PI3K inhibitors for cancer treatment: where do we stand?
In contrast with cytotoxic agents that do not differentiate between normal proliferating and tumour cells, targeted therapies primarily exert their actions in cancer cells. Initiation and maintenance of tumours are due to genetic alterations in specific loci. The identification of the genes in which these alterations occur has opened new opportunities for cancer treatment. The PI3K (phosphoinositide 3-kinase) pathway is often overactive in human cancers, and various genetic alterations have been found to cause this. In all cases, PI3K inhibition is considered to be one of the most promising targeted therapies for cancer treatment. The present mini-review provides an update on new PI3K inhibitors currently in or entering clinical development. Recent discoveries, challenges and future prospects will be discussed.
Maira
Sauveur-Michel
SM
Novartis Institutes for Biomedical Research, Oncology Disease Area, Novartis Pharma AG, CH4002 Basel, Switzerland. sauveur-michel.maira@novartis.com
Stauffer
Frédéric
F
Schnell
Christian
C
García-Echeverría
Carlos
C
D000818:Animals; D002199:Capillary Permeability / Q000187:drug effects; D002986:Clinical Trials as Topic; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy* / Q000201:enzymology*; D000081082:Phosphoinositide-3 Kinase Inhibitors; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use*; D011494:Protein Kinases / Q000378:metabolism; D058570:TOR Serine-Threonine Kinases
D000081082:Phosphoinositide-3 Kinase Inhibitors; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases; C546842:MTOR protein, human; D058570:TOR Serine-Threonine Kinases