Novel reversible XPO1 inhibitor demonstrates potent anticancer activity

Our newest research has been published in Nature Communications:

“Preclinical characterization of a reversible XPO1 inhibitor for cancer therapy”

Exportin 1 (XPO1) is a clinically validated anticancer target that plays a key role in transporting proteins from the nucleus to the cytoplasm. Inhibiting XPO1 can trigger cancer cell death, but currently available inhibitors are often associated with toxicity.
In this study, we describe FR-027, a novel reversible XPO1 inhibitor with a distinct mechanism of action. Unlike currently used clinical-stage XPO1 inhibitors, FR-027 does not promote XPO1 degradation while maintaining potent anticancer activity across multiple cancer models. Importantly, FR-027 delayed disease progression and improved survival in preclinical models, including intracranial tumor models, while showing an improved safety profile in mice.
 
These findings highlight the potential of reversible XPO1 inhibition as a next-generation therapeutic strategy and support the further clinical development of FR-027 for the treatment of cancers with high unmet medical need. 

Congratulations to Janne Van Hauwenhuyse and all co-authors on this achievement!
 
Read the full paper here: https://www.nature.com/articles/s41467-026-75741-y

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