G-protein-coupled receptors (GPCRs) represent the most numerous and diverse class of membrane receptors found in eukaryotes. These receptors play a pivotal role in regulating nearly every aspect of human physiology and disease, making them crucial therapeutic targets, particularly in the field of cardiovascular disease. Over the years, GPCR drug discovery has evolved from random ligand screening to a more knowledge-driven approach, significantly enhancing the development of targeted therapies.
Currently, there are over 500 new drug candidates undergoing clinical testing, with a majority still being small molecules. However, there is a growing emphasis on peptide-activated GPCRs, with 134 drug candidates specifically designed for this receptor type. The increasing understanding of GPCRs has spurred significant investments and research collaborations to advance therapeutic solutions targeting these essential proteins.
The global G-protein coupled receptors market size is calculated at US$ 3.86 billion in 2024, grew to US$ 4.06 billion in 2025, and is projected to reach around US$ 6.37 billion by 2034. The market is expanding at a CAGR of 5.14% between 2024 and 2034. This steady growth reflects the increasing demand for new drugs that target GPCRs, further driving research and investment in this field.
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Superluminal Medicines, Inc. successfully closed a $120 million Series A fundraising round in September 2024. The funding will facilitate the clinical development of Superluminal’s lead program and support the expansion of small molecule therapeutic discovery initiatives focused on high-value GPCR targets. This investment underscores the increasing interest in developing novel GPCR-targeted therapies to address various medical conditions.
In January 2024, St. Jude Children’s Research Hospital announced an investment of nearly $13 million in a collaborative research initiative with Stanford, Columbia, and Duke universities. This partnership aims to enhance the understanding of GPCRs and their role in human health and disease. The research efforts are expected to provide deeper insights into the molecular mechanisms governing GPCR function, which could lead to the discovery of new therapeutic approaches.
Septerna, a biotechnology company specializing in the discovery and development of novel oral small molecule drugs targeting GPCRs, closed a $150 million Series B investment in July 2023. The company plans to utilize the funding to further expand its pipeline of innovative GPCR-targeting therapeutics. This investment highlights the strong financial backing and confidence in Septerna’s approach to developing GPCR-based treatments.
Before securing its Series B funding, Septerna launched a $100 million Series A fundraising round in January 2022. This initial investment provided the foundation for the company’s mission to identify and develop small molecule drugs targeting GPCRs, setting the stage for its subsequent expansion and continued success in the biotechnology sector.
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