Chemistry:PRT543
From HandWiki
PRT543 is an experimental anticancer drug which acts as an inhibitor of the enzyme protein arginine methyltransferase 5. This protein is involved in repairs to DNA following damage, so inhibiting it makes cancer cells more susceptible to other chemotherapy drugs. PRT543 is in early stage clinical trials against adenoid cystic carcinoma.[1][2][3][4][5]
References
- ↑ "Protein Arginine Methyltransferase 5 (PRMT5) Inhibitors in Oncology Clinical Trials: A review". Journal of Immunotherapy and Precision Oncology 5 (3): 58–67. August 2022. doi:10.36401/JIPO-22-1. PMID 36034581.
- ↑ "PRMT5 Inhibitors Regulate DNA Damage Repair Pathways in Cancer Cells and Improve Response to PARP Inhibition and Chemotherapies". Cancer Research Communications 3 (11): 2233–2243. November 2023. doi:10.1158/2767-9764.CRC-23-0070. PMID 37861290.
- ↑ "PRT543, a protein arginine methyltransferase 5 inhibitor, in patients with advanced adenoid cystic carcinoma: An open-label, phase I dose-expansion study". Oral Oncology 149. February 2024. doi:10.1016/j.oraloncology.2023.106634. PMID 38118249.
- ↑ "PRMT5 inhibition has a potent anti-tumor activity against adenoid cystic carcinoma of salivary glands". Journal of Experimental & Clinical Cancer Research 44 (1). January 2025. doi:10.1186/s13046-024-03270-x. PMID 39794830.
- ↑ "Phase Ib study of PRT543, an oral protein arginine methyltransferase 5 (PRMT5) inhibitor, in patients with advanced splicing factor-mutant myeloid malignancies". Leukemia 39 (3): 765–769. January 2025. doi:10.1038/s41375-025-02515-8. PMID 39856223.
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