Drug Table - Misc Agents Flashcards
Imatinib (Gleevac) Class
Tyrosine Kinase
inhibitor
Imatinib (Gleevac) Mechanism
Inhibits Abl kinase by binding where ATP
should go; also inhibits PDGFR and c-kit;
metabolized by cytochrome P450
Imatinib (Gleevac) Therapeutics
First line therapy for CML; also, gastrointestinal tumor (GIST)
Imatinib (Gleevac) Imp Side effects
Nausea and vomiting, fluid
retention, muscle cramps,
arthralgia
Imatinib (Gleevac) Other side effects
Myelosuppression
Imatinib (Gleevac) Misc
Oral (1/day)
Gefitinib (Iressa) Class
Tyrosine Kinase
inhibitor
Gefitinib (Iressa) Mechanism
Inhibit epidermal growth factor receptor
(EGFR) tyrosine kinase
Gefitinib (Iressa) Therapeutics
Non-small lung cancer
Erlotinib (Tarceva) Class
Tyrosine Kinase
inhibitor
Erlotinib (Tarceva) Mechanism
Inhibit epidermal growth factor receptor
(EGFR) tyrosine kinase
Erlotinib (Tarceva) Therapeutics
Non-small lung cancer
Nilotinib (Tasigna) class
Tyrosine Kinase
inhibitor
Nilotinib (Tasigna) Mechanism
Inhibits Abl kinase
Nilotinib (Tasigna) Therapeutics
Imatinib-resistant CML
Nilotinib (Tasigna) Imp side effects
Myelosuppression
Nilotinib (Tasigna) other side effects
QT prolongation, hepatotoxicity,
electrolyte abnormalities
Nilotinib (Tasigna) misc
Oral (2/day)
Dasatinib (Sprycel) class
Tyrosine Kinase
inhibitor
Dasatinib (Sprycel) mechanism
Inhibits Abl & Src kinases
Dasatinib (Sprycel) therapeutics
Imatinib-resistant CML
Dasatinib (Sprycel) Imp side effects
Myelosuppression, bleeding, fluid
retention, pulmonary arterial
hypertension
Dasatinib (Sprycel) other side effects
Diarrhea, nausea and vomiting,
weakness, infections
Dasatinib (Sprycel) misc
Oral (1/day)
Rituximab (Rituxan) class
Monoclonal
antibody
Rituximab (Rituxan) mechanism
CD20 B-cell antibody that can directly
activate apoptosis, activate complement, or
activate cell-mediated cytotoxicity (e.g., T
cells, NK cells)
Rituximab (Rituxan) therapeutics
Non-Hodgkin’s lymphomas
Rituximab (Rituxan) imp side effects
Infusion reactions, tumor lysis syndrome (TLS), severe mucocutaneous reactions, progressive multifocal leukoencephalopathy (PML)
Rituximab (Rituxan) other side effects
Skin reactions, irregular
heartbeat, muscle or joint pain
Rituximab (Rituxan) misc
Patients need careful monitoring
Trastuzumab (Herceptin) class
Monoclonal
antibody
Trastuzumab (Herceptin) mechanism
Unknown HER2/neu (ErbB2) receptor
antibody mechanism (enhanced receptor
endocytosis or blocking homo- or
heterodimerization)
Trastuzumab (Herceptin) therapeutics
HER2/neu-overexpressing metastatic
breast cancer
Trastuzumab (Herceptin) Imp side effects
Hypersentivity reaction; ventricular
dysfunction
Trastuzumab (Herceptin) misc
Usually combined with taxanes;
enhances doxorubicin cardiotoxicity
Cetuximab (Erbitux) class
Monoclonal
antibody
Cetuximab (Erbitux) mechanism
EGFR1 (ErbB1)
Cetuximab (Erbitux) therapeutics
EGFR-positive metastatic colorectal
cancer
Cetuximab (Erbitux) imp side effects
Allergic reactions, sudden cardiac
death, dermatologic problems,
infections, renal failure, electrolyte
abnormalities
Cetuximab (Erbitux) other side effects
Asthenia/malaise, fever,
nausea, constipation, interstitial
pneumonitis
Cetuximab (Erbitux) misc
Clinical trials, probably combine with
cisplatin
Cetuximab (Erbitux) class
Monoclonal
antibody
Cetuximab (Erbitux) mechanism
EGFR1 (ErbB1)
Cetuximab (Erbitux) therapeutics
EGFR-positive metastatic colorectal
cancer
Cetuximab (Erbitux) imp side effects
Allergic reactions, sudden cardiac
death, dermatologic problems,
infections, renal failure, electrolyte
abnormalities
Cetuximab (Erbitux) other side effects
Asthenia/malaise, fever,
nausea, constipation, interstitial
pneumonitis
Cetuximab (Erbitux) misc
Clinical trials, probably combine with
cisplatin
Ipilimumab (Yervoy) class
Human
monoclonal
antibody
Ipilimumab (Yervoy) mechanism
Cytotoxic T-Lymphocyte Antigen 4 inhibitor;
stimulates immune system
Ipilimumab (Yervoy) therapeutics
Melanoma
Vemurafenib (Zelboraf) class
Serine/threonine
kinase inhibitor
Vemurafenib (Zelboraf) mechanism
Inhibits oncogenic BRAF kinase
Vemurafenib (Zelboraf) therapeutics
Unresectable Stage III and IV or
metastatic melanomas w/BRAF
mutations
Vemurafenib (Zelboraf) imp side effects
Arthralgia, fatigue, photosensitivity,
nausea, alopecia, diarrhea, QT
prolongation
Vemurafenib (Zelboraf) other side effects
Cutaneous squamous cell
carcinoma, keratoacanthoma,
new primary cutaneous
melanoma
Vemurafenib (Zelboraf) misc
Superior to dacarbazine in Phase III
trials
Dabrafenib (Tafinlar) class
Serine/threonine
kinase inhibitor
Dabrafenib (Tafinlar) mechanism
Inhibits oncogenic BRAF kinase
Dabrafenib (Tafinlar) therapeutics
Unresectable Stage III and IV or
metastatic melanomas w/BRAF
mutations
Dabrafenib (Tafinlar) imp side effects
Serious febrile drug reactions,
uveitis and iritis, hyperglycemia,
hyperkeratosis
Dabrafenib (Tafinlar) other side effects
Higher risk of developing:
Serious febrile drug reactions,
uveitis and iritis, hyperglycemia,
hyperkeratosis
Dabrafenib (Tafinlar) misc
May cause male infertility
Trametinib (Mekinist) mechanism
Inhibits MEK
Trametinib (Mekinist) therapeutics
Unresectable Stage III and IV or
metastatic melanomas w/BRAF
mutations
Trametinib (Mekinist) imp side effects
Cardiomyopathy, retinal disorders,
interstitial lung disease, serious
skin toxicities
Trametinib (Mekinist) other side effects
Rash, diarrhea, stomatitis,
hypertension, pruritis
Trametinib (Mekinist) misc
May cause female infertility
Hydroxyurea (Hydrea) mechanism
Inhibits ribonucleoside diphosphate
reductase
Hydroxyurea (Hydrea) therapeutics
CML (replaced by Imatinib),
polycythemia vera, essential
thrombocythemia; treatment for sickle
cell disease (increases Hb-F)
Retinoids Mechanism
ATRA induces terminal differentiation in
malignant immature promyelocytes, which
subsequently apoptose
Retinoids Therapeutics
APL
Retinoids imp side effects
“Leukocyte Activation Syndrome”
(LAS), an increase in WBCs (fever,
weight gain, respiratory distress,
serosal effusion, renal failure)
Retinoids misc
Combined w/anthracyclines;
corticosteroids used to block “LAS”
Arsenic Trioxide (Trisenox) Therapeutics
Relapsed APL
Thalidomide (Thalomid) Therapeutics
Multiple myeloma and myelodysplastic
syndromes
Interferons
Hairy-cell leukemia, CML, and AIDSrelated
Kaposi’s sarcoma