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What are the names of the two ANTITUMOR ANTIBIOTICS?
What is the brand name for Doxorubicin?
Doxorubicin - MOA
which can intercalate between base pairs, inhibit topoisomerase II
, and generate free radicals
, binding to cellular membranes to alter fluidity and ion transport
- • Blocks the synthesis of RNA and DNA
- and causes DNA strand scission.
Doxorubicin - CCNS or CCS?
Doxorubicin – Pharmacokinetics
•Must be given IV.
- •Metabolized in the liver and excreted in
- the urine, imparting to it a red color.
Doxorubicin - Clinical use
- acute leukemia,
- and ovary
Doxorubicin – Toxicity
- GI distress,
- and alopecia.
- Unique side effect is cardiotoxicity.
Bleomycin - MOA
- acts by binding to DNA, which results in
- single-strand and double-strand breaks following free radical formation, and inhibition of DNA biosynthesis
- Cell cycle-specific drug that causes
- accumulation of cells in the G2 phase of the cell cycle.
Bleomycin - Clinical treatment of
- Hodgkin's and non-Hodgkin's lymphomas,
- germ cell tumor,
- head and neck cancer,
- and squamous cell cancer of the skin, cervix, and vulva.
Bleomycin - Pharmokinetics
May be given IV, IM, or SQ
Bleomycin - Toxicity
Plant Alkaloids are CCS drugs which include?
- vinca alkaloids,
- the podophyllotoxins,
- and the taxenes.
Brand name for Vincristine?
Vincristine - MOA
A spindle poison derived from the periwinkle plant. Prevents the assembly of tubulin dimers into microtubules, and blocks the formation of the mitotic spindle.
Acts on the M phase of the cell cycle
Vincristine – Resistance
occurs as a result of increased efflux from the cell by a transporter molecule.
Vincristine – Pharmacokinetics
- Given IV.
- Good tissue penetration except into the CSF.
- Cleared mainly by biliary excretion
Vincristine - Clinical use
- Hodgkin’s disease,
- Wilm’s tumor,
- childhood acute leukemia
Vincristine – Toxicity
- GI distress,
- Peripheral neuropathy.
What type of plant alkaloid is Etoposide?
- a podophyllotoxin
- derived from the May apple plant
Etoposide - MOA
- Interacts with Topoisomerase II to increase the degradation of DNA.
- - Most active in the late S and early G2 phases.
Etoposide – Pharmacokinetics
- Good oral absorption,
- eliminated via the kidney
Etoposide – Toxicity
Etoposide - Clinical use
- treat germ cell cancers,
- small cell and non-small cell lung cancers,
- Hodgkin’s and non-Hodgkin’s lymphomas,
- and gastric cancer.
Brand name for Paclitaxel?
Paclitaxel - What type of plant alkaloid is it?
- A taxane derived from the Pacific yew tree.
Paclitaxel - MOA
- Mitotic spindle poison,
- M phase specific
Paclitaxel - Clinical use
Breast and ovarian cancer
Paclitaxel – Toxicity
- and hypersensitivity reactions
What are SERM’s?
SERM’s are mixed estrogen agonists that act as antagonists in certain tissues
Name two hormones used in the treatment of cancer.
- Tamoxifen (Nolvadex)
Prednisone is used to treat?
- acute leukemia,
- Hodgkin’s disease,
- and lymphoma
Brand name for Tamoxifen?
Tamoxifen - MOA
- Selective Estrogen Receptor Modifier
- (SERM) which blocks the binding of estrogen to receptors of estrogen-sensitive cancer cells in breast tissue.
- acts as an antagonist in hormone-responsive breast cancers where it prevents receptor activation by endogenous estrogen.
Tamoxifen - Clinical use
- Used in the treatment of receptor-positive breast cancers and may help prevent cancer in high risk women.
- has more agonist than antagonist action on bone and thus helps to prevent osteoporosis.
Tamoxifen - Toxicity
- hot flushes,
- vaginal bleeding,
- and peripheral edema.
Interferon alfa-2 - MOA
- Made by lymphocytes,
- inhibits cell proliferation,
Interferon alfa-2 - Clinical use
- hairy cell leukemia,
- Kaposi’s sarcoma,
- and hepatitis.
Interferon alfa-2 - Side effects
- –Causes flu-like symptoms,
Imatinib - MOA
- the first member of a new class of drugs that act by specifically inhibiting an enzyme that is characteristic of a cancer cell rather than non-specifically killing all rapidly dividing cells.
- inhibitor of the tyrosine kinase domain of the Bcr-Abl oncoprotein
Imatinib - Clinical use
Indication - chronic myelogenous leukemia (CML),
- - Given orally,
- - Metabolized by CYP3A4
What does EGFR stand for?
Epidermal growth factor receptor
What is the anticancer drug classified as an
Epidermal growth factor receptor inhibitor?
Cetuximab - Clinical use
metastatic colon cancer
Cetuximab - Toxicity
- Acneiform skin rash,
- and hypomagnesemia
What does VEGF stand for?
vascular endothelial growth factor
- - (VEGF) is one of the most important angiogenic growth factors. The growth of both primary and metastatic tumors requires an
- intact vasculature. As a result, the VEGF-signaling pathway represents an
- attractive target for chemotherapy.
Bevacizumab - MOA
- Bevacizumab is a recombinant humanized monoclonal antibody that targets all forms of VEGF-A.
- This antibody binds to and prevents VEGF-A from interacting with the target VEGF receptors.
Bevacizumab - Clinical use
- can be safely and effectively combined with 5-FU-, irinotecan-, and oxaliplatin-based chemotherapy
- - in the treatment of
- metastatic colorectal cancer.
Name 3 drugs used to treat renal cell cancer.