PRMT5 inhibitors, global pipeline

Last Update: Aug 15, 2022

Company Candidate MoA Indication Phase
Janssen JNJ-646191781 SAM competitive AND peptide competitive NHL, MDS I
Prelude Therapeutics PRT811 Brain-penetrant SAM competitive GBM, CNS lymphoma, CNS metastases I
Prelude Therapeutics PRT543 SAM competitive ACC, HRD+ tumors (BRCA1/2) Myelofibrosis, MDS I
Tango Therapeutics TNG908 MTA cooperative inhibitor MTAP-deleted cancers I
Mirati MRTX9768 PRMT5-MTA complex inhibitor, MTA competitive MTAP-deleted cancers I/Ib
Amgen AMG 1934 MTA cooperative inhibitor MTAP-deleted solid tumors +- docetaxel I
Eli Lilly LLY-283 Brain-penetrant SAM competitive Gliomas Preclin
Jubilant Therapeutics JBI-778 Brain-penetrant peptide competitive Glioblastoma, Brain metastases Preclin
GSK GSK33265952 Peptide competitive MDS, AML, Advanced solid tumors (ACC) I
Pfizer PF-069399993 SAM competitive NSCLC, HNSCC, esophageal, endometrial, cervical, bladder I
GSK GSK3368715 SAM uncompetitive - 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. GSK33265952: Phase I results here. Program discontinued in Q122.
3. PF-06939999: Initial results here. Discontinued in Q122.
4. AMG 193 - Ph1 (NCT05094336) initiated Feb 1 2022. Also in clinical evaluation with IDYA's MAT2A inhibitor, IDE397.

NHL = Non-Hodgkins lymphoma. MDS = Myelodysplastic syndromes. GBM = Glioblastoma multiforme. ACC = Adenoid cystic carcinoma. AML = Acute myeloid leukemia. NSCLC = Non-small cell lung cancer. HNSCC = Head and neck squamous cell carcinoma.

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