Recent developments in anti-cancer agents targeting PI3K, Akt and mTORC1/2

Rodrigo Dienstmann, Jordi Rodon, Ben Markman, Josep Tabernero

Research output: Contribution to journalArticleResearchpeer-review

21 Citations (Scopus)


Inappropriate PI3K signaling is one of the most frequent occurrences in human cancer and is critical for tumor progression. A variety of genetic mutations and amplifications have been described affecting key components of this pathway, with implications not only for tumorigenesis but also for resistance to targeted agents. Emerging preclinical research has significantly advanced our understanding of the PI3K pathway and its complex downstream signalling, interactions and crosstalk. This knowledge, combined with the limited clinical antitumor activity of mTOR complex 1 inhibitors, has led to the development of rationally designed drugs targeting key elements of this pathway, such as pure PI3K inhibitors (both pan-PI3K and isoform-specific), dual PI3K/ mTOR inhibitors, Akt inhibitors, and mTOR complexes 1 and 2 catalytic site inhibitors. This review will focus primarily on an analysis of newly developed inhibitors of this pathway that have entered clinical trials, and recently registered patents in this field. © 2011 Bentham Science Publishers Ltd.
Original languageEnglish
Pages (from-to)210-236
JournalRecent Patents on Anti-Cancer Drug Discovery
Issue number2
Publication statusPublished - 25 Apr 2011


  • Cancer
  • Drug development
  • MTORC1
  • MTORC2
  • Patent
  • PI3K
  • Protein kinase B/Akt


Dive into the research topics of 'Recent developments in anti-cancer agents targeting PI3K, Akt and mTORC1/2'. Together they form a unique fingerprint.

Cite this