Icotinib (trade nameConmana) is a highly selective, first generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI). Icotinib is approved for use in China as first-line monotherapy in patients with non-small-cell lung cancer with somatic EGFR mutations.
Icotinib was first synthesized in 2002 by the companyBetta Pharma.[1] The US patent application for the preparation of icotinib and icotinib hydrochloride was filed on December 28, 2012, and granted on July 21, 2015.[2]
Icotinib is approved in China for the treatment ofnon-small cell lung cancer in patients with an EGFR mutation who have advanced or metastatic disease.[4]
The ICOGEN trial was adouble-blind, head-to-head phase III study comparing icotinib withgefitinib in 399 patients across 27 centers in China. Results showed icotinib to have a medianprogression-free survival of 4.6 months (95% CI 3.5 – 6.3) as compared togefitinib which has a PFS of 3.4 months (95% CI 2.3 – 3.8). Post-hoc analysis found feweradverse events with icotinib than gefitinib (61% versus 70% respectively, p = 0.046).[5]
The ISAFE trial was a phase IV study evaluating the safety and toxicity of icotinib in 5,549 patients. It showed an overall adverse event rate of 31.5% and response rate of 30% to the drug.[6]
After receiving approval from theFDA to study icotinib in NSCLC patients,[7] a phase 1 study was planned to be conducted atRoswell Park Comprehensive Cancer Center inNew York State, however the trial was withdrawn prior to enrollment. No further pursuits of US-based studies of icotinib have transpired since.[8]
Icotinib was approved in China by theSFDA in June, 2011.[9] An indication for icotinib was approved in China by the SFDA in November 2014 as first-line treatment for patients with advanced-stage NSCLC with EGFR mutation.[10]
^"About Us".Beta Pharma. Retrieved31 October 2017.
^US 9085588, Hu S, Long W, Wang F, Li Z, "Methods of preparing icotinib and icotinib hydrochloride, and intermediates thereof", issued 21 July 2015, assigned to Betta Pharmaceuticals Co Ltd
^Shi Y, Zhang L, Liu X, Zhou C, Zhang L, Zhang S, et al. (September 2013). "Icotinib versus gefitinib in previously treated advanced non-small-cell lung cancer (ICOGEN): a randomised, double-blind phase 3 non-inferiority trial".The Lancet. Oncology.14 (10):953–61.doi:10.1016/S1470-2045(13)70355-3.PMID23948351.
^Tan F, Gu A, Zhang Y, Jiao SC, Wang CL, He J, et al. (2013). "Safety and efficacy results of a phase IV, open-label, multicenter, safety-monitoring study of icotinib in treating advanced non-small cell lung cancer (NSCLC): ISAFE study".ASCO 2013 Meeting: e19161.
