Linking receptor occupancy with the efficacy of CXCR4 antagonists

An in vitro assay measures CXCR4 receptor occupancy in human cells to determine therapeutic efficacy, addressing the challenge of assessing anti-CXCR4 polypeptides' effectiveness by linking migration inhibition to in vivo outcomes, demonstrating that low RO levels can significantly inhibit cell migration.

JP2026524908APending Publication Date: 2026-07-24ADALTA
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Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
ADALTA
Filing Date
2024-07-05
Publication Date
2026-07-24

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Abstract

This disclosure is based on a novel assay that links the degree of CXCR4 receptor occupancy (RO) by anti-CXCR4 polypeptides to the efficacy of anti-CXCR4 polypeptides, based on the determination of SDF-1α-induced migration of primary human CXCR4 cells in the presence of anti-CXCR4 polypeptides. Inhibition of migration, measured by the in vitro assay, provides a surrogate for the in vivo efficacy of anti-CXCR4 polypeptides.
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