Drugs in MeSH Category Cytochrome P-450 CYP2B6 Inducers

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Avet Lifesciences	RIFAMPIN	rifampin	INJECTABLE;INJECTION	204101-001	Aug 18, 2014		DISCN	No	No
Hikma	RIFAMPIN	rifampin	CAPSULE;ORAL	065028-001	Mar 14, 2001		DISCN	No	No
Epic Pharma Llc	RIFAMPIN	rifampin	INJECTABLE;INJECTION	065502-001	Sep 21, 2010	AP	RX	No	No
Sanofi Aventis Us	RIFADIN	rifampin	CAPSULE;ORAL	050420-001	Approved Prior to Jan 1, 1982		DISCN	Yes	No

Cytochrome P-450 CYP2B6 Inducers Market Analysis and Financial Projection

The market for drugs classified as Cytochrome P-450 CYP2B6 inducers is shaped by their role in treating HIV, cancer, and depression, coupled with challenges in predicting drug-drug interactions (DDIs) and personalized dosing requirements. Below is an analysis of the market dynamics, patent landscape, and emerging trends for these drugs.

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Market Overview

CYP2B6 is a polymorphic enzyme critical for metabolizing 10–12% of clinically used drugs, including antiretrovirals (efavirenz), antidepressants (bupropion), and chemotherapies (cyclophosphamide)[2][7]. Key drivers include:

• HIV therapy demand: Efavirenz, a cornerstone of HIV treatment, relies heavily on CYP2B6 metabolism but faces variability due to genetic polymorphisms (e.g., CYP2B66 allele)[3][7].
• Oncology applications: Cyclophosphamide’s bioactivation via CYP2B6 underpins its use in cancer and autoimmune diseases[7].
• Personalized medicine: Genetic testing for CYP2B6 polymorphisms is gaining traction to optimize dosing and reduce adverse effects[2][7].

However, induction challenges (e.g., DDIs from enzyme upregulation by rifampicin or phenobarbital) complicate clinical use and necessitate rigorous monitoring[6][8].

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Key Drugs and Therapeutic Areas

Drug	Therapeutic Use	Market Impact Factors
Efavirenz	HIV/AIDS	High CNS toxicity linked to CYP2B6 polymorphisms; requires genotype-guided dosing[3][7].
Bupropion	Depression, smoking cessation	Used as a CYP2B6 probe substrate but lacks selectivity due to CYP3A4 co-induction[1][6].
Cyclophosphamide	Cancer, autoimmune diseases	Efficacy depends on CYP2B6-mediated bioactivation; variability affects outcomes[7][8].
Methadone	Opioid addiction	Metabolism influenced by CYP2B6 polymorphisms, impacting dose requirements[7].

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Patent Landscape

Key Patents and Strategies

1. Mitapivat (US11878049B1)
   • Covers methods to adjust dosing for CYP3A4/CYP2B6 modulators in treating blood disorders[12].
2. Pirfenidone (US8754109B2)
   • Focuses on avoiding adverse DDIs with CYP inducers like smoking[4].
3. Genetic Polymorphisms (EP1272663A2)
   • Exploits CYP2B6 SNPs for diagnostics and personalized therapy[5].

Trends in Filings

• Pharmacogenomic innovations: Patents targeting CYP2B6 genetic testing (e.g., CYP2B66 detection) aim to optimize drug safety[2][5].
• DDI mitigation: Novel formulations to reduce induction risks (e.g., pirfenidone dosing adjustments)[4].
• Biosimilar competition: Major drugs like efavirenz face patent expirations, accelerating generic entry[11].

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Key Players and Strategies

• Novartis/GlaxoSmithKline: Invest in CYP2B6 induction studies and predictive modeling[14].
• Biotech Startups: Emerging firms focus on CYP2B6-targeted therapies and diagnostic tools[9].
• Generics Manufacturers: Capitalizing on aging patents (e.g., antiretrovirals) to expand market share[11].

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Regulatory and Clinical Factors

• FDA guidance mandates DDI evaluations for CYP2B6 substrates, driving investments in physiologically based pharmacokinetic (PBPK) models[1][10].
• Pharmacogenomic labeling: Drugs like efavirenz now include genetic testing recommendations to mitigate toxicity[3][7].
• Global disparities: Higher CYP2B6 variant frequencies in African populations necessitate region-specific dosing guidelines[2][5].

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Future Trends

1. Predictive Modeling: Machine learning tools to forecast CYP2B6 inhibition/induction risks (AUC >0.9 in validation)[15].
2. Next-Generation Probes: Development of selective CYP2B6 substrates (fm >0.9) to improve DDI predictions[1][6].
3. Combo Therapies: Bispecific antibodies (e.g., targeting cancer antigens + CYP2B6 modulation) may emerge[9].
4. Gene-Editing: CRISPR-based approaches to normalize CYP2B6 activity in high-risk populations[2][5].

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"Current methods and probe substrates preclude accurate prediction of CYP2B6 induction. Identification of a sensitive and selective clinical substrate is critical." [1][6]

This field’s evolution hinges on resolving enzyme selectivity challenges and integrating pharmacogenomics into clinical practice, ensuring safer, more effective therapies.

References

1. https://pubmed.ncbi.nlm.nih.gov/27422672/
2. https://pmc.ncbi.nlm.nih.gov/articles/PMC8313315/
3. https://pmc.ncbi.nlm.nih.gov/articles/PMC5045548/
4. https://patents.google.com/patent/US8754109B2/en
5. https://patents.google.com/patent/EP1272663A2/en
6. https://pmc.ncbi.nlm.nih.gov/articles/PMC11024975/
7. https://pmc.ncbi.nlm.nih.gov/articles/PMC3588594/
8. https://pmc.ncbi.nlm.nih.gov/articles/PMC5979536/
9. https://www.knowmade.com/wp-content/uploads/2025/01/Bispecific-Ab-Patent-Landscape-2025-FLYER.pdf
10. https://pubmed.ncbi.nlm.nih.gov/35857278/
11. https://www.fiercepharma.com/pharma/closer-look-pharmas-top-patent-losses-2025
12. https://patents.google.com/patent/US11878049B1/en
13. https://meshb.nlm.nih.gov/record/ui?ui=D065695
14. https://citeseerx.ist.psu.edu/document?repid=rep1&type=pdf&doi=4bfa3719f62761a84fba1483e53ba41792590d61
15. https://pubs.acs.org/doi/abs/10.1021/acs.chemrestox.3c00065