Forward -- Past -- mTOR inhibitors: a little bit of history -- Present -- The mTOR pathway -- The evolving role of mTOR inhibitors in renal cell carcinoma -- The role of mTOR inhibitors in breast cancer -- The role of mTOR inhibitors in neuroendocrine tumors -- New indications of mTOR inhibitors in rare tumors -- The role of mTOR inhibitors in the treatment of hematological malignancies -- The clinical pharmacology and toxicity profile of rapalogs -- Resistance to mTOR inhibitors -- Rational combinations of mTOR inhibitors as anticancer strategies -- Future -- Predictive biomarkers of response to mTOR inhibitors -- The potential future indication of rapamycin analogs for the treatment of other solid tumors -- mTOR inhibition beyond rapalogs -- mTOR, aging and cancer: the missing link? -- New study design for mTOR inhibitors and other biological agents -- Future directions for the development of mTOR inhibitors.

This book describes the challenges involved in developing mTOR inhibitors for cancer treatment, starting with an in-depth examination of their molecular mechanism of action, with emphasis on the class side-effects, efficacy and mechanisms of resistance, as well as on promising novel directions for their development, including novel compounds and rational combinations with other anti-neoplastic drugs. Over the last 10 years, inhibitors of mTOR have emerged as a major class of anticancer drugs. Two rapamycin analogs are currently approved for the treatment of renal cell carcinoma, and it is estimated that a variety of other tumor types could benefit from mTOR inhibition, with numerous clinical trials (including pivotal registration trials) already underway. Second-generation small-molecule inhibitors of the pathway have also shown promise in terms of their superior tolerability and efficacy and are undergoing extensive clinical evaluation, with an estimated 30+ compounds currently under evaluation.