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Targeted Therapies
N/A
41
Other
Post-Graduate
11/21/2011

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Cards

Term
What 3 things can be affected to block proliferation?
Definition
-Blocking the cell surface receptor
-Targeting Tyr kinase
-Targeting mTOR
Term
How are Cell surface receptors Ab administered?
Definition
SubQ
Term
What are the disadvantages of cell surface receptor Ab?
Definition
Large mass-> poor tumor penetration
Heterogeneous/insufficient tumor Ag expression
Specificity - normal cells express Ag
Mouse Ab and derivative ofter induce human anti-mouse Ab - treatment loses efficacy
Term
What is the mechanism of cell surface receptor Ab?
Definition
Complement dependent cytotoxicity
Term
Trastuzumab
Definition
Breast
-apoptosis, ADCC
-EGFR-2, Her-2/neu
Term
Bevacizumab
Definition
Colorectal
Non-small-cell Lung Carcinoma
Renal
Pancreatic
-Antiangiogenesis, neovascularization
-VEGF block
(**GI perforation**)
Term
Rituximab
Definition
Non-Hodgkins Lymphoma
Chronic Lymphocytic Leukemia
RA
-apoptosis, ADCC, CDC
-Targets CD20
(Vaccination?)
Term
Alemtuzumab
Definition
Chronic Lymphocytic Lymphoma
Stem Cell Prep for transplantation
-Apoptosis, ADCC, CDC
-Targets CD-52
Term
What Antibody therapies are used to treat Colorectal Cancer?
Definition

Cetuximab (EGFR-1/Her-1)

Panitumuma (EGFR-1/Her-1)

Bevacizumab (VEGF)

Term
What Antibody treatments are used to treat Non-Hodgkins Lymphoma?
Definition

Rituximab (CD20)

Ibritumomab Tiuxetan (CD20)

Tositumomab (CD20)

Term
What antibody treatments are used to treat Chronic Lympocytic Leukemia?
Definition

Rituximab (CD20)

Ofatumumab (CD20)

Alemtuzumab (CD52)

Term
What antibody treatments are used for stem cell preparation for transplantation?
Definition

Alemtuzumab (CD52)

Tositumomamab (CD20)

Term
What Agents have antibodies to VEGFR?
Definition
Bevacizumab Trastuzumab
Term
What agent has antibodies to CD20?
Definition

Rituximab

Term
What agents have antibodies to CD52?
Definition
Alemtuzumab
Term
What are the problems with Tyrosine Kinase Inhibitors and their specificity?
Definition
TKIs may target TK involved in normal body function
Many TK's are structurally related
Most TKI's act on ATP binding sites which are highly conserved
Term
What are the EGFR TKIs?
Definition

Gefitinib Erlotinib

(GEL)

Term
What tumors are all the EGFR TKIs used against?
Definition
Breast
Term
What are Gefitinib and Erlotinib used for? (EGFR TKIs)
Definition
Breast
Ovarian
NSCLC
mesothelioma
colorectal
head & neck cancers
Term
What are the BCR-ABL TKIs?
Definition
Imatinib
Dasatinib
Term
What cancers are the BCR-ABL TKIs effective against?
(Imatinib, Dasatinib)
Definition
Chronic Myelogenous Leukemia
Acute Lymphoblastic Leukemia
Term
If a patient is resistant to Imatinib what agent can be used? why?
Definition
Dasatinib
due to different binding
Term
What is the VEGF TKIs?
Definition

Sunitinib

(SSP)

Term
What are all of the VEGF TKIs effective against?
(Sunitinib)
Definition
Renal Cell
Term
What VEGF TKI is effective against GI stromal cancer?
Definition
Sunitinib
Term
What VEGF TKIs may cause QT Prolongation?
Definition
Sunitinib
Term
What is the mTOR Inhibitor?
Definition
Sirolimus
Term
What is the antiviral and antineoplastic activity of IFN-alpha-2a?
Definition
Arrests cell cycle in G0
Induces apoptosis
Induces IR (CTLs, NK cells)
Term
What is done to IFN-alpha-2a to make it better tolerated and longer lasting?
Definition
pegylated
Term
What are the side effects of INF-alpha-2a?
Definition
Neuropsychiatric
Extended Flu-like symptoms
Term
What is the mechanism of Bortezomib?
Definition
Inhibits proteosome function-> incr IkB-> incr IkB bound to NFkB-> decreased transcription of proliferative and antiapoptotic genes-> apoptosis, growth inhibition, reduced angiogenesis
Term
what other proteins are affected by Bortezomib?
Definition
Cyclin-dependent kinases
p53
Bax
Cyclins
Term
What are the GnRH Agonists?
Definition
Leuprolide
Goserelin
Term
What Hormone agents are used to treat metastasis for prostatic tumors?
Definition
Leuprolide
Goserelin
Term
What is the Androgen Receptor Blockers? Where does it bind?
Definition
Flutamide


Irreversibly inhibit androgen binding at hypothalamus, pituitary, and prostate
Term
What are the Selective estrogen receptor modulators?
Definition
Tamoxifen
Raloxifene
Term
What do Both the SERMs have a blackbox warning against? (Tamoxifen, Raloxifene)
Definition
Thromboembolic disease, Stroke
Term
What does Tamoxifen have a blackbox warning against?
Definition
Endometrial Hypertrophy and cancer
vaginal bleeding
thomboembolic disease
Stroke
Term
What are the Aromatase Inhibitors?
Definition
Anastrazole
Letrozole
Exmestane
Term
How do the Aromatase Inhibitors work?
(Anastrazole, Letrozole, Exmestane)
Definition
Interrupt normal metabolism of estrogen/testosterone - Bind to heme center of CYP protein
Term
What are the 2 types of Aromatase Inhibitors?
Definition
Non-Steroidal - reversible
Steroidal - irreversible
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