Quiz 10

Question 1

tamoxifen 1

Answer 1

Brand: Nolvadex, Soltamox
Class: Estrogen Receptor Antagonist; SERM
Indication: Metastatic (female and male) breast cancer; adjuvant treatment of breast cancer after primary treatment with surgery and radiation; reduce risk of invasive breast cancer in women with ductal carcinoma in situ (DCIS) after surgery and radiation; reduce the incidence of breast cancer in women at high risk

Question 2

tamoxifen 2

Answer 2

MOA: Competitively binds to ER on tumors & other tissue targets, producing a nuclear complex that decreases DNA synthesis & inhibits estrogen effects; cells accumulate in the G0 & G1 phases; therefore, tamoxifen is cytostatic rather than cytocidal.
BBW: Ductal carcinoma in situ/women at high risk for breast cancer
SE: Menopausal flushing, irregular periods, vaginal discharge

Question 3

anastrozole 1

Answer 3

Brand: Arimidex
Class: Aromatase Inhibitor
Indication: First-line treatment of locally-advanced or metastatic breast cancer in postmenopausal women, Adjuvant treatment of early hormone receptor-positive breast cancer in postmenopausal women, Treatment of advanced breast cancer in postmenopausal women with disease progression following tamoxifen therapy

Question 4

anastrozole 2

Answer 4

MOA: Potent & selective nonsteroidal aromatase inhibitor. By inhibiting aromatase, the conversion of androstenedione to estrone & testosterone to estradiol is prevented, thereby decreasing tumor mass or delaying progression in patients with tumors responsive to hormones. Anastrozole causes an 85% decrease in estrone sulfate levels.
BBW: N/A
SE: vasodilation, ischemic heart disease, HTN, angina pectoris, edema, fatigue, mood disorder, HA, pain, depression, skin rash, hot flash, GI distress, N/V, weakness, arthritis, arthralgia, back pain, ostealgia, osteoporosis, pharyngitis, dyspnea, increased cough

Question 5

trastuzumab 1

Answer 5

Brand: Herceptin
Class: Anti-HER2 humanized Monoclonal Antibody
Indication: breast CA, gastric CA

Question 6

trastuzumab 2

Answer 6

MOA: binds to the extracellular domain of the human epidermal growth factor receptor 2 protein (HER-2); mediates antibody-dependent cellular cytotoxicity by inhibiting proliferation of cells which overexpress HER-2 protein
BBW: Cardiomyopathy, infusion reactions & pulmonary toxicity, embryo-fetal toxicity
SE: decreased LVEF, pain, chills, HA, insomnia, dizziness, skin rash, N/V/D, abdominal pain, anorexia, infection, weakness, back pain, cough, dyspnea, rhinitis, pharyngitis, infusion related reaction, fever

Question 7

rituximab 1

Answer 7

Brand: Rituxan
Class: Anti-CD20; Chimeric Monoclonal Antibody; Antirheumatic, immunosuppressant
Indication: Non-Hodgkin’s Lymphoma, CLL, rheumatoid arthritis, granulomatosis with polyangiitis, microscopic polyangiitis

Question 8

rituximab 2

Answer 8

MOA: directed against the CD20 antigen on B-cells. CD20 regulates cell cycle initiation; & possibly functions as a Ca channel. Binds to the antigen on the cell surface, activating complement-dependent B-cell cytotoxicity; & to human Fc receptors, mediating cell killing through an antibody-dependent cellular toxicity. B-cells are believed to play a role in the development & progression of rheumatoid arthritis. Signs & symptoms of RA are reduced by targeting B-cells & the progression of structural damage is delayed.
BBW: Fatal infusion reactions, severe mucocutaneous infections, HBV reactivation, progressive multifocal leukoencephalopathy
SE: peripheral edema, HTN, fever, fatigue, chills, HA, insomnia, pain, rash, pruritus, angioedema, N/D, abdominal pain, weight gain, cytopenias, lymphopenia, anemia, leukopenia, neutropenia, neutropenic fever, thrombocytopenia, ALT increased, neuropathy, weakness, muscle spasms, arthralgia, cough, rhinitis, epistaxis, infusion-related reaction, infection, human antichimeric antibody positive, night sweats

Question 9

erlotinib 1

Answer 9

Brand: Tarceva
Class: EGFR Inhibitor; Tyrosine Kinase Inhibitor
Indication: NSCLC, pancreatic cancer

Question 10

erlotinib 2

Answer 10

MOA: Reversibly inhibits overall epidermal growth factor receptor (HER1/EGFR) - tyrosine kinase activity. Intracellular phosphorylation is inhibited which prevents further downstream signaling, resulting in cell death. It has higher binding affinity for EGFR exon 19 deletion or exon 21 L858R mutations than for the wild type receptor.
BBW: N/A
SE: chest pain, fatigue, skin rash, , paronychia, alopecia, acne vulgaris, N/V/D, anorexia, decreased appetite, mucositis, stomatitis, abdominal pain, constipation, UTI, anemia, increased susceptibility to infection, fever, weakness, back pain, arthralgia, musculoskeletal pain, conjunctivitis, keratoconjunctivitis sicca, cough, dyspnea

Question 11

imatinib 1

Answer 11

Gleevec
Class: BCR-ABL Tyrosine Kinase Inhibitor
Indication: GI stromal tumors, Ph (+) CML, Ph (+) ALL, aggressive systemic mastocytosis (ASM), dermatofibrosarcoma protuberans (DFSP), hypereosinophilic syndrome +/- chronic eosinophilic leukemia (CEL), myelodysplastic/myeloproliferative disease (MDS/MPD)

Question 12

imatinib 2

Answer 12

MOA: Inhibits Bcr-Abl tyrosine kinase, the constitutive abnormal gene product of the Philadelphia chromosome in CML. Inhibition of this enzyme blocks proliferation & induces apoptosis in Bcr-Abl positive cell lines as well as in fresh leukemic cells in Philadelphia chromosome positive CML. Also inhibits tyrosine kinase for platelet-derived growth factor (PDGF), stem cell factor (SCF), c-Kit, & cellular events mediated by PDGF & SCF.
BBW: N/A
SE: everything, according to UpToDate

Question 13

bevacizumab 1

Answer 13

Brand: Avastin
Class: Humanized Monoclonal Antibody - VEGF Inhibitor
Indication: cervical cancer, colorectal cancer, glioblastoma, NSCLC, renal cell carcinoma

Question 14

bevacizumab 2

Answer 14

MOA: Binds to & neutralizes VEGF, preventing its association with endothelial receptors, Flt-1 and KDR. VEGF binding initiates angiogenesis (endothelial proliferation & the formation of new blood vessels). The inhibition of microvascular growth is believed to retard the growth of all tissues (including metastatic tissue)
BBW: GI perforations, surgery and wound healing complications, hemorrhage
SE: HTN, VTE, hypotension, peripheral edema, pain, fatigue, HA, dizziness, taste disorder, neuropathy, alopecia, xeroderma, exfoliative dermatitis, skin discoloration, ovarian failure, weight loss, abd pain, proteinuria, hemorrhage, leukopenia, neutropenia, infection, myalgia, upper respiratory tract infection, postoperative wound complication, dyspnea, rhinitis, epistaxis, UTI, GI hemorrhage, increased SCr, N/V/D

Question 15

cetuximab 1

Answer 15

Brand: Erbitux
Class: EGFR Inhibitor; Chimeric Monoclonal Antibody
Indication: KRAS mutation-negative (wild-type), EGFR-expressing metastatic colorectal cancer; head & neck cancer,

Question 16

cetuximab 2

Answer 16

MOA: binds specifically to the epidermal growth factor receptor (EGFR, HER1, c-ErbB-1) & competitively inhibits the binding of epidermal growth factor (EGF) & other ligands. Binding to the EGFR blocks phosphorylation & activation of receptor-associated kinases, resulting in inhibition of cell growth, induction of apoptosis, & decreased matrix metalloproteinase & vascular endothelial growth factor production. EGFR signal transduction results in KRAS wild-type activation; cells with KRAS mutations appear to be unaffected by EGFR inhibition
BBW: infusion reaction, cardiopulmonary arrest
SE: fatigue, malaise, pain, peripheral sensory neuropathy, HA, insomnia, confusion, chills, rigors, anxiety, depression, desquamation, acneiform eruption, radiodermatitis, xeroderma, pruritis, changes in nails, acne vulgaris, paronychia, palmar-plantar erythrodysesthesia, skin fissure, alopecia, weight loss, rash, hypocalcemia, hypokalemia, dehydration, neutropenia, leukopenia, increased ALT/AST/ALP, hypomagnesemia, N/V/D, stomatitis, infection, ostealgia, dyspnea, arthraliga, conjunctivitis, fever, infusion related reaction, pharyngitis,

Question 17

nivolumab 1

Answer 17

Opdivo
Class: Anti PD-1 Human Monoclonal Antibody
Indication: Hodgkin lymphoma, melanoma, NSCLC, renal cell CA

Question 18

nivolumab 2

Answer 18

MOA: IgG4 monoclonal antibody that inhibits programmed cell death-1 (PD-1) activity by binding to the PD-1 receptor to block the ligands PD-L1 and PD-L2 from binding. The negative PD-1 receptor signaling that regulates T-cell activation and proliferation is therefore disrupted. This releases PD-1 pathway-mediated inhibition of the immune response, including the antitumor immune response.
BBW: N/A
SE: edema, peripheral edema, fatigue, HA, peripheral neuropathy, peripheral sensory neuropathy, skin rash, pruritis, vitiligo, exfoliative dermatitis, hyponatremia, elevated triglycerides, hyperkalemia, increased TSH, hypocalcemia, elevated cholesterol, hypercalcemia, hypothyroid, hypomagnesemia, hyopkalemia, hyperglycemia, diarrhea, colitis, decreased appetite, constipation, vomiting, josh spencer, abd pain, increased serum amylase, increased serum lipase, lymphocytopenia, anemia, neutropenia, antibody development, fever, infusion reactions, elevated ALT & bilirubin, pneumonia, dyspnea, cough

Question 19

bortezomib 1

Answer 19

Brand: Velcade
Class: Proteasome Inhibitor
Indication: mantle cell lymphoma, multiple myeloma

Question 20

bortezomib 2

Answer 20

MOA: inhibits proteasomes, enzyme complexes which regulate protein homeostasis within the cell. Specifically, it reversibly inhibits chymotrypsin-like activity at the 26S proteasome, leading to activation of signaling cascades, cell-cycle arrest, and apoptosis.
BBW: N/A
SE: Just read Micromedex. I ain’t typing all that shit.

Question 21

abiraterone 1

Answer 21

Brand: Zytiga
Class: Antiandrogen
Indication: prostate CA

Question 22

abiraterone 2

Answer 22

MOA: Selectively and irreversibly inhibits CYP17, an enzyme required for androgen biosynthesis which is expressed in testicular, adrenal, & prostatic tumor tissues. Inhibits the formation of the testosterone precursors dehydroepiandrosterone & androstenedione.
BBW: N/A
SE: elevated trigylcerides, hyperglycemia, hypernatermia, hypoK, hypoPhos, hot flash, diarrhea, dyspepsia, UTI, lymphocytopenia, elevated ALT/AST, joint swelling, myalgia, cough, dyspnea, nasopharyngitis, edema, HTN, fatigue, insomnia, bruise

Question 23

lenalidomide 1

Answer 23

Brand: Revlimid
Class: Angiogenesis inhibitor, immunomodulator
Indication: mantle cell lymphoma, multiple myeloma, myelodysplastic syndrome

Question 24

lenalidomide 2

Answer 24

MOA: Immunomodulatory, antiangiogenic, & antineoplastic characteristics via multiple mechanisms. Selectively inhibits secretion of proinflammatory cytokines (potent inhibitor of TNF-alpha); enhances cell-mediated immunity by stimulating proliferation of anti-CD3 stimulated T cells (resulting in increased IL-2 and interferon gamma secretion); inhibits trophic signals to angiogenic factors in cells. Inhibits the growth of myeloma cells by inducing cell cycle arrest & cell death.
BBW: fetal & hematologic toxicity, venous & arterial thromboembolism
SE: bunches