Mechanism of Action: Partial Opioid Agonists

Drugs with Mechanism of Action: Partial Opioid Agonists

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Bdsi	BELBUCA	buprenorphine hydrochloride	FILM;BUCCAL	207932-005	Oct 23, 2015		RX	Yes	No			Y
Bdsi	BELBUCA	buprenorphine hydrochloride	FILM;BUCCAL	207932-002	Oct 23, 2015		RX	Yes	No			Y
Bdsi	BELBUCA	buprenorphine hydrochloride	FILM;BUCCAL	207932-007	Oct 23, 2015		RX	Yes	Yes			Y
Bdsi	BELBUCA	buprenorphine hydrochloride	FILM;BUCCAL	207932-005	Oct 23, 2015		RX	Yes	No			Y
Bdsi	BELBUCA	buprenorphine hydrochloride	FILM;BUCCAL	207932-002	Oct 23, 2015		RX	Yes	No			Y

Partial Opioid Agonists Market Analysis and Financial Projection

The market for partial opioid agonists is shaped by increasing opioid use disorder (OUD) prevalence, evolving treatment paradigms, and strategic patent innovations. Here’s a detailed analysis:

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Market Dynamics

1. Growth Drivers

   • Rising OUD Cases: Over 145,000 new U.S. OUD diagnoses in 2022 and global opioid misuse fuel demand for treatments like buprenorphine, a partial agonist[12][15].
   • Safer Profiles: Partial agonists (e.g., buprenorphine) offer reduced respiratory depression and overdose risk due to a ceiling effect, making them preferred over full agonists like methadone[1][3].
   • Pipeline Innovations: Non-opioid adjuncts (e.g., cannabidiol, mazindol CR) and novel formulations (e.g., Trevena’s TRV-734, a partial mu agonist) aim to diversify treatment options[5][6].

2. Market Segmentation

   • Dominance of Buprenorphine: Held ~60% of the OUD market in 2024 due to its dual action (partial agonist + naloxone) and tamper-resistant formulations[12][15].
   • Regional Trends:
     • North America: Largest market (74% share in 2023), driven by high OUD prevalence and pricing[5][12].
     • Asia-Pacific and LMICs: Fastest-growing regions (CAGR 6.9–7.4%) due to expanding healthcare access and harm-reduction programs[9][10].

3. Competitive Landscape

   • Key players include Indivior, Alkermes, and Braeburn, focusing on extended-release injectables (e.g., Sublocade, Brixadi) to improve adherence[12][17].
   • Generic Erosion: Expected to curb growth, particularly in the U.S., though formulation patents delay competition[5][12].

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Patent Landscape

1. Core Strategies

   • Tamper-Resistant Formulations: Patents like US6696088B2 protect oral agonists paired with sequestered antagonists (e.g., naloxone) to deter misuse[2].
   • Delivery Innovations:
     • BioDelivery Sciences’ BEMA technology extends exclusivity for buprenorphine until 2027 via mucoadhesive films[16].
     • Braeburn’s Brixadi (weekly/monthly injectable buprenorphine) has patents filed through 2025, with exclusivity until 2032[17].

2. Litigation and Non-Obviousness

   • Orexo’s patent (US8,940,330) for citric acid-based sublingual tablets survived challenges, emphasizing novel carrier particles as non-obvious[4].

3. Emerging Targets

   • δ-Opioid Receptor (δOR) Agonists: Partial agonists like C6-Quino show promise for chronic pain without µOR-related side effects or seizures[14].

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Future Outlook

• Revenue Projections:
  • Global OUD market: $10.24B by 2030 (11.15% CAGR)[15].
  • Partial agonists remain central, but non-opioid pipeline drugs (e.g., TRV-734) could capture $171M by 2033[5].
• Innovation Frontiers:
  • Biased Signaling: Designing partial agonists with pathway selectivity (e.g., G-protein vs. arrestin) to minimize adverse effects[14].
  • Expanded Access: LMIC markets (e.g., India, Brazil) to grow via opioid substitution therapy programs[10].

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Key Challenges

• Generic Competition: Post-2030, buprenorphine/naltrexone generics may reduce prices, but abuse-deterrent formulations retain value[12][17].
• Regulatory Hurdles: Balancing efficacy and safety in δOR-targeted drugs requires robust preclinical validation[14].

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"The need for effective non-opioid treatments that do not target the mu receptor remains critical to transforming addiction care." – GlobalData Analyst, 2024[5].

This dynamic interplay of clinical need, strategic IP, and R&D innovation positions partial opioid agonists as enduring pillars in OUD management.

References

1. https://www.naabt.org/education/technical_explanation_buprenorphine.cfm
2. https://patents.google.com/patent/US6696088B2/en
3. https://journals.sagepub.com/doi/10.1177/0963689718811060
4. https://ipwatchdog.com/2018/09/22/invalidation-orexos-opioid-patent-obvious-reversed/id=101585/
5. https://www.expresspharma.in/opioid-addiction-market-to-reach-2-4-billion-in-8mm-by-2033-globaldata/
6. https://pubs.acs.org/doi/10.1021/acs.jmedchem.4c00590
7. https://pmc.ncbi.nlm.nih.gov/articles/PMC2752300/
8. https://patents.google.com/patent/NZ517997A/de
9. https://www.futuremarketinsights.com/reports/opioid-use-disorder-treatment-market
10. https://www.persistencemarketresearch.com/market-research/low-middle-income-countries-opioid-substitution-therapy-market.asp
11. https://www.databridgemarketresearch.com/reports/global-opioid-receptor-agonist-market
12. https://www.grandviewresearch.com/industry-analysis/naltrexone-buprenorphine-market-report
13. https://www.grandviewresearch.com/press-release/global-opioid-use-disorder-market
14. https://pmc.ncbi.nlm.nih.gov/articles/PMC11906898/
15. https://www.grandviewresearch.com/industry-analysis/opioid-use-disorder-market
16. https://www.biospace.com/biodelivery-sciences-international-receives-patent-allowance-triggering-15-million-milestone-payment-from-endo-pharmaceuticals
17. https://pharsight.greyb.com/drug/brixadi-patent-expiration