Drug intelligence / Profile preview

GsMTx4

Development stage
Preclinical
Lead developer
Akashi Therapeutics
Modality
Peptides
Administration
Intravenous, Intramuscular (preclinical/investigational)
01

Overview

GsMTx4 is a **peptide toxin** originally found in the venom of the tarantula Grammostola spatulata. It is a member of the inhibitory cysteine knot (ICK) peptide family and is a gating modifier of mechanosensitive ion channels, with a unique structural motif enabling high potency for inhibiting mechanosensitive cation channels. GsMTx4 inhibits a range of mechanosensitive cationic channels, including Piezo1, Piezo2, and members of the TRP channel family (such as TRPC1 and TRPC6). Unlike most drugs, its inhibition is not stereospecific—both L- and D- forms are active, suggesting a membrane-mediated mechanism of action. It has demonstrated protective effects in preclinical models of muscular dystrophy and cardiac arrhythmias, and shows promise in conditions such as Duchenne muscular dystrophy, atrial fibrillation, mechanical pain, and possibly neurodegenerative diseases and osteoarthritis. GsMTx4 is not currently approved for human therapeutic use but is being developed as an investigational agent and research tool[1][3][4][5][6][7][10].

Other names
GsMTx4GsMTx-4GsMTx 4
02

Targets

PIEZO1 (Piezo-type mechanosensitive ion channel component 1)TRPC1 (Short transient receptor potential channel 1)sAC (Soluble adenylyl cyclase)PIEZO2 (Piezo2 mechanosensitive channel)

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