Drug intelligence / Profile preview

JBI-778

Development stage
Phase 2
Lead developer
Jubilant Therapeutics
Modality
Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

JBI-778 is an oral, brain-penetrant small molecule inhibitor of protein arginine methyltransferase 5 (PRMT5), developed by Jubilant Therapeutics. It is a substrate-competitive and S-adenosylmethionine (SAM)-cooperative PRMT5 inhibitor designed to address both systemic and central nervous system tumors, including those with specific genetic signatures such as MTAP deletions. The drug demonstrates potent anti-proliferative activity in preclinical models across several cancer types, including glioblastoma and mantle cell lymphoma. Its unique pharmacological profile enables balanced exposure in the brain and plasma, facilitating treatment of primary brain tumors (such as glioblastoma) and CNS metastases alongside systemic disease. JBI-778 has received orphan drug designation for glioblastoma from the FDA and is currently being evaluated in Phase I clinical trials for solid tumors with a focus on high-grade gliomas, EGFR mutation lung cancer with brain metastases, and other advanced cancers[2][4][5][6][8].

02

Targets

PRMT5 (Protein arginine N-methyltransferase 5)

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