Fitz- Antimitotics and Antineoplastics Flashcards by Sarah Carlson

Compare the mechanism of action among anti-mitotic drugs:
Vinca alkaloids
Taxanes
Epilone

Vinca alkaloids: Prevent extension of spindles

Taxanes: Enhance assembly

Epilone: Enhance spindle assembly

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What is the primary advantage of ixabepilone w/ respect to development of resistance?

It is NOT limited by MDR (p-glycoprotein)

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What are the mechanisms of resistance for VA and taxanes?

VA- decrease accumulation by increasing p glycoprotein, change tubulin so the drug doesn’t bind

Taxanes-p glycoprotein

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What toxicities are associated w/ VA?

Neuotoxicity
cytotoxic- BMS, N/V
Vesicant

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vinCristine is related to ______toxicity, so it’s more likely to be ___________.

Cns toicity (more lipid soluble–> fatal intrathecally)

neuotoxic

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vinBlastine is realted to __________, so it’s more like to cause

cytotoxic sxs: BMS and N and V

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When treating with vincristine, what does a loss of reflexes show? What does parasthesis show?

Loss of reflexes occurs in 100% of pts ands is a sign that you have titrated the drug correctly.

Parasthesis (pins and needles) is a severe side effect and suggests that you should decrease the dose.

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What toxicities are associated w/ taxanes?

Drug interactions
Hypersensitivity
hypotension and arrythmias

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What are the main differences in the use of glucocorticoids for cancer chemotherapy vs. immunosuppression?

Immunosuppression: glucocorticoids are given at a continuous low dose (targets specific antigens and synchronized cell division)

Cancer chemotherapy: glucocorticoids are given at a HIGH dose, pulse (allows normal cells to recover) (cell division is unstimulated and random)

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What cytokines have been approved for use in cancer treatment?

IL-2
INF alpha
TNF alpha

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How do the MOAs differ for the three cytokines?

IL-2-Induce and expand T cell
INF alpha- decrease FGF and decrease cell division
TNF alpha- causes fibroblast proliferation, increases IL-6 and 8 to activate B and T cells

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Which cytokine has a t 1/2 of 13 mins and can cause fatal hypotension and a coma?

IL-2

It must be given continously or in multiple daily doses

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Which cytokine causes BMS and depression?

IFN alpha

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Which cytokine has a short half life and causes flu-like sxs?

TNF alpha

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What monoclonal ab targets anti-CD 20 B cells?

Rituximab

NHL

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What monoclonal ab targets anti-CD 53 B cells?

ALEM

CLL

What monoclonal ab targets IL-2 and diptheria toxin?

Denileukin diffitux

What are the common side effects of monoclonal antibodies?

Hypersensitivity rxns

Infections

What monoclonal antibodies cause heart or lung toxicity?

Alem

Rituximab

What monoclonal antibodies cause tumor lysis syndrome?

Alem

Rituximab

What are the vinca alkaloids?

vincristine
vinblastine
vinorelbine

What are taxanes?

cabazitaxel
cocetaxel
paclitaxel

What is ixabepilone?

An epilone

What type of drug resistance is commonly seen with vinca alkaloids?

Increased expression of p glycoprotein

Why is ixabepilone often approved for use in breast cancer pts who have failed anthracycline antibioitc and taxane treatments?

Because it DOES NOT produce MDR

This drug when used for cancer chemo therapy is given in higher doses w/ a "pulse" regimen.

Glucocorticoids | Dexamethasone and prednisone

What immunosuppressive antibioitcs are used to prevent rejection following bone marrow transplants?

cyclosporin | tacrolimus

What immunosuppressive antibiotics are used as angiogenesis inhibitors?

Everolimus | Temsirolimus

Immunosuppressive antibiotics play a role in what two pathways?

1. NFAT mediated regulation of IL synthesis | 2. mTOR regulation of cell growth and angiogenesis

What are the common characteristics shared by cytokines used for cancer chemotherapy?

Short half lives | NOT cytotoxic by themselves--> recruit immune cells to do the actual killing

How are monoclonal antibodies used as drugs and what do they target?

They can selectively recruit the immune system to destroy cancer cells (specifically ones w/ molecular targets that distinguish cancer cells from normal cells) They target CDs and surface proteins.

What is the common dose limiting complication of many antineoplastic drugs?

BMS

To combat BMS colony stimulating factors have been developed. What do they do?

Erythropoietin- RBC FIlgrastim- neutrophils Sagramostim- gm-csf--> granulocytes, eosinophils, basophils, monocytes IL-11 and THrobopoietin--> platelets

What protein function inhibitors target a unique aspect of a specific cancer type?

L asparaginase | Imatinib

What protein function inhibitors target less specific cancer types and exploit the overexpression of a particular protein?

Erlotinib | Gefitinib

What drugs target rapidly dividing cells and/or angiogenesis?

Bortezomib ovrniostat sorafenib sunitinib

What drugs can induce tumor cell differentiation and lead to apoptosis?

Tretinoin | rexinoids like bexarotene