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Pharmacology

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Cancer Chemotherapy

Question
76 out of 100
 

EGFR antagonist, Cetuximab is used in cases of



A Palliative t/t of head and neck cancer

B Anal canal carcinoma

C Gastric carcinoma

D Small cell lung carcinoma

Ans. A palliative therapy of head and neck cancer.

a. Cetuximab and pemtumomab (Vectibix) are directed against the epidermal growth factor receptor (EGFR), a transmembrane glycoprotein involved in signaling pathways affecting growth and proliferation of tumor cells.

b. Both cetuximab and pemtumomab, when given alone, have been shown to benefit a small proportion of previously treated patients

c. Cetuximab appears to have therapeutic synergy with such chemotherapeutic agents as irinotecan, even in patients previously resistant to this drug; this suggests that cetuximab can reverse cellular resistance to cytotoxic chemotherapy.

d. The use of both cetuximab and pemtumomab can lead to an acne-like rash with the development and severity of the rash being correlated with the likelihood of antitumor efficacy.

e. Inhibitors of the EGFR tyrosine kinase such as erlotinib (TarcevA. do not appear to be effective in colorectal cancer

Harrison has given a extensive table for molecularly targeted therapy. In this use of cetuximab in head & neck cancers is mentioned.

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 the PML-RAR

Imatinib

Bcr-Abl, c-Abl, c-Kit, PDGFR-/,

Chronic myelogenous leukemia; GIST

Blocks ATP binding to tyrosine kinase active site.

Sunitinib

c-Kit, VEGFR-2, PDGFR-, Flt-3

GIST; renal cell cancer

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

Sorafinib

RAF, VEGFR-2, PDGFR-/, Flt-3, c-Kit

RCC; may have activity in melanoma when combined with chemotherapy

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.

Gefitinb

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 chemotherapy and radiotherapy.

Panitumomab

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.

Note: PML-RAR, promyelocytic leukemia–retinoic acid receptor-alpha; AML, acute myeloid leukemia; t(15;17), translocation between chromosomes 15 and 17; VEGFR, vascular endothelial growth factor receptor; PDGFR, platelet-derived growth factor receptor; Flt-3, fms-like tyrosine kinase-3; GIST, gastrointestinal stromal tumor; RCC, renal cell cancer; EGFR, epidermal growth factor receptor; TGF-, transforming growth factor alphA.

According to GG – cetuximab can be used in all those cancers, which express EGFR – head & neck, breast, lung, kidney, prostate, brain and Pancreas.

Cancer Chemotherapy Flashcard List

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