G Protein-Coupled Receptors (GPCR) Structure-Based Drug Design Market Report 2025

The G protein-coupled receptors (GPCR) structure-based drug design market size has grown rapidly in recent years. It will grow from $2.33 billion in 2024 to $2.64 billion in 2025 at a compound annual growth rate (CAGR) of 13.5%. Growth in the historic period was driven by increasing adoption of structure-based drug discovery, rising demand for targeted therapeutics, growing prevalence of chronic diseases, higher healthcare expenditure, and expansion of biomarker-driven drug development strategies.

The G protein-coupled receptors (GPCR) structure-based drug design market size is expected to see rapid growth in the next few years. It will grow to $4.33 billion in 2029 at a compound annual growth rate (CAGR) of 13.1%. Growth in the forecast period is expected to be supported by rising demand for personalized medicine, expansion of contract research organizations (CROs), increased funding for drug discovery, growing collaborations between biotech and pharmaceutical companies, and a higher need for highly specific drugs. Key trends anticipated for the forecast period include advancements in cryo-electron microscopy and X-ray crystallography, innovation in computational docking software, developments in AI-driven drug design, investment in high-throughput screening platforms, and progress in peptide and antibody therapeutics.

The rising demand for precision medicine is expected to drive growth in the G protein-coupled receptors (GPCR) structure-based drug design market in the coming years. Precision medicine involves treatment strategies that utilize specific biological markers to guide therapy development tailored to individual patient characteristics and disease profiles. This demand is fueled by the superior effectiveness and fewer side effects of precision therapies compared to traditional treatments, as healthcare systems increasingly focus on personalized approaches targeting specific molecular pathways rather than broad-spectrum treatments. The emphasis on precision medicine is directly accelerating the adoption of GPCR structure-based drug design platforms, as pharmaceutical companies seek advanced computational tools to identify and optimize receptor-specific compounds that meet the molecular precision required by personalized treatments. For example, in February 2024, the Personalized Medicine Coalition, a US-based non-profit organization, reported that the FDA approved 16 new personalized treatments for rare diseases in 2023, a notable increase from six approvals in 2022. Among these new treatments, seven are cancer drugs, while three address other diseases and conditions. Therefore, the growing demand for precision medicine is propelling the expansion of the GPCR structure-based drug design market.

Leading companies in the GPCR structure-based drug design market are developing innovative solutions such as structure-based drug design platforms to speed up novel drug discovery and enhance therapeutic targeting. These platforms combine computational and experimental techniques that utilize the three-dimensional structure of target proteins to design and optimize drug candidates, enabling the identification of more precise, effective, and safer treatments. For instance, in January 2025, Septerna Inc., a US-based pharmaceutical company, launched initiatives to advance its Native Complex Platform, following a $100 million Series A funding round. This platform supports GPCR structure-based drug design by preserving their native structure and dynamics outside the cellular environment. It aids in the development of GPCR-targeted therapies for previously undruggable targets across multiple therapeutic areas and provides a scalable foundation for industrialized drug discovery, integration of novel screening technologies, and the discovery of new GPCR modulation mechanisms. Additionally, the platform opens opportunities to explore the entire GPCR superfamily systematically, broadening the scope of potential therapeutic interventions.

In May 2024, Incyte Corporation, a US-based biopharmaceutical firm, acquired Escient Pharmaceuticals, Inc. for $750 million. This acquisition strengthens Incyte’s inflammation and autoimmunity pipeline by adding first-in-class oral GPCR-targeting MRGPR antagonists, EP262 and EP547. These compounds block key Mas-related G protein-coupled receptors involved in mast cell activation and severe pruritus, advancing therapies for a wide range of mast cell-mediated and cholestatic pruritus-related diseases that have significant unmet medical needs. Escient Pharmaceuticals, Inc. is a US-based biopharmaceutical company specializing in the development of first-in-class oral antagonists targeting mas-related G protein-coupled receptor X2 and X4.

Major players in the G protein-coupled receptors (GPCR) structure-based drug design market are F. Hoffmann-La Roche Ltd., Pfizer Inc., Sanofi S.A., AstraZeneca plc, Thermo Fisher Scientific Inc., Boehringer Ingelheim International GmbH, WuXi AppTec Co. Ltd., Charles River Laboratories International Inc., Evotec SE, Acadia Pharmaceuticals Inc., Promega Corporation, Domain Therapeutics SA, Schrödinger Inc., Kallyope Inc., Domainex Ltd., Structure Therapeutics Inc., Creative Biolabs Inc., InterAx Biotech Inc., Abalone Bio Inc., Octant Inc.

North America was the largest region in the G protein-coupled receptors (GPCR) structure-based drug design market in 2024. The regions covered in G protein-coupled receptors (GPCR) structure-based drug design report are Asia-Pacific, Western Europe, Eastern Europe, North America, South America, Middle East and Africa. The countries covered in the G protein-coupled receptors (GPCR) structure-based drug design market report are Australia, Brazil, China, France, Germany, India, Indonesia, Japan, Russia, South Korea, UK, USA, Canada, Italy, Spain.

Note that the outlook for this market is being affected by rapid changes in trade relations and tariffs globally. The report will be updated prior to delivery to reflect the latest status, including revised forecasts and quantified impact analysis. The report’s Recommendations and Conclusions sections will be updated to give strategies for entities dealing with the fast-moving international environment.

The sudden escalation of U.S. tariffs and the consequent trade frictions in spring 2025 are severely impacting the pharmaceutical companies contend with tariffs on APIs, glass vials, and lab equipment inputs with few alternative sources. Generic drug makers, operating on razor-thin margins, are especially vulnerable, with some reducing production of low-profit medicines. Biotech firms face delays in clinical trials due to tariff-related shortages of specialized reagents. In response, the industry is expanding API production in India and Europe, increasing inventory stockpiles, and pushing for trade exemptions for essential medicines.

G protein-coupled receptor (GPCR) structure-based drug design is an approach that develops drugs by leveraging the detailed three-dimensional structures of GPCRs to optimize binding and selectivity. This method allows researchers to design molecules that precisely interact with atomic-level features of GPCR binding sites, enhancing specificity and minimizing off-target effects.

The primary drug types in GPCR structure-based drug design include small molecules, biologics, peptides, and others. Small molecules are low-molecular-weight compounds that can easily enter cells to selectively modulate biological targets, such as enzymes or receptors. Key technologies used in this approach include X-ray crystallography, cryo-electron microscopy, computational modeling, and nuclear magnetic resonance (NMR) spectroscopy. These methods are applied across therapeutic areas such as oncology, cardiovascular diseases, neurological disorders, and metabolic disorders. End-users include pharmaceutical companies, biotechnology firms, academic institutions, and research institutes.

The G protein-coupled receptor (GPCR) structure-based drug design market research report is one of a series of new reports that provides G protein-coupled receptor (GPCR) structure-based drug design market statistics, including G protein-coupled receptor (GPCR) structure-based drug design industry global market size, regional shares, competitors with the G protein-coupled receptor (GPCR) structure-based drug design market share, G protein-coupled receptor (GPCR) structure-based drug design market segments, market trends, and opportunities, and any further data you may need to thrive in the G protein-coupled receptor (GPCR) structure-based drug design industry. This G protein-coupled receptor (GPCR) structure-based drug design market research report delivers a complete perspective of everything you need, with an in-depth analysis of the current and future scenario of the industry.

The G protein-coupled receptors (GPCR) structure-based drug design market consists of revenues earned by entities by providing services such as computational modeling, assay development and screening, hit identification and lead optimization, medicinal chemistry and compound synthesis, biologics and antibody development, specialized assay services for safety, efficacy, and biomarker discovery. The market value includes the value of related goods sold by the service provider or included within the service offering. The G protein-coupled receptors (GPCR) structure-based drug design market also includes sales of GPCR-expressing cell lines, detection kits, cell culture reagents, ligands, and assay systems. Values in this market are ‘factory gate’ values, that is the value of goods sold by the manufacturers or creators of the goods, whether to other entities (including downstream manufacturers, wholesalers, distributors and retailers) or directly to end customers. The value of goods in this market includes related services sold by the creators of the goods.

The market value is defined as the revenues that enterprises gain from the sale of goods and/or services within the specified market and geography through sales, grants, or donations in terms of the currency (in USD unless otherwise specified).

The revenues for a specified geography are consumption values that are revenues generated by organizations in the specified geography within the market, irrespective of where they are produced. It does not include revenues from resales along the supply chain, either further along the supply chain or as part of other products.

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