Exam 2- 3/4/5 Flashcards Preview

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Flashcards in Exam 2- 3/4/5 Deck (50):
1

3 types of SMKI

tyrosine kinase, serine/threonine kinase, and lipid kinase inhibitors

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tyrosine kinase inhibitors

acting on Bcr-Abl, EGFR,
imatinib and erlotinib

3

serine/threonine kinase inhibitors

acting on B-raf
vemurafenib and trametinib

4

lipid kinase inhibitor

acting on PI-3K
idelalisib

5

mechanisms of tyrosine kinase activation include

genetic alteration, gene amplification, point mutation, protein accumulation

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irreversible inhibition

SMKI forms a covalent bond with the cysteine residues in the active site of a protein kinase

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reversible inhibition

type inhibition I to IV

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group 1: targeting Bcr-Abl oncoprotein in chronic myeloid leukemia

imatinib (1st generation), nilotinib (2nd generation)

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major cause of CML

the philadelphia chromosome (fusion of 9 and 22)
- this one mutation leads to cancer

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imatinib clinical indication

- PH+ CML in blast crisis, accelerated phase or chronic phase after IFN therapy
- pediatric patients with PH+ CML in chronic phase
- PH+ ALL
- Kit+ GI stromal tumors (GIST)

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monitoring PH+ CML after treatment

- hematologic tests: normal range of blood cell counts
- cytogenic tests: numbers of cells with PH+ chromosome
- molecular tests: q-RT-PCR: existence of PH+ DNA/mRNA

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nilotinib is cabable of

overcoming imatinib reisistance resulting from Brc-Abl kinase mutations

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Nilotinib clinical indication

chronic phase and accelerated phase PH+ CML resistant or intolerate to imatinib

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effectiveness of nilotinib is based on

hematologic and cytogenetic response rates

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do not use nilotinib is patients with

hypokalemia, long QT syndrome or hypomagnesemia.

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gemfitinib

EGFR

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erlotinib

EGFR
Tarceva
NSCLC, metastatic pancreatic cancer

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lapatinib

EGFR/Her2
Tykerb
breast cancer

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Afatinib

EGFR/Her2

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cigarette smoking decreases

erlotinib plasma concentrations

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severe ADRs of erlotinib

GI bleeding or perforations, renal disorders, hepatic disorders, ocular disorders- abnormal eyelash growth

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common ADRs of lapatinib

GI- diarrhea, dermatologic, fatigue

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severe ADRs of lapatinib

cardiac toxicity, hepatic toxicity, interstitial lung disease/pneumonitis

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multiple tyrosine kinases

sunitinib, sorafenib

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sunitinib

VEGFR, PDGFR, etc
Sutent
GIST, metastatic renal cell carcinoma

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sorafenib

mutiple tyrosine kinases/serine/threonine kinases
VEGFR, PDGFR, raf, etc
administer w/out food
Nexavar
hepatocellular carcinoma (HCC), renal cell carcinoma (RCC)

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sorafenib drug interactions

decetaxel, fluorouracil, gemcitabine, oxaliplatin, paclitaxel, doxorubicine, irinotecan

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sorafenib severe ADRs

wound healing complications

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interferones (IFNs)

are cytokines produced by the cells of the immune system in response to various challengers, particularly virus with double stranded RNA

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biological potency of IFNs are determined as

millium IU

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specific activity of IFN alfa-2b

2.6 X10^8 IU/mg protein

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potential MOA of IFN in tumor therapy (4)

- direct inhibition of cancer cell proliferation
- enhancement of cytotoxic T cell activities that kill cancer cells
- cell cycle regulation leading to tumor cells cytostasis and apoptosis
- increased expression of cell surface antigen/protein which facilitates immune cell recognition and cytotoxicity

33

main site for catabolism of IFN?

kidney. No IFN in urine after administration

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;abeled indications for IFN therapy

PH+ CML, hairy cell leukemia, follicular lymphoma, AIDS-related kaposi's sarcoma, melanoma
18 yo and up

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IFN also has an unlabeled indiction for

renal cancer

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IFN drug interaction

may potentiate risk of renal failure in combo with IL-2

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acute ADRs of IFN

flu-like symptoms- fever, chills, HA

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chronic ADRs of IFN

depression, fatigue/weakness (most dose-limiting)

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incomplete Reiter's syndrom induced by

systemic IFN alpha
(tongue ulcers)

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do not use IFN-alpha with

autoimmune hepatitis (positive anti-nuclear antibody)

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interleukin-2

Proleukin

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biological potency of IL-2 is shown as

international units (IU)

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IL-2 receptor

1. requires binding to its IL-2 receptor
2. receptor belongs to class I cytokine receptor family
3. IL-2 receptor is composed of 3 units (alpha, beta and gammaC)
4. signaling is transmitted by members of JAK and STAT family

44

IL-2 MOAs

1. enhancing lymphocyte mitogenesis and stimulation of long-term growth of IL-2-dependent cells
2. enhancing lymphocyte cytotoxicity
3. inducing lymphokine-activated (LAK) and NK activity
- pretty much increase number and function

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IL-2 rapidly distributes to

extravascular space

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IL-2 clinical indication

renal cell carcinoma, melanoma

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IL-2 injection should be reserved for patients with normal

cardiac and pulmonary function

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IL-2 and glucocorticoids

glucocorticoids reduce IL-2 induced side effects (Fever, renal insufficiency, hyperbilirubinemia, confusion and dyspnea) however, they also reduce the effectiveness and should be AVOIDED

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IL-2 has been associated with

- capillary-leak syndrome (CLS)
- impaired neutrophil function and increased risk of sepsis and bacterial endocarditis

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IL-2 ADRs

hypotension, pulmonary congestion, anemia, thrombocytopenia, capillary leak syndrome