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Last Updated: April 15, 2025

Mechanism of Action: Cytochrome P450 2C19 Inhibitors


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Drugs with Mechanism of Action: Cytochrome P450 2C19 Inhibitors

ApplicantTradenameGeneric NameDosageNDAApproval DateTETypeRLDRSPatent No.Patent ExpirationProductSubstanceDelist Req.Exclusivity Expiration
Sumitomo Pharma Am APTIOM eslicarbazepine acetate TABLET;ORAL 022416-001 Nov 8, 2013 AB RX Yes No 9,566,244 ⤷  Try for Free Y ⤷  Try for Free
Sumitomo Pharma Am APTIOM eslicarbazepine acetate TABLET;ORAL 022416-003 Nov 8, 2013 AB RX Yes No 9,763,954 ⤷  Try for Free ⤷  Try for Free
Sumitomo Pharma Am APTIOM eslicarbazepine acetate TABLET;ORAL 022416-004 Nov 8, 2013 AB RX Yes Yes 9,566,244 ⤷  Try for Free Y ⤷  Try for Free
>Applicant>Tradename>Generic Name>Dosage>NDA>Approval Date>TE>Type>RLD>RS>Patent No.>Patent Expiration>Product>Substance>Delist Req.>Exclusivity Expiration
Showing 1 to 3 of 3 entries

P2C19 Inhibitors: Market Dynamics and Patent Landscape Analysis

CYP2C19 inhibitors play a critical role in drug metabolism, impacting therapeutic outcomes across cardiovascular, psychiatric, and infectious disease treatments. This enzyme’s inhibition alters drug efficacy and safety, driving innovation in pharmacogenomics and personalized medicine. Below, we analyze the market dynamics, patent trends, clinical applications, and future directions for drugs targeting CYP2C19 inhibition.


Market Dynamics of CYP2C19 Inhibitors

Growth Drivers

  1. Increasing Demand for Precision Medicine: CYP2C19 genotyping (e.g., Genomadix Cube CYP2C19 System [7]) enables tailored therapies, reducing adverse drug reactions (ADRs) and improving outcomes for drugs like clopidogrel and antidepressants[4][15].
  2. Rising Chronic Disease Burden: Cardiovascular diseases and psychiatric disorders necessitate optimized dosing of CYP2C19-dependent drugs[9][15].
  3. Expanding Use in HIV Treatment: Ritonavir, a CYP2C19 inducer and protease inhibitor, remains pivotal in HIV therapy, with ongoing patent filings for synthesis and formulation improvements[2][6].

Market Segmentation

  • By Drug Class: Proton pump inhibitors (e.g., omeprazole), antidepressants (e.g., citalopram), and antifungals (e.g., voriconazole)[1][14].
  • By Region: North America dominates due to high healthcare expenditure, while Asia-Pacific shows rapid growth[10].

Key Players

  • Genomadix: FDA-cleared CYP2C19 genotyping system[7].
  • Abbott Laboratories: Major patent holder for ritonavir formulations and synthesis[2].
  • Pharmaceutical Innovators: Companies developing novel inhibitors (e.g., omeprazole derivatives)[17].

Patent Landscape and Innovation Trends

Key Patents

Patent Focus Description Example Patents
Diagnostic Methods Detection of CYP2C19 polymorphisms (2, 3, *17) to predict drug metabolism[11]. US20030059774A1[11]
Therapeutic Combinations Voriconazole paired with CYP2C19 inhibitors to enhance antifungal efficacy[13]. US20050182074A1[13]
Synthesis and Formulations Ritonavir’s liquid/solid dosage forms and intermediates[2]. WO2001021603[2]
Novel Inhibitors Omeprazole-based analogues with improved metabolic stability[17]. US7682800B2 (antibody inhibitors)[8]

Innovation Tracks

  1. Polymorph Characterization: Over 50% of recent patents focus on genetic variants influencing drug response[11][15].
  2. Drug-Drug Interaction Mitigation: Formulations minimizing CYP2C19-mediated interactions (e.g., clopidogrel with PPIs)[4][9].
  3. Nanotechnology: Enhancing inhibitor delivery to reduce off-target effects[6].

Clinical Applications and Challenges

Cardiovascular Therapeutics

  • Clopidogrel: CYP2C19 loss-of-function variants reduce active metabolite formation, increasing cardiovascular risks. Genotyping shifts market share toward prasugrel/ticagrelor (12% and 5% increases, respectively)[15].
  • Drug Interactions: Fluoxetine and fluvoxamine (strong CYP2C19 inhibitors) elevate clopidogrel toxicity risks[3][14].

Psychiatric Drugs

  • Citalopram/Escitalopram: CYP2C19 poor metabolizers exhibit 95% higher drug exposure, necessitating dose adjustments[5].

Adverse Events

  • Proton Pump Inhibitors: Omeprazole inhibits CYP2C19, reducing clopidogrel efficacy[9].
  • Antifungals: Voriconazole requires therapeutic drug monitoring to avoid toxicity in CYP2C19 ultrarapid metabolizers[1][13].

Future Directions

  1. Personalized Dosing Algorithms: Integration of real-world data from genotyping tests to optimize prescriptions[7][15].
  2. Next-Gen Inhibitors: Compounds like ACT-1014-6470 show weak CYP2C19 inhibition, reducing interaction risks[16].
  3. Global Patent Expansion: Emerging markets in Asia and Africa drive filings for cost-effective formulations[10].

"CYP2C19 genotype-guided therapy is no longer a luxury—it’s a necessity to avoid preventable adverse events." – Clinical Pharmacology & Therapeutics[4].


Key Takeaways

  • CYP2C19 inhibitors are pivotal in managing drug efficacy and safety across multiple therapeutic areas.
  • Patent activity centers on diagnostics, combination therapies, and novel formulations.
  • Market growth hinges on precision medicine adoption and emerging economies.

FAQs

  1. How does CYP2C19 genotyping impact drug costs?
    It reduces long-term expenses by preventing ADRs and hospitalizations[15].
  2. Which drugs require CYP2C19 testing?
    Clopidogrel, voriconazole, and SSRIs like citalopram[4][5][13].
  3. What are the risks of unmonitored CYP2C19 inhibition?
    Therapeutic failure (e.g., clopidogrel) or toxicity (e.g., escitalopram)[9][5].
  4. Are there CYP2C19 inhibitors in development?
    Yes, including antibody-based agents and metabolically stable omeprazole analogues[8][17].
  5. How does ritonavir’s patent landscape affect HIV treatment?
    Continuously evolving formulations improve bioavailability and compliance[2][6].

References

  1. https://int.diasorin.com/sites/default/files/products-documentation-tool/WP637.0616.2C19.v2.pdf
  2. https://www.wipo.int/edocs/pubdocs/en/patents/946/wipo_pub_946.pdf
  3. https://www.fda.gov/drugs/drug-interactions-labeling/healthcare-professionals-fdas-examples-drugs-interact-cyp-enzymes-and-transporter-systems
  4. https://pmc.ncbi.nlm.nih.gov/articles/PMC7444625/
  5. https://pubmed.ncbi.nlm.nih.gov/25154506/
  6. https://pmc.ncbi.nlm.nih.gov/articles/PMC6497396/
  7. https://www.biospace.com/genomadix-announces-fda-clearance-to-market-the-genomadix-cube-cyp2c19-system
  8. https://patents.google.com/patent/US7682800B2/en
  9. https://www.mdpi.com/2075-4426/8/1/8
  10. https://www.databridgemarketresearch.com/reports/global-cytochrome-inhibitors-market
  11. https://patents.google.com/patent/US20030059774A1/en
  12. https://www.drugpatentwatch.com/p/generic-api/TOPIRAMATE
  13. https://patents.google.com/patent/US20050182074A1/en
  14. https://examine.com/glossary/cyp2c19-inhibitors/
  15. https://pubmed.ncbi.nlm.nih.gov/26108379/
  16. https://pmc.ncbi.nlm.nih.gov/articles/PMC10339695/
  17. https://pubs.acs.org/doi/10.1021/jm201346g

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