GPCR Therapeutics Demonstrates Clinical Improvement in Mobilization of Hematopoietic Stem Cells Using GPC-100/Burixafor in Clinical Pharmacology in Drug Development
Seoul, Korea, & Redwood City, California, 15 August 2023 – GPCR Therapeutics, Inc., a clinical stage, international biopharmaceutical company with an innovative approach to drug discovery based on targeting G Protein Coupled Receptors (GPCR) pairs, announced today publication of their paper in Clinical Pharmacology in Drug Development (1), in collaboration with Taiwan’s TaiGen Biotechnology Co. Ltd. The paper is entitled, “Pharmacokinetics and Pharmacodynamics of Burixafor Hydrobromide (GPC-100), a Novel C-X-C Chemokine Receptor 4 Antagonist and Mobilizer of Hematopoietic Stem/Progenitor Cells, in Mice and Healthy Subjects.” The results demonstrate that the company’s lead small molecule asset, GPC-100/burixafor, is generally safe and well tolerated. PK profile and marked increase of peripheral CD34+ cells after GPC-100 administration support further clinical development of GPC-100 for mobilization of hematopoietic stem/progenitor cells.
Adequate mobilization of hematopoietic stem cells (HSC), especially CD34+ cells, is necessary for stem cell transplantation in patients with hematological malignancies. GPC-100 is an inhibitor of the C-X-C chemokine receptor 4 (CXCR4) that disrupts the CXCL12/CXCR4 axis in the bone marrow releasing HSCs into circulation. Going further from mice studies, GPC-100 was administered intravenously to 64 healthy subjects in a randomized, double-blind, placebo-controlled single ascending dose study (0.10 to 4.40 mg/kg in eight cohorts) to evaluate safety, pharmacokinetics, and pharmacodynamics. As expected, white blood cells, CD133+ and CD 34+ cell concentrations generally increased with the increases in GPC-100 dose from 0.10 to 3.14 mg/kg. At maximal levels, the CD34+ cell counts increased 3- to 14-fold from baseline levels.
Dr. Dong Seung Seen, GPCR Therapeutics’ founder and CEO, commented, “Following on from our paper in March in Nature Scientific Reports, this paper is crucial as it represents yet another case for our drug development program to be peer-reviewed and validated in academia. This paper provides strong scientific evidence that GPC-100 is an excellent molecule to be used in our combination treatment program for better patient outcomes that any CXCR4 inhibitor cannot achieve alone.”
GPCR Therapeutics, Inc. is developing a diverse pipeline targeting CXCR4, one of the most prevalent chemokine GPCRs overexpressed in more than 23 cancers. The company has demonstrated more potent effect of CXCR4 inhibitors when administered in combination with other GPCR inhibitors than when given alone. A Phase 2 clinical trial of the combination of the CXCR4 inhibitor GPC-100 and the ADRB2 inhibitor propranolol is currently underway in the United States.
References
(1) https://accp1.onlinelibrary.wiley.com/doi/10.1002/cpdd.1302
