GPCRs (G protein-coupled receptors) also known as seven helical transmembrane receptors, are a large group of evolutionary related proteins that are cell surface receptors, which detect molecules outside the cell and activate cellular responses. GPCRs are targeted for the treatment of diseases from oncology, immunology, cardiovascular, neurological, and metabolic disorders. GPCR agonists facilitate cellular effects upon binding to their receptor and promoting a conformational change in that population of receptors that is conducive to signaling. GPCR agonists are currently in clinical development phases for conditions such as migraine, muscular dystrophies, lymphoma, malignant melanoma, solid tumors, glioblastoma, and others. Revalesio, GSK, BridgeBio Pharma, Amgen, Aditum Bio, Artelo Bioscience, and adMare BioInnovations are some of the major players with GPCR agonists in their pipeline.
Key Market Developments:
- In Jan 2023, Linnaeus Therapeutics’s LNS 8801, a GPCR agonist, received Orphan Drug status for malignant melanoma in the USA.
- In Apr 2023, Treneva received patent protection for compositions and methods of using TRV 250, a GPCR agonist in the USA.
Drugs under the Pipeline for GPCR Agonists:
- RNS60
- Camicinal (GSK962040)
- Encaleret (BBP-305)
- AMG 133
- ANC-501
- 13
- Beraprost isomer (CTO1681)
- 212Pb-DOTAM-GRPR1
- 2?Hydroxyoleic acid (NFX88)
- Cu-67 SAR-Bombesin
- JTT-851
- LNS8801
- NCP112
- OK-101
- TRV250
- UISH001
Clinical Activity and Developments of GPCR Agonists:
Currently, there are 16 drug molecules in the GPCR agonists and all of them are in the clinical development phases.
- In Oct 2022, Beech Tree Labs released pharmacodynamics data from a preclinical study in muscular dystrophies and also conducted preclinical trials in muscular dystrophies in the USA for UISH-OO1, a Histamine/Serotonin combination.
- In Feb 2023, Amgen conducted a phase-II clinical trials for obesity in Spain and Hungary for AMG-133, a GPCR agonist.
|
Molecule Name |
Number of Studies |
|
RNS60 |
15 |
|
Camicinal (GSK962040) |
13 |
|
Encaleret (BBP-305) |
4 |
|
AMG 133 |
3 |
|
ANC-501 |
3 |
|
ART27.13 |
3 |
|
Beraprost isomer (CTO1681) |
2 |
|
212Pb-DOTAM-GRPR1 |
1 |
|
2?Hydroxyoleic acid (NFX88) |
1 |
|
Cu-67 SAR-Bombesin |
1 |
|
JTT-851 |
1 |
|
LNS8801 |
1 |
|
NCP112 |
1 |
|
OK-101 |
1 |
|
TRV250 |
1 |
|
UISH001 |
1 |
Target Indication Analysis of GPCR Agonists
GPCR agonists are in preclinical trials for conditions such as CNS disorders, muscular dystrophies, pancreatic cancer, uveal melanoma, cachexia, Alzheimer’s disease, Parkinson’s disease, and traumatic brain injuries, in phase-I/II for anorexia, glioma, solid tumors, lymphoma, malignant melanoma, and solid tumors, and in phase-II for migraine, glioblastoma, major depressive disorder, obesity, diabetic gastroparesis, amyotrophic lateral sclerosis, asthma, multiple sclerosis, and stroke.
Regional Analysis
GPCR Agonists Market
Migraine is the most common neurological disorder and had a global prevalence of 1.1 billion cases in 2019, and the highest age-standardized prevalence rates were found in Belgium (22,400) and Italy (20,337). Glioblastoma accounts for 49% of primary brain tumors and has the highest incidence rates among malignant brain and CNS tumors affecting primarily the elderly population. According to the World Health Organization, approximately 280 million people in the world have depression, which is 50% more common among women than men, and Ukraine (6.3%), the USA (5.9%), Australia (5.9%), Brazil (5.8%) have the highest rates of depression. Multiple sclerosis across the globe has increased from 2.3 million in 2013 to 2.8 million in 2020 and 2.9 million in 2023. All of these diseases and their incidence and prevalence rates depict the market potential for GPCR agonists.
Latin America
Europe
Asia Pacific
Middle East
North America
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Frequently Asked Questions
Camicinal (GSK962040), Encaleret (BBP-305), Beraprost isomer (CTO1681), 212Pb-DOTAM-GRPR1, 2?Hydroxyoleic acid (NFX88), Cu-67 SAR-Bombesin are few of the drugs in the pipeline for GPCR agonists.
Revalesio, GSK, BridgeBio Pharma, Amgen, Aditum Bio, Artelo Bioscience, and adMare BioInnovations are some of the major players in the GPCR agonists market.
Major indications for GPCR agonists are migraine, glioblastoma, major depressive disorder, obesity, diabetic gastroparesis, amyotrophic lateral sclerosis, asthma, multiple sclerosis, and stroke.
There are a total of 16 molecules in the clinical development phases for GPCR agonists.
- Revalesio
- GSK
- BridgeBio Pharma
- Amgen
- Aditum Bio
- Artelo Bioscience
- adMare BioInnovations
- CytoAgents
- Orano
- Neurofix Pharma
- Clarity Pharma
- Linnaeus Therapeutics
- DongKoo Bio & Pharma
- OKYO Pharma
- Trevena
- Beech Tree Labs