Hematology & Oncology: Microtubule Targeting Agents

Front 1

4 classes of Microtubule Targeting Agents?

Back 1

-vinca alkyloids
-taxanes
-epothilones
- and estramustine

Front 2

Vinca alkaloids?

Back 2

vincristine, vinblastine, vindesine, vinorelbine

Front 3

Taxanes?

Back 3

paclitaxel, docetaxel

Front 4

Epothilones?

Back 4

ixabepilone

Front 5

The microtubule structure is composed of?

Back 5

α- and β- heterodimers

Front 6

All anti-micotubular drugs are ___phase specific?

Back 6

M phase

Front 7

Microtubules are required for?

Back 7

cell shape, transport of vesicles, signaling and mitosis

Front 8

Vinca alkyloids based on the catharanthine stucture?

Back 8

vincristine, vinblastine, vindesine,

Front 9

Vinca alkyloids based on the induline stucture?

Back 9

vinorelbine

Front 10

Vinca alkyloids can cause neuropathy due to?

Back 10

Neuron sensitivity to drugs that affect microtubules

Front 11

Vinca alkyloid MOA?

Back 11

binds β-tubulin, blocking its ability to polymerize with α-tubulin into microtubules
• M phase-specific

Front 12

Vinca alkyloids are extensively metabolized by?

Back 12

CYP-3A4

Front 13

Vinca alkyloids require?

Back 13

dose reduction for hepatic impairment

Front 14

Vinblastine is given IV and is used to treat?

Back 14

Lymphomas, lung cancer, prostate cancer and melanoma

Front 15

Vinblastine is also a strong ______?

Back 15

Vesicant

Front 16

Vincristine is given IV and is used to treat?

Back 16

ALL, Lymphoma and pediatric solid timors

Front 17

The major toxicity associated with Vincristine is?

Back 17

neuropathy

Front 18

True or false, vincristine is not a vesicant like vinblastine?

Back 18

false, vincristine and vinblastine are both vesicants

Front 19

True or false, all vinca alkyloids are potent 3A4 inhibitors that require dose adjustments for hepatic impairment?

Back 19

True

Front 20

Vinca alkaloids are derivatives of the sap from the _______________?

Back 20

Madagascar periwinkle

Front 21

Taxanes are derived from the?

Back 21

Western yew tree

Front 22

Modifying the R1 and R2 groups on taxanes makes the drugs more ____and_____.

Back 22

water soluble and poten

Front 23

The MOA of taxanes?

Back 23

Bind Beta-tubulin subunit, thus promoting polymerization

Front 24

The taxane structure responsible for activity is the?

Back 24

8 membered hexane ring

Front 25

Paclitaxel is used to treat?

Back 25

breast, lung, ovarian and head and neck cancer

Front 26

The IV vehicle for Paclitaxel is?

Back 26

50%ehtanol and 50% polyethoxylated castor oil (CREMOPHOR EL)

Front 27

Albumin bound Paclitaxel is?

Back 27

Abraxane

Front 28

Paclitaxel pharmacokinteics are?

Back 28

Non-linear (dose-dependent)

Front 29

Myelosuppression due to Paclitaxel treatment is alleviated by?

Back 29

Filgrastim (NEUPOGEN) a granulocyte colony-stimulating factor (G-CSF) analog

Front 30

Hypersensitivity reactions (e.g. dyspnea, chest pain,
hypotension) caused by paclitaxel can be prevented by?

Back 30

dexamethasone and antihistamines

Front 31

The vehicle in Docetaxel is?

Back 31

polysorbate 80

Front 32

Docetaxel is used to treat?

Back 32

Lung, prostate, ovarian, breast and head and neck cancers

Front 33

The primary clinical toxicity associated with Decetaxel is?

Back 33

Severe myelosuppression

Front 34

Ixabepilone MOA?

Back 34

binds to β-tubulin, promoting the
polymerization of microtubules

Front 35

Ixabepilone is used to treat?

Back 35

breast cancer

Front 36

True or false, all plant derived microtubule drugs are potent 3A4 inhibitors?

Back 36

True

Front 37

The non-plant derived antimicrotubule is?

Back 37

Estrmustine

Front 38

The antimicrotubule in oral dosage is?

Back 38

Estrmustine

Front 39

Estramustine is based on?

Back 39

Estradiol

Front 40

Estramustine is used to treat?

Back 40

prostate cancer

Front 41

The functional group on estramustine is?

Back 41

a nitrogen mustard
-however, estramustine does not function as a nitrogen mustard. The function is that of a microtubule inhibitor