Drug intelligence / Profile preview

LNP7457

Development stage
Unknown
Lead developer
Lupin
Modality
Small Molecules
Administration
Oral
01

Overview

LNP7457 is an investigational small molecule drug developed by Lupin Limited that acts as a SAM-competitive inhibitor of PRMT5 (Protein Arginine Methyltransferase 5). PRMT5 is an enzyme involved in epigenetic regulation and cancer cell proliferation. By competitively inhibiting the binding of S-adenosylmethionine (SAM) to PRMT5, LNP7457 disrupts cancer cell growth and survival, particularly targeting tumors with MTAP deletions which are common in certain solid tumors such as pancreatic ductal adenocarcinoma. The drug has demonstrated a favorable safety profile and pharmacokinetics in Phase 1a clinical trials involving patients with advanced or metastatic solid tumors. It shows no significant dose-limiting toxicities at doses up to 2 mg daily, exhibits food-independent pharmacokinetics, and reduces plasma symmetric dimethylarginine (SDMA), a biomarker for PRMT5 inhibition. Lupin is advancing LNP7457 into Phase 1b trials focusing on difficult-to-treat cancers with unmet medical needs.

Other names
LNP-7457LNP7457LNP 7457
02

Targets

PRMT5 (Protein arginine N-methyltransferase 5)

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