PMID- 22508830 OWN - NLM STAT- MEDLINE DCOM- 20120816 LR - 20220330 IS - 1527-7755 (Electronic) IS - 0732-183X (Print) IS - 0732-183X (Linking) VI - 30 IP - 18 DP - 2012 Jun 20 TI - Randomized phase II trial of erlotinib with and without entinostat in patients with advanced non-small-cell lung cancer who progressed on prior chemotherapy. PG - 2248-55 LID - 10.1200/JCO.2011.38.9411 [doi] AB - PURPOSE: Histone deacetylase inhibitors (HDACis) have been shown to overcome resistance to epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) linked to epigenetic changes and epithelial-mesenchymal transition (EMT) state. This randomized phase II study evaluated the outcome of erlotinib with and without the isoform selective HDACi, entinostat. PATIENTS AND METHODS: Previously treated patients with stage IIIB/IV non-small-cell lung cancer, no prior EGFR-TKIs, and performance status </= 2 were randomly administered erlotinib 150 mg on days 1 through 28 plus entinostat 10 mg orally on days 1 and 15 every 28 days (EE) or erlotinib plus placebo (EP). The primary end point was 4-month progression-free survival (PFS) rate with additional end points including 6-month PFS rate, PFS, and overall survival (OS). Exploratory analyses included EMT- and EGFR-related biomarker analysis on archival tissue. RESULTS: One hundred thirty-two patients were enrolled (EE, 67; EP, 65). The 4-month PFS rate was comparable for both groups (EE, 18% v EP, 20%; P = .7). In the subset of patients with high E-cadherin levels, OS was longer in the EE group compared with the EP group (9.4 v 5.4 months; hazard ratio, 0.35; 95% CI, 0.13 to 0.92; P = .03) with a corresponding trend toward increased PFS. The adverse event (AE) profile was acceptable, with rash, fatigue, diarrhea, and nausea the most common AEs in both groups. CONCLUSION: Erlotinib combined with entinostat did not improve the outcomes of patients in the overall study population when compared with erlotinib monotherapy. High E-cadherin expression levels at time of diagnosis indicate an increased sensitivity to HDACi/EGFR-TKI inhibition providing the basis for a biomarker-driven validation study. FAU - Witta, Samir E AU - Witta SE AD - University of Colorado Cancer Center, 12801 E 17th Ave, Mail Stop 8117, Aurora, CO 80045, USA. FAU - Jotte, Robert M AU - Jotte RM FAU - Konduri, Katrik AU - Konduri K FAU - Neubauer, Marcus A AU - Neubauer MA FAU - Spira, Alexander I AU - Spira AI FAU - Ruxer, Robert L AU - Ruxer RL FAU - Varella-Garcia, Marileila AU - Varella-Garcia M FAU - Bunn, Paul A Jr AU - Bunn PA Jr FAU - Hirsch, Fred R AU - Hirsch FR LA - eng GR - P30 CA046934/CA/NCI NIH HHS/United States GR - U01 CA157715/CA/NCI NIH HHS/United States PT - Clinical Trial, Phase II PT - Journal Article PT - Randomized Controlled Trial PT - Research Support, Non-U.S. Gov't DEP - 20120416 PL - United States TA - J Clin Oncol JT - Journal of clinical oncology : official journal of the American Society of Clinical Oncology JID - 8309333 RN - 0 (Benzamides) RN - 0 (Biomarkers, Tumor) RN - 0 (Cadherins) RN - 0 (Histone Deacetylase Inhibitors) RN - 0 (Pyridines) RN - 0 (Quinazolines) RN - 1ZNY4FKK9H (entinostat) RN - DA87705X9K (Erlotinib Hydrochloride) SB - IM MH - Aged MH - Antineoplastic Combined Chemotherapy Protocols/therapeutic use MH - Benzamides/*administration & dosage MH - Biomarkers, Tumor/metabolism MH - Cadherins/metabolism MH - Carcinoma, Non-Small-Cell Lung/*drug therapy MH - Erlotinib Hydrochloride MH - Female MH - Histone Deacetylase Inhibitors/*administration & dosage MH - Humans MH - Lung Neoplasms/*drug therapy MH - Male MH - Middle Aged MH - Pyridines/*administration & dosage MH - Quinazolines/*therapeutic use PMC - PMC4798782 MID - NIHMS742858 COIS- Authors' disclosures of potential conflicts of interest and author contributions are found at the end of this article. EDAT- 2012/04/18 06:00 MHDA- 2012/08/17 06:00 PMCR- 2013/01/20 CRDT- 2012/04/18 06:00 PHST- 2012/04/18 06:00 [entrez] PHST- 2012/04/18 06:00 [pubmed] PHST- 2012/08/17 06:00 [medline] PHST- 2013/01/20 00:00 [pmc-release] AID - JCO.2011.38.9411 [pii] AID - 89411 [pii] AID - 10.1200/JCO.2011.38.9411 [doi] PST - ppublish SO - J Clin Oncol. 2012 Jun 20;30(18):2248-55. doi: 10.1200/JCO.2011.38.9411. Epub 2012 Apr 16.