PRMT5 inhibitors, global pipeline

Last Update: Aug 16, 2021

Company Candidate MoA Indication Phase
GSK GSK3326595 Peptide competitive MDS, AML, Advanced solid tumors (ACC) I/II
Janssen JNJ-646191781 SAM competitive AND peptide competitive NHL, MDS I
Pfizer PF-069399992 SAM competitive NSCLC, HNSCC, esophageal, endometrial, cervical, bladder I
Prelude Therapeutics PRT543 SAM competitive ACC, HRD+ tumors (BRCA1/2) Myelofibrosis, MDS I
Prelude Therapeutics PRT811 Brain-penetrant SAM competitive GBM, CNS lymphoma, CNS metastases I
Eli Lilly LLY-283 Brain-penetrant SAM competitive Gliomas Preclin
Jubilant Therapeutics JBI-778 Brain-penetrant peptide competitive Glioblastoma, Brain metastases, MCL Preclin
Tango Therapeutics TNG908 MTA cooperative inhibitor MTAP-deleted cancers Preclin
Mirati MRTX9768 PRMT5-MTA complex inhibitor, MTA competitive MTAP-deleted cancers Preclin
1. Phase I results here. Binds simultaneously to the SAM- and protein substrate- binding pockets of the PRMT5/MEP50 complex with a pseudo-irreversible mode-of-action.
2. Initial results here.

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