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SEOUL, Korea and REDWOOD CITY, Calif., Dec. 14, 2023 (GLOBE NEWSWIRE) -- GPCR Therapeutics, Inc., a clinical-stage international biopharmaceutical company, announces it enters into an out-licensing agreement with Bridge Biotherapeutics (KQ288330) for the CXCR4-LPA1 inhibitor combination method of treatment. GPCR receives an upfront payment of KRW 2 billion (approx. USD 1.5 million), and a 50:50 profit-share on future commercialization, including sub-licenses. In collaboration with Bridge Biotherapeutics, GPCR will pursue joint development and commercialization of the combination therapy. Conducting a multinational phase 2a clinical trial of BBT-877, an autotaxin inhibitor for the treatment of IPF, Bridge Biotherapeutics has been accelerating development of its proprietary IPF pipeline. Last September, GPCR published the paper on the direct interaction between two different GPCRs, CXCR4 and LPA1, in the peer-reviewed academic journal ‘Cell Communication and Signaling’(1). The target GPCRs are known to promote fibrotic diseases such as idiopathic pulmonary fibrosis (IPF). Through various in vitro experiments, the company found that the efficacy of LPA1 inhibition can be further maximized by inhibition of CXCR4, thereby securing a scientific basis that the CXCR4- LPA1 inhibitor combination may be necessary for full anti-fibrotic activity. Based on this finding, GPCR filed a provisional patent application on the CXCR4-LPA1 inhibitor combination method of treatment. Dr. Dong Seung Seen, founder and CEO of GPCR Therapeutics, commented, “Since the publication of our paper, various global companies have expressed interest in the relationship between LPA1 and CXCR4 and its inhibitory effect. Due to the versatility of our patent, we look forward to collaborating with many IPF-targeting companies, starting with Bridge Biotherapeutics.” James Lee, founder and CEO of Bridge Biotherapeutics, said, “We are encouraged to collaborate with GPCR Therapeutics to uncover new possibilities of IPF treatment. Our collaboration will help us move forward to identifying and bringing novel treatment of IPF, such as a combination therapy of LPA1 and CXCR4 inhibitor, based on GPCR’s latest research.” IPF is a progressive chronic lung condition that causes scarring (fibrosis) of a patients’ lungs which makes breathing increasingly difficult as the lungs become stiffer and lose their elasticity. The lungs become less efficient at transferring oxygen so that when someone with IPF breathes in, the transfer of oxygen through air sacs in their lungs and into their blood stream is impaired. Lung damage from IPF is irreversible, and there is currently no treatment that stops or reverses the scarring. In the US there are around 495 cases per 100,000 people, with median survival estimated at 2–5 years from the time of diagnosis. (2) (3) References (1) Cell Communication and Signaling paper, “LPA1-mediated inhibition of CXCR4 attenuates CXCL12-induced signaling and cell migration”: (2) American Lung Association data on IPF: (3) PubMed paper on incidence and prevalence of IPF: About GPCR Therapeutics GPCR Therapeutics, Inc. is a clinical-stage international biopharmaceutical company with an innovative approach to developing therapeutics built on its proprietary GPCR data. The company’s lead small molecule asset, GPC-100/Burixafor, targets CXCR4, one of the most prevalent chemokine GPCRs overexpressed in various cancers. The company has an ongoing US Phase 2 clinical trial assessing the efficacy of the combination of GPC-100 and propranolol in patients with multiple myeloma. In addition, the company is engaged in active collaborations with domestic and international biotechnology companies. By targeting the unique pharmacology of GPCR pairs, the company aims to develop life-changing treatments for cancer and other diseases. The company has identified that CXCR4 interacts with the beta-2 adrenergic receptor (B2AR), and this GPCR pair presents an alternate signaling pathway that is synergistically dependent on CXCR4 and B2AR activation. GPCR Therapeutics has its HQ in Seoul, Korea with additional R&D facilities in the San Francisco Bay Area, USA. For more information, visit gpcr.co.kr and follow us on LinkedIn. For more information, please contact: GPCR Therapeutics (in Seoul) DaYoon Kim - Business Development Manager Tel: +82-2-878-2848 dayoon.kim@gpcr.co.kr Scius Communications (in London): Katja Stout - Founder & Managing Partner +44 778 943 5990 katja@sciuscommunications.com Daniel Gooch - Partner +44 774 787 5479 daniel@sciuscommunications.com About Bridge Biotherapeutics, Inc. Bridge Biotherapeutics Inc., based in the Republic of Korea and the U.S., is a publicly traded, clinical-stage biotech company founded in 2015. Bridge Biotherapeutics is engaged in the discovery and development of novel therapeutics, focusing on therapeutic areas with high unmet needs, including fibrotic diseases and cancers. The company is developing BBT-877, a novel autotaxin inhibitor for the treatment of fibrotic diseases including idiopathic pulmonary fibrosis (IPF), and BBT-207, a potent targeted cancer therapy for non-small cell lung cancer (NSCLC) with EGFR C797S mutations. Learn more at

Paper in PLOS ONE Reinforces Potential for Combination Therapy in Hematological MalignanciesSEOUL, Korea and REDWOOD CITY, Calif., Oct. 26, 2023 (GLOBE NEWSWIRE) -- GPCR Therapeutics, Inc., a clinical stage international biopharmaceutical company with an innovative approach to developing cancer therapeutics based on targeting G Protein Coupled Receptors (GPCR) pairs, announces publication of a research paper in PLOS ONE. The paper shows that the company’s lead small molecule asset, GPC-100, a novel CXCR4 antagonist and a potent hematopoietic stem cell (HSC) mobilizer, when combined with the beta-adrenergic receptor blocker propranolol, results in a significant increase in circulating HSCs in mice. These findings strongly support the use of this combination for peripheral blood HSC harvest in autologous stem cell transplant treatment in hematological cancers. The paper, authored in collaboration with Seoul National University’s School of Biological Sciences and Institute of Microbiology, is entitled, “GPC-100, a novel CXCR4 antagonist, improves in vivo hematopoietic cell mobilization when combined with propranolol” (1). The authors highlight that GPC-100 alone shows greater mobilization efficacy than a drug already approved for stem cell mobilization. Importantly, when combined with propranolol, GPC-100-induced HSC mobilization increases by another 2-fold. The mobilization efficiency by GPC-100 plus propranolol is similar to that of the standard of care treatment with granulocyte-colony stimulating factor (G-CSF). Together, this study suggests a strategy with a potential to mobilize sufficient HSC without the use of G-CSF, and thereby reduce the risk of G-CSF associated moderate to severe side effects such as severe bone pain. This also provides a better stem cell transplant treatment option for cancer patients with autoimmune diseases which may be exacerbated by G-CSF or sickle cell disease, where it is contraindicated. Finally, the paper supports that the triple combination of GPC-100 plus propranolol and G-CSF mobilizes a greater number of HSCs compared to the standards of care and is predicted to be a best-in-class mobilizer. Dr. Dong Seung Seen, GPCR Therapeutics’ founder and CEO, commented, “This latest high-quality paper, produced in close collaboration between our Korean and US sites, together with Seoul National University, shines a spotlight on the potential for our lead asset, GPC-100, to be used with propranolol as a combination therapy for hematological malignancies, including multiple myeloma. Our discovery of this powerful functional relationship provides new hope in this notoriously hard to treat cancer.” Hematological malignancies, such as multiple myeloma, are hard to treat. Increasingly, clinicians are using Autologous Stem Cell Transplant (ASCT) to treat patients, which has improved the anti-cancer response and survival compared to conventional chemotherapy. However, for ASCT to work well, hematopoietic stem cells, especially CD34+ cells, need to be successfully mobilized out of the patient’s bone marrow and into their peripheral blood, where the cells are more easily collected, and can then be stored for later transplantation. A key limiting factor is that mobilization is often inadequate, and insufficient cells are harvested for use in the patient’s treatment. This paper reports on how this common treatment limitation could be overcome through use of a combination of GPC-100 and propranolol. As announced on 17 January 2023, the company has initiated a phase 2 trial in the US for GPC-100, which targets CXCR4, one of the most prevalent chemokine GPCRs over-expressed in more than 23 cancers. This randomized, open-label phase 2 study assesses the efficacy of GPC-100 and propranolol, with and without G-CSF, for the mobilization of stem cells in patients with multiple myeloma undergoing ASCT. The paper announced today supports this clinical trial. References (1) https://journals.plos.org/plosone/article?id=10.1371/journal.pone.0287863 ※ More than 35% of FDA approved drugs are GPCRs. Still, GPCRs’ complex pharmacology arising from their interactions with other GPCRs presents unique opportunities for drug development. About GPCR Therapeutics GPCR Therapeutics, Inc. is a clinical stage international biopharmaceutical company with an innovative approach to developing therapeutics built on its proprietary GPCR data. The company’s lead small molecule asset, GPC-100/Burixafor, targets CXCR4, one of the most prevalent chemokine GPCRs overexpressed in various cancers. The company has recently initiated a US Phase 2 clinical trial assessing the efficacy of the combination of GPC-100 and propranolol in patients with multiple myeloma. In addition, the company is engaged in active collaborations with domestic and international biotechnology companies. By targeting the unique pharmacology of GPCR pairs, the company aims to develop life changing treatments for cancer and other diseases. The company has identified that CXCR4 interacts with the beta-2 adrenergic receptor (B2AR), and this GPCR pair presents an alternate signaling pathway that is synergistically dependent on CXCR4 and B2AR activation. GPCR Therapeutics has its HQ in Seoul, Korea with additional R&D facilities in the San Francisco Bay Area, USA. For more information, visit gpcr.co.kr and follow us on LinkedIn. For more information, please contact: GPCR Therapeutics (in Seoul)DaYoon Kim - Business Development ManagerTel: +82-2-878-2848dayoon.kim@gpcr.co.kr