Icotinib

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Icotinib
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Icotinib (trade name Conmana) 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.

Development

Icotinib was first synthesized in 2002 by the company Betta 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]

Mechanism of action

Icotinib is a

mitosis.[3]

Indications

Icotinib is approved in China for the treatment of

non-small cell lung cancer in patients with an EGFR mutation who have advanced or metastatic disease.[4]

Clinical research

The ICOGEN trial was a

double-blind, head-to-head phase III study comparing icotinib with gefitinib in 399 patients across 27 centers in China. Results showed icotinib to have a median progression-free survival of 4.6 months (95% CI 3.5 – 6.3) as compared to gefitinib which has a PFS of 3.4 months (95% CI 2.3 – 3.8). Post-hoc analysis found fewer adverse 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 the

New York State, however the trial was withdrawn prior to enrollment. No further pursuits of US-based studies of icotinib have transpired since.[8]

Regulatory approvals

Icotinib was approved in China by the

SFDA 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]

References

  1. ^ "About Us". Beta Pharma. Retrieved 31 October 2017.
  2. ^ 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 
  3. S2CID 34389318
    .
  4. ^ "Product: Icotinib". Betta Pharma. Retrieved 1 November 2017.
  5. PMID 23948351
    .
  6. ^ 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.
  7. ^ "Icotinib & Phase IV ISAFE Trial Poster" (PDF). Beta Pharma. Retrieved 1 November 2017.
  8. ^ Clinical trial number NCT02033148 for "Icotinib Hydrochloride in Treating Patients With Advanced Cancers" at ClinicalTrials.gov
  9. PMID 24836053
    .
  10. ^ "Betta Pharmaceuticals received marketing approval of Icotinib indicating for first-line treatment of patients with advanced-stage NSCLC with EGFR mutation". Betta Pharmaceuticals. Retrieved 1 November 2017.
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