Hem/onc Test 1

Front 1

What Topo class are the camptothecin analogs?

Back 1

Topoisomerase I inhibitors

Hint 1

RM: the drugs are topotecan and irinotecan

RM: Topo I causes single stranded DNA breaks

Front 2

Topotecan and Irinotecan are in what drug class?

Back 2

Camptothecin analong --> Topo I inhibitors

Front 3

What are the 2 Topo II inhibitors? (subclasses)

Back 3

anthracycline analogs
Epipodophyyotoxins

Front 4

The 2 epipodophyllotoxins are...

Back 4

Etoposide
Teneposide

Front 5

Doxorubicin, daunorubicin, idarubicin, epirubicin, & mitoxantrone are in what subclass and class?

Back 5

subclass: anthracycline analogs

Hint 5

class: Topo II inhibitors

Front 6

Camptothecin analogs are ___ phase-specific drugs.

Back 6

S

What do they inhibit?

Hint 6

The religation of single-stranded breaks in DNA

Front 7

Brand and Cancer type for Topotecan?

Back 7

Hycamtin

(Camptothecin Analogs)

Hint 7

solid

Front 8

Topotecan undergoes hydrolysis and then the _____ opens up?

Back 8

lactone ring

Hint 8

RM dose reduction for renal impairment & short half life

Front 9

Irinotcan Class?

Back 9

Camptothecin Analogs
(Topo I inhibitor)

Front 10

Irinotecan is metabolized by hepatic carboxylesterase to _____ which is the active form.

Back 10

SN-38

Why is this less hydrolyzed?

Hint 10

bc high plasma protein binding

Front 11

Serious SE of Irinotecan?

Back 11

diarrhea

why?

Hint 11

bc high level of SN-38 in GI from beta glucorionodase reactivating it

Front 12

Anthracyclines are good for ___ tumors.

Back 12

solid

Front 13

Big SE of Anthracyclines?

Back 13

Cardiotoxicity

why?

Hint 13

bc produces toxins for H2O2 and in heart there's low dexrazoxane (and Fe chelator) and so can't prevent hydroxy radical formation

Front 14

How are anthracyclines eliminated?

Back 14

liver

(so dose adjustment needed if impaired)

Front 15

Class of Doxorubicin?

Back 15

anthracyclines

(topo II inhibitors)

Front 16

Avoid ____ in combo with Doxorubicin?

Back 16

cyclophosphamide

(also anthracyclines and herceptin)

Hint 16

can further cardiotoxicity

Front 17

This anthracycline causes infusion rxns and hand-foot syndrome...

Back 17

Doxorubicin Liposoaml

(BRAND: DOXIL)

Front 18

Brand and class for Daunorubicin?

Back 18

Cerubidine

Hint 18

anthracycline

(Topo II inhibitor)

Front 19

Daunorubicin is eliminated by....

Back 19

kidneys

(result...)

Hint 19

red-urine

Front 20

This anthracycline is metabolized by hepatic and renal systems...

Back 20

Epirubicin (Ellence)

Front 21

Brand and cancer type for Epirubicin?

Back 21

Ellence

(anthracyclines)

Hint 21

solid

Front 22

Brand and cancer type for Idarubicin?

Back 22

Idamycin

(anthracyclines)

Hint 22

AML
ALL

Front 23

____ has less cardiotoxicity than the other anthracyclines

Back 23

Mitoxantrone
(Novantrone)

Front 24

Brand and Class for Mitoxantrone?

Back 24

Novantrone

Hint 24

(anthracycline)

Front 25

Epipodophyllotoxins are most sensitive in cells during the _____ and G2 phase.

Back 25

S

Front 26

Brand and Class for Etoposide?

Back 26

Vp-16
Vepesid

Hint 26

Epipodophyllotxins

(lymphoma and solid)

Front 27

Vincristine, vinblastine, vindesine, and vinorelbine are all _____

Back 27

vinca alkaloids

Hint 27

antimitotic agents

Front 28

Antimitotic agents target _____

Back 28

microtubule

Front 29

Name the 3 taxanes (antimitotics)

Back 29

paclitaxel
docetaxel
cabazitaxel

Front 30

Ixabepilone subclass? And class?

Back 30

epothilones

Hint 30

antimitotic

Front 31

Eribulin subclass? and class?

Back 31

Halichondrin B analog

Hint 31

antimitotic

Front 32

All antimitotic agents are ____ phase-specific cytotoxins

Back 32

M

Front 33

Vinca alkaloids bind to _____ and blocks its abilty to polymerize with ____

Back 33

B-tubulin

Hint 33

alpha-tubulin

RM hepatic metabolism

Front 34

Brand and cancer type for Vincristine...

Back 34

Oncovin
Vincasar

Hint 34

ALL
lymphoma
solid

Front 35

Vincristine is in a _____ formulation

Back 35

liposomal

Hint 35

RM: big t1/2 range bc hepatic

Front 36

Brand and cancer type for Vinblastine...

Back 36

Velban

Hint 36

lymphoma
solid

Front 37

Brand and cancer type for Vindesine?

Back 37

Eldisine

Hint 37

ALL
CML
lymphoma
solid

Front 38

Do vinca alkaloids cause vesicant?

Back 38

yes

Front 39

Class for Vinorelbine?

Back 39

vinca alkaloid

(solid cancer type)

Front 40

Taxanes promote the _____ of microtubules and is ___ phase-specific

Back 40

polymerization

Hint 40

M

Front 41

Taxanes have extensive _____ metabolism

Back 41

hepatic

Front 42

Brand and class for Paclitaxel?

Back 42

Taxol

Hint 42

taxane (antimitotic)

Front 43

You add 50% ethanol with this to prevent toxicity

Back 43

cremophor EL

Front 44

Which taxane is dose-dependent? How is it's severe myleosuppression alleviated?

Back 44

Paclitaxel (Taxol)

Hint 44

by filgrastim

Front 45

Abraxane generic?

Back 45

Paclitaxel protein-bound

(albumin)

Hint 45

solid cancer type

Front 46

Docetaxel has ____ PK.

Back 46

linear

Front 47

Does Taxotere cause fluid retention?

Back 47

yes --> leads to peripheral edema

Front 48

Brand for Cabazitaxel and class?

Back 48

Jevtanan

Hint 48

taxane

Front 49

Class for Ixabepilone?

Back 49

epothilones (antimitotic)

Front 50

Brand for Eribulin?

Back 50

Halaven

Front 51

Brand for Estramustine?

Back 51

Emcyt

Front 52

Estramustine is made up of ____ and ____

Back 52

estradiol and normustin

Hint 52

RM good bc little myelosuppression but get impotence and edema

Front 53

Etoposide has a ___ in it's R group. Teniposide has a ____ in it's R group.

Back 53

CH3

C=C-S-C=C-C (penta ring)

Hint 53

these are epipodophyllotoxins (topo II)

Front 54

Which taxane is more water soluble and is more potent?

Back 54

Docetaxel

Front 55

The 2 differentiating agents?

Back 55

All-Trans Retinoic Acid (ATRA)
Arsenic Trioxide (ATO)

Front 56

This drug promotes the degradation of PML-RAR-alpha fusion protein...

Back 56

ATRA

Front 57

2 unique toxicities for differentiating agents?

Back 57

leukocytosis
APL differentiation syndrome

Hint 57

RM ATO can cause QT prolongation bc of metal in formulation

Front 58

Tamoxifen, toremifene and raloxifene are what type of Anti-Estrogen therapies?

Back 58

SERMS
selective estrogen-receptor modulators

Front 59

Aromatase inhibitors? (3)

Back 59

exemestane, anastrozole, and letrozole

what good for?

Hint 59

breast cancer

RM all 3 of these agents cause dec in bone mineral density

Front 60

Fulvestrant is a ____. Goserelin is a _____.

Back 60

SERD
selective estrogen-receptor down-regulator

Hint 60

LHRH
Lutinizing hormone-releasing hormone agonists

Front 61

Tamoxifen is ____ in breast cells and ___ in the uterus' endometric cells

Back 61

anti-estrogenic

Hint 61

estrogenic

Front 62

Fulvestrant is given ____.

Back 62

IM

It _____ ER dimerization and ____ its degradation.

Hint 62

inhibit

increase

Front 63

Goserelin is given ____.

Back 63

SQ

is it ok for men?

Hint 63

yes

breast and prostate

Front 64

Goserelin is given ____.

Back 64

SQ

is it ok for men?

Hint 64

yes

breast and prostate
(but tmax and t1/2 differ)

Front 65

Aromatase is resp for converting _____ to ____

Back 65

testosterone

Hint 65

estrone (estradiol)

Front 66

Exemestane is a Type ___ AI because it has a ____ in it.

Back 66

1

Hint 66

steroid

Front 67

Degarelix is a ____ anatagonist.

Back 67

LHRH

Front 68

Leuprolide and Triptorelin drug class and use?

Back 68

LHRH agonist

Hint 68

prostate cancer

(along with goserelin which is used for breast cancer also)

Front 69

Flutamide, Bicalutamide, and Nilutamide are ______

Back 69

androgen receptor blockers

Front 70

Leuprolide is given ___ and ____. Triptoerlin is given ___.

Back 70

IM and SQ

Hint 70

IM only

RM Trip can get hypersensitivity bc it is a peptide itself

Front 71

Degarelix is given ____

Back 71

SQ

Hint 71

RM competes with LHRH

Front 72

The androgen receptors can cause _____ bc extensive ____ metabolism.

Back 72

hepatotoxicity

Hint 72

liver

Front 73

Bortezomib is given ___ or ____

Back 73

IV or SQ

What does it inactivate?

Hint 73

NFKA

(by being a 26S proteasome inhibitor)

Front 74

Big toxicity of thalidomide?

Back 74

birth defects

Hint 74

used for multiple myelomas

Front 75

L-asparaginase inhibits _____ and causes cell death.

Back 75

protein synthesis

How is it given?

Hint 75

IV or IM

Front 76

Due to it's protein synthesis inhibition this drug causes hyperglycemia, clotting abnormalities, and hyperTG's leading to pancreatitis...

Back 76

L-Asparaginase

Front 77

Bleomycin max dose is ___

Back 77

400 units per lifetime

How given?

Hint 77

Given IM, IV, and SQ

Front 78

What is gene mutation is responsible for acute promyelocytic leukemia (APL)?

Back 78

PML-RAR-alpha

Hint 78

RM: APL is a subtype of AML

Front 79

To treat APL, ATRA is given ____ and arsenic trioxide is given _____

Back 79

PO

Hint 79

IV

Front 80

Which anti-cancer drug depends on whether or not the cancer cell is ER-positive?

Back 80

Anti-Estrogen therapy

Hint 80

*breast cancer cells

Front 81

Is Tamoxifen useful in postmenopausal cancer?

Back 81

no

Front 82

What 2 toxicities does Raloxifene have increased vs Tamoxifen?

Back 82

inc stroke w/ coronary heart disease
inc thromboembolic disease

Front 83

This drug is known as the "pure ant-estrogen"

Back 83

Fulvestrant

Hint 83

RM good for tamoxifen resistant cells

Front 84

Megestrol is a synthetic ____

Back 84

progesterone

Hint 84

RM: will act on neg FB can dec estrogen levels

Front 85

What will help Exemestane's absorption?

Back 85

if taken after a high fat meal

Front 86

This drug has an increased risk for CV disease due to androgen deprivation.

Back 86

Bicalutamide

Hint 86

Anti-androgen med
Blocks the androgen receptor

Front 87

These two drugs have 4 possible MOA's including: G1 arrest, apoptosis
inhibits cell adhesion
decreases angiogenesis
increases NK cell activity

Back 87

Thalidomide
Lenalidomide

Hint 87

RM: both given by mouth

Front 88

With this drug can get high distribution in skin and lungs, plus can cause pulmonary fibrosis.

Back 88

Bleomycin

Hint 88

RM also can cause cutaneous rxns (hyperpigmentation, erythema, and ulceration)

Front 89

MOA for Bleomycin?

Back 89

causes single and double stranded breaks

Cancer types?

Hint 89

lymphoma
melanoma
testicular

Front 90

4 subclasses of kinase inhibitors?

Back 90

ABL inhibitors
EGFR inhibitors
B-Raf inhibitor
ALK inhibitor

Front 91

Imatinib, dasatinib, and nilotinib???

Back 91

ABL inhibitors

Front 92

Gefitinib, erlotinib, and lapatinib class?

Back 92

EGFR inhibitors

Hint 92

Kinase inhibitors

Front 93

MOA of ABL inhibitors?

Back 93

inhibit kinase activity by binding to the pocket of ABL and thus competes with ATP needed for phosphylation

Front 94

Most potent ABL Kinase Inhibitor?

Back 94

Nilotinib

Front 95

Which ABL inhibitor causes cardiotoxicity?

Back 95

Nilotinib

Front 96

ErbB2 is overexpressed in ____ cancer

Back 96

breast

Front 97

MOA of EGFR inhibitors?

Back 97

inhibits EGFR tyrosine kinase

Front 98

What is the special toxicity of EGFR inhibition?

Back 98

rash development

Front 99

This is a dual tyrosine kinase inhibitor

Back 99

Lapatinib

inhibits EGFR and HER2

Front 100

This is a dual tyrosine kinase inhibitor

Back 100

Lapatinib

inhibits EGFR and HER2

Hint 100

RM causes cardio and pulmonary toxicity

Front 101

This drug inhibits proliferation of melanoma cells with B-RAF(V600E), and causes apoptosis.

Back 101

Vemurafenib

Toxicities?

Hint 101

cutaneous squamous cell carc

Front 102

Kinases inhibitors are given ____

Back 102

by mouth

Front 103

This drug blocks ALK?

Back 103

Crizotinib

Toxicities (3 main)

Hint 103

vision impairment
GI
cardio

Front 104

Rituximab is anti-____

Back 104

CD20

Hint 104

induces apoptosis in tumor cells via ADCC and CDC

Front 105

Ofatumumab is anti-____

Back 105

CD20

(but not identical to Rituximab)

Front 106

Alemtuzumab is anti-____

Back 106

CD52

Hint 106

induces apoptosis in tumor cells via ADCC and CDC

Front 107

Brentuximab vedotin is anti-____

Back 107

CD30

Hint 107

RM: it's an antibody-drug conjugate (made of 3 components --> CD30, MMAE, and protease-cleavable linker)

Front 108

Cetuximab is anti-____

Back 108

EGFR (ErbB1, HER1) --> very good for colon cancer therapy

Hint 108

induces apoptosis in tumor cells via ADCC
RM can cause rash/dry skin & cardiopulmonary arrest

Front 109

Panitumumab is anti-____

Back 109

EGFR (ErbB1, HER1)

Hint 109

does NOT induce ADCC (unlike cetuximab)

Front 110

Trastuzmab is anti-____

Back 110

HER2/neu (ErbB1)

Hint 110

induces apoptosis in tumor cells via ADCC & blocks angiogenesis

Front 111

Bevacizumab is anti-____

Back 111

VEGF (needed for tumor BV development)

most serious toxicity (4)?

Hint 111

hemorrhaging
GI perforation
thromboemolism
poor wound healing

Front 112

Which part of Brentuximab Vedotin causes disruption of micro-tubules (apoptosis) and cytotoxicity as well?

Back 112

MMAE

(free = cytotoxicity)

Hint 112

RM get peripheral neuropathy bc of microtubule distruption of MMAE

Front 113

To prevent cardiotoxicity of Trastuzumab, which 2 drugs should it not be combined with?

Back 113

Doxorubicin
Cyclophosphamide

Front 114

5 alkylating agents that treat solid tumors?

Back 114

cyclophosphamide
cisplatin
carboplatin
ifosfamide
oxalitplatin

Front 115

Alkylating agents that are PO?

Back 115

cyclophosphamide
chlorambucil
busulfan
procarbazine

Hint 115

rest are by IV

Front 116

Antimetaboites are all ___ phase specific.

Back 116

S

Hint 116

bc they block DNA synthesis

Front 117

5-FU and prodrug capecitabine MOA?

Back 117

inhibit thymidylate synthase

Hint 117

antimetaboites

RM: capecitabine bc 5-FU in body

Front 118

MOA of pyrimidine analogs?

Back 118

block DNA synthesis by getting incorp in DNA

Front 119

What 5 antimetabolites work on solid tumors?

Back 119

MTX
Pemetrexed
5-FU
Capecitabine
Gemcitabine

Front 120

What 4 antimetabolites are given PO?

Back 120

Capecitabine
6-Mercaptopurine
Fludarabine
Hydroxyurea

Hint 120

rest are IV infusion

Front 121

Which 2 antimetabolites cause Hand-Foot syndrome?

Back 121

5-FU
capecitabine

Hint 121

also seen in Doxurubcin lip formulation

Front 122

Which two topo inhibitors treat luekemia/lymphoma?

Back 122

daunorubicin
idarubicin

Hint 122

rest treat solid

Front 123

All Topo Inhibitors are give ____

Back 123

IV

Front 124

Taxanes and Ixabepilone ___ microtubule polymerization?

Back 124

promote

Hint 124

RM these two get hypersensitivity rxn bc of solvents

Front 125

Which 3 antimitoic agents can be used for solid and leukemia?

Back 125

vincristine
vinblastine
Vindesine

Hint 125

all others = solid

Front 126

Vincristine and estramustine both have very limited _____

Back 126

myelosuppression

Hint 126

all other antimitotics cause more

Front 127

BCR-ABL inhibitors are used for ____

Back 127

CML

Hint 127

RM imatinib is least potent and maybe resistant for CML
and this subclass only ones that cause myelosuppression

Front 128

All kinase inhibitors undergo extensive _____ metabolism

Back 128

hepatic

Front 129

All MAb are given ____ and are dose-_____.

Back 129

IV

(RM infusion rxn bc large amounts of protein)

Hint 129

dependent

Front 130

Which 3 drug target of MAb cause myleosuppression?

Back 130

CD20
CD30
CD52

Hint 130

all others do not cause