The GPCR-targeting therapies market is expected to grow significantly in the coming years. This is due to the increasing number of patients who are being diagnosed with cancer, the growing awareness of GPCR-Targeting therapies, and the increasing number of GPCR-Targeting therapies that are under clinical trials and filed for approval by various companies.

LAS VEGAS, June 30, 2025 /PRNewswire/ -- DelveInsight's GPCR-Targeting Therapies Market Size, Target Population, Competitive Landscape & Market Forecast report includes a comprehensive understanding of current treatment practices, addressable patient population, which includes top indications such as PTCL, CTCL, migraine, NASH, and others. The selected indications are based on approved therapies and ongoing pipeline activity. The report also provides insights into the emerging GPCR-targeting therapies, market share of individual therapies, and current and forecasted GPCR-targeting therapies market size from 2020 to 2034, segmented into 7MM.

Key Takeaways from the GPCR-Targeting Therapies Market Report

• As per DelveInsight's analysis, the total market size of GPCR-targeting therapies in the 7MM is expected to surge significantly by 2034.
• The United States is expected to hold the largest share of the total GPCR inhibitors market among the 7MM.
• The report provides the total potential number of patients in the indications, such as PTCL, CTCL, Migraine, NASH, and others.
• Leading GPCR-targeting therapies companies, such as CytoDyn, REMD Biotherapeutics, GPCR Therapeutics, Structure Therapeutics, and others, are developing novel GPCR-targeting therapies that can be available in the GPCR-targeting therapies market in the coming years. 
• Some of the key GPCR-targeting therapies in the pipeline include Leronlimab, Volagidemab, GPC-100, GSBR-1290, and others.
• In July 2024, Radionetics Oncology entered into a strategic agreement with Eli Lilly and Company, providing Lilly access to Radionetics' proprietary GPCR targeting small molecule radiopharmaceuticals.

Discover which indication is expected to grab the major GPCR-targeting therapies market share @ GPCR-Targeting Therapies Market Report

GPCR-Targeting Therapies Market Dynamics

The GPCR-targeting therapies market is experiencing dynamic growth, driven by advances in drug discovery technologies, an expanding understanding of GPCR biology, and the therapeutic relevance of these receptors in a wide array of diseases. GPCRs represent the largest family of membrane receptors in humans and are involved in regulating various physiological processes, making them attractive targets for drug development. Approximately 30–40% of currently approved drugs act on GPCRs, underscoring their clinical and commercial significance.

One of the key market dynamics is the diversification of therapeutic areas beyond traditional indications such as cardiovascular diseases and neurological disorders. Recent research has highlighted the role of GPCRs in oncology, metabolic disorders, and immune-mediated diseases, fueling interest in developing novel ligands, biased agonists, and allosteric modulators that offer greater specificity and reduced side effects. The development of precision medicine approaches and better structural characterization of GPCRs using cryo-electron microscopy have further enabled the design of highly targeted therapies.

Pharmaceutical companies are increasingly investing in GPCR-focused pipelines, often in collaboration with biotechnology firms and academic research institutions. Strategic partnerships, licensing deals, and acquisitions are common, aiming to access novel chemistries and platform technologies, such as structure-based drug design, high-throughput screening, and artificial intelligence-enabled ligand discovery. These collaborations are vital for accelerating R&D timelines and reducing attrition rates in clinical development.

However, the market also faces several challenges, including the inherent complexity of GPCR signaling pathways, the risk of off-target effects, and the difficulty of achieving functional selectivity. Regulatory hurdles, high development costs, and the need for robust biomarkers for patient stratification further complicate commercialization efforts. Despite these barriers, the pipeline remains robust, with a growing number of GPCR-targeting candidates advancing through preclinical and clinical stages.

Overall, the GPCR-targeting therapies market is poised for sustained expansion, supported by scientific innovation, a growing demand for targeted treatments, and the therapeutic versatility of GPCRs. With the convergence of computational biology, structural pharmacology, and translational research, the next wave of GPCR-targeting drugs is expected to offer novel mechanisms of action and improved patient outcomes across diverse indications.

GPCR-Targeting Therapies Treatment Market 

The market outlook for GPCR-targeting therapies is promising, driven by successful drugs like ZAVZPRET, POTELIGEO, AIMOVIG, and VYEPTI. ZAVZPRET is an innovative small-molecule antagonist of the CGRP receptor, approved for the acute treatment of migraines, both with and without aura, in adults. It works by inhibiting the CGRP receptor, which plays a key role in migraine development by contributing to neurogenic inflammation and blood vessel dilation. Administered as a nasal spray, ZAVZPRET allows for quick absorption through the nasal lining, providing direct access to the bloodstream while bypassing the digestive system and first-pass liver metabolism.

POTELIGEO, developed by Kyowa Kirin, is a humanized monoclonal antibody that targets the CCR4 receptor—a protein commonly found on certain cancerous T-cells. By binding to CCR4, the drug helps recruit immune cells to attack and eliminate malignant cells, thereby boosting the body's immune defense against cancer. Initially approved in Japan in 2012 for relapsed or refractory CCR4-positive adult T-cell leukemia (ATL), its indication was expanded in 2014 to include relapsed or refractory CCR4-positive peripheral T-cell lymphoma (PTCL) and cutaneous T-cell lymphoma (CTCL). The U.S. FDA approved POTELIGEO in 2018 for Mycosis Fungoides and Sézary Syndrome, with similar approvals granted in Europe. In June 2020, the drug became commercially available in Germany for adults with Mycosis Fungoides or Sézary Syndrome who had undergone at least one prior systemic treatment.

Erenumab, co-developed by Amgen and Novartis, is a fully human monoclonal antibody that selectively binds to and blocks CGRP receptors. CGRP ligands, which are small neuropeptides, contribute to migraine and chronic pain through strong vasodilatory effects. By directly competing with CGRP, erenumab provides a high degree of specificity and effectiveness compared to small-molecule therapies. It is used to treat conditions such as migraine, vasoconstriction, hot flashes, and stable angina pectoris. The antibody received approval in the U.S. in May 2018 and in the EU in July 2018.

Learn more about the FDA-approved GPCR-targeting therapies @ GPCR-Targeting Therapies Drugs

Key Emerging GPCR-Targeting Therapies and Companies

Several key players, including CytoDyn (Leronlimab), REMD Biotherapeutics (Volagidemab), Structure Therapeutics (GSBR-1290), GPCR Therapeutics (GPC-100), and others, are involved in developing drugs for GPCR-targeting therapies for various indications such as NASH, Multiple Myeloma, Diabetes, and others.

Volagidemab (REMD-477) is a human monoclonal antibody targeting the glucagon receptor (GCGR), developed by REMD Biotherapeutics for the treatment of juvenile type I diabetes (T1D) and type II diabetes (T2D). It functions by binding to GCGR and competitively inhibiting its signaling pathway. This action enhances glucose uptake by the liver, reduces the breakdown of glycogen and gluconeogenesis, and stimulates glycogen synthesis—collectively contributing to its blood sugar-lowering effects (CK060182). As of March 2021, the drug was being investigated in multiple indications: T1D and T2D were in Phase II clinical trials, glucose intolerance was in Phase I, and metabolic disorders were in the preclinical stage (CK060183).

Leronlimab is classified as a viral entry inhibitor, a type of HIV therapy that blocks the virus from penetrating and infecting healthy cells. In contrast to Highly Active Antiretroviral Therapy (HAART), which targets HIV after cell entry and replication, Leronlimab intervenes earlier in the viral life cycle. The critical role of the CCR5 receptor in HIV infection is highlighted by the natural immunity observed in individuals with a genetic mutation that disables CCR5 expression. Leronlimab is currently under development for the treatment of Nonalcoholic Steatohepatitis (NASH), HIV-associated NASH, and various solid tumors, with development efforts currently in Phase II.

In April 2019, the company signed multiple agreements with Samsung for the transfer of technology, process validation, manufacturing, and pre-approval inspection services, aimed at supporting the commercial production of Leronlimab's bulk drug substance.

The anticipated launch of these emerging therapies are poised to transform the GPCR-targeting therapies market landscape in the coming years. As these cutting-edge therapies continue to mature and gain regulatory approval, they are expected to reshape the GPCR-targeting therapies market landscape, offering new standards of care and unlocking opportunities for medical innovation and economic growth.

To know more about GPCR-targeting therapies clinical trials, visit @ GPCR-Targeting Therapies Treatment Drugs 

GPCR-Targeting Therapies Overview

G protein-coupled receptors (GPCRs) are a vital group of cell surface receptors that regulate numerous physiological processes. In many cancers, GPCR pathways are often dysregulated due to abnormal expression, increased activity, or mutations, contributing to uncontrolled cell growth, blood vessel formation, and metastasis. GPCRs are categorized into several classes based on their structure and function. In humans, the primary classes include Class A (Rhodopsin-like), Class B (Secretin and Adhesion), Class C (Metabotropic glutamate/pheromone), and Class F (Frizzled/TAS2). 

Additional classes, such as Class D (fungal mating pheromone receptors) and Class E (cyclic AMP receptors), are present in non-human organisms. Among these, Class A is the most extensive, encompassing a majority of hormone, neurotransmitter, and sensory receptors. Class B is split into secretin and adhesion subgroups, Class C comprises receptors for glutamate and GABA, and Class F includes receptors like frizzled and smoothened involved in Wnt signaling. This classification underscores the structural and functional diversity of GPCRs and their critical roles in both normal physiology and disease.

GPCR-Targeting Therapies Epidemiology Segmentation

The GPCR-targeting therapies market report proffers epidemiological analysis for the study period 2020–2034 in the 7MM, segmented into:

• Total Cases in Selected Indications for GPCR-Targeting Therapies
• Total Eligible Patient Pool in Selected Indications for GPCR-Targeting Therapies
• Total Treated Cases in Selected Indications for GPCR-Targeting Therapies

Scope of the GPCR-Targeting Therapies Market Report

• GPCR-Targeting Therapies Therapeutic Assessment: GPCR-Targeting Therapies current marketed and emerging therapies
• GPCR-Targeting Therapies Market Dynamics: Conjoint Analysis of Emerging GPCR-Targeting Therapies Drugs
• Competitive Intelligence Analysis: SWOT analysis and Market entry strategies
• Unmet Needs, KOL's views, Analyst's views, GPCR-Targeting Therapies Market Access and Reimbursement

Discover more about GPCR-targeting therapies in development @ GPCR-Targeting Therapies Clinical Trials

Table of Contents

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