Drugs in MeSH Category Cytochrome P-450 CYP2C9 Inhibitors

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Ani Pharms	FLUCONAZOLE	fluconazole	TABLET;ORAL	078423-003	Mar 7, 2011	AB	RX	No	No
Baxter Hlthcare Corp	FLUCONAZOLE IN SODIUM CHLORIDE 0.9%	fluconazole	INJECTABLE;INJECTION	077947-001	May 26, 2010		DISCN	No	No
Dr Reddys Labs Sa	AMIODARONE HYDROCHLORIDE	amiodarone hydrochloride	TABLET;ORAL	075389-003	Dec 28, 2017	AB	RX	No	No
Ani Pharms	FLUCONAZOLE	fluconazole	TABLET;ORAL	076086-004	Jul 29, 2004		DISCN	No	No

Cytochrome P-450 CYP2C9 Inhibitors Market Analysis and Financial Projection

The market dynamics and patent landscape for Cytochrome P-450 CYP2C9 inhibitors reflect a growing focus on personalized medicine, drug safety, and innovative therapeutic development. Below is a detailed analysis:

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Market Dynamics

Key Players and Growth Trends

• Leading Companies: Alvogen, Bayer AG, and Shaanxi Xiangju Pharmaceutical Co. Ltd. are prominent in advancing CYP2C9 inhibitors through clinical stages, with several drugs already approved for conditions like hyperuricemia, infectious diseases, and dermatomycoses[6].
• Regional Dominance:
  • North America leads due to high healthcare expenditure and R&D investment.
  • Asia-Pacific (notably China) is emerging rapidly, driven by increasing pharmaceutical capabilities and TB-related demand for drugs like rifapentine[12][14].
• Small Molecule Dominance: Over 85% of pipeline drugs are small molecules, favored for their cost-effectiveness and established formulation pipelines[6][14].

Therapeutic Applications

• CYP2C9 inhibitors are critical in managing drug interactions and adverse effects (e.g., NSAIDs like celecoxib and anticoagulants like warfarin)[1][7][16].
• Approved indications include dermatomycoses, hyperuricemia, and infectious diseases, with growing interest in metabolic disorders[6][14].

Challenges and Drivers

• Adverse Drug Reactions: NSAIDs metabolized by CYP2C9 (e.g., meloxicam, piroxicam) require dose adjustments in patients with genetic polymorphisms (e.g., CYP2C9*3)[1][16].
• Pharmacogenomics: Genetic testing for variants like CYP2C92 and 3 is becoming standard to optimize dosing[1][8][16].
• Regulatory Pressures: The FDA emphasizes pharmacogenomic data in drug development to minimize toxicities[8].

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Patent Landscape

Key Innovation Tracks

1. Synthesis and Intermediates
   • Patents cover synthesis routes for CYP2C9 inhibitors (e.g., intermediates in ritonavir production)[2][15]. For example, US20060069042A1 claims luteolin derivatives as potent inhibitors[15].
2. Formulation Technologies
   • Focus on liquid/solid dosage forms and polymorphs to enhance bioavailability (e.g., Sanofi’s TB drug 3HP formulation patents)[12].
3. Biologic Approaches
   • Monoclonal antibodies (e.g., EP2000532A1) targeting CYP2C9 for diagnostic and therapeutic use, inhibiting >90% enzyme activity[18].

Strategic Patent Filings

• Geographic Distribution: Major filings in the U.S., Germany, and China, with corporations like Abbott Laboratories dominating synthesis and formulation patents[2][14].
• Niche Protection: Patents increasingly target narrow claims (e.g., crystalline structures, reaction conditions) to extend market exclusivity[2][12].

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Emerging Technologies and Competition

• Machine Learning: Models predicting CYP2C9 inhibition (80% accuracy) accelerate drug discovery. Recent hits include vatalanib (IC50 0.067 μM) and ticagrelor[11][17].
• Structural Insights: Atomic-resolution models of CYP2C9-membrane interactions inform rational inhibitor design[4].
• Collaborative R&D: Partnerships between academia and industry (e.g., SignalGene’s closed patent) highlight the shift toward precision medicine[8][14].

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Future Outlook

• Market Expansion: Expected CAGR growth driven by Asia-Pacific investments and demand for safer NSAIDs[6][14].
• Personalized Therapies: Integration of pharmacogenomics (e.g., CPIC guidelines for NSAID dosing) will dominate clinical practice[1][16].
• Patent Complexity: Rising litigation around combination therapies (e.g., ritonavir-isoniazid) may delay generics[12].

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Key Takeaways

• CYP2C9 inhibitors are pivotal in reducing adverse drug reactions, with a market skewed toward small molecules and personalized dosing.
• Patent strategies prioritize synthesis intermediates and biologic agents, while machine learning reshapes discovery pipelines.
• Regional growth in Asia-Pacific and regulatory emphasis on pharmacogenomics are critical market drivers.

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"Genetic variations in CYP450 enzymes affect their metabolic activity, thus impacting the hepatic clearance, elimination half-life, and risk of adverse effects of drugs metabolized by that CYP." — *US Pharm.* 2021[1]

References

1. https://www.uspharmacist.com/article/cyp2c9-polymorphism-and-use-of-oral-nonsteroidal-antiinflammatory-drugs
2. https://www.wipo.int/edocs/pubdocs/en/patents/946/wipo_pub_946.pdf
3. https://pubmed.ncbi.nlm.nih.gov/19515014/
4. https://journals.plos.org/ploscompbiol/article?id=10.1371%2Fjournal.pcbi.1002152
5. https://pmc.ncbi.nlm.nih.gov/articles/PMC2879957/
6. https://synapse.patsnap.com/blog/analysis-on-the-clinical-research-progress-of-cyp2c9-inhibitors
7. https://pubmed.ncbi.nlm.nih.gov/15822186/
8. http://science-metrix.com/pdf/SM_2003_015_IC_Pharmacogenomics_Potential_Canada.pdf
9. https://examine.com/glossary/cyp2c9-inhibitors/
10. https://onlinelibrary.wiley.com/doi/10.1155/2014/150351
11. https://pubmed.ncbi.nlm.nih.gov/35081108/
12. https://www.treatmentactiongroup.org/wp-content/uploads/2020/03/3hp_access_roadmap_and_patent_landscape.pdf
13. https://pmc.ncbi.nlm.nih.gov/articles/PMC11280062/
14. https://www.databridgemarketresearch.com/reports/global-cytochrome-inhibitors-market
15. https://patents.google.com/patent/US20060069042A1/en
16. https://pmc.ncbi.nlm.nih.gov/articles/PMC5872075/
17. https://pubmed.ncbi.nlm.nih.gov/32221780/
18. https://patents.google.com/patent/EP2000532A1/en

Last updated: 2025-03-24