Everolimus in combination with exemestane: a review of its use in the treatment
of patients with postmenopausal hormone receptor-positive, HER2-negative advanced
breast cancer.
Author(s): Dhillon S.
Affiliation(s): Author information:
Adis, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, North Shore, 0754
Auckland, New Zealand. demail@springer.com
Publication date & source: 2013, Drugs. , 73(5):475-85
Oral everolimus (Afinitor(®)) in combination with exemestane is indicated for the
treatment of hormone receptor-positive, human epidermal growth factor receptor
(HER) 2-negative advanced breast cancer in postmenopausal women after failure of
treatment with letrozole or anastrozole (in the USA) or after recurrence of
progression following a nonsteroidal aromatase inhibitor (AI) in women without
symptomatic visceral disease (in the EU). Everolimus, a selective inhibitor of
mammalian target of rapamycin (mTOR), inhibits the downstream signalling events
of the mTOR pathway. This review summarizes the pharmacology of everolimus and
reviews its efficacy and tolerability when administered in combination with
exemestane in postmenopausal women with oestrogen receptor-positive,
HER2-negative advanced breast cancer refractory to nonsteroidal AIs. In the
well-designed BOLERO-2 study, the addition of everolimus to exemestane was shown
to significantly prolong progression-free survival in this patient population.
However, treatment-emergent adverse events and treatment discontinuations
occurred more frequently with combination therapy than with exemestane alone,
suggesting a need for careful benefit/risk assessment prior to initiating
therapy. Mature survival data from this study are awaited and additional studies
would help to further demonstrate the benefit of combination therapy.
Nevertheless, current evidence suggests that everolimus plus exemestane
combination therapy may be a useful treatment option in patients with
postmenopausal hormone receptor-positive, HER2-negative, advanced breast cancer
refractory to nonsteroidal AIs.
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