title: New, tolerable γ-secretase inhibitor takes desmoid down a notch.
abstract: A phase I trial of PF-03084014, an oral reversible γ-secretase inhibitor, in solid tumor malignancies shows drug tolerability in patients. Evidence of Notch pathway inhibition was demonstrated in peripheral blood. A surprisingly high rate of response was seen in desmoid tumors, a rare but sometimes locally aggressive sarcoma.
authors.affiliation: Department of Pediatrics-Research, The Children's Cancer Hospital at MD Anderson Cancer Center, Houston, Texas.
authors.forename: Dennis P M
authors.initials: DP
authors.lastname: Hughes
authors.affiliation: Division of Cancer Treatment and Diagnosis, National Cancer Institute, Bethesda, Maryland.
authors.forename: Shivaani
authors.initials: S
authors.lastname: Kummar
authors.affiliation: Department of Pathology and Sarcoma Research Center, The University of Texas MD Anderson Cancer Center, Houston, Texas. alazar@mdanderson.org.
authors.forename: Alexander J
authors.initials: AJ
authors.lastname: Lazar
mesh_terms: D053829:Amyloid Precursor Protein Secretases / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000008:administration & dosage*; D005260:Female; D006801:Humans; D008297:Male; D009369:Neoplasms / Q000188:drug therapy*; D013764:Tetrahydronaphthalenes / Q000008:administration & dosage*; D014633:Valine / Q000031:analogs & derivatives*
chemical_list: D004791:Enzyme Inhibitors; D013764:Tetrahydronaphthalenes; D053829:Amyloid Precursor Protein Secretases; D014633:Valine