China’s first diamide insecticide, tetrachlorantraniliprole, developed by the Shenyang Research Institute of Chemical Industry (SYRICI), is nearing a significant milestone: the expiration of its core patent (ZL200810116198.4) in July 2028. Its core patent (ZL200810116198.4) is set to expire in July 2028, which will pave the way for generic competition in the diamide insecticide market. This article explores the compound’s market performance, mode of action, current registrations, and formulation strategies to provide insights into its future prospects.
Market Performance and Commercial Potential
Since its introduction to the market, tetrachlorantraniliprole has demonstrated significant appeal. In its first year, it generated sales of ¥70 million (approximately $10 million). By 2021, annual sales had increased to $35 million. The insecticide benefits from a cost-effective production process, with raw material costs 30%-40% lower than those of chlorantraniliprole. This cost advantage, coupled with its structural similarity to chlorantraniliprole, positions tetrachlorantraniliprole favorably for increased market penetration following patent expiration.
Mode of Action and Biological Performance
Tetrachlorantraniliprole functions as a ryanodine receptor modulator. It binds to insect ryanodine receptors (RyRs), which causes uncontrolled calcium release from the sarcoplasmic reticulum. This leads to irreversible muscle contractions, resulting in feeding cessation, paralysis, and eventual death. The compound demonstrates strong larvicidal activity, particularly against first- to third-instar larvae, and provides 17 days of residual efficacy. It also has sublethal effects on pupal development, reducing pupal weight by 25%-30% and extending developmental duration by 15%-20%. Its triple action—contact, stomach, and limited systemic—further enhances its effectiveness. It is highly effective against various pests, including rice pests such as Chilo suppressalis and Cnaphalocrocis medinalis; vegetable pests such as Plutella xylostella and Spodoptera exigua; and fruit tree pests such as Grapholita molesta.
Global Registration Status
Currently, twelve tetrachlorantraniliprole formulations are registered in China, primarily as suspension concentrates (SC), wettable powders (WG), and odorless dusts (OD). However, there are no established registrations in key markets such as the EPA, PMRA, or EU jurisdictions. Notable patents include Chinese Patent No. ZL200810116198.4, which is set to expire in July 2028. There are also international filings in Europe (EP2295425), Brazil (BRPI0914217), the United States (US20110046186), and the PCT (WO201003350).
Resistance Management and Formulation Strategies
To effectively manage resistance, tetrachlorantraniliprole can be combined with other compounds. For instance, a ratio of 1:10 to 10:1 of a combination with flonicamid achieves 92% control of resistant Plutella xylostella populations. Blends of novel chemistries, such as cyantraniliprole at a ratio of 1:40, are 94% effective against rice stem borers. Methoxyfenozide at a ratio of 1:20 targets fruit borers with 89% efficacy. Dinotefuran at a ratio of 1:5 controls sucking pests at 95%. Afidopyropen at a ratio of 1:3 demonstrates 97% efficacy against rice planthoppers. Additionally, tetrachlorantraniliprole is compatible with conventional insecticides, including pyrethroids, benzoylureas, and carbamates.
| Partner Compound | Optimal Ratio | Target Pests | Field Efficacy |
| Cyantraniliprole | 1:40 | Rice stem borers | 94% |
| Methoxyfenozide | 1:20 | Fruit borers | 89% |
| Dinotefuran | 1:5 | Sucking pests | 95% |
| Afidopyropen | 1:3 | Rice planthoppers | 97% |
Post-Patent Market Outlook
The impending expiration of the tetrachlorantraniliprole patent presents challenges and opportunities. There is significant potential for market expansion, with a projected market value of $150-$200 million. Southeast Asian and Latin American markets offer particularly promising opportunities. However, successful market entry requires precise timing of applications, targeting of early instars, and integration of tetrachlorantraniliprole into IPM programs through rotation with non-diamide chemistries. Generic manufacturers must also prepare comprehensive regulatory submissions, including toxicology and environmental fate studies and residue data for major crops.
Conclusion
As China’s first domestically developed diamide insecticide approaches patent expiration, tetrachlorantraniliprole presents a significant opportunity for generic manufacturers. Its cost-effective production, proven efficacy against key lepidopteran pests, and compatibility with multiple insecticide classes make it a valuable asset for global pest management programs. Industry stakeholders are advised to begin preparing regulatory submissions and market development strategies to capitalize fully on the opportunities presented by the impending patent expiration.
