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22 Cards in this Set

  • Front
  • Back

Targeted Therapy

Human EGFR Family

erbB1, erbB2, erbB3 (no RTK activity), erbB4



erbB1 = HER1, EGFR


erbB2 = HER2, neu


erbB3 = HER3


erbB4 = HER4

EGFR antagonist

-예: Cetuximab, Trastuzumab, Pantimumab




Cetuximab

-EGFR1 targeting


-Colon, H&N cancer


-used in comb with chemo & radiation


-KRAS mutation: important prognostic factor (KRAS 없는 사람한테 약이 더 잘 든다)


-IV infusion

Trastuzumab (aka Herceptin)

-HER2 targeting


-Breast cancer


-IV infusion.


-30 % 의 HER2 positive cancer breast cancer 에 매우 효과적이다.

Panitumumab

-EGFR1 targeting


-Metastatic colorectal cancer 에 사용/monotherapy 가능.

Lapatinib (TKI)

-works inside the cell: targeting both ErbB1 & ErbB2.


Non Receptor Tyrosine Kinase (Src/ABL)

-Philadelphia chromosome: section of chromosome 22 breaks off and translocates to chromosome 9 --> formation of Bcr/Abl


-Inhibitor: Imatinib

Imatinib (aka Gleevec)

-TKI


-GIST (Gastrointestinal stromal tumors) with cKIT positive; Ph+ CML, Ph+ ALL


-administration: Oral

Nilotonib

-modification of imatinib structure to allow tighter binding


-TKI inhibitor


-Ph+ CML in chronic/accelerated phase


-administration: Oral

Dasatinib

-Src/Abl inhibitor


-CMLs that are resistant to imatinib


-administration: Oral

Gefitinib

-loclly advanced stage or metastatic NSCLC


-oral

Erlotinib

-TKI


-locally advanged or metastatic NSCLC

Lapatinib

-ErbB1 and ErbB2 TKI


-HER2 overexpressing advanced or metastatic breast cancer


-Oral administration.

VEGF targeting drugs

Bevacizumab

-anti-VEGF monoclonal antibody


-Metastatic colorectal cancer, NSCLC, HER2 negative breeast cancer, glioblastoma, RCC.


-Oral with food.


-Serious ophthalmic adverse effect + rebound 로 혈관 생성

Sunitinib

-VEGFR TK inhibitor


-GIST resistant to imatinib; advanced RCC

Sorafenib

-multitarget TKI


-Advanced RCC, HCC.

Bortezomib

-26S proteasome inhibitor


-multiple myeloma/relapsed lymphoma


-rapid IV

ATRA (all-trans-retinoic acid)

-targets the PML-RAR fusion protein


-acute promyelocytic leukemia (APL)

Bexarotene

-A synthetic retinoid X receptor (RXR) ligand


-cutaneous T cell lymphoma

Vorinostat

-Histone Deacetylase Inhibitor


-Progressive, persistent T-cell lymphoma 에 사용.