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CMOD/PCM- Block 2 > Pharm: Targeted Drugs for Cancers > Flashcards

Pharm: Targeted Drugs for Cancers Flashcards

1
Q

When you see a drug ending in “-ib” think:

A

It inhibits something

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2
Q

What is the drug that targets VEGF in treating colorectal cancer and non-small cell lung cancer (NSCLC)?

A

Bevacizumab

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3
Q

What is the drug that targets EGFR in treating colorectal and head & neck cancers?

A

Cetuximab

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4
Q

What is the drug that targets EGFR in colorectal cancer only?

A

Panitumumab

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5
Q

What is the drug that targets CD20 in treatment of chronic lymphocytic leukemia (CLL) and non-hodgkin’s lymphoma (NHL)?

A

Rituximab

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6
Q

What drug targets HER-2 in treating breast cancer?

A

Trastuzumab

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7
Q

What drug targets CTLA-4 in treating melanoma?

A

Ipilimumab

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8
Q

What other drug targets CD20 in treating chronic lymphocytic leukemia (CLL)?

A

Ofatumumab

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9
Q

Which drug is a 26-S Proteosome inhibitor used to treat multiple myeloma?

A

Bortezomib

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10
Q

Which drug is a hedgehog pathway inhibitor used to treat basal cell carcinoma?

A

Vismodegib

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11
Q

EGFR/HER1 (growth factor receptor) oncogenes are associated with which tumor types?

A

glioblastoma
lung
breast cancer

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12
Q

HER2/Neu (growth factor receptor) is an oncogene associated with which tumor types?

A

Breast
ovarian
gastric cancer

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13
Q

K-Ras (signal transduction) is an oncogene associated with which tumor type?

A

multiple tumor types

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14
Q

B-Raf (signal transduction) is an oncogene associated with which tumor type?

A

Multiple tumor types, melanomas

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15
Q

p53 and RB are tumor suppressor genes associated with which cellular function?

A

cell cycle regulation

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16
Q

PTEN is a tumor suppressor gene associated with which cellular function?

A

signal transduction, adhesion signaling

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17
Q

PTEN is a tumor suppressor gene associated with which tumor types?

A

glioblastomas
prostate
breast

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18
Q

BRCA1/2 are tumor suppressor genes associated with what cellular function?

A

DNA ds-break repair

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19
Q

BRCA1/2 are tumor suppressor genes associated with which types of tumors?

A

breast

ovarian

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20
Q

VHL is a tumor suppressor gene associated with which cellular function?

A

Ubiquitin ligase

21
Q

VHL is a tumor suppressor gene associated with which tumor types?

A

kidney

others

22
Q

p16/CDKN2 is a tumor suppressor gene associated with which cellular functions?

A

Cell cycle regulator

23
Q

p16/CDKN2 is a tumor suppressor gene associated with which tumor types?

A

melanoma
pancreatic
esophageal

24
Q

This drug is an immunostimulant because it binds to CTLA-4, inhibiting it from binding to B7 in place of CD28. If CTLA-4 was allowed to bind to B7, this would inhibit the secondary signal of activation of T cells, causing them to become anergic.

A

Ipilimumab

25
Q

Which drug produces a rapid and sustained depletion of B-cells lasting for several months by binding to CD20 on B cells?

A

Rituximab

26
Q

Is VEGF particularly important for solid tumors or liquid tumors more, and why?

A

Solid tumors. For recruitment of blood vessels as they outgrow their vascular supply.

27
Q

Which protein, under conditions of low oxygen, stops being degraded by the 26S proteosome pathway and translocates to the nucleus to promote upregulation and expression of VEGF?

A

hypoxia inducible factor (HIF-1)

28
Q

What characteristic of mAbs makes them potential poor penetrators of large, solid tumors?

A

Large molecular weight

29
Q

Current mAbs are based on which immunoglobulin isotype?

A

IgG

30
Q

Describe the ADEs associated with antibody drugs.

How can you overcome these effects?

A

infusion related rxns: anaphylaxis, angioedema, and pulmonary toxicity.
Overcome with: pre-medicate with antihistamines and/or corticosteroids before resumption of infusions.

Left ventricular dysfunction and CHF; HTN

Depletion of cell populations in blood where target is expressed in component of this tissue.

31
Q

List mechanisms of resistance to tyrosine kinase inhibitors.

A

kinase over-expression

binding site mutations (do not affect kinase function, shift drug dose-response curves right for inhibitors)

32
Q

Describe a complication associated with use of tyrosine kinase inhibitors.

A

Because RTKs are present everywhere in the body, off-target effects are expected.

33
Q

Explain the relationship of tyrosine kinase inhibitors with CYP.

A

Most TK inhibitors are substrates for CYP3A4 and a few are inhibitors of other isoforms. Therefore, the potential for drug-drug interaction cannot be overstated.

34
Q

A common theme amongst the RTK inhibitors is their ability to disrupt _______ function through “off-target” effects. Therefore these things should be monitored in a pt:

A

endocrine function.
monitor: thyroid function, bone density, PTH, 25-OH Vit. D
child growth & pubertal development
Women who may become pregnant should be counseled about the known averse effects of KIs on fetal development.
Monitor diabetics for blood glucose levels

35
Q

List the tyrosine kinase inhibitors known to have the ADE thyroid dysfunction commonly.

A

Sorafenib
Sunitinib
Imatinib

36
Q

List the common ADEs of tyrosine kinase inhibitors.

A

rash, fatigue, N/V, dyspnea, stomatitis, anorexia, blood dysplasias, QT prolongation, Hand-foot syndrome

37
Q

Mutations of which downstream proteins in intracellular signaling are important in determining if treatment with tyrosine kinase inhibitors will be efficacious and why?

A

KRAS & BRAF
If the pt has downstream mutations of KRAS of BRAF, they are likely to continue constitutive expression of EGFR signaling, even when EGFR is inhibited by TKIs.

38
Q

List the 6 major resistance mechanisms of tumors to TKIs.

A

Decreased intracellular drug levels
Increased plasma protein binding
MDR-1 mediated efflux
Genomic amplification of kinase
Clonal evolution of kinase-independent mechanism
Mutations of ATP-binding site affecting drug binding or kinase activity

39
Q

What is the best way to overcome the compensatory downstream recruitment of secondary tyrosine kinases that may render targeted primary RTK inhibition useless?

A

Shotgun approach- multiple drugs targeting multiple pathways and critical fragile points, concurrently. Administered with a shotgun.

40
Q

mTOR is a central regulator of these three cell functions:

A

cell proliferation
angiogenesis
cell metabolism

41
Q

How can mTOR be inhibited, mechanistically?

-don’t name exact drugs

A

small molecular weight molecules that form a three-way complex involving inhibitor, FKBP-12, and mTOR.

42
Q

BIG picture, what does mTOR regulate that mediates cell proliferation, angiogenesis, and cell metabolism?

A

Protein synthesis

43
Q

Which two mTOR inhibitors are approved for the tx of advanced renal cell cancer?

A

temsirolimus & everolimus

44
Q

Are the mTOR inhibitors suitable for all tumor types?

A

No, that goes for pretty much all anticancer drugs though.

45
Q

The ____________ is another intracellular target of anticancer drugs whose function is to degrade proteins which have been targeted by ubiquination.

A

26S proteasome

46
Q

Generally speaking, what is wrong with the 26S proteasome that causes cancer?

A

The 26S proteasome is overactive, cleaving inhibitors of cell signaling and transcriptional regulation. This transcription of proteins that are necessary for cellular proliferation is constitutive, and then BOOM CANCER.

47
Q

How does Bortezomib work?

A

It inhibits the proteasomal activity of the 26S proteasome, allowing IkB-alpha to remain bound (inhibiting) to NfkB, preventing the transcriptional regulation of NfkB, and thus proliferation.

48
Q

What are the major ADEs of Bortezomib use?

A

Cardiotoxicity, hepatotoxicity

CMOD/PCM- Block 2 (41 decks)

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