Drug intelligence / Profile preview

GsMTx4-D

Development stage
Preclinical
Lead developer
University at Buffalo
Modality
Peptides
Administration
Intravenous, Subcutaneous
01

Overview

GsMTx4-D is a modified peptide inhibitor of mechanosensitive ion channels (MSCs), specifically the D-enantiomer of the peptide GsMTx4 originally isolated from the venom of the tarantula Grammostola spatulata. By utilizing D-amino acids, the peptide exhibits improved pharmacodynamics and resistance to proteolysis compared to its L-amino acid counterpart, resulting in a favorable half-life of approximately one week. GsMTx4-D is being investigated for the treatment of Duchenne muscular dystrophy (DMD) and cardiac ischemic reperfusion injury. It works by blocking MSCs that are dysregulated under pathological mechanical stress, thereby reducing muscle mass loss, susceptibility to contraction-induced injury, and cardiac infarct size without affecting normal cardiac output or electrical activity.

Other names
D-GsMTx4D-GsMTx-4D-GsMTx 4GsMTx4 (D-form)
02

Targets

Nav1.1–Nav1.7 (Voltage-gated sodium channel alpha subunits Nav1.1–Nav1.7)AChR (Acetylcholine receptor)KCNMA1 (Calcium-activated potassium channel subfamily M alpha member 1)TMEM120A (Transmembrane protein 120A)TRPC1 (Short transient receptor potential channel 1)PIEZO1 (Piezo-type mechanosensitive ion channel component 1)

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