China’s First Diamide Insecticide Tetrachlorantraniliprole Approaches Patent Expiration in Three Years

Tetrachlorantraniliprole, China’s pioneering diamide insecticide developed by Shenyang Research Institute of Chemical Industry (SYRICI), will see its core patent (ZL200810116198.4) expire in July 2028. This technical review examines the compound’s market performance, mode of action, current registrations, and formulation strategies as the agrochemical industry prepares for generic competition in the diamide insecticide market.

1. Market Performance and Commercial Potential

Since its commercial launch, tetrachlorantraniliprole has demonstrated remarkable market traction:

• Achieved ¥70 million (≈$10 million) in first-year sales

• Maintained consistent sales growth trajectory

• Reached $35 million in annual sales by 2021

• Cost-effective production process (30-40% lower raw material costs than chlorantraniliprole)

The compound’s structural similarity to chlorantraniliprole (Figure 1) while offering production cost advantages positions it favorably for expanded market penetration post-patent expiration.

[Insert Figure 1: Chemical structure comparison of tetrachlorantraniliprole and chlorantraniliprole]

2. Mode of Action and Biological Performance

As a ryanodine receptor modulator, tetrachlorantraniliprole exhibits:

2.1 Primary Mechanism

• Binds to insect ryanodine receptors (RyRs)

• Induces uncontrolled calcium release from sarcoplasmic reticulum

• Causes irreversible muscle contractions

• Leads to feeding cessation, paralysis, and death

2.2 Unique Biological Characteristics

• Strong larvicidal activity (particularly 1st-3rd instars)

• No ovicidal activity

• 17-day residual efficacy

• Sublethal effects on pupal development:

  • 25-30% reduction in pupal weight

  • 15-20% extension of developmental duration

• Triple action: contact, stomach, and limited systemic activity

2.3 Spectrum of Activity

Demonstrates exceptional efficacy against:

• Rice pests: Chilo suppressalis, Cnaphalocrocis medinalis

• Vegetable pests: Plutella xylostella, Spodoptera exigua

• Fruit tree pests: Grapholita molesta

3. Global Registration Status

3.1 Current Registrations

• China: 12 formulations registered (SC, WG, OD)

• Other markets: No established registrations in EPA, PMRA, or EU jurisdictions

3.2 Patent Landscape

• Chinese patent ZL200810116198.4 (filed 07/07/2008, expires 07/06/2028)

• International filings:

  • EP2295425 (Europe)

  • BRPI0914217 (Brazil)

  • US20110046186 (United States)

  • WO201003350 (PCT)

4. Resistance Management and Formulation Strategies

Research indicates optimal tank mix partners for resistance management:

4.1 Diamide Combinations

• Flonicamid (1:10 to 10:1): 92% control of resistant P. xylostella populations

4.2 Novel Chemistry Blends

4.3 Conventional Insecticide Blends

Demonstrates excellent compatibility with:

• Pyrethroids (λ-cyhalothrin, bifenthrin)

• Benzoylureas (chlorfluazuron)

• Carbamates (carbosulfan)

5. Post-Patent Market Outlook

The impending patent expiration presents both challenges and opportunities:

5.1 Market Expansion Potential

• Projected

• Estimated $150-200 million market p

• Significant opportunities in Southeast Asian and Latin American markets

5.2 Technical Considerations

• Requires application timing precision (early instar targeting)

• Benefits from rotation with non-diamide chemistries

• Ideal for integrated pest management (IPM) programs

5.3 Regulatory Pathway

Generic manufacturers should prepare:

• Complete toxicology

• Environmental fate studies

• Residue data for major crops

Conclusion

As China’s first indigenously developed diamide insecticide approaches patent expiration, tetrachlorantraniliprole represents a significant opportunity for generic manufacturers. Its cost-effective production, established efficacy against key lepidopteran pests, and compatibility with multiple insecticide classes position it as a valuable tool for pest management programs worldwide. Industry stakeholders should begin preparation for regulatory submissions and market development strategies to capitalize on this impending patent expiration.