G-Protein-Coupled Receptor (GPCR) targeting drives key pharma innovations, with fresh 2025-2026 insights on pipelines, biologics, and AI tools.

G-Protein-Coupled-Receptor-Targeting Market Size and Forecast

DataM Intelligence has published a new research report on "G-Protein-Coupled-Receptor-Targeting Market Size 2025". The report explores comprehensive and insightful Information about various key factors like Regional Growth, Segmentation, CAGR, Business Revenue Status of Top Key Players and Drivers. The purpose of this report is to provide a telescopic view of the current market size by value and volume, opportunities, and development status.

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➢ Approved Drugs:

✦ 516 FDA-approved drugs target GPCRs, comprising 36% of all approved drugs and acting on 121 targets (one-third of non-sensory GPCRs).

✦ Key antibody examples include erenumab (CGRPR for migraine, >$2B sales by 2024), fremanezumab/galcanezumab (CGRP for migraine, combined >$5B sales), and mogamulizumab (CCR4 for lymphoma, $420M sales).​

✦ No novel GPCR-targeted drugs appear in FDA's 2025 approval lists (46 total novels), though earlier ones like talquetamab (GPRC5D bispecific for multiple myeloma, 2023) highlight ongoing success.

➢ Clinical Pipeline:

✦ 337 agents target 133 GPCRs in trials, including 30 novel targets; many are repurposed approved drugs, allosteric modulators, or biologics.

✦ Focus areas: metabolic diseases (e.g., obesity/diabetes drugs generated ~$30B in 2023 sales), oncology, immunology; increasing trials in these.​

✦ Examples: Superluminal's melanocortin-4 AI candidate for obesity entering human trials (Lilly deal up to $1.3B, 2025); GMA102 (GLP-1R antibody) advancing to Phase III for diabetes/obesity.

➢ Emerging Trends:

✦ Shift to biologics/antibodies for better specificity, longer half-life, and peripheral action; >170 antibody pipelines across 76 targets (oncology, metabolic, inflammation).​

✦ AI/ML for structure prediction, ligand design, biased signaling; addressing orphan GPCRs and allosteric sites via cryo-EM, omics.

✦ ADCs targeting GPCRs like GPRC5D (e.g., AZD0305 Phase II for myeloma); RNA therapies, synthetic biology.

➢ Recent Developments:

➠ January 2026

✦ Oral small-molecule GLP-1 receptor agonists continue to gain momentum as late-stage clinical data strengthens confidence in GPCR-based obesity therapies.

✦ GPCR-focused drug discovery remains a priority area as pharma companies expand pipelines across metabolic, CNS, and inflammatory indications.

➠ December 2025

✦ Positive Phase 2b clinical outcomes for an oral GLP-1 receptor agonist reinforce the shift toward non-injectable GPCR-targeted metabolic treatments.

✦ Advancement of first-in-human studies for novel GPCR-based amylin receptor agonists highlights growing innovation in obesity drug development.

➠ November 2025

✦ Strategic collaborations emerge to identify previously unexplored GPCR targets, particularly for central nervous system disorders.

✦ Expansion of GPCR-targeted programs for obesity and metabolic diseases reflects sustained pharma investment in next-generation receptor-based therapeutics.

➢ Key Players:

Abcam plc, Enzo Life Sciences, Inc, Promega Corporation, PerkinElmer Inc, Thermo Fisher Scientific, Eurofins DiscoverX Products, WuXi AppTec (HD Biosciences Co. Ltd), BioInvenu Inc, Danaher Corporation (Molecular Devices LLC) and Merck KGaA.

Growth Forecast Projected:

The Global G-Protein-Coupled-Receptor-Targeting Market is anticipated to rise at a considerable rate during the forecast period, between 2025 and 2032. In 2024, the market is growing at a steady rate, and with the rising adoption of strategies by key players, the market is expected to rise over the projected horizon.

Research Process:

Both primary and secondary data sources have been used in the global G-Protein-Coupled-Receptor-Targeting Market research report. During the research process, a wide range of industry-affecting factors are examined, including governmental regulations, market conditions, competitive levels, historical data, market situation, technological advancements, upcoming developments, in related businesses, as well as market volatility, prospects, potential barriers, and challenges.

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➢ Key Segments:

By Product:
The market is segmented by product into cell lines, detection kits, cell culture reagents, and ligands. Cell lines hold a significant share as they are essential tools for studying receptor signaling and cellular responses in controlled environments. Detection kits are widely used for accurate and reproducible measurement of intracellular signaling pathways. Cell culture reagents support cell growth, viability, and assay consistency, while ligands play a critical role in receptor activation or inhibition studies, supporting drug discovery and validation workflows.

By Application Segment:
Based on application segment, the market includes cancer research, CNS research, metabolic research, cardiovascular research, respiratory research, inflammation research, and other applications. Cancer research dominates due to extensive use of functional assays to understand tumor biology and evaluate targeted therapies. CNS and metabolic research are growing steadily with increasing focus on neurological disorders and metabolic diseases. Cardiovascular and respiratory research leverage these assays to study receptor-mediated pathways, while inflammation research supports the development of immunomodulatory and anti-inflammatory drugs. The "other application" segment includes rare diseases and emerging therapeutic areas.

By End-User (Assay Type):
By end-user, the market is segmented into cAMP functional assays, calcium functional assays, β-arrestin functional assays, radioligand binding and GTPγS functional assays, internalization assays, trafficking assays, and other assays. cAMP and calcium functional assays are widely adopted due to their reliability and relevance in GPCR signaling studies. β-arrestin assays are increasingly used to analyze biased signaling mechanisms. Radioligand binding and GTPγS assays remain important for receptor binding and activation analysis, while internalization and trafficking assays provide insights into receptor regulation and cellular dynamics. The "other assays" category includes emerging and customized assay formats used in advanced research settings.

➢ Regional Analysis for Market:

⇥ North America (U.S., Canada, Mexico)

⇥ Europe (U.K., Italy, Germany, Russia, France, Spain, The Netherlands and Rest of Europe)

⇥ Asia-Pacific (India, Japan, China, South Korea, Australia, Indonesia Rest of Asia Pacific)

⇥ South America (Colombia, Brazil, Argentina, Rest of South America)

⇥ Middle East & Africa (Saudi Arabia, U.A.E., South Africa, Rest of Middle East & Africa)

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