RPT04402 is a first-in-class molecular glue that selectively targets specific PP2A complexes to restore their tumor-suppressing function. Preclinical studies have demonstrated that activating PP2A can suppress oncogenic signaling pathways, potentially slowing or reversing prostate cancer progression. This approach offers a novel mechanism to address the limitations of current therapies, particularly in treatment-resistant forms of prostate cancer.

Protein Phosphatase 2A (PP2A) is a tumor suppressor enzyme that regulates protein dephosphorylation, playing a crucial role in controlling cell growth and division. In prostate cancer, PP2A activity is often diminished, leading to unchecked cellular proliferation and tumor progression. Reactivating PP2A has emerged as a promising therapeutic strategy to inhibit cancer cell growth and enhance the effectiveness of existing treatments.

An Investigational New Drug (IND) application will be filed by the end of 2025, aiming to bring this innovative therapy into clinical trials.

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