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36 Cards in this Set

  • Front
  • Back

Anti-CTLA4

reduces T cell regulatory, incr. immune response




S/E = autoimmune dz

Anti-CTLA4 used for

metastatic melanoma

CTLA4 agonists

increase T cell regulatory


approved for Rx of rheumatoid arthritis

Anti PD-1, PDL-1, PDL-2 MOA

programmed cell death; reduces T reg so increases the immune response

Anti PD-1 Rx

metastatic non small cell lung cancer, metastatic melanoma

Interleukin-2

stimulates lymphocytes

Interferon

increase immune response to infection & cancer




S/E = symptoms of viral infection

Hypomethylating agents

increase tumor suppressor, useful in myelodysplasia


Methylation in Glioblastoma

methylation of MGMT reduces expression of MGMT, making chemotherapy more effective & prognosis improved

Histone deacetylase inhibitors (HDAC)

express genes that may stop tumor suppressors = useful in T cell lymphoma

EGFR

epidermal growth factor, transmembrane protein

other names for EGFR

EGFR1, ERB1, HER1

EGFR inside drugs

tyrosine kinase inhibitors = nibs

EGFR activation =

apoptosis resistance, proliferation, angiogenesis, metastasis

Adenocarcinoma of lung with EGFR mutation

most prevalent in Asia, women, non-smokers


erlotinib treatment

EML4/ALK translocation causing adenocarcinoma of the lung

more common in non smokers


respond to crizotinib

Rx stage IV adenocarcinoma lung

EGFR mutation exon 19, 21 = erlotinib


EML4/ALK = crizotinib


Squamous or small cell = Pemetrexed

KRAS mutation

colorectal cancer

EGFR-targeted monoclonal antibodies in metastatic colorectal cancer

Cetuximab (chimeric protein), Panitumumab (fully humanized)

when KRAS gene is mutation...

protein is active regardless of EGFR activation




40-45% of colorectal cancer patients




don't give EGFR monoclonal antibody

Luminal A breast cancer

strongly estrogen receptor positive


responds to anti-hormone therapy

Luminal B breast cancer

weakly estrogen receptor positive


give anti-hormone therapy and chemotherapy

Basal breast cancer

Triple negative


give chemotherapy

Her 2 Neu

type of breast cancer


chromosome 17


overexpression leads to increased cell signaling


one of the best prognosis due to targeted Rx

prevent proliferation of Her2

extracellular antibody, TK inhibitor, prevent dimerization of 2/3, link antibody w/ potent chemo-rx

prevent Her2 dimerization

Pertuzumab

Lapatinib

TK inhibitor: EGFR (Her1) and Her2

side effects of EGFR1 inhibitors

diarrhea, rash

Trastuzumab emtansine (T-DM1)

monoclonal antibody (anti-Her2) linked w/ potent chemotherapy (Her 2 breast cancer)

Her2 is expressed in 20% of

gastric cancers - use trastuzumab for metastatic gastric cancer, less effective than in breast cancer

Tamoxifen (SERM)

anti-estrogen (breast, ovarian fxn)


pro-estrogen (bones, CV, uterus)

Anti-VEGF antibodies

Bevacizumab (VEGF-A), Ramucirumab (VEGFR2)

uses of bevacizumab

colon, lung, glioblastoma, stomach, kidney cancer

Soluble VEGF receptors

VEGF-TRAP, treat colon cancer

small-molecule VEGFR inhibitors

axitinib, pazotinib, sunitinib, sorafenib

uses of axitinib, pazotinib, sunitinib, sorafenib

renal, hepatoma, gastro-intestinal stromal cancers