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Disease and defense random > Anti-Tumor agents > Flashcards

Anti-Tumor agents Flashcards

1
Q

EX of alkylating agent

A

Cyclophosphamide

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2
Q

Cells with ____ are resistant to cyclophosphamide

A

High ALDH

*** hematopoietic and intestinal cells have high levels so this drug has low toxicity compare to other alkylating agents

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3
Q

Resistance to alkylating agents (3)

A
  • High levels of GSH
  • removal of alkyl group
  • cross link repair
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4
Q

Toxicity of alkylating agents (5)

A
  • hematopoietic
  • GI
  • Gonadal
  • Alopecia
  • Carcinogenesis
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5
Q

Cisplatin and analogues

A

Crosslink DNA

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6
Q

Pt compounds resistance (5)

A
  • Reduced accumulation
  • inactivation
  • increased DNA repar
  • Increased tolerance for DNA damage
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7
Q

Cisplatin toxixity

A

nephrotoxivity

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8
Q

carboplatin toxicity

A

myelosupression

platelet toxicity

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9
Q

oxaliplatin toxicity

A

sensory neuropathy

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10
Q

2 EX of antimetabolites

A
  1. Methotrexate

2. 5- fluorouracil

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11
Q

Methotrexate is a ___, ___ inhibitor of ___

A

reversible, competitive

dihydro folate reductase (DHFR)

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12
Q

MTX is metabolized to

A

polyglutamated MTX

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13
Q

MTX resistance (3)

A
  • decreased capacity to make polyglutamated MTX
  • Increased expression of DHFR
  • Mutant DHFR
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14
Q

DHFR is required for _____ synthesis

A

purine

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15
Q

5_flurouracil is a ___ analog

A

pyrimadine

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16
Q

5-FU resistance (2)

A
  • alterations in target enzyme (TS, causes dTTP depletion)

- Increased levels of TS

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17
Q

5-FU toxicity

A
  • hematological
  • GI
  • alopecia
  • derm problems
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18
Q

Topoisomerase inhibitors are derived from

A

natural products

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19
Q

Topoisomerase inhibitors inhibit

A

DNA relegation to leave DNA breakes

20
Q

camptothecins

A

Topo I and II inhibitors

21
Q

Anthracyclines

A

Topo II inhibitors (doxorubicin)

22
Q

Topoisomerase inhibitors resistance (2)

A
  • increased drug efflux

- mutations in toposiomerases

23
Q

Topo drugs toxicity

A
  • myelosupression

- secondary malignancies

24
Q

anthracyclins toxicity

A

cardiotoxicity

25
Q

2 antimicrotubule agents

A
  1. Vinca alkaloids

2. Taxanes

26
Q

Vinca alkaloids ____ microtubules

A

stabilize

27
Q

Taxanes ___ microtubules

A

de stabilize

28
Q

Vinca alkaloids resistance (2)

A
  • increased drug efflux

- mutations is tubulin that alter binding

29
Q

Vinka alkaloids toxicity (2)

A
  • NEUROTOXICITY

- myelosuppression

30
Q

Taxanes resistance (3)

A
  • drug efflux
  • mutations in tubulin
  • inhibition of apoptosis
31
Q

Taxanes toxicity (3)

A
  • myelosuppresion
  • peripheral neuropathy
  • alopecia
32
Q

Tamoxifen

A

ER inhibitor

33
Q

antiandrogens (2 examples) and action

A
  • bicalutamide, flutamide

bind to AR and inhibit function as tf

34
Q

Steroid receptor resistance

A
  • activate recptor by other mechanisms

- mutations in receptor cause drug binding to activate rather than inactivate

35
Q

mutations in receptor in response to flutamide

A
  • activate rather than inhibit
36
Q

Aromatase inhibitor (1 EX) and action

A

Letrozole

inhibit synthesis of estrogen from androgens

37
Q

Gonadotropin-releasing hormone analogues

A

leuprolide

Inhibit testosterone production

38
Q

Hormonal agents toxicities

A
  • altered steroid function
39
Q

Rituximab

A

Anti CD20 used to treat B cell tumors

  • dependent on different stages
40
Q

Trastuzumab/ Herceptin

A

Anti- Her2 breast cancer

41
Q

Bevacizumab/ Avastin

A

anti-VEGF colon cancer

42
Q

Antibody function against cancer (2)

A
  • inhibit function of target

- cell mediated toxicity

43
Q

Poster child for kinase inhibitors

A

Imatinib/Glebevec

44
Q

Imatinib treats

A

CML and GIST

Bcr-ABL translocation

45
Q

Resistance to imatinib

A

inhibitor insensitive BCR-ABL alleles (alter drug binding)

Disease and defense random (6 decks)

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