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Alkylating agents: general
MOA: Cross-link DNA
Proliferative dependent -cell cycle nonspecific!

Toxicity: cause bone marrow depression and acrolein (byproduct) causes hemorrhagic cystitis

examples: nitrogen compounds, mustards, etc.
Mechlorethamine
Not excreted
Use for Hodgkins disease (stage 3 and 4)
Cyclophosphamide
Must be activated  by MFO in liver
Use for Burkitts lymphoma
Chlorambucil
Use for CLL
MESNA
Less hemorrhagic cystitis
Reacts with intermediates in the urine
Busulfan
Causes pulmonary fibrosis
Nitrosoureas
Liberates alkylating species
Highly lipophilic
Unique toxicities-CNS
Procarbazine
Pt of MOPP regimen
Avoid MAO inhibitors
Dacarbazine
Methylates DNA and RNA; CCNS
ABVD* for use in Hodgkins disease
Cisplatin
Useful for metastatic testicular and ovarian tumors
Dose limiting toxicities- nephrotoxic and neurotoxic
Agents that directly damage DNA
Tight BPing between adj BPs
Doxorubicin/Daunorubicin
MOA: tight binding b/w adj. base pairs
Single and double-strand breaks
CCNS
Unique toxicity: cardiotoxicity
Mitoxantrone
binds w/ DNA like doxorubicin to make drug-DNA-topoisomerase 2 complexes that lead to DNA strand breaks
Epipodophyllotoxins
MOA-Increase DNA-topoisomerase 2 axn to cleave DNA

Use: testicular cancer
Camptothecin analog
Irininotecan most common
Inhib DNA topoisomerase 2
Bleomycin
MOA: bind reduced iron, leads to DNA scission and inhib of repair due to high free radical formation
Toxicity-pulmonary fibrosis, cutaneous reactions
Dactinomycin
MOA-interact with dsDNA to inhibit DNA-dep RNA synthesis
CCNS
Use: MTX-resistant choriocarcinoma, Wilms tumor, Rhabdomyosarcoma
Methotrexate
MOA: inhib dihydrofolate reductase
CCS-S phase
Unique toxicity-oral and GI ulceration
Use: choriocarcinoma
Pyrimidine analogs
5-fU
Cytarabine
5-FU
MOA: inhibit thymidylate synthetase, decrease DNA synthesis
Cytarabine
MOA: inhibits DNA polymerase alpha
Incorporation into DNA -> chain termination

CCS -s phase
Purine analogs
Mercaptopurine
Thioguanine
Mercaptopurine
MOA: inhib synthesis of adenine and guanine by blocking purine precursors

CCS at S phase

Metabolism inhibited by allopurinol
Thioguanine
MOA: inhibits biosynth of purines

CCS at S phase
Vinca alkaloids
MOA: bind to soluble tubulin, arrest mitosis in Metaphase

Toxicity: peripheral neuropathy
Uses: vincristine- Hodgkins disease
Vinblastine-Testicular carcinoma, MOPP-resistant Hodgkins (ABV*D)
Paclitaxel
Peripheral neuropathy
L-asparaginase
enzyme which hydrolyzes asparagine to aspartic acid
Mitotane
Selective for adrenocortical cells
Prednisone
Use: Manage frank hemolytic anemia and hemorrhagic complications of lymphomas and CLL

Use: Hodgkins (MOPP*)
Antiestrogens
ex) tamixofen
for breast cancer when E2 receptors are present
Antiandrogens
Combined with leuprolide
Antibodies
"-mab" s
Trastuzumab
Ab vs HER2 protein in breast cancer
Exemestane
irreversible aromatase inhibitor

other drugs in class-anastrazole
Thalidomide
Treat multiple myeloma - antiangiogenic properties.

Teratogenic
Imatinib mesylate
Oral tyr kinase inhibitor given speedy approval - treats all phases of CML
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