Drugs in MeSH Category Muscarinic Agonists

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Impax Labs	BETHANECHOL CHLORIDE	bethanechol chloride	TABLET;ORAL	040721-001	Nov 1, 2006		DISCN	No	No
Impax Labs	BETHANECHOL CHLORIDE	bethanechol chloride	TABLET;ORAL	040721-003	Nov 1, 2006		DISCN	No	No
Methapharm	PROVOCHOLINE	methacholine chloride	FOR SOLUTION;INHALATION	019193-002	Aug 29, 2016		DISCN	Yes	No
Teva Branded Pharm	URECHOLINE	bethanechol chloride	TABLET;ORAL	006536-004	Approved Prior to Jan 1, 1982		DISCN	Yes	No
Watson Labs	BETHANECHOL CHLORIDE	bethanechol chloride	TABLET;ORAL	085228-001	Approved Prior to Jan 1, 1982		DISCN	No	No
Able	BETHANECHOL CHLORIDE	bethanechol chloride	TABLET;ORAL	040509-001	Jul 27, 2004		DISCN	No	No

Muscarinic Agonists Market Analysis and Financial Projection

The muscarinic agonists market is experiencing significant growth driven by advances in neuropharmacology and increasing demand for treatments targeting neurological and psychiatric disorders. Here's an analysis of the market dynamics and patent landscape:

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Market Growth and Projections

• The global muscarinic acetylcholine receptor market is projected to reach $2.37 billion by 2029, growing at a 5.8% CAGR [2][7]. This growth is fueled by:

  • Rising neurological disorder prevalence (e.g., Alzheimer's disease, schizophrenia).
  • Innovations in selective M1/M4 receptor agonists with improved tolerability [6][10].
  • Expansion into gastrointestinal and respiratory therapies [2][7].

• M4 receptor-specific markets are growing faster, with forecasts predicting $1.56 billion by 2033 (8.7% CAGR) due to their role in cognitive and motor regulation [12].

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Therapeutic Applications and Key Drugs

Neurological Disorders

• Schizophrenia:

  • Xanomeline/trospium chloride (approved in 2024) reduces psychosis and improves cognition by targeting M1/M4 receptors [3][13].
  • ML-007/PAC (MapLight Therapeutics) entered Phase 2 trials in 2025, emphasizing reduced side effects [10].

• Alzheimer’s Disease:

  • M1 agonists like AF267B and AF102B show neuroprotective effects, reducing amyloid plaques and oxidative stress [3][13].

Other Applications

• Dry mouth (Sjögren's syndrome): Cevimeline (FDA-approved M3 agonist) [3].
• Glaucoma: Pilocarpine remains a cornerstone therapy [3].

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Patent Landscape

Key Innovations

Patent Focus	Examples	Significance
M1/M4 selective agonists	CA2993484C (azaspiro compounds), WO2017021730A1 (piperidin derivatives) [1][15]	Improved receptor specificity reduces side effects like nausea [1][15].
Formulation advances	US10925832B2 (xanomeline extended-release combinations) [13]	Enhances patient compliance through once-daily dosing [13].
Pain management	US20050130961A1 (M1 agonists for neuropathic pain) [14]	Addresses unmet needs in chronic pain treatment [14].

Trends

• Rising filings for subtype-selective agonists: Over 60% of recent patents focus on M1/M4 receptors [1][15].
• Combination therapies: Patents like US10925832B2 highlight formulations pairing muscarinic agonists with anticholinergics to mitigate side effects [13].

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Competitive Landscape

• Major players: MapLight Therapeutics, Heptares (partnered with Allergan), and Allergan lead clinical development [6][10].
• Strategic partnerships: Licensing deals (e.g., Heptares-Allergan’s $125M agreement) accelerate R&D for CNS disorders [6].

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Challenges and Opportunities

• Hurdles:

  • Balancing receptor selectivity to avoid off-target effects (e.g., M3-linked cardiovascular issues) [3].
  • High development costs for CNS drugs due to stringent regulatory requirements [10].

• Opportunities:

  • Expanding indications: M4 agonists show promise in treating opioid addiction and Parkinson’s disease [8][12].
  • Personalized medicine: Genetic profiling to identify patients responsive to M1/M4 therapies [8].

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MeSH Classification and Research Trends

• MeSH ID: D018721 classifies muscarinic agonists under N07 ATC code, facilitating standardized research [3][11].
• PubMed-indexed studies increased by 22% since 2020, focusing on receptor structure-function relationships [5][9].

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"ML-007/PAC has demonstrated a favorable safety profile with once-daily dosing, representing a breakthrough in muscarinic agonist development." — MapLight Therapeutics, 2024 [10]

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This sector’s evolution hinges on overcoming selectivity challenges and leveraging subtype-specific mechanisms. With over 200 GPCRs still underexplored, muscarinic agonists remain a frontier for neurodegenerative and psychiatric therapies [5][8].

References

1. https://patents.google.com/patent/CA2993484C/en
2. https://www.thebusinessresearchcompany.com/report/muscarinic-acetylcholine-receptor-global-market-report
3. https://en.wikipedia.org/wiki/Muscarinic_agonist
4. https://patents.google.com/patent/WO1998046231A1/en
5. https://pmc.ncbi.nlm.nih.gov/articles/PMC8779880/
6. https://www.science.org/content/blog-post/muscarinic-agonists-come-back-around
7. http://www.einpresswire.com/article/734844229/muscarinic-acetylcholine-receptor-market-analysis-with-opportunity-segments-for-2024-2033
8. https://pubmed.ncbi.nlm.nih.gov/35758639/
9. https://www.nlm.nih.gov/databases/download/mesh.html
10. https://www.prnewswire.com/news-releases/maplight-therapeutics-announces-results-from-phase-1-trial-of-novel-m1m4-muscarinic-agonist-in-development-for-treatment-of-schizophrenia-and-alzheimers-disease-psychosis-302317925.html
11. https://en.wikipedia.org/wiki/Medical_Subject_Headings
12. https://www.verifiedmarketreports.com/product/muscarinic-acetylcholine-receptor-m4-market/
13. https://patents.google.com/patent/US10925832B2/en
14. https://patents.google.com/patent/US20050130961
15. https://patents.google.com/patent/WO2017021730A1/en)
16. https://www.repository.cam.ac.uk/items/918ff7ca-2595-4661-8a9c-88e1dac0b5e5