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Monoclonal Antibodies: MABS

 

Some FDA-Approved Molecularly Targeted Agents for the Treatment of Cancer

 

Drug

Molecular Target

Disease

Mechanism of Action

All-trans retinoic acid (ATRA)

PML-RAR oncogene

Acute promyelocytic leukemia M3 AML; t(15;17)

Inhibits transcriptional repression by PML-RAR

Imatinib

Dasatinib

 

Nilotinib

Bcr-Abl, c-Abl, c-Kit, PDGFR-â/β

Chronic myeloid leukemia; GIST

Blocks ATP binding to tyrosine kinase active site

Sunitinib

c-Kit, VEGFR-2, PDGFR-ââ, Flt-3

GIST; renal cell cancer

Inhibits activated c-Kit and PDGFR in GIST; inhibits VEGFR in RCC

Sorafenib

RAF, VEGFR-2, PDGFR α/β, Flt-3, c-Kit

RCC; hepatocellular carcinoma

Targets VEGFR pathways in RCC. Possible activity against BRAF in melanoma, colon cancer, and others

Erlotinib

EGFR

Non-small cell lung cancer; pancreatic cancer

Competitive inhibitor of the ATP-binding site of the EGFR

Gefitinib

EGFR

Non-small cell lung cancer

Inhibitor of EGFR tyrosine kinase


Bortezomib

Proteasome

Multiple myeloma

Inhibits proteolytic degradation of multiple cellular proteins

 

Monoclonal Antibodies 

Trastuzumab

HER2/neu (ERBB2)

Breast cancer

Binds HER2 on tumor cell surface and induces receptor internalization

Cetuximab

EGFR

Colon cancer, squamous cell carcinoma of the head and neck

Binds extracellular domain of EGFR and blocks binding of EGF and TGF-; induces receptor internalization. Potentiates the efficacy of chemotherapy and radiotherapy

Panitumumab

EGFR

Colon cancer

Like cetuximab; likely to be very similar in clinical activity

Rituximab

CD20

B cell lymphomas and leukemias that express CD20

Multiple potential mechanisms, including direct induction of tumor cell apoptosis and immune mechanisms

Alemtuzumab

CD52

Chronic lymphocytic leukemia and CD52-expressing lymphoid tumors

Immune mechanisms

Bevacizumab

VEGF

Colon, lung, breast cancers; data pending in other tumors

Inhibits angiogenesis by high-affinity binding to VEGF





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