Linvemastat

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Linvemastat

CAS 2389060-50-6

MF C20H17N3O4S MW395.43

5-[3-[4-[(2-methyl-4-pyridinyl)methoxy]phenyl]sulfanylfuran-2-yl]imidazolidine-2,4-dione

matrix metalloproteinase-12 inhibitor, lung diseases, FP 020, FP2AMM4SVF

Linvemastat (also known by its developmental code FP-020) is an investigational, orally active small-molecule drug designed to selectively inhibit matrix metalloproteinase-12 (MMP-12). It is being developed as a potential disease-modifying therapy for chronic inflammatory and fibrotic diseases, primarily targeting respiratory conditions and gastrointestinal disorders.

How Linvemastat Works

Targeting MMP-12: MMP-12 is an enzyme secreted by macrophages that breaks down extracellular matrix proteins like elastin.
Controlling Damage: Overexpression of MMP-12 is strongly linked to tissue destruction, chronic inflammation, and fibrosis in the lungs and gut.
High Selectivity: Unlike older matrix metalloproteinase inhibitors, linvemastat targets MMP-12 with high specificity, avoiding off-target interactions with other vital MMP enzymes.

Primary Therapeutic Indications under Research

Severe, Uncontrolled Asthma: Evaluated to reduce airway inflammation and improve overall lung function.
Chronic Obstructive Pulmonary Disease (COPD): Investigated for preventing structural lung damage and progressive emphysema.
Inflammatory Bowel Disease (IBD): Researched to minimize continuous gut wall inflammation and intestinal fibrosis.
Other Fibrotic Conditions: Explored in preclinical models for conditions like idiopathic pulmonary fibrosis (IPF) and kidney damage.

Current Clinical Status

Initially developed by Foresee Pharmaceuticals, global development rights for the program were transitioned to Primevera Therapeutics LLC.

Phase 1 Trial: Completed trials in healthy volunteers demonstrated a favorable safety and pharmacokinetic profile, with only minor, recoverable side effects like mild nausea or headache.
Phase 2 Trial: Undergoing mid-stage clinical evaluation, such as the global, randomized syMMPonia study. This trial is measuring changes in forced expiratory volume (FEV₁) to assess the drug’s impact on adults with partially controlled, moderate-to-severe asthma.

Effect of Linvemastat in Patients With Partially Controlled Asthma (syMMPonia)

CTID: NCT07191535

Phase: Phase 2

Status: Not yet recruiting

Date: 2025-10-20

SYN

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2019222157&_cid=P10-MQOLFP-71317-1