What GPCR Therapeutics does

GPCR Therapeutics is a clinical-stage biopharmaceutical company founded in 2013 in Seoul, South Korea that develops therapeutics targeting G-protein coupled receptor (GPCR) heteromers, with a primary focus on CXCR4 combinations. Its core technology is the proprietary C-Het™ drug discovery platform, which has catalogued over 1,000 GPCR pairs and systematically identified synergistic heteromer mechanisms — most notably CXCR4-B2AR, CXCR4-LPA1, and CXCR4-HRH1 — validated through peer-reviewed publications in PNAS, Blood, Nature Scientific Reports, PLOS ONE, and Cell Communication and Signaling. The lead clinical asset is GPC-100/Burixafor, a small-molecule CXCR4 antagonist being advanced as a combination therapy with propranolol (GPC201) for hematopoietic stem cell mobilization in multiple myeloma patients undergoing autologous stem cell transplantation.

The business is structured around two product layers: a proprietary pipeline built on the C-Het™ platform, and out-licensed or partnered assets. GPC-100/Burixafor progressed through a US Phase 2 trial that reported an 89.7% primary-endpoint success rate, received FDA Orphan Drug Designation in October 2024, and is now being advanced by Exicure, Inc. following its January 2025 acquisition of the US subsidiary. The CXCR4-LPA1 combination for idiopathic pulmonary fibrosis has been out-licensed to Bridge Biotherapeutics under a 50:50 profit-share arrangement, while the CXCR4-HRH1 program remains research-stage. The company has raised approximately KRW 714 billion (cumulative across 6 funding rounds from 20+ institutional investors), passed the KOSDAQ Technology Evaluation with A-BBB grades, and was preparing for a KOSDAQ listing prior to the Exicure transaction.

Monetization is event-driven rather than product-based: revenue consists of licensing upfronts, milestone payments tied to clinical and regulatory progress, and profit-share on partnered commercialization. The company has not disclosed product pricing, has no approved drug, and is pre-revenue in the conventional sense. Its customers and counterparties are research collaborators and pharmaceutical partners — including MD Anderson, Dana-Farber, Memorial Sloan Kettering, Cleveland Clinic, City of Hope, Seoul National University, AdAlta, TaiGen, Bridge Biotherapeutics, and Exicure — rather than payers or end-prescribers.

Name

GPCR Therapeutics

Legal name

GPCR Therapeutics, Inc.

Website

https://gpcr.co.kr

Company type

Private

Founded year

2013

Operating status

Operating

Headcount range

11–50 employees

Short description

GPCR Therapeutics is a clinical-stage biopharmaceutical company that develops small-molecule and combination therapies targeting CXCR4 GPCR heteromers for oncology and fibrosis, serving patients via out-licensing, partnerships, and post-acquisition commercialization through Exicure.

Ownership category

akta.pro rank

Product category

Clinical-stage Biopharmaceuticals

NAICS

Research and Development in Biotechnology (except Nanobiotechnology) (541714), Biological Product (except Diagnostic) Manufacturing (325414), Scientific Research and Development Services (5417)

SIC

Biological Products, (No Disgnostic Substances) (2836), Pharmaceutical Preparations (2834)

akta.pro primary industry

Target Identification & Validation Platforms (omics-driven, chemoproteomics, genetic validation) (HLAAAIAI)

akta.pro secondary industries

Protein Interaction & Structural Biology Platforms (cryo-EM, X-ray, NMR, biophysics) (HLAAAIAH), Translational Medicine & Biomarkers (HLAIALAF)

Keywords

• GPCR drug discovery
• Clinical-stage biopharmaceutical
• Stem cell mobilization
• Hematological cancer therapeutics
• CXCR4 antagonist development

Headquarters

HQ city

Seoul

HQ country

South Korea

HQ region

Asia

Offices2 records

Markets served

GTM type

B2B

Offering type

Services

Cost components

Personnel, Technology or R&D, Operations, Marketing or Sales, Infrastructure

Revenue model

1. Drug Development Milestones: Revenue from milestone payments as drug candidates progress through clinical development stages under licensing and partnership agreements
2. Technology Licensing: Out-licensing of proprietary GPCR heteromer targeting technology and combination therapy patents for IPF and other indications. Received KRW 2 billion upfront from Bridge Biotherapeutics with 50:50 profit share on future commercialization.
3. Future Product Commercialization: Revenue from commercialization of proprietary drug candidates including GPC-100/Burixafor for stem cell mobilization and combination therapies. Expected to generate first revenue from technology exports from 2025.
4. Acquisition Payment: Following January 2025 acquisition by Exicure, Inc., receiving milestone payments including $1 million Phase 2 trial completion payment in January 2026

Go-to-market motion2 records

Distribution channels3 records

Marketing channels6 records

Core offering

GPCR Therapeutics is a clinical-stage international biopharmaceutical company developing novel therapeutics targeting GPCR (G-protein coupled receptor) heteromers, particularly CXCR4 in combination with other GPCRs. The company's lead asset GPC-100/Burixafor is a CXCR4 antagonist being developed as a combination therapy (GPC201) with propranolol for hematopoietic stem cell mobilization in multiple myeloma patients undergoing autologous stem cell transplantation. The proprietary C-Het drug discovery platform has identified over 1,000 GPCR pairs for therapeutic development across cancer, fibrotic diseases, and stem cell mobilization indications.

Product overview

GPCR Therapeutics is a clinical-stage biopharmaceutical company developing therapeutics targeting GPCR heteromers in cancer. The company operates its proprietary C-Het drug discovery platform and has a pipeline of combination therapies. Lead product GPC-100/Burixafor is a CXCR4 antagonist being developed as GPC201 (combined with propranolol) for stem cell mobilization in multiple myeloma. The company also has pipeline programs targeting CXCR4-LPA1 for fibrosis (out-licensed to Bridge Biotherapeutics) and CXCR4-HRH1 for solid tumors.

Differentiator

Problem solved

Functional benefit

Brands

• C-Het™ Platform: GPCR Therapeutics' proprietary drug discovery platform based on CXCR4 Heteromer Interactome and CXCR4 Heteromer Evaluator for systematic analysis of CXCR4-GPCRx target mechanisms.
• GPC-100 + Propranolol (GPC201)

Products and services

• GPC-100 (Burixafor) A novel CXCR4 antagonist and potent hematopoietic stem cell mobilizer that disrupts the CXCL12/CXCR4 axis in the bone marrow, releasing hematopoietic stem cells into circulation. It targets CXCR4, one of the most prevalent chemokine GPCRs overexpressed in more than 23 cancers.
• GPC201 (GPC-100 + Propranolol) A combination therapy consisting of GPC-100 (CXCR4 antagonist) and propranolol (FDA-approved ADRB2 inhibitor) for stem cell mobilization in multiple myeloma patients. The combination targets CXCR4 and B2AR GPCR pairs, demonstrating synergistic effects that improve upon standard of care treatments.
• C-Het Drug Discovery Platform A proprietary drug discovery platform based on CXCR4 Heteromer Interactome data that systematically analyzes and validates mechanisms of action for CXCR4-GPCRx combinations, enabling efficient and continuous development of therapeutic products through licensing and partnership arrangements.
• CXCR4-LPA1 Combination Therapy for IPF A combination therapy targeting CXCR4 and LPA1 receptors for the treatment of idiopathic pulmonary fibrosis (IPF) and other fibrotic diseases. Out-licensed to Bridge Biotherapeutics for joint development and commercialization with 50:50 profit share arrangement.
• CXCR4-HRH1 Combination Therapy Research-stage combination therapy targeting CXCR4 and histamine receptor H1 (HRH1) for anticancer therapy, based on findings that co-expression correlates with poor prognosis in breast cancer patients.

Quantifiable outcome

• 89.7% of multiple myeloma patients achieved primary endpoint of successful hematopoietic progenitor cell mobilization within two leukapheresis sessions
• +4 more outcomes

Named customers7 records

Segments5 records

Ideal customer profiles2 records

Technology focussed Yes

API detail

Has API

No

API docs

API detail

Core technology

AI maturity

App detail

Feature6 records

Partnerships

Six partnerships are on record, tiered core and secondary.

• Exicure, Inc.coreStrategic or Co-development Partner · 1 January 2025Exicure acquired GPCR Therapeutics USA Inc. in January 2025 to expand its GPCR-targeted therapeutics capabilities. The acquisition brought burixafor (GPC-100) into Exicure's pipeline. Following the acquisition, Exicure achieved a Phase 2 trial milestone triggering a $1 million payment to GPCR Therapeutics in January 2026. GPCR's operations continue under Exicure with focus on stem cell mobilization assets.
• Bridge BiotherapeuticscoreStrategic or Co-development Partner · 14 December 2023Out-licensing agreement for CXCR4-LPA1 inhibitor combination method for treatment of idiopathic pulmonary fibrosis (IPF). GPCR received upfront payment of KRW 2 billion (~$1.5 million) with 50:50 profit-share on future commercialization including sub-licenses. Collaboration leverages Bridge's BBT-877 autotaxin inhibitor for IPF combined with GPCR's CXCR4 targeting technology.
• TaiGen Biotechnology Co. Ltd.secondaryStrategic or Co-development Partner · 1 August 2023Collaboration on clinical development of GPC-100 (burixafor) for stem cell mobilization. Joint publication in Clinical Pharmacology in Drug Development demonstrating safety, PK/PD profile, and 3-14 fold increase in CD34+ cells in healthy subjects.
• City of Hope National Medical CentersecondaryStrategic or Co-development Partner · 1 February 2023Joint research collaboration with Dr. Pamela Becker on acute myeloid leukemia (AML) treatment strategy targeting CXCR4 and ADRB2 simultaneously. Analysis of 124 AML patient samples showing CXCR4 overexpression correlation. Results presented at AACR 2024.
• AdAlta LimitedsecondaryStrategic or Co-development Partner · 13 October 2022Collaboration to evaluate AdAlta's CXCR4 inhibiting i-bodies combined with beta blockers from GPCR's platform for novel cancer therapeutics. AdAlta supplies panel of CXCR4 inhibiting i-bodies; GPCR evaluates in combination with B2AR inhibitors for in vitro and in vivo studies. AdAlta has first option to license resulting products for treating cancer.
• Seoul National UniversitysecondaryStrategic or Co-development Partner · 1 January 2020Academic collaboration with Professor Won-Ki Huh's laboratory for research on GPCR heteromers including CXCR4-B2AR, CXCR4-HRH1, and CXCR4-LPA1 interactions. Multiple joint publications in Nature Scientific Reports, PLOS ONE, Cell Communication and Signaling, and PNAS.

Scale indicators9 records

Recent moves5 records

Expansion highlights6 records

Direct peers

• BioLineRx: Direct competitor in CXCR4 antagonism and stem cell mobilization. BioLineRx's motixafortide (Aphexda) is FDA-approved in combination with G-CSF for autologous stem cell transplantation in multiple myeloma, representing the most direct commercial benchmark to GPCR's GPC-100/burixafor program.
• X4 Pharmaceuticals: CXCR4 antagonist developer with FDA-approved mavorixafor (Xolremdi) for WHIM syndrome. X4 targets overlapping CXCR4 biology with a focus on rare immunology indications, making it directly comparable in mechanism of action and target validation.

Emerging players

• AdAlta Limited: Australian biotech developing CXCR4-targeting i-bodies for cancer and fibrosis. AdAlta is an active collaboration partner of GPCR, evaluating i-body + beta-blocker combinations, making it both a peer and partner in the CXCR4 modality space.
• Magenta Therapeutics: Stem cell mobilization and gene therapy preparation company developing MGTA-456 and related mobilization programs. Although focused on different mobilization approaches, Magenta operates in the same target indication (stem cell mobilization for transplant/gene therapy) as GPCR.
• Bridge Biotherapeutics: Korean clinical-stage biotech developing BBT-877 (autotaxin inhibitor) for IPF. Bridge Biotherapeutics is the licensee of GPCR's CXCR4-LPA1 combination for IPF, making it both a partner and a comparable Korean-listed clinical-stage biotech with respiratory/fibrosis focus.
• Structure Therapeutics: Clinical-stage GPCR-focused biopharmaceutical company developing oral small molecules for metabolic and cardiopulmonary diseases. While focused on different indications, Structure Therapeutics represents a comparable next-generation GPCR drug discovery platform with similar business model and development stage.

Broad incumbents

• Sosei Heptares: Major GPCR-focused biopharmaceutical company with proprietary StaR platform and multiple clinical-stage GPCR-targeted programs. Sosei Heptares represents the largest and most established commercial player in GPCR drug discovery, comparable in underlying science focus though broader in scope.
• Exicure: Clinical-stage biotechnology company that acquired GPCR Therapeutics USA Inc. in January 2025. Now the developer and commercializer of burixafor in the US, Exicure is both the acquirer and a strategic peer operating in the same GPCR-targeted therapeutic space.

Market position

Strengths5 records

Weaknesses4 records

Competitive moat5 records

Key risks5 records

Key highlights6 records

Customer concentration

• LinkedInlinkedin.com/company/gpcr-therapeutics

Compliance1 record

Revenue estimate

Valuation estimate

Number of profiles

Profiles8 records

Subsidiaries1 record

Funding overview

Funding rounds4 records

Investors7 records

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M&A

Investments

M&A and investment is available on the Subscription and Enterprise plan.Contact sales →

Frequently asked questions about GPCR Therapeutics