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XNW5004 (igermetostat) is a rationally designed, highly selective and potent small molecule inhibitor of the histone lysine N-methyltransferase EZH2. It inhibits both wild-type and mutant forms of EZH2, leading to suppression of H3K27Me3 levels, cell cycle arrest in G1/S phase, and promotion of apoptosis in tumor cells. The drug is being developed primarily for hematological malignancies such as relapsed or refractory non-Hodgkin lymphoma (including follicular lymphoma and peripheral T-cell lymphomas), as well as a range of solid tumors including prostate cancer, cervical cancer, head and neck squamous cell carcinoma, urothelial carcinoma (bladder), small-cell lung cancer, non-small cell lung cancer, among others. XNW5004 has demonstrated significant anti-tumor efficacy across various tumor types in early clinical trials and shows potential for synergistic effects when combined with AR inhibitors, PARP inhibitors, or anti-PD-1 therapies. The drug is administered orally.
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