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31 Cards in this Set

  • Front
  • Back

G1 Phase

L-Asparaginase

L-Asparaginase

Deprives cells of asparagine
-> inhibition of protein synthesis

G2 Phase

Bleomycin

Bleomycin

Complex undergoes oxidation
-> generating superoxide and
hydroxyl radicals -> DNA strand breaks

M Phase

Paclitaxel
Docetaxel


Vinblastine
Vincristine

Paclitaxel
Docetaxel


 

Hyperstabilizes
polymerized microtubules
-> anaphase cannot occur

Vinblastine
Vincristine

Prevent microtubule
polymerization -> preventing
mitotic spindle formation -> M-phase
arrest

S/G2 Phase

Etoposide
(Podophyllotoxins)

Etoposide
(Podophyllotoxins)

Inhibits topoisomerase II
-> ↑ DNA degredation

Non-specific Cell Cycle

Alkylating Agents


Platinum Complexes


Antitumor Antibiotics

Platinum Complexes

Cisplatin
Carboplatin
Oxaliplatin

Cisplatin
Carboplatin
Oxaliplatin

Cross-link
DNA

Antitumor Antibiotics

Dactinomycin
(Actinomycin D)


Anthracyclins
(-rubicins)

Anthracyclins
(-rubicins)


 

-Intercalates in DNA ->
breaks in DNA -> ↓ replication


-Inhibition of
topoisomerase II


-Generates free radicals

Dactinomycin
(Actinomycin D)

-Intercalates between
adjacent G-C pairs in
DNA


-Inhibition of
topoisomerase I


-Generates free radicals

Alkylating Agents

Carmustine
Lomustine


Busulfan


Cyclophosphamide
Ifosphamide


 


 Others:


Procarbazine


Temozolamide


Melphalan


Mechlorethamine


Chlorambucil

Carmustine
Lomustine
(Nitrosoureas)

Requires bioactivation
-> crosses blood-brain barrier
-> cross links DNA

Busulfan

Cross-links DNA

Cyclophosphamide
Ifosphamide

Covalently X-link (interstrand) DNA at guanine N-7. Require bioactivation  by liver (CYP450)

S Phase

Cytarabine


Methotrexate


6-Mercaptopurine
6-Thioguanine


Irinotecan
Topotecan


5-FU


Hydroxyurea

6-Mercaptopurine
6-Thioguanine

Purine analog, causing decreased de novo
pruine synthesis

Irinotecan
Topotecan

Topoisomerase I inhibition -> DNA
strand breaks

5-FU

Pyrimidine analog, activated
into 5F-dUMP, which covalently
complexes folic acid ->thymidylate synthase


inhibition -> ↓dTMP -> ↓DNA and
↓ protein synthesis.

Hydroxyurea

Inhibits ribonucleotide 
reductase -> ↓ DNA synthesis

Methotrexate

Folic acid analog that inhibits
dihydrofolate reductase
 -> ↓dTMP -> ↓DNA and
↓ protein synthesis


 

Cytarabine

Pyrimidine analog, causing
DNA polymerase inhibition

Trastuzumab 
(Herceptin)

Antibody against HER-2 (c-erbB2), a tyrosine kinase receptor

Imatinib


(Gleevec)

Tyrosine kinase inhibitor of bcr-abl (Philidelphia chromosome in CML) and c-Kit

Rituximab

Antibody against CD20, found in most B-cell neoplasms

Bevacizumab

Antibody against VEGF, inhibits angiogenesis

Common Chemotoxicities