Views: 54 Author: Site Editor Publish Time: 2020-08-03 Origin: Site
1.Abstract
Icotinib (cas no. 610798-31-7) is a epidermal growth factor receptor tyrosine kinase (EGRF-TKI) inhibitor. It is used for treatment of advanced non-small cell lung cancer (NSCLC). It is the first small molecule targeted anti-cancer drug with independent intellectual property rights in China developed and produced by Zhejiang Beta Pharmaceutical Co., Ltd.
It is mainly distributed in gastrointestinal tract, bladder, stomach wall, small intestine, ovary, liver and adipose tissue. Its physicochemical properties, mechanism of action and clinical efficacy in the treatment of NSCLC are comparable with similar foreign drugs Gefitinib and Erlotinib, and its safety is even superior to the above two drugs.
2, Basic information
Chemical name | Icotinib |
English synonym | N-(3-Ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine |
Cas No | 610798-31-7 |
Chemical fomula | C22H21N3O4 |
Molecular weight | 391.43 |
Structure |
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3,Launched Drug
Dose form | Strength | Active ingredient | Trade name | Marketer
| Launch country | Pack launch date |
Tablet | 125mg | Icotinib hydrochloride | CONMANA | Betapharma Shanghai Co., Ltd | China | 31 Jul 2011 |
4, Therapeutic Category Competitors
Active ingredient | Constraint Date in US | US Generic Forecast |
Afatinib dimaleate | 22 Jan 2022 | Highly competitive |
Dacomitinib | 27 Sep 2025 | Delayed |
Erlotinib hydrochloride | ||
Gefitinib | Competitive | |
Osimertinib mesylate | 25 Jul 2032 | Highly competitive |
As per updated researches, Icotinib have similar even better pharmacological performance than Erlotinib and Gefitinib.
The results showed that the efficacy of Icotinib hydrochloride was no worse than that of Gefitinib. The median number of disease-free progression days was 137 days in the Icotinib group and 102 days in the Gefitinib group. Median time to disease progression, 154 days in the Icotinib group and 109 days in the Gefitinib group.
In terms of safety, the incidence of adverse reactions was 60.5% for Icotinib, 70.4% for Gefitinib, 40.0% and 49.2% for rash and 18.5% and 27.6% for diarrhea. Preliminary studies suggest that the efficacy and toxicity of Icotinib is similar to that of Gefitinib and may be superior in toxicity, but oral administration is required multiple times a day.
6, Global market information
Market information in China
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