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Hematology and oncology ` hematology and oncology—PhaRmacology Hematology and oncology ` hematology and oncology—PhaRmacology SectIon III 443

Imatinib, dasatinib, nilotinib
mechanISm Tyrosine kinase inhibitors of bcr-abl (encoded by Philadelphia chromosome fusion gene in CML)
and c-kit (common in GI stromal tumors).

clInIcal USe CML, GI stromal tumors (GISTs).
adVeRSe eFFectS Fluid retention.

Rituximab
mechanISm Monoclonal antibody against CD20, which is found on most B-cell neoplasms.
clInIcal USe Non-Hodgkin lymphoma, CLL, ITP, rheumatoid arthritis, TTP, AIHA.
adVeRSe eFFectS  risk of progressive multifocal leukoencephalopathy.

Bortezomib, carfilzomib

mechanISm Proteasome inhibitors, induce arrest at G2-M phase and apoptosis.
clInIcal USe Multiple myeloma, mantle cell lymphoma.
adVeRSe eFFectS Peripheral neuropathy, herpes zoster reactivation.

Tamoxifen, raloxifene
mechanISm Selective estrogen receptor modulators (SERMs)—receptor antagonists in breast and agonists in
bone. Block the binding of estrogen to ER ⊕ cells.

clInIcal USe Breast cancer treatment (tamoxifen only) and prevention. Raloxifene also useful to prevent
osteoporosis.
adVeRSe eFFectS Tamoxifen—partial agonist in endometrium, which  the risk of endometrial cancer.
Raloxifene—no  in endometrial carcinoma (so you can relax!), because it is an estrogen receptor
antagonist in endometrial tissue.
Both  risk of thromboembolic events (eg, DVT, PE) and “hot flashes.”

Trastuzumab
mechanISm Monoclonal antibody against HER-2 (c-erbB2), a tyrosine kinase receptor. Helps kill cancer cells
that overexpress HER-2 through inhibition of HER-2 initiated cellular signaling and antibody-
dependent cytotoxicity.
clInIcal USe HER-2 ⊕ breast cancer and gastric cancer (tras2zumab).
adVeRSe eFFectS Dilated cardiomyopathy. “Heartceptin” damages the heart.

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