PRT543

PRT543
Identifiers
	IUPAC name (2R,3R,4S,5R)-2-(4-aminopyrrolo[2,3-d]pyrimidin-7-yl)-5-[(R)-(4-chlorophenyl)-hydroxymethyl]oxolane-3,4-diol;
CAS Number	1989620-03-2;
PubChem CID	122497020;
ChemSpider	128941842;
ChEMBL	ChEMBL4585781;
Chemical and physical data
Formula	C17H17ClN4O4
Molar mass	376.80 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1=CC(=CC=C1[C@H]([C@@H]2[C@H]([C@H]([C@@H](O2)N3C=CC4=C(N=CN=C43)N)O)O)O)Cl;
	InChI InChI=1S/C17H17ClN4O4/c18-9-3-1-8(2-4-9)11(23)14-12(24)13(25)17(26-14)22-6-5-10-15(19)20-7-21-16(10)22/h1-7,11-14,17,23-25H,(H2,19,20,21)/t11-,12+,13-,14-,17-/m1/s1; Key:ITEKIFMGFZAFPM-QFRSUPTLSA-N;

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

↑ Feustel K, Falchook GS (August 2022). "Protein Arginine Methyltransferase 5 (PRMT5) Inhibitors in Oncology Clinical Trials: A review". Journal of Immunotherapy and Precision Oncology. 5 (3): 58–67. doi:10.36401/JIPO-22-1. PMC 9390703. PMID 36034581.
↑ Carter J, Hulse M, Sivakumar M, Burtell J, Thodima V, Wang M, et al. (November 2023). "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. doi:10.1158/2767-9764.CRC-23-0070. PMC 10627093. PMID 37861290.
↑ Ferrarotto R, Swiecicki PL, Zandberg DP, Baiocchi RA, Wesolowski R, Rodriguez CP, et al. (February 2024). "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 106634. doi:10.1016/j.oraloncology.2023.106634. PMID 38118249.
↑ Mishra V, Singh A, Korzinkin M, Cheng X, Wing C, Sarkisova V, et al. (January 2025). "PRMT5 inhibition has a potent anti-tumor activity against adenoid cystic carcinoma of salivary glands". Journal of Experimental & Clinical Cancer Research. 44 (1) 11. doi:10.1186/s13046-024-03270-x. PMC 11724466. PMID 39794830.
↑ Bewersdorf JP, Mi X, Lu B, Kuykendall A, Sallman D, Patel M, et al. (January 2025). "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. doi:10.1038/s41375-025-02515-8. PMC 11879867. PMID 39856223.

[1] Feustel K, Falchook GS (August 2022). "Protein Arginine Methyltransferase 5 (PRMT5) Inhibitors in Oncology Clinical Trials: A review". Journal of Immunotherapy and Precision Oncology. 5 (3): 58–67. doi:10.36401/JIPO-22-1. PMC 9390703. PMID 36034581.

[2] Carter J, Hulse M, Sivakumar M, Burtell J, Thodima V, Wang M, et al. (November 2023). "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. doi:10.1158/2767-9764.CRC-23-0070. PMC 10627093. PMID 37861290.

[3] Ferrarotto R, Swiecicki PL, Zandberg DP, Baiocchi RA, Wesolowski R, Rodriguez CP, et al. (February 2024). "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 106634. doi:10.1016/j.oraloncology.2023.106634. PMID 38118249.

[4] Mishra V, Singh A, Korzinkin M, Cheng X, Wing C, Sarkisova V, et al. (January 2025). "PRMT5 inhibition has a potent anti-tumor activity against adenoid cystic carcinoma of salivary glands". Journal of Experimental & Clinical Cancer Research. 44 (1) 11. doi:10.1186/s13046-024-03270-x. PMC 11724466. PMID 39794830.

[5] Bewersdorf JP, Mi X, Lu B, Kuykendall A, Sallman D, Patel M, et al. (January 2025). "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. doi:10.1038/s41375-025-02515-8. PMC 11879867. PMID 39856223.

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PRT543

References