerase II
What's teniposide?
- Epipodophyllotoxin
- Inhibition of topoisomerase II
What's Irinotecan?

Inhibition of Topoisomerase I
What's topotecan?

Inhibition of Topoisomerase I
What's Dactinomycin? (MoA & SE)
- Antibiotic
- Intercalates between G:C
- Low conc: inhibit RNA synthesis
- High conc: inhibit RNA & DNA synthesis
- SE: radiation sensitization
What's Daunorubicin?
- MoA: DNA intercalation & single stratnded breaks
- SE: Cumulative cardiotoxicity (lack of superoxide dismutase to fix ROS)
What's Dexrazoxane?

Inhibits ROS to reduce cardiotoxicity from Daunorubicin/doxorubicin
What's doxorubicin?
- MoA: DNA intercalation & single stratnded breaks
- SE: Cumulative cardiotoxicity (lack of superoxide dismutase to fix ROS)
What's Bleomycin? (MoA/SE)
- MoA: DNA/Fe binding => single/double stranded breaks
- SE: pneumonitis with oxygen reaction
What's the mechanism of resistance for Bleomycin?

Bleomycin hydrolase -> inactivation of drug
What's Methotrexate (MoA)
- Folic Acid analogue -> competative inhibition of DHFR
- Block dUMP-> dTMP DNA synthesis
- Block FH₄ co-factor rxns
What's the mechanism of resistance for Methotrexate?

Increased DHFR activity
What's the toxicity of Methotrexate?
- Low: Myelosuppression
- High: Mylosuppression, renal & liver toxicity
What's Leucovorin?

Abort MTX tocity by supplying already reduced folate to cells (bypass DHFR)
What's 5-Fluorouracil?
- Metabolized to 5-FdUMP in cell
- Suicide inhibitor of thymidylate synthase
- Defective RNA synthesis
What's the mechanism of resistance to 5-Fluorouracil?

Overexpression of TS
What's capecitabine?

5-FU prodrug selectively activated in target cell
What's azacitidine?
- Pyrimidine Analogue
- Inhibit DNA methyltransferase; inhibited RNA
What's 6-mercaptopurine? (MoA/Resistance)
- MoA: inhibit de novo purine synthesis -> inhibit biosynthetic reactions
- Resistance: HPRT mutations
What's 6-thioguanine?
- MoA: inhibit de novo purine synthesis -> inhibit biosynthetic reactions
- Resistance: HPRT mutations
What's asparaginase?
- MoA: Deprivation of asparagine (-> aspartate)
- SE: reduction on concentration of proteins (albumin, clotting, insulin); HS, hepatotoxicity
What's imatinib mesylate? (MoA/SE)
- Competatively blocks ATP binding site of c-abl kinase
- SE: CHF
What's erlotinib/gefitinib? (MoA/SE)
- Inhibitors of EGF receptor associated tyrosine kinase
- SE: CHF
What's Cetuximab?

Antibody against EGF receptor
What's trantuzumab?
- Ab against VGEF
- Anti-angiogenesis
- SE: increased Thromboembolic events
What's rituximab?

anti CD-20 against B-cells
What's gemtuzumab/ozogamin?

Ab against CD33
What's vorinostat?

histone deacetylase inhibitor
What's bortezomib?

proteasome inhibitor
What's all-trans-retinoic acid?

Vitamin a

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Chemo Drugs

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Updated

2011-04-27T15:18:55Z

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