title: Investigational therapies up to Phase II which target PDGF receptors: potential anti-cancer therapeutics.
abstract: BACKGROUND
  The platelet-derived growth factor receptor (PDGFR) pathway has important functions in cell growth and, by overexpression or mutation, could also be a driver for tumor development. Moreover, PDGFR is expressed in a tumoral microenvironment and could promote tumorigenesis. With these biological considerations, the PDGFR pathway could be an interesting target for therapeutics. Currently, there are many molecules under development that target the PDGFR pathway in different types of cancer.
  
  
  METHODS
  In this review, the authors report the different molecules under development, as well as those approved albeit briefly, which inhibit the PDGFR pathway. Furthermore, the authors summarize their specificities, their toxicities, and their development.
  
  
  CONCLUSIONS
  Currently, most PDGFR kinase inhibitors are multikinase inhibitors and therefore do not simply target the PDGFR pathway. The development of more specific PDGFR inhibitors could improve drug efficacy. Moreover, selecting tumors harboring mutations or amplifications of PDGFR could improve outcomes associated with the use of these molecules. The authors believe that new technologies, such as kinome arrays or pharmacologic assays, could be of benefit to understanding resistance mechanisms and develop more selective PDGFR inhibitors.
authors.affiliation: Paris Descartes University, Cochin Hospital, AP-HP, Medical Oncology Department, Angiogenesis Inhibitors Multidisciplinary Study Group (CERIA) , Paris , France francois.goldwasser@cch.ap-hop-paris.fr.
authors.forename: Jennifer
authors.initials: J
authors.lastname: Arrondeau
authors.forename: Olivier
authors.initials: O
authors.lastname: Huillard
authors.forename: Camille
authors.initials: C
authors.lastname: Tlemsani
authors.forename: Anatole
authors.initials: A
authors.lastname: Cessot
authors.forename: Pascaline
authors.initials: P
authors.lastname: Boudou-Rouquette
authors.forename: Benoit
authors.initials: B
authors.lastname: Blanchet
authors.forename: Audrey
authors.initials: A
authors.lastname: Thomas-Schoemann
authors.forename: Michel
authors.initials: M
authors.lastname: Vidal
authors.forename: Jean-Marie
authors.initials: JM
authors.lastname: Tigaud
authors.forename: Jean-Philippe
authors.initials: JP
authors.lastname: Durand
authors.forename: Jerome
authors.initials: J
authors.lastname: Alexandre
authors.forename: Francois
authors.initials: F
authors.lastname: Goldwasser
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000009:adverse effects / Q000494:pharmacology*; D017322:Clinical Trials, Phase II as Topic; D015195:Drug Design; D015507:Drugs, Investigational / Q000009:adverse effects / Q000494:pharmacology; D006801:Humans; D058990:Molecular Targeted Therapy; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D017479:Receptors, Platelet-Derived Growth Factor / Q000037:antagonists & inhibitors*; D059016:Tumor Microenvironment
chemical_list: D000970:Antineoplastic Agents; D015507:Drugs, Investigational; D017479:Receptors, Platelet-Derived Growth Factor
keywords: anti-cancer therapies; platelet-derived growth factor; platelet-derived growth factor receptor pathway; targeted therapies