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Cancer Drugs MOD 254
OUCOM cancer drug information to know
78
Health Care
Professional
09/17/2011

Additional Health Care Flashcards

 


 

Cards

Term
EPO
Definition

Erythropoietin, Epoetin, Epogen

 

glycoprotein hormone,

produced naturally in kidney(90%) & liver(10%)

 

Used for: Anemias (NOT TO USE in erythroid-base cancer)

 

Mechanism: controls RBC production, cytokine for RBC production in bone marrow

Term
G-CSF
Definition

Filgrastam

 

produced naturally by immune cells

 

stimulates the production of neutrophiles

 

NO USE in leukemias

Term
GM-CSF
Definition

Sargramostim, Leukine

 

produced by activated T-Cells, B-Cells, mast cells, & macrophages

 

stimulates production of monocytes and granulocytes

Term
Filgrastam
Definition

G-CSF

 

NO USE in leukemias

 

stimulates the production of neutrophiles

Term

Sargramostim 

 

Leukine

Definition

GM-CSF

 

stimulates the production of monocytes and granulocytes

Term
cyclophosphamide
Definition

Alkylating Agent

 

(Nitrogen Mustard)

 

mechanism: irreversible DNA changes

(including in cross-linking)

Also changes in RNA and proteins

 

important side effects: Mutagenic, Teratogenic, carcinogenic

Term
Alkylating Agents
Definition

cytotoxic.


Drug: Cyclophosphamide (nitrogen mustard)


Mechanism:inhibit cell division by reacting with DNA

Term
Methotrexate
Definition

Anti-Metabolite

 

mechanism:  folic acid analog, inhibits dihydrofolate reductase, slows DNA/RNA synthesis, inhibits protein synthesis

Term
Anti-Metabolite
Definition

Methotrexate, Thiopurines (mercaptopurine, azathioprine, 6-thioguanine), Fluorouracil

 

mechanism:  inhibit metabolite use, resulting in halting of cell division or cell growth

Term
Thiopurines
Definition

Anti-Metabolite

 

Mercaptopurine (6-MP)

Azathioprine

6-Thioguanine (6-TG)

 

used in: acute leukemia & chronic myelogenous leukemia

 

mechanism: must be activated by purine salvage pathway, induce mutations by pairing with C & T, inhibit de novo purine synthesis

 

High incidence of therapy induced cancer associated

 

TPMT enzyme test must be done before therapy

Term
Mercaptopurine
Definition

Anti-Metabolite, Thiopurine

 

used in: acute leukemia & chronic myelogenous leukemia

 

mechanism: must be activated by purine salvage pathway, induce mutations by pairing with C & T, inhibit de novo purine synthesis

 

High incidence of therapy induced cancer associated

 

TPMT enzyme test must be done before therapy

Term
Azathioprine
Definition

 

Anti-Metabolite, Thiopurine

 

used in: acute leukemia & chronic myelogenous leukemia

 

mechanism: must be activated by purine salvage pathway, induce mutations by pairing with C & T, inhibit de novo purine synthesis

 

High incidence of therapy induced cancer associated

 

TPMT enzyme test must be done before therapy

 

Term
6-Thioguanine
Definition

 

Anti-Metabolite, Thiopurine

 

used in: acute leukemia & chronic myelogenous leukemia

 

mechanism: must be activated by purine salvage pathway, induce mutations by pairing with C & T, inhibit de novo purine synthesis

 

High incidence of therapy induced cancer associated

 

TPMT enzyme test must be done before therapy

 

Term
Fluorouracil (5-FU)
Definition

Anti-metabolite

 

Mechanism: blocks thymidylate synthase

works as a pyrimidine analog

Converted to FdUMP, FdUTP, or FUTP

 

Term
FdUMP
Definition

fluorodeoxyuridine monophosphate

 

inhibits thymidylate synthase by blocking access of dUMP

 

causes dNTP imbalance and high dUTP levels, leading to DNA damage

Term
FdUTP
Definition

fluorodeoxyuridine triphosphate

 

incorporated into DNA

 

induces nucleotide  excision repair, which is futile in the presence of high concentration of FdUTP/dTTP.  this leads to DNA strand breaks and cell death

Term
FUTP
Definition

incorporates into RNA

 

inhibits many processes like:

- processing of mRNA into mature RNA

-modification of tRNA

 

profound effects on cell metabolism and viability

Term
Vinblastine
Definition

Vinca Alkaloid

 

isolated from vinca rosa shrub

 

mechanism: targets microtubules. bind tubulin and prevent mitotic spindle formation = "metaphase arrest"

Term
Vinca Alkaloids
Definition

Vinblastine

 

mechanism: targets microtubules. bind tubuulin and prevent mitotic spindle formation = "metaphase arrest"

 

Term
Taxoids
Definition

paclitaxel/Taxol

 

isolated from yew tree bark

 

used for: metastatic cancer of breast and ovary

 

mechanism:  induces polymerization/stabilization of microtubules

Term

Taxol

 

Paclitaxel

Definition

Taxoids

 

isolated from yew tree bark

 

used for: metastatic cancer of breast and ovary

 

mechanism:  induces polymerization/stabilization of microtubules

 

 

Term
Streptomyces-derived Anti-biotics
Definition

Actinomycin D

 

Doxurubicin (Adriamycin)

 

Mitomycin

 

Bleomycin

Term
Actinomycin-D
Definition

Streptomyces-derived Antibiotic

 

mechanism:  intercalates in DNA and inhibits transcription and DNA synthesis

Term
Doxorubicin
Definition

 (adriamycin)

 

Streptomyces-derived Antibiotic

 

mechanism: intercalates in DNA

 

Term
Mitomycin
Definition

Streptomyces-derived Antibiotic

 

mechanism: after intracellular synthesis, reacts with DNA and inhibits synthesis

Term
Bleomycin
Definition

Streptomyces-derived Antibiotic

 

mechanism:  chelates metal ions --> produces superoxide and hydroxide-free radicals which leads to DNA cleavage, lipid (and other) peroxidation

Term
Camptothecins
Definition

Topotecan / Irinotecan


isolated from camptoteca acuminata (happy tree)

 

mechanism:  inhibits topoisomerase I which leads to single-strand breaks in DNA 

inhibits replication and transcription


Term
Topotecan / Irinotecan
Definition

Camptothecins

 

isolated from camptoteca acuminata (happy tree)

 

mechanism:  inhibits topoisomerase I which leads to single-strand breaks in DNA 

inhibits replication and transcription

Term
Epipodophyllotoxins
Definition

etopside / teniposide

 

isolated form mayapple plant

 

mechanism: inhibits topoisomerase II, which leads to double strand breaks in DNA

causes erroer during DNA replication and eventual apoptosis

Term

etopside

 

teniposide

Definition

 Epipodophyllotoxins

 

isolated form mayapple plant

 

mechanism: inhibits topoisomerase II, which leads to double strand breaks in DNA

causes erroer during DNA replication and eventual apoptosis

Term
Cisplatin
Definition

lance armstrong used successfully

 

mechanism:  intra-interstrand crosslinks in DNA

Term
Arsenic Trioxide (As2O3)
Definition

used for:  acute promyelocytic leukemia (APL)

 

mechanism: it works

 

used in combination with  ATRA (all trans retinoic acid)

Term
Asparaginase
Definition

conjugated to PEG and derived from bacteria

 

mechanism:  suppress leukemia by lowering ammonia levels

 

Asn --> Asp + NH3

--Asn(asparagine) levels are depleted

 

( ALL leukemic cells are unable to synthesize the non-essential amino acid asparagine, whereas normal cells are able to make their own asparagine; thus leukemic cells require high amount of asparagine. These leukemic cells depend on circulating asparagine. Asparaginase, however, catalyzes the conversion of L-asparagine to aspartic acid and ammonia. This deprives the leukemic cell of circulating asparagine.)

Term
Sex Hormones
Definition

Androgens

 

Anti-Androgens

 

Estrogen

 

Anti-Estrogens

 

Anti-Androgens and Anti-Estrogens used more than androgens and estrogens

Term
Androgen
Definition

Sex Hormone

 

used for: metastatic breast cancer

 

(not used much because may be bad)

Term
Anti-Androgen
Definition

Sex Hormone

 

example:  Flutamide

 

used for: prostate carcinoma

Term
Flutamide
Definition

 

 

Anti-Androgen Sex Hormone

 

used for: prostate carcinoma

 

 

Term
Estrogen
Definition

Sex Hormone

 

Mechanism:  Give a very high dose = toxicity

 

used for:  postmenopausal breast cancer; prostate cancer

 

not used often beause may be bad

Term
Anti-Estrogen
Definition

 

Sex Hormone

 

example:  Tamoxifen

 

used for: post menopausal breast cancer; metastatic melanoma (this use is controversial and under trial)

 

Term
Tamoxifen
Definition

 

Anti-Estrogen Sex Hormone

 

used for: post menopausal breast cancer; metastatic melanoma (this use is controversial and under trial)

 

Term
Letrozole
Definition

Aromatase inhibitor

 

used for: advanced breast cancer

 

mechanism:  prevents the conversion of testosterone to estradiol

Term
Aromatase inhibitor
Definition

Letrozole

 

used for: advanced breast cancer

 

mechanism:  prevents the conversion of testosterone to estradiol

(Aromatase is the enzyme that does the conversion)

Term
Fulvestrant
Definition

Selective Estrogen receptor downregulators

 

used for:  tamoxifen resistant patients

 

mechanism: destruction of estrogen receptors

Term
Selective Estrogen receptor downregulators
Definition

Fulvestrant

 

used for:  tamoxifen resistant patients

 

mechanism: destruction of estrogen receptors

Term
what drug should you use if your patient is resistant to tamoxifen?
Definition

FULVESTRANT

 

(a selective estrogen receptor downregulator)

Term
Retinoic Acid Receptor Drugs
Definition

Tretinoin

 

Alitretinoin

 

Bexarotene

Term
Tretinoin
Definition

Retinoic Acid Receptor Drugs

 

used for:  acne vulgaris, keratosis pilaris, anti-aging and wrinkle cosmetics

 

mechanism: acid form of vitamin A; All-trans retinoic acid (ATRA)

 

negative effects: teratogen, skin irritation, sun-sensitive

Term
Alitretinoin
Definition

Retinoic Acid Receptor Drugs

 

used for: AIDS-related kaposi's sarcoma; severe chronic hand eczema

 

mechanism:  targets RAR and RXR

Term
Bexarotene
Definition

Retinoic Acid Receptor Drugs

 

used for: cutaneous t-cell lymphoma; lung cancer; breast cancer; kaposi's sarcoma

Term
Imatinib (Gleevec)
Definition

used for: Ph+ chronic myeloid lymphoma;

Ph+ Acute Lymphocytic Leukemia; GI stromal tumors

 

ASSOCIATION: Philadelphia Chromosome

 

mechanism:  tyrosine kinase inhibitor.

targets:

Abl (intracellularly); cKit and PDGFR (surface receptors)

 

Term
Which drug should be used on patients with a Ph+ philadelphia chromosome mutation?
Definition
Imatinib (Gleevec)
Term

what is the difference between

-mab and -nib?

Definition

-mab = monoclonal antibody

 

-nib = kinase inhibitor

Term
Trastuzumab
Definition

Herceptin

 

used for: breast cancers with HER2 amplification

 

mechanism: anti-HER2 antibody

 

dose: IV every week during chemo and once every 3 weeks after chemo/surgery

 

cons: cardiac dysfunction (must be checked routinely)

Term
Herceptin
Definition

(Trastuzumab)

 

used for: breast cancers with HER2 amplification

 

mechanism: anti-HER2 antibody

 

dose: IV every week during chemo and once every 3 weeks after chemo/surgery

 

cons: cardiac dysfunction (must be checked routinely)

Term
Drugs used in HER2 amplified breast cancer
Definition

Trastuzumab (Herceptin)

 

and

 

Lapatinib

Term
Lapatinib
Definition

used for: breast cancers with HER2 amplification

 

mechanism:  HER2/Neu and EGFR kinase inhibitor

 

dose: Pill taken daily

 

cons: nausea/vomiting/heartburn/fatigue

Term
Erlotinib (tarceva)
Definition

used for:  advanced non-small-cell lung cancer (NSCLC)

 

mechanism:  EGFR kinase inhibitor

 

PROs: + 3 months of life

 

CONs: rash, diarrhea, fatigue

Term

Gefitinib (Iressa)

 

Definition

used for: advanced NSCLC

 

mechanism: EGFR kinase inhibitor

 

cons: acne, diarrhea, nausea, vomiting

Term
Drugs used for NSCLC
Definition

Erlotinib (Tarceva)

 

and

 

Gefitinib (Iressa)

 

and 

 

Bevacizumab (Avastin)

Term
Cetuximab (Erbitux)
Definition

used for: squamous cell carcinoma and colon cancer 

 

mechanism: prevents EGF binding

monoclonal antibody

 

***ONLY USED IN PATIENTS THAT DON'T HAVE A KRAS MUTATION***

(this is tested for before therapy can begin)

Term
Angiogenesis Inhibitors
Definition

Bevacizumab (Avastin)

 

Sunitinib (Sutent)

 

Sorafenib (Nexavar)

Term
Bevacizumab (Avastin)
Definition

Angiogenesis Inhibitor

 

used for:  NSCLC; metastatic colorectal cancer; age-related macular degeneration

 

mechanism: VEGF antibody

(prevents VEGF from binding to its receptor)

 

CONs: risk of bleeding, bowel perforation

 

*** was approved for metastatic breast cancer, but this was revoked in 2010***

Term
Sunitinib (Sutent)
Definition

Angiogenesis Inhibitor

 

used for: Renal Cell Carcinoma (RCC) and Imatinib-resistant GI stromal tumors

 

Mechanism: inhibitor or VEGFRs, PDGFR, and cKit

Term
Sorafenib (Nexavar)
Definition

used for: Advanced Renal cell Carcinoma (RCC); unresectable hepatocellular carcinoma

 

mechanism: inhibitor of VEGFR2, VEGFR3, PDGFR, cKit, Raf-1, B-Raf

Term
Vemurafenib (Zelboraf)
Definition

used for: late stage melanoma

 

mechanism:inhibits v600e b-raf, not the wild-type b-raf

(60% of melanomas have the v600e b-raf mutation)

 

***this is a brand new drug***

Term
Bortezomib (Velcade)
Definition

used for: multiple myeloma

 

mechanism:  inhibits active-site for 26S proteasome

Term
DNA Demethylating Agents
Definition

Azacitidine (Vidaza)

 

and 

 

5-Aza-2-deoxycytidine (Decitabine)

 

Term

Azacitidine (Vidaza)

 

Definition

DNA Demethylating Agent

 

used for: myelodysplastic syndrome (pre-leukemia)

 

mechanism: DNA incorporation (direct and irreversible)

inhibition of DNA methyltransferase

incorporates into RNA

"reactivates" tumor suppressor genes

 

 

Term

5-Aza-2-deoxycytidine (Decitabine)

 

 

Definition

DNA Demethylating Agent

 

used for: myelodysplastic syndrom (pre-leukemia)

 

mechanism: DNA incorporation (direct and irreversible)

inhibition of DNA methyltransferase

"reactivates" tumor suppressor genes

Term
Vorinostat/SAHA (Zolinza)
Definition

Histone deacetylase inhibitor

 

used for: cutaneous t-cell lymphoma

Term
Romidepsin (istodax)
Definition

Histone deacetylase inhibitor

 

isolated from chromobacterium violaceum

 

used for: cutaneous t-cell lymphoma

Term

Histone deacetylase inhibitors

Definition

Vorinostat/SAHA (Zolinza)

 

and

 

Romidepsin (Istodax)

Term
Levamisole
Definition

used for: colon cancer, melanoma, head, neck cancers

 

mechanism:  non-specific immunostimulatory properties

 

CONs: inflammatory destruction of RBC, leukocyte suppression

 

***not in US market, also, seen as a cocaine cutting agent***

Term

Cutaneous T-Cell Lymphoma Drugs

 

(4)

Definition

Retinoid Bexatene (RXR)

 

Denileukin difitox/Onkak

-immunotoxin

-IL-2 conjugated Diptheria toxin

 

Vorinostat/SAHA (Zolinza)

-histone deacetylase inhibitor

 

Romidepsin (Istodax)

-histone deactetylase inhibitor

 

Off label:  Methotrexate (retards DNA, stops proteins)

Cyclophosphamide (crosslinks guanines) = lowered immunoresponse

 

 

Term
Sipuleucel-T (provenge)
Definition

used for:  metastatic castration-resistant prostate cancer

 

mechanism:  autologous cellular immunotherapy "cancer vaccine"

1)leukocytes extracted (esp. APC)

2)sent to company, fused with PAP and GM-CSF

-APC's mature

3)reintroduced into the patient

 

PROs: 4-month gain

Term
Ipilimumab
Definition

used for: late-state melanoma (in clinical trials for prostrate and lung)

 

mechanism: human monoclonal antibody

blocks CTLA-4 

-CTLA-4 makes sure t-cell isn't always active

 

CONs:  potentially fatal immunological adverse effects, GI effects, fever

Term
Denileukin Difitox (Ontak)
Definition

used for: cutaneous T-cell Lymphoma

 

mechanism: Immunotoxin

IL-2 conjugated to diptheria toxin

block of protein synthesis

Term

Brentuximab vedotin (Adcetris)

 

Definition

used for: hodgkins lymphoma; systematic anaplastic large-cell lymphoma

 

mechanism:  antibody conjugated to toxin

targets CD30; stable in blood, cleaved in cell

blocks polymerization of tubulin which leads to halting of cell division

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