Drug Table - Misc Agents Flashcards

1
Q

Imatinib (Gleevac) Class

A

Tyrosine Kinase

inhibitor

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2
Q

Imatinib (Gleevac) Mechanism

A

Inhibits Abl kinase by binding where ATP
should go; also inhibits PDGFR and c-kit;
metabolized by cytochrome P450

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3
Q

Imatinib (Gleevac) Therapeutics

A
First line therapy for CML; also,
gastrointestinal tumor (GIST)
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4
Q

Imatinib (Gleevac) Imp Side effects

A

Nausea and vomiting, fluid
retention, muscle cramps,
arthralgia

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5
Q

Imatinib (Gleevac) Other side effects

A

Myelosuppression

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6
Q

Imatinib (Gleevac) Misc

A

Oral (1/day)

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7
Q

Gefitinib (Iressa) Class

A

Tyrosine Kinase

inhibitor

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8
Q

Gefitinib (Iressa) Mechanism

A

Inhibit epidermal growth factor receptor

(EGFR) tyrosine kinase

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9
Q

Gefitinib (Iressa) Therapeutics

A

Non-small lung cancer

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10
Q

Erlotinib (Tarceva) Class

A

Tyrosine Kinase

inhibitor

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11
Q

Erlotinib (Tarceva) Mechanism

A

Inhibit epidermal growth factor receptor

(EGFR) tyrosine kinase

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12
Q

Erlotinib (Tarceva) Therapeutics

A

Non-small lung cancer

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13
Q

Nilotinib (Tasigna) class

A

Tyrosine Kinase

inhibitor

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14
Q

Nilotinib (Tasigna) Mechanism

A

Inhibits Abl kinase

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15
Q

Nilotinib (Tasigna) Therapeutics

A

Imatinib-resistant CML

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16
Q

Nilotinib (Tasigna) Imp side effects

A

Myelosuppression

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17
Q

Nilotinib (Tasigna) other side effects

A

QT prolongation, hepatotoxicity,

electrolyte abnormalities

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18
Q

Nilotinib (Tasigna) misc

A

Oral (2/day)

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19
Q

Dasatinib (Sprycel) class

A

Tyrosine Kinase

inhibitor

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20
Q

Dasatinib (Sprycel) mechanism

A

Inhibits Abl & Src kinases

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21
Q

Dasatinib (Sprycel) therapeutics

A

Imatinib-resistant CML

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22
Q

Dasatinib (Sprycel) Imp side effects

A

Myelosuppression, bleeding, fluid
retention, pulmonary arterial
hypertension

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23
Q

Dasatinib (Sprycel) other side effects

A

Diarrhea, nausea and vomiting,

weakness, infections

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24
Q

Dasatinib (Sprycel) misc

A

Oral (1/day)

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25
Q

Rituximab (Rituxan) class

A

Monoclonal

antibody

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26
Q

Rituximab (Rituxan) mechanism

A

CD20 B-cell antibody that can directly
activate apoptosis, activate complement, or
activate cell-mediated cytotoxicity (e.g., T
cells, NK cells)

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27
Q

Rituximab (Rituxan) therapeutics

A

Non-Hodgkin’s lymphomas

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28
Q

Rituximab (Rituxan) imp side effects

A
Infusion reactions, tumor lysis
syndrome (TLS), severe
mucocutaneous reactions,
progressive multifocal
leukoencephalopathy (PML)
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29
Q

Rituximab (Rituxan) other side effects

A

Skin reactions, irregular

heartbeat, muscle or joint pain

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30
Q

Rituximab (Rituxan) misc

A

Patients need careful monitoring

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31
Q

Trastuzumab (Herceptin) class

A

Monoclonal

antibody

32
Q

Trastuzumab (Herceptin) mechanism

A

Unknown HER2/neu (ErbB2) receptor
antibody mechanism (enhanced receptor
endocytosis or blocking homo- or
heterodimerization)

33
Q

Trastuzumab (Herceptin) therapeutics

A

HER2/neu-overexpressing metastatic

breast cancer

34
Q

Trastuzumab (Herceptin) Imp side effects

A

Hypersentivity reaction; ventricular

dysfunction

35
Q

Trastuzumab (Herceptin) misc

A

Usually combined with taxanes;

enhances doxorubicin cardiotoxicity

36
Q

Cetuximab (Erbitux) class

A

Monoclonal

antibody

37
Q

Cetuximab (Erbitux) mechanism

A

EGFR1 (ErbB1)

38
Q

Cetuximab (Erbitux) therapeutics

A

EGFR-positive metastatic colorectal

cancer

39
Q

Cetuximab (Erbitux) imp side effects

A

Allergic reactions, sudden cardiac
death, dermatologic problems,
infections, renal failure, electrolyte
abnormalities

40
Q

Cetuximab (Erbitux) other side effects

A

Asthenia/malaise, fever,
nausea, constipation, interstitial
pneumonitis

41
Q

Cetuximab (Erbitux) misc

A

Clinical trials, probably combine with

cisplatin

42
Q

Cetuximab (Erbitux) class

A

Monoclonal

antibody

43
Q

Cetuximab (Erbitux) mechanism

A

EGFR1 (ErbB1)

44
Q

Cetuximab (Erbitux) therapeutics

A

EGFR-positive metastatic colorectal

cancer

45
Q

Cetuximab (Erbitux) imp side effects

A

Allergic reactions, sudden cardiac
death, dermatologic problems,
infections, renal failure, electrolyte
abnormalities

46
Q

Cetuximab (Erbitux) other side effects

A

Asthenia/malaise, fever,
nausea, constipation, interstitial
pneumonitis

47
Q

Cetuximab (Erbitux) misc

A

Clinical trials, probably combine with

cisplatin

48
Q

Ipilimumab (Yervoy) class

A

Human
monoclonal
antibody

49
Q

Ipilimumab (Yervoy) mechanism

A

Cytotoxic T-Lymphocyte Antigen 4 inhibitor;

stimulates immune system

50
Q

Ipilimumab (Yervoy) therapeutics

A

Melanoma

51
Q

Vemurafenib (Zelboraf) class

A

Serine/threonine

kinase inhibitor

52
Q

Vemurafenib (Zelboraf) mechanism

A

Inhibits oncogenic BRAF kinase

53
Q

Vemurafenib (Zelboraf) therapeutics

A

Unresectable Stage III and IV or
metastatic melanomas w/BRAF
mutations

54
Q

Vemurafenib (Zelboraf) imp side effects

A

Arthralgia, fatigue, photosensitivity,
nausea, alopecia, diarrhea, QT
prolongation

55
Q

Vemurafenib (Zelboraf) other side effects

A

Cutaneous squamous cell
carcinoma, keratoacanthoma,
new primary cutaneous
melanoma

56
Q

Vemurafenib (Zelboraf) misc

A

Superior to dacarbazine in Phase III

trials

57
Q

Dabrafenib (Tafinlar) class

A

Serine/threonine

kinase inhibitor

58
Q

Dabrafenib (Tafinlar) mechanism

A

Inhibits oncogenic BRAF kinase

59
Q

Dabrafenib (Tafinlar) therapeutics

A

Unresectable Stage III and IV or
metastatic melanomas w/BRAF
mutations

60
Q

Dabrafenib (Tafinlar) imp side effects

A

Serious febrile drug reactions,
uveitis and iritis, hyperglycemia,
hyperkeratosis

61
Q

Dabrafenib (Tafinlar) other side effects

A

Higher risk of developing:
Serious febrile drug reactions,
uveitis and iritis, hyperglycemia,
hyperkeratosis

62
Q

Dabrafenib (Tafinlar) misc

A

May cause male infertility

63
Q

Trametinib (Mekinist) mechanism

A

Inhibits MEK

64
Q

Trametinib (Mekinist) therapeutics

A

Unresectable Stage III and IV or
metastatic melanomas w/BRAF
mutations

65
Q

Trametinib (Mekinist) imp side effects

A

Cardiomyopathy, retinal disorders,
interstitial lung disease, serious
skin toxicities

66
Q

Trametinib (Mekinist) other side effects

A

Rash, diarrhea, stomatitis,

hypertension, pruritis

67
Q

Trametinib (Mekinist) misc

A

May cause female infertility

68
Q

Hydroxyurea (Hydrea) mechanism

A

Inhibits ribonucleoside diphosphate

reductase

69
Q

Hydroxyurea (Hydrea) therapeutics

A

CML (replaced by Imatinib),
polycythemia vera, essential
thrombocythemia; treatment for sickle
cell disease (increases Hb-F)

70
Q

Retinoids Mechanism

A

ATRA induces terminal differentiation in
malignant immature promyelocytes, which
subsequently apoptose

71
Q

Retinoids Therapeutics

A

APL

72
Q

Retinoids imp side effects

A

“Leukocyte Activation Syndrome”
(LAS), an increase in WBCs (fever,
weight gain, respiratory distress,
serosal effusion, renal failure)

73
Q

Retinoids misc

A

Combined w/anthracyclines;

corticosteroids used to block “LAS”

74
Q

Arsenic Trioxide (Trisenox) Therapeutics

A

Relapsed APL

75
Q

Thalidomide (Thalomid) Therapeutics

A

Multiple myeloma and myelodysplastic

syndromes

76
Q

Interferons

A

Hairy-cell leukemia, CML, and AIDSrelated

Kaposi’s sarcoma