Brilacidin

Brilacidin (PMX-30063) is a synthetic small-molecule defensin-mimetic (MW ~564 g/mol) developed by Innovation Pharmaceuticals (formerly Cellceutix). It is a peptidomimetic, not a true peptide, designed to mimic the amphipathic structure and antimicrobial mechanism of host defense peptides (defensins). Brilacidin has been investigated in Phase II clinical trials for acute bacterial skin and skin structure infections (ABSSSI) and oral mucositis, and was explored for COVID-19.

Category: Antimicrobial / Immune. Evidence rating: C (early/mixed human evidence).

Clinical status: Phase II completed for ABSSSI (positive results). Phase II for oral mucositis. Investigated for COVID-19 (in vitro). No Phase III initiated.

Brilacidin is an arylamide foldamer that mimics the cationic amphipathic structure of natural defensins. Like defensins, it disrupts bacterial membranes through electrostatic interaction with anionic membrane components, but as a small molecule it has superior pharmacokinetic properties to…

Safety considerations: Phase II ABSSSI trial reported brilacidin was generally well-tolerated; Infusion-related reactions observed with IV administration; Elevated creatine phosphokinase levels reported in some subjects.

Reviewed by the PeptideAtlas Editorial Team.

Brilacidin — measured properties

Molecular weight~564 g/mol
Production methodsynthetic
Anti-doping statusnot-listed
US regulatory statusNot FDA-approved. Phase II completed for ABSSSI. No Phase III initiated. Classified as investigational new drug.

Related peptides: LL-37, Beta-Defensins, Alpha-Defensins.

Compare: Brilacidin vs LL-37.

Frequently asked questions

Is brilacidin a peptide?

No. Brilacidin is a peptidomimetic — a synthetic small molecule designed to mimic the structure and function of natural defensin peptides. It has advantages over true peptides including oral bioavailability potential, protease resistance, and more favorable pharmacokinetics.

Why has brilacidin not advanced to Phase III?

Despite positive Phase II results for ABSSSI, the developer (Innovation Pharmaceuticals, a small company) has faced challenges securing funding and partnerships for the costly Phase III trials required for FDA approval.

Can brilacidin treat COVID-19?

Brilacidin showed in vitro activity against SARS-CoV-2, but no clinical trial for COVID-19 was completed. In vitro antiviral activity does not necessarily translate to clinical efficacy.