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Pharmacology- Test 2 Material > 09- Antineoplastics > Flashcards

09- Antineoplastics Flashcards

1
Q

capecitabine

A

Pyrimidine Antagonist (anti-tumor anti-metabolite)

-Converted to 5-FU (prodrug) via thymidine phosphorylase.

+thymidine phosphorylase is found in higher concentration in tumor cells.

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2
Q

HER2- positive

A

HER2 is an epidermal growth factor over expression in breast cancer

lapatinib-HER2 kinase inhibitor

trastuzumab- humanized HER2 antibody

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3
Q

tumor suppressor

A

block or suppress development of cancer helps regulate cell division

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4
Q

cytosine arbinoside (cytrabine)

A

Pyrimidine Antagonist (anti-tumor anti-metabolite)

  • resembles CTP and is incorporated into DNA leading to damage.
  • Activation by deoxycytidine kinase.
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5
Q

oncogene addiction

A

tumor cells proliferation becomes dependent upon activated oncogenes

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6
Q

RALOXifene (Evista)

A
  • antagonist of hormone action
  • selective estrogen response modulator (SERM)
  • approved for prevention of breast cancer in patients with osteoporosis
  • less adverse effects noted
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7
Q

flutamide

A
  • antagonist of hormone action, specifically androgen receptor
  • ineffective when used alone in prostate CA d/t rapid androgen receptor mutation
  • used in conjunction with leuprolide to block effects of the initial pulse androgen levels and associated “flare” of prostate CA at the start of leuprolide therapy
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8
Q

methchlorethamine

A

Anti-tumor alkylating Agent (bischlorethyl amine).

  • nitrogen mustard
  • highly reactive alkylating agent (must be given IV).
  • chlorethyl groups are elctrophilic and react with nucleophils. Leads to DNA cross-linkage.
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9
Q

cyclophosphamide

A

Anti-tumor alkylating Agent (bischlorethyl amine).

  • PO prodrug of methclorethamine; less reactive.
  • chlorethyl groups are elctrophilic and react with nucleophils. Leads to DNA cross-linkage.
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10
Q

DHFR- dihydrofolate reductase

A

inhibited by methotrexate normally converts FH2 into FH4

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11
Q

leuprolide

A
  • antagonist of hormone action
  • synthetic analog of GnRH, a GnRH-R agonist
  • continuous, high dose treatment greatly lowers androgen levels in men and estrogen levels in women
  • high doses cause down regulation of receptors and system for hormone production shuts down
  • as effective as estrogen therapy or orchiectomy in treatment of prostate CA with fewer s/fx
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12
Q

vinCRISTINE (Oncovin)

A
  • mitotic spindle poison that is a vinca alkaloid
  • M Phase specific
  • DOSE LIMITING: neurotoxicity (no acute side effects and milder, non-dose limiting bone marrow suppression
  • uses: acute childhood leukemia
  • Hodkin’s Disease M”O”PP regimen (Oncovin= vincristine)
  • resistance by tubulin gene mutations
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13
Q

EGF receptor protein tyrosine kinase

A

overexpressed/mutationally activated in various cancers (lung, brain, head and neck)

-over expression and overactivity increases tumor growth

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14
Q

HER2 protein tyrosine kinase

A

(EGF receptor related) overexpressed/activated in various cancers causing aggressive tumor growth

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15
Q

DAUNOrubicin

A
  • anti-tumor antibiotic (Anthracycline) AND topoisomerase II inhibitor
  • DNA intercalation (mutagenic, carcinogenic)
  • DNA topoisomerase II binding (double-strand break), DNA scission
  • widely used with broad spectrum of activity
  • DOSE LIMITING: irreversible cardiac toxicity at high doses
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16
Q

bleomycin

A
  • anti-tumor antibiotic
  • cytotoxicity from DNA strand scission
  • DOSE LIMITING: pulmonary toxicity (pulmonary fibrosis) at large doses (fibrosis with 100% O2)
  • no significant myelosuppression so useful in combination therapies (A”B”VD, in Hodgkin Lymphoma)
  • can cause anaphylaxis so give small doses at first
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17
Q

letrozole

A
  • antagonist of hormone action
  • AROMATASE inhibitor that inhibits conversion of androgens to estrogen
  • effectively blocks estrogen production in POSTMENOPAUSAL women
  • not used in premenopausal women because of compensatory gonadotropin and ovarian estrogen production
  • MORE effective than tamoxifen in treatment of ER+ breast cancers in postmenopausal women
  • no enhanced risk of thrombosis or uterine cancer
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18
Q

tumor growth fraction

A

fraction of cells not in G0 cells that are actually dividing responsive to conventional chemotherapy

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19
Q

neoadjuvant

A

chemotherapy is given before surgery

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20
Q

trastuzumab (Herceptin)

A

Targeted agent

  • “humanized” HER2 antibody that recognizes surface antigen HER2 that is elevated in many breast tumors
  • effective against in HER2+ breast cancers
  • direct tumor cell effects and immune system mediated effects
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21
Q

Normal cells susceptible to toxic side effects

A

bone marrow–myelosuppression

intestinal epithelial– N/V oral mucosa

gonadal cells– infertility

hair follicles

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22
Q

estrogen receptor status

A

presence of estrogen receptors in breast cancer tissue predicts benefit of tamoxifen treatmen

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23
Q

nitrosoureas

A
  • Alkylating agents -can cross BBB and useful against brain tumors.
  • BCNU, CCNU, methyl-CCNU.
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24
Q

erlotinib (Tarceva)

A

Targeted agent

  • EGFR KINASE INHIBITOR
  • used to treat non-small cell lung cancer, head/neck cancer
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25
Q

deoxycytidine kinase

A

required to activated cytarabine (cytosine arabinoside) mutational loss is a mechanism of resistance

26
Q

vinBLASTINE

A
  • mitotic spindle poison that is a vinca alkaloid
  • M Phase specific action
  • inhibitor of microtubule polymerization (mitotic arrest)
  • DOSE LIMITING: bone marrow suppression
  • used in combination therapy (AB”V”D in Hodgkin Lymphoma)
  • resistance by tubulin gene mutations which cause mitotic spindles to have less binding affinity for drug
27
Q

cisplatin

A

Pt Coordination Complex

  • Cell-cycle nonspecific, DNA cross-linking.
  • nephrotoxic, acoustic nerve injury.
28
Q

“targeted” agent

A

inhibit the function of activated oncogenes or proteins necessary for tumor cell proliferation and tumor angiogenesis

29
Q

6-thioguanine

A

Purine Antagonist (anti-tumor anti-metabolite)

  • S-Phase specific
  • incorporated into DNA/RNA via DNA polymerase.
  • Activated by hypoxanthine-guanine phosphoribosyl transferase (HGPRT).
  • Not inactivated by xanthine oxidase.
30
Q

TOPOtecan

A
  • topoisomerase I inhibitor that is a camptothecin
  • bind to “cleavable complex” of DNA topoisomerase I and DNA, block religation of single-strand break
  • double strand breaks occur with DNA replication
  • S Phase-specific

***(Grayed out on slide)- Uses: ovarian and lung cancers and Dose Limiting: myelosuppression

31
Q

imatinib (Gleevac)

A

Targeted agent

  • inhibitor of abl protein tyrosine kinase (and activated bcr/abl fustion)
  • approved for chronic myelogenous leukemia (bcr/abl mutation) (activated bcr/abl protein tyrosine kinase arises from gene rearrangement/fusion in chronic myelogenous leukemia
32
Q

procarbazine

A

Alkylating agent: Misc

  • metabolized to alkylating free radicals.
  • part of MOPP Tx for Hodgkin’s
  • Leukemogenic in 5-10% of pt receiving MOPP therapy.
33
Q

TAMOxifen

A
  • antagonist of hormone action
  • Selective estrogen response modulator (SERM)
  • PARTIAL AGONIST of estrogen receptor (some competitive inhibition) (efficacy depends on tissue)
  • low toxicity and manageable side-effects
  • Uses: estrogen-responsive tissues (female/male breast; uterine endometrium)
  • presence of estrogen receptor in breast cancer predicts efficacy in treatment
  • prophylactic treatment has been suggested in high risk women but may not prolong life span
  • reduce risk of bone fractures in postmenopausal women
  • enhanced risk of thrombosis or uterine cancer
34
Q

methotrexate

A

Anti-tumor anti-metabolite

  • dihydrofolate reductase inhibitor (inhibit the synthesis of FH4 from FH2).
  • S-Phase specific
  • Myelosuppression
  • Can be “reversed” with leucovorin (increases FH4)
35
Q

cell cycle

A

mitosis, cell divison

36
Q

microtubule

A

tubulin required for M phase cell divison

37
Q

leukemogenic

A

relating to the development of leukemia side effect of procarbazine

38
Q

alkylating agent

A

add an alkyl group to the DNA causing breakage and cell death

39
Q

prednisone

A

Adrenocorticosteroid

  • induces apoptosis in leukemia cells
  • used in drug regimens for leukemia, lymphoma, myeloma
  • does not cure leukemia but useful for inducing remission in childhood
  • palliative agent in other cancers (reduce inflammation, N/V)
40
Q

6-mercaptopurine

A

Purine Antagonist (anti-tumor anti-metabolite)

  • S-Phase specific
  • incorporated into DNA/RNA via DNA polymerase.
  • Activated by hypoxanthine-guanine phosphoribosyl transferase (HGPRT).
  • Inactivated by xanthine oxidase

+high xanthine oxidase in cow’s milk

+allopurinol decreases xanthine oxidase.

41
Q

oncogene

A

gene that can convert a normal cell into a tumor cell

42
Q

HGPRT- hypoxanthine-guanine phosphoribosyl transferase

A

converst purine antagonist to NMPs, and NTPs

-down regulation of enzyme is common mechanism of resistance

43
Q

exemestane

A
  • antagonist of hormone action
  • AROMATASE inhibitor that inhibits conversion of androgens to estrogen
  • effectively blocks estrogen production in POSTMENOPAUSAL women
  • not used in premenopausal women because of compensatory gonadotropin and ovarian estrogen production
  • MORE effective than tamoxifen in treatment of ER+ breast cancers in postmenopausal women
  • great reduction in Breast CA in high risk PostM women
  • no enhanced risk of thrombosis or uterine cancer
44
Q

M phase-specific

A

Mitotic phase Cell Divison

45
Q

therapeutic index

A

TD50/ED50 low in chemotherapeutic

46
Q

etoposide

A
  • topoisomerase II inhibitor
  • form ternary complex with toposisomerase II and DNA -interfere with religation of double-strand break
  • DNA strand scission
47
Q

brentuximab vedotin (Adcetris)

A

Targeted agent

  • targets CD30 surface antigen of some Hodgkin and Non-Hodgkin lymphomas
  • chimeric IgG conjugated to highly toxic mitotic spindle poison vendotin with cleavable linker
  • upon binding to CD30-positive tumor cells, vedotin is internalized and cleaved to release toxin
48
Q

paclitaxel (Taxol)

A
  • mitotic spindle poison
  • plant alkaloid (western yew)
  • enhances tubulin polymerization (blocks microtubule disassembly)
  • disassembly block triggers cell death
  • uses: ovarian and advanced breast cancers
49
Q

xanthine oxidase

A

metabolically inactivates 6-mercaptopurine high in cow’s milk inhibited by allopurinol (used to reduce uric acid/kidney toxicity)

50
Q

IRINOtecan

A
  • topoisomerase I inhibitor that is a camptothecin
  • bind to “cleavable complex” of DNA topoisomerase I and DNA, block religation of single-strand break
  • double strand breaks occur with DNA replication
  • S Phase-specific

***(Grayed out on slide)- Uses: colorectal cancer, and Dose Limiting: severe diarrhea

51
Q

leucovorin

A

“Folic Acid Rescue;” formyl H4-folate.

-reverses the effects of methotrexate

52
Q

lapatinib

A

Targeted Agent

  • EGFR AND HER2 kinase inhibitor
  • used in breast cancer
53
Q

5-fluorouracil

A

Pyrimidine Antagonist (anti-tumor anti-metabolite)

  • metabolite fDUMP inhibits thymidylate synthetase leading to thymineless death.
  • S-Phase specific
  • synergistic effects when administered with leucovorin
54
Q

DNA intercalation

A

insertion of molecules between the planar bases of DNA

55
Q

DOXOrubicin (Adriamycin)

A
  • anti-tumor antibiotic (Anthracycline) AND topoisomerase II inhibitor
  • DNA intercalation (mutagenic, carcinogenic)
  • DNA topoisomerase II binding (double-strand break), DNA scission
  • widely used with broad spectrum of activity
  • DOSE LIMITING: irreversible cardiac toxicity at high doses
  • most commonly used anti-tumor antibiotic
  • used in combination therapies (“A”BVD in Hodgkin Lymphoma)
56
Q

cetuximab (Erbitux)

A

Targeted agent

  • CHIMERIC EGFR ANTIBODY that prevents receptor activation
  • colon, head and neck cancer
57
Q

S phase-specific

A

synthetic phase DNA replication

58
Q

anastrozole

A
  • antagonist of hormone action
  • AROMATASE inhibitor that inhibits conversion of androgens to estrogen
  • effectively blocks estrogen production in POSTMENOPAUSAL women
  • not used in premenopausal women because of compensatory gonadotropin and ovarian estrogen production
  • MORE effective than tamoxifen in treatment of ER+ breast cancers in postmenopausal women
  • no enhanced risk of thrombosis or uterine cancer
59
Q

DNA topoisomerase

A

disconnects one or both DNA strands and allows them to unwind, also reconnects the strands drugs can interfere with reconnection

60
Q

adjuvant

A

chemotherapy used in addition to surgery

61
Q

bioactivation

A

process in which enzymes activate drugs

Pharmacology- Test 2 Material (10 decks)

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