Open AccessPilot trial of EZN-2968, an antisense oligonucleotide inhibitor of hypoxia-inducible factor-1 alpha (HIF-1α), in patients with refractory solid tumors
Author(s) -
Woondong Jeong,
Annamaria Rapisarda,
Sook Ryun Park,
Robert J. Kinders,
Alice Chen,
Giovanni Melillo,
Barış Türkbey,
Seth M. Steinberg,
Peter Choyke,
James H. Doroshow,
Shivaani Kummar
Publication year - 2013
Publication title -
cancer chemotherapy and pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.112
H-Index - 111
eISSN - 1432-0843
pISSN - 0344-5704
DOI - 10.1007/s00280-013-2362-z
Subject(s) - refractory (planetary science) , hif1a , hypoxia inducible factors , hypoxia (environmental) , cancer research , medicine , hypoxia inducible factor 1 , oligonucleotide , chemistry , pharmacology , biology , transcription factor , biochemistry , angiogenesis , dna , gene , oxygen , organic chemistry , astrobiology
Hypoxia-inducible factor-1 (HIF-1) facilitates the adaptation of normal and tumor tissues to oxygen deprivation. HIF-1 is frequently overexpressed in cancer cells, where it is involved in the upregulation of many genes necessary for survival. EZN-2968 is an antisense oligodeoxynucleotide that specifically targets HIF-1α, one of the subunits of HIF-1. We conducted a trial of EZN-2968 in patients with refractory solid tumors to evaluate antitumor response and to measure modulation of HIF-1α mRNA and protein levels as well as HIF-1 target genes.