Muscarinic receptors are the sites for the neurotransmitters of the parasympathetic autonomic nervous system, acetylcholine, thus muscarinic receptors are responsible for responses including, cardiac slowing, contraction of smooth muscles, vasodilation and increased secretion from exocrine glands. Muscarinic receptor antagonists act on these 5 subtypes of muscarinic receptors i.e., M1, M2, M3, M4, and M5, and induce actions like bronchodilation, reduced gastric acid, reduce secretions from glands, inhibition of bladder contraction, and others. Muscarinic receptor antagonists are indicated for conditions such as chronic obstructive pulmonary disease, overactive bladder, motion sickness, asthma, and myopia. Boehringer Ingelheim, Novartis, AstraZeneca, LENZ Therapeutics, Orient Europharma, and GSK are some of the major market players in muscarinic receptor antagonists. Moreover, there are drugs in the pipeline of pharmaceutical companies for other health conditions.
Key Market Developments:
- In Feb 2022, Journey Medical Corporation entered into an exclusive licensing agreement with Mahuro for the manufacturing and marketing of Rapifort wipes 2.5% (Glycopyrrolate topical).
- In Feb 2023, Karuna Therapeutics announced its intention to submit NDA to the US FDA for schizophrenia in Q3 2023 for the combination drug Trospium chloride/Xanomeline.
Approved Drug Molecules and Brand Names for Muscarinic Receptor Antagonists:
- Tolterodine
- Fesoterodine
- Stiolto Respimat (Olodaterol/Tiotropium Fdc)
- Anoro Ellipta (Umeclidinium/Vilanterol)
- Tiotropium Bromide Dry Powder Inhaler
- Ultibro (Glycopyrronium/Indacaterol)
- Hyoscine Butylbromide Oral
- Ipratropium Bromide
- Riarify (Beclometasone/Formoterol/Glycopyrrolate)
- Incruse Ellipta (Umeclidinium)
- Breztri Aerosphere (Budesonide/Formoterol Fumarate/Glycopyrronium)
- Spiriva Respimat (Tiotropium Bromide)
- Trelegy Ellipta (Fluticasone Furoate/Umeclidinium Bromide/Vilanterol)
- Tudorza (Aclidinium Bromide)
- Combivent (Ipratropium/Salbutamol)
- Duaklir (Aclidinium Bromide/Formoterol Fumarate)
- Hyoscine Butylbromide Injection
- Bevespi Aerosphere (Formoterol/Glycopyrrolate)
- Nefopam
- Yupelri (Revefenacin)
- Oxybutynin Transdermal
- Berodual N (Ipratropium Bromide/Fenoterol Hydrobromide)
- Scopolamine Intranasal (Dpi-386)
- Enerzair Breezhaler (Glycopyrrolate/Indacaterol/Mometasone)
- Lonhala Magnair (Glycopyrrolate)
- Qbrexza (Glycopyrronium Cloth)
- Akineton (Biperiden)
- Atrovent Hfa (Ipratropium Bromide Hydrofluoroalkane Inhalation)
- Trospium Chloride Extended Release
- Combivent Respimat (Ipratropium/Albuterol Metered Spray Inhalation)
- Chlorprothixene
- Metapain (Nefopam/Paracetamol)
- Acetaminophen/Caffeine/Diclofenac/Orphenadrine
Drugs under the Pipeline for Muscarinic Receptor Antagonists:
- Glycopyrrolate (PT001)
- Batefenterol (GSK961081)
- Darotropium bromide (GSK233705)
- Xanomeline/Trospium (KarXT)
- Aroxybutynin/Atomoxetine (AD109)
- AZD2115
- Easyhaler Tiotropium (Tiotropium bromide)
- Navafenterol (AZD8871)
- ASM-024
- Diphenhydramine/Lorazepam/Zolpidem (SM-1)
- Oxybutynin/Atomoxetine (AD036)
- Fluticasone/Batefenterol (FF/GSK-961081)
- Aceclidine/Tropicamide (PRX-100)
- Tiotropium bromide inhalation (VR410)
- Trospium chloride inhalation (ALKS 27)
- AZD8999
- CHF6366
- Enablex (Darifenacin)
- Afacifenacin fumarate (SMP-986)
- Atropine (CBT-009)
- Atropine (OT-101 ophthalmic solution)
- Atropine Sulfate (DE-127)
- Clonidine/Oxybutynin (OP-014)
- Glycopyrronium bromide (PSX-1002)
- Ketamine/Scopolamine
Clinical Activity and Developments of Muscarinic Receptor Antagonists:
As of June 2023, more than 30 companies have approximately 29 molecules for above 549 diseases. For these molecules, more than 493 clinical trials are being conducted by players across the globe. For instance,
- In Jan 2023, Cloudbreak Therapeutics completed a phase-I/II trial for Atropine ophthalmic in volunteers for myopia.
- In May 2023, AstraZeneca in collaboration with Paraxel completed a phase-I trial in chronic obstructive pulmonary disease in the USA for Breztri Aerosphere (Budesonide/Formoterol/Glycopyrrolate).
|
Molecule Name |
Number of Studies |
|
Glycopyrrolate (PT001) |
19 |
|
Batefenterol (GSK961081) |
13 |
|
Darotropium bromide (GSK233705) |
11 |
|
Xanomeline/Trospium (KarXT) |
11 |
|
Aroxybutynin/Atomoxetine (AD109) |
6 |
|
AZD2115 |
6 |
|
Easyhaler Tiotropium (Tiotropium bromide) |
5 |
|
Navafenterol (AZD8871) |
5 |
|
ASM-024 |
4 |
|
Diphenhydramine/Lorazepam/Zolpidem (SM-1) |
4 |
|
Oxybutynin/Atomoxetine (AD036) |
4 |
|
Fluticasone/Batefenterol (FF/GSK-961081) |
3 |
|
Aceclidine/Tropicamide (PRX-100) |
2 |
|
Tiotropium bromide inhalation (VR410) |
2 |
|
Trospium chloride inhalation (ALKS 27) |
2 |
|
AZD8999 |
1 |
|
CHF6366 |
1 |
|
Enablex (Darifenacin) |
1 |
|
Afacifenacin fumarate (SMP-986) |
1 |
|
Atropine (CBT-009) |
1 |
|
Atropine (OT-101 ophthalmic solution) |
1 |
|
Atropine Sulfate (DE-127) |
1 |
|
Clonidine/Oxybutynin (OP-014) |
1 |
|
Glycopyrronium bromide (PSX-1002) |
1 |
|
Ketamine/Scopolamine |
1 |
Target Indication Analysis of Muscarinic Receptor Antagonists:
Muscarinic receptor antagonists such as Darifenacin, and Tolterodine are used for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency. Glycopyrronium is indicated to reduce the volume and acidity of gastric secretions, and airway secretion, and block cardiac inhibitory reflexes during the induction of anesthesia and intubation. Aclidinium is indicated for the long-term, maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease, including chronic bronchitis and emphysema. Additionally, there are drug molecules in the clinical trial phases for conditions like myopia, presbyopia, and others.
Regional Analysis of Muscarinic Receptor Antagonists:
Muscarinic Receptor Antagonist Market
According to the World Health Organization at present 2.2 billion people around the world have vision impairment. According to a research report, the global prevalence of gastric secretion-related diseases such as peptic ulcer was approximately 8.09 million, representing a 25.82% increase from 1990, where the highest age-standardized prevalence rate was in South Asia. All these growing burdens of diseases indicate a high growth potential for the muscarinic receptor antagonist market. AstraZeneca’s Breztri had a total product sale of US$ 398 million in 2022, including, US$ 239 million in the USA, US$ 92 million in the emerging markets, US$ 34 million in Europe, and US$ 34 million in the rest of the world. Boehringer Ingelheim’s Spiriva had net sales of US$169 million in 2021 and witnessed an insignificant increase in sales of US$ 170 million in 2022 due to currency reasons.
Latin America
Europe
Asia Pacific
Middle East
North America
Key Features of the Reports
- The report provides granular level information about the market size, regional market share, historic market (2018-2022), and forecast (2023-2029)
- The report covers in-detail insights about the competitor’s overview, company share analysis, key market developments, and their key strategies
- The report outlines drivers, restraints, unmet needs, and trends that are currently affecting the market
- The report tracks recent innovations, key developments, and start-up details that are actively working in the market
- The report provides a plethora of information about market entry strategies, regulatory framework, and reimbursement scenario
Frequently Asked Questions
Tolterodine, Fesoterodine, Stiolto Respimat (Olodaterol/Tiotropium Fdc), Anoro Ellipta (Umeclidinium/Vilanterol), Tiotropium Bromide Dry Powder Inhaler, and Ultibro (Glycopyrronium/Indacaterol) are some of the approved muscarinic receptor antagonists.
Boehringer Ingelheim, Novartis, AstraZeneca, LENZ Therapeutics, Orient Europharma, and GSK are some of the major market players in muscarinic receptor antagonists.
Major indications for muscarinic receptor antagonists are chronic obstructive pulmonary disease, overactive bladder, motion sickness, asthma, and myopia.
There are a total of 28 molecules in the clinical development phases for muscarinic receptor antagonists.
- Boehringer Ingelheim
- Novartis
- AstraZeneca
- LENZ Therapeutics
- Orient Europharma
- GSK
- Sanofi
- Eli Lilly & Company
- AbbVie