Drug intelligence / Profile preview

Linebacker-1

Development stage
Preclinical
Lead developer
ProPhase BioPharma
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral (anticipated Based On Small Molecule Class; Specific Route Not Explicitly Stated)
01

Overview

Linebacker-1 is a small molecule multi-kinase inhibitor developed as a modified polyphenol based on myricetin, a plant-derived flavonoid. Specifically, it is mono-chlorinated myricetin with a chlorine atom substituted for the hydroxy group at position 5 on the B-ring. The drug is designed to act as both a monotherapy and co-therapy for hard-to-treat cancers such as lung and colon cancer. Preclinical studies have shown that Linebacker-1 inhibits multiple cancer-relevant kinases—most notably members of the phosphoinositide 3-kinase family (e.g., PIKfyve, PIP5k1/2), mitogen-activated protein kinase family (e.g., MEK3/4/5), and down-regulates PIM kinase (proviral integration site for Moloney murine leukemia virus), which plays an oncogenic role in solid tumors. The compound has also demonstrated potential applications in inflammatory diseases and neurological disorders due to its anti-inflammatory and neuroprotective properties[1][2][4][5][6][8].

Brand names
Linebacker-1Linebacker1Linebacker 1
Other names
LB-1LB1LB 1Mono-chlorinated Myricetin
02

Targets

PI3K (Phosphoinositide-3-kinase regulatory subunit 6)MEKPIM3 (Proviral integration site for Moloney murine leukemia virus kinase 3)

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