GPCR Therapeutics Announces Publication on Improving Hematopoietic Stem Cell Mobilization Using Propranolol with GPC-100

Paper in PLOS ONE Reinforces Potential for Combination Therapy in Hematological Malignancies

SEOUL, 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.



※ 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 and follow us on LinkedIn.

For more information, please contact:

GPCR Therapeutics (in Seoul)
DaYoon Kim - Business Development Manager
Tel: +82-2-878-2848