Companies & Research Resources

Pharmaceutical Industry Involvement

Numerous pharmaceutical companies have invested in research and development targeting the GHS-R1a receptor, exploring its potential across various therapeutic areas. The following list highlights some key players based on published research and development activities [1, 2]. (Note: This information is based on available literature and may not reflect the most current pipeline status.)

• Pfizer: Developed the agonist Capromorelin and the inverse agonist PF-5190457, which entered clinical trials for obesity and alcohol use disorder.
• Merck: Developed the agonist Ibutamoren (MK-0677), though its development was halted due to safety concerns.
• AstraZeneca: Explored multiple chemical scaffolds for both GHS-R1a agonists and antagonists.
• Helsinn Healthcare: Licensed the agonist Anamorelin from Ono Pharmaceutical; Anamorelin (Adlumiz) is approved in Japan for cancer cachexia.
• Ono Pharmaceutical: Originator of Anamorelin.
• Teijin Pharma: Licensed Capromorelin from Pfizer for the Japanese market.
• Aratana Therapeutics: Licensed Capromorelin from Pfizer for veterinary applications.
• Tranzyme Pharma (later Ocera/Mallinckrodt): Developed the agonist Ulimorelin for GI motility disorders.
• Asubio Pharma (Daiichi Sankyo): Identified specific GHS-R1a inverse agonists.
• Bayer: Developed YIL781, a biased GHS-R1a antagonist.
• Abbott: Developed Abb13d, a Gαq/11 inverse agonist.
• Eli Lilly & Takeda Pharmaceuticals: Have patents related to inhibitors of GOAT, the enzyme that activates ghrelin [2].

This diverse involvement underscores the significant interest in GHS-R1a as a therapeutic target within the pharmaceutical industry.

Key Publications & Reviews

The understanding of GHS-R1a biology and pharmacology is rapidly evolving. The following publications provide comprehensive reviews of the field:

• [1] Giorgioni, G., Del Bello, F., Quaglia, W., Botticelli, L., Cifani, C., Di Bonaventura, E. M., ... & Piergentili, A. (2022). Advances in the Development of Nonpeptide Small Molecules Targeting Ghrelin Receptor. *Journal of medicinal chemistry*, *65*(5), 3796–3830. https://pmc.ncbi.nlm.nih.gov/articles/PMC8883476/
• [2] Müller, T. D., et al. (2020). Ghrelin signaling: GOAT and GHS-R1a take a LEAP in complexity. *Endocrinology*, *161*(7), bqaa061. https://pmc.ncbi.nlm.nih.gov/articles/PMC7299083/
• (Additional significant publications could be added here)

Scientific Resources

For further research and information, the following resources are valuable:

• PubMed - Search for the latest biomedical literature on GHS-R1a.
• IUPHAR/BPS Guide to Pharmacology - Ghrelin Receptor - Detailed pharmacological data.
• ClinicalTrials.gov - Database of ongoing and completed clinical studies involving GHS-R1a modulators.