GP01CR01

GP01CR01 is a controlled-release, fixed-dose combination of the CXCR4 antagonist burixafor and the non-selective beta-blocker propranolol. Developed by GPCR Therapeutics, this therapeutic candidate is designed to target the CXCR4-ADRB2 heteromer, a molecular complex discovered by the company to play a critical role in cancer cell survival, metastasis, and resistance to standard treatments. By simultaneously inhibiting the C-X-C chemokine receptor type 4 (CXCR4) and the beta-2 adrenergic receptor (ADRB2), GP01CR01 aims to disrupt oncogenic signaling more effectively than monotherapy. The drug is currently in IND-enabling development for the treatment of various solid tumors—including breast, lung, and brain cancers—as well as hematologic malignancies.