Wednesday, May 4, 2016

Mechanism of action of Everolimus in breast cancer


Did you guys know that everolimus, an immunosuppressant, is used for cancers like renal cell carcinoma, pancreatic neuroendocrine tumors, etc?

The mechanism of action is really cool, especially in ER (Estrogen receptor) +ve, HER2 -ve breast cancers.

Sometimes ER +ve tumors develop resistance to endocrine treatment such as aromatase inhibitors.

The mechanism of endocrine resistance is mainly driven by aberrant signaling along the phosphoinositide 3-kinase (PI3K) - Akt - mammalian target of rapamycin (mTOR) signaling pathway. mTOR is a Ser/Thr protein kinase that constitutes a central downstream part of this intracellular signaling pathway. Its activation enhances cell growth, proliferation and metabolism, and promotes angiogenesis. The inhibition of the mTOR pathway by targeted therapies, such as everolimus or temsirolimus, can therefore block tumor growth and induce apoptosis.

Isn't that awesome?


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