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78 Cards in this Set

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What sort of drug is cyclophosphamide?
nitrogen mustard
Describe the process of activation of cyclophosphamide.
p450 -> adds active alkyl groups
How does activated cyclophosphamide work?
Active alkyl groups bind 2 DNA strands.
How broad of a clinical spectrum does cyclophosphamide cover. Examples? (2)
CLL and many solid tumors
What nitrosoureas are used as chemotherapeutics? (3)
Carmustine
Lomustine

Streptozocin
Musty, not musty
How are nitrosoureas activated?
Non-enzymatic (ie, spontaneous breakdown)
What are the activated forms of nitrosoureas?
1) reactive alkylating agents

2) Isothiocyanate -> modifies protein, especially DNA repair enzymes -> impared DNA repair
Which nitrosoureas are myelosuppressive?
Carmustine
Lomustine

Streptozocin is NOT myelosuppresive
Which nitrosoureas are lipid soluble?
Carmustine
Lomustine
Which nitrosoureas are used to treat primary brain tumors?
Carmustine
Lomustine
Which nitrosourea is used to treat insulinomas? Why?
Streptozocin -> glucose analogue -> high affinity for GLUT-2 transporter on islet cells
How does cisplatin work?
Like alkylating agents, it cross-links DNA. However, cisplatin is NOT an alkylating agent.
What is the main side effect of cisplatin?
nephrotoxity -> slowly reversible, controlled by hydration and diuresis
What is cisplatin used for?
IT IS A FIRST LINE DRUG FOR MANY SOLID TUMORS.

Useful in treating melanoma.
What enzyme does MTX interfere with?
DHFR
What cellular processes does MTX interfere with? (2)
1) Inhibits conversion from dUMP to dTMP.

2) Inhibits DE NOVO purine ring synthesis, due to lack of a 1-carbon donor.
What are the main side effects of MTX?
1) Bone marrow suppression

2) Mucosal ulceration
What is the antidote for MTX overdose?
Leucovorin (folinic acid)
How does MTX accumulate inside cells?
It is ACTIVELY TRANSPORTED into cells, then POLYGLUTAMATED.
What are the main mechanisms of MTX resistance? (3)
1) Block transport
2) Block polyglutamation
3) Overexpress DHFR
What are the two metabolites of fluorouracil? How do they interfere with cancer?
F-dUMP -> inhibits thymidylate synthase

F-UTP -> interferes with RNA synthesis
What is the exclusive use of fluorouracil?
Exclusively used for SOLID TUMORS, most notable example is actinic keratoses
What is the most important antimetabolite drug for the treatment of AML?
Cytarabine
Which leukemia is associated with the philadelphia chromosome?
CML
What are the main side effects of 5-FU? (2)
1) Myelosupression

2) Mucosal damage
A 45 yo man is diagnosed with AML. He is treated with two antimetabolite drugs, one for induction and one for maintenance. What are they?
Induction: cytarabine

Maintenance: 6-thioguanine
What drug is used for the maintenance of ALL?
6-Mercaptopurine
What is 6-mercaptopurine an analogue of?
hypoxanthine
What was the first agent used to "cure" a cancer? Which cancer?
MTX -> choriocarcinoma
You learned one drugs for the maintenance of ALL and one for the maintenance of AML. What are they?
ALL: 6-mercaptopurine

AML: 6-thioguanine
How do anthracyclines work? (3)
1) Most important: inhibits topoisomerase II

2)Intercalating agent

3) Quinone moieties -> free radicals
What is the suffix of anthracyclines?
-rubicin
What are the 2 anthracyclines that we learned?

Which one is broad spectrum, and which one is narrow spectrum?
Narrow spectrum: daunorubicin

Broad specturm: doxorubicin
What is the primary use of daunorubicin?
non-lymphoytic leukemias
What is the most important side effect of the anthracyclines?
Cumulative, dose-related cardiac damage.

Also causes total hair loss
Which drug is the best antimetabolite for most breast cancers?
Doxorubicin
How does bleomycin work?
Bleomycin binds iron -> forms psudoenzyme -> generates free radicals -> fragments DNA
What stage of the cell cycle does bleomycin work best in?
Bleomycin works best in G2, but actually works in all the phases even in non-dividing cells (ie, G0)
How broad of a spectrum does bleomycin have?
Very broad
What is the main toxicity of bleomycin?
Pulmonary fibrosis.

FYI, bleomycin does NOT cause myelosuppression
How do vinca alkaloids work?
Bind to tubulin monomers, preventing polymerization.
What is the difference between taxol and the vince alkaloids?
Taxol -> binds tubulin polymers -> prevents depolymerization

Vinca alkaloids -> bind tubulin monomers -> prevent polymerization
What is the one thing that vinca alkaloids and taxol have in common?
Both act exclusively on the M phase, because mitosis is the point in the cell cycle most dependent on microtubule fxn.
What are the two vinca alkaloids that we learned?
Vincristine
Vinblastine
What are the main side effects of the vinca alkaloids?
VinBLASTine -> BLASTS your bone marrow (dose-related myelosuppression)

VinCRISTine -> angers the nerves in your hands and feet, much like crucifiction would (peripheral neuropathy)
What is the most important use of taxol?
Metastatic breast and ovarian cancers
What are the side effects of taxol? (4)
Bone marrow suppression
Peripheral neuropathy
Fibromyalgia
Alopecia
How does tamoxifen work?
anti-estrogen
What drug is better than tamoxifen in chemoprevention in early stages of breat cancer?
anastrazole
How does anastrazole work?
Inhibits aromatase -> blocks conversion of testosterone to estrogen
Aside from chemoprevention, what is the other main use of anastrazole?
Adjuvant treatment for metastatic breast cancer in post-menopausal women
Which drug is an androgen antagonist?
flutamide
What cancer does flutamide treat?
prostate cancer
Which cancers does IL-2 treat? (3)
Renal cell carcinoma
Melanoma
Colorectal cancer
What is the main side effect of herceptin?
Cardiotoxicity
Which molecule on NSCLC is a target of newer mechanism-based anticancer agents?
EGFR (a tyrosine kinase)
What two newer mechanism-based anticancer agents can treat NSCLC?
Iressa (small molecule)
Erlotinib (small molecule)
Which of the two EGFR antagonists has DEMONSTRATED efficacy against NSCLC?
Iressa
What population is iressa most effective in? Why?
Asians -> due to higher rates of EGFR mutations
What sort of drug is iressa?
Small molecule inhibitor of EGFR
What sort of drug is erlontinib?
Small molecule inhibitor of EGFR
Which drug is an angiogenesis inhibitor?
Avastin
What cancers are susceptible to avastin?
Metastatic colon and rectal cancers
What drug is a general tyrosine kinase antagonist?
Gleevac (imatinib)
What is the generic name for Gleevac?
Imatinib
Which tyrosine kinases are targeted by imatinib? (3)
Bcr-Abl

c-kit

PDGF-R
Which tumors are targeted by Gleevac? (3)
CML (Bcr-abl)

GIST (c-kit)

Glioblastoma (PDGF-R)
What are the main side effects of Gleevac? (3)
Muscle cramps

Diarrhea

RASH
Which cells have CD20?
B cells
What monoclonal antibody targets CD20?
Rituximab
What diseases are treated by anti-CD20?
B cell lymphomas
What diseases are treated by rituximab?
B cell lymphomas
Which cells have CD33?
Cells of the myeloid/monocyte lineage
What monoclonal antibody targets CD33?
Gemtuzumab
What diseases are treated by anti-CD33?
CD33+ AML
What diseases are treated by gemtuzumab?
CD33+ AML
What is the monoclonal antibody against EGF-R?
Cetuximab
What are anti-EGF-R antibodies used to treat?
Colorectal cancers (not NSCLC, that’s iressa and erlotinib)