GPCR Therapeutics Expands Pipeline into Fibrosis with a Combination Approach Targeting LPA1
Seoul, Korea, & Redwood City, California, 10 October 2023 – GPCR Therapeutics, Inc., a clinical-stage, international biopharmaceutical company, announced today the expansion of its pipeline into fibrosis with the publication of a paper in Cell Communication and Signaling. The paper, authored in collaboration with Seoul National University’s School of Biological Sciences and Institute of Microbiology, supports the need to fully inhibit two signaling receptors, lysophosphatidic acid receptor 1 (LPA1) and CXCR4, for the effective treatment of Idiopathic Pulmonary Fibrosis (IPF).
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. (1) (2)
LPA1 and CXCR4 are among the few targets for which IPF therapeutics are being clinically developed respectively. However, this research shows that an IPF therapeutic approach based on inhibiting only LPA1 is likely to be insufficient, as CXCR4, which has been repressed by LPA1, will be activated and induce aberrant cell signaling. The paper “LPA1-mediated inhibition of CXCR4 attenuates CXCL12-induced signaling and cell migration” reports that complete inhibition of cell migration was only achieved in the presence of both CXCR4 and LPA1 antagonists. (3)
GPCR Therapeutics, Inc. is developing a diverse pipeline targeting both CXCR4, one of the most prevalent chemokine GPCRs overexpressed in more than 23 cancers, and other GPCRs that promote or inhibit CXCR4. The company’s lead pipeline targets CXCR4 and B2AR (beta-2 adrenergic receptor) in cancer and is currently undergoing a phase 2 clinical trial. Based in part on the research announced today, the company has expanded its portfolio and begun developing a pipeline targeting CXCR4 and LPA1 in fibrosis.
Dr. Pina Cardarelli, GPCR’s CSO and President of US operations, commented, “This paper showcases the high quality of the research into understanding the pathological role of GPCRs in cancer and inflammatory diseases. It is another example of the potential of our CXCR4-GPCR pairs approach, where several novel valuable mechanisms can be discovered. We are very eager to leverage our combination approach and explore the field of fibrosis.”
GPCR recently launched a US phase 2 trial of GPC-100 in combination with Propranolol for stem cell mobilization in patients with multiple myeloma.
References
(1) https://www.lung.org/lung-health-diseases/lung-disease-lookup/idiopathic-pulmonary-fibrosis
(2) https://pubmed.ncbi.nlm.nih.gov/27126689/
(3) https://biosignaling.biomedcentral.com/articles/10.1186/s12964-023-01261-7
About GPCR Therapeutics
GPCR Therapeutics, Inc. is a clinical-stage international biopharmaceutical company with an innovative approach to developing therapeutics built on its proprietary G Protein Coupled Receptors (GPCR) data. The company’s proprietary data-driven approach has identified over 1,000 GPCR pairs upon which drug screening campaigns can be pursued. Identifying the best GPCR pair to target for specific disease indications and patient subpopulations creates a precision approach to combination therapy. By targeting the unique pharmacology of GPCR pairs, the company aims to develop life-changing treatments for cancer and other diseases.
GPCR Therapeutics is developing multiple programs with the aim of advancing therapies for hematological malignancies as well as solid tumors. 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 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. Furthermore, the company has identified LPA1 as a CXCR4 interactor that represses CXCR4 activity.
The company has recently initiated a US Phase 2 clinical trial assessing the efficacy of the combination of GPC-100 and Propranolol in autologous stem cell transplant in patients with multiple myeloma. In addition, the company is engaged in active collaborations with domestic and international biotechnology companies, including Australia’s AdAlta.
GPCR Therapeutics is headquartered 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.
