Chapter 8 anticancer - hormonal anticancer agents + hematopoetic agents

Question 1

estrogen

hormonal

Answer 1

• counteracts endogenous testosterone (since it enhances tumor growth) in patients w/ prostate cancer

Question 2

progestin

hormonal

Answer 2

• progesteron receptor agonist

indication:
* endometrial carcinoma
* metasatic renal carinoma
* breast cancer

mechanism unclear..

Question 3

tamoxifen

hormonal

Answer 3

estrogen receptor antagonist
* prevent endogenous estrogens from stimulating tumor growth
* used to tx estrogen receptor positive bresat cancer in postmenopausal women

effect
* increased risk of uterine cancer observed in women tx’d w/ tamoxifen

Question 4

aromatase inhibitor

hormonal

Answer 4

• non steroidal aromatae inhibitor selectively reduecs circulation estradiol levles for tx of advanced breast cancer
• anastrazole and letrozole are the drug names

Question 5

androgen

hormonal

Answer 5

testerone receptor agonist
* active against some breast and renal cancers

Question 6

flutamide

hormonal

Answer 6

• testosterone receptor antagonist
• augments late effects of leuprolide
• stiulates LH and FSH via leuprolide

treat men with prostate cancer

Question 7

abiraterone (zytiga)

hormonal

Answer 7

• prodrug => abirterone, which inhibits androgen biosynthesis
• drug itself blocks CYP17, which is expressed in testicular, adrenal and prostatic tumors and is required in androgen biosynthesis
• abiraterone is used with prednisone for tx of castration-resistant metastatic prostate cancer (androgen antagonists no longer work!)

Question 8

adrenocorticosteroid

hormonal

Answer 8

lnhibit DNA and protein synthesis + mitosis

indication
* acute lymphocytic lekemia
* chronic lymphocytic leukemia
* acute myelogenous (bone marrow) leukemia
* multiple myeloma (plasma cells in bone marrow)
* breast cancer
* lymphoma (starts in lymph node)

Question 9

leuprolide, goserelin

hormonal

Answer 9

• analog of gonadotropin releasing hormone (GNRH)
• densensitizes GNR receptors in pituitary causing dec release of gonadotropin
• results in decreased sex hormone release

indication
* advanced prostate cancer

effect
* initally stimulates transient release of sex hormones (LH anad FSH) — initial leuprolide effect

Question 10

estramustine (EmCyt)

Answer 10

estrogen agonist linked to alkylating agent
* drug uptake is enhanced in estrogen receptor + cells => l/t selective accumulation of alkylating agent in tumor cells

indication
* prostate carcinoma

Question 11

epoetin alpha (epogen)

hematopoetic agent

Answer 11

• recombinant human erthropoetin
• erythropoetin is synthesized in kidney in repsone to hypoxia or anemia, stimulates erythropoiesis

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indication
* drug is indicated for anema in pts w/ chronic renal failure (unable to synthesize erthropoetin
* for correcting zidovudine (AZT)-induced anemia in HIV infected + chemotherapy induced anema in cancer pts

pharmco
* takes several weeks of therapy before hematocrit rise; this drug cannot replace transfusions for acute tx of severe anemia

contra
* not used in pts w/ uncontrolled HTN d/t elevated hematocrit exacerbating HTN

Question 12

filgrastim (G-CSF) (neupogen)

hematopoetic agent

Answer 12

• human recombinant granulocyte colonyl stimulating factor (G-CSF)
• helps induces synthesis of neutrophils from progenitor cells
• prevent neutropenia espcially with chemotherapy that includes highers doses of myelosuppressive drugs — l/t potential development of toxicities that were previously rarely seen

indication:
* tx of severe cyclic neutropenia and severe chronic neutropenia

effect
* medullary bone pain d/t rapid cell proliferation wtihin marrow

contra
* should not be used within 24 hrs of administration of cancer drugs d/t effect of cytotoxic agent w/ rapidly dividing myleloid cells not clear

Question 13

sargramostim (GM-CSF)

hematopoetic agent

Answer 13

• human recombinant granulocyte-macrophage colony timualting factor (GM-CSF)
• stimulates proliferation of all lines of blood cells
• induces maturation of granulocytes and macrophages BUT NOT erthrocytes or megakaryoctes
• this drug also activates the former two as well!

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indication
* accerlerate bone marrow replenishment following autologus (obtained from same individual) bone marrow transplantation

risk of it acting as a growth factor for other cancer types unknown…

Question 14

oprelvekin (interleukin II, neumega)

hematopoetic agent

Answer 14

• recombinant growth factor that stimulates platelet production

indication
* maintaining platelet counts following chemotherapy
* shows limited efficacy

toxicity includes
* fluid retention
* tachycardia
* other CV rxn