GR-2397

GR-2397 is the first of a new class of small molecule antifungal agents being developed for the treatment of serious fungal infections. GR-2397 is differentiated by its novel mechanism of action that confers rapid fungicidal activity, activity against difficult-to-treat resistant fungal pathogens, including azole-resistant strains, and its highly favorable clinical pharmacology profile, including a low propensity for CYP 450 related DDIs.

Structurally, GR-2397 resembles ferrichrome, an iron-chelating siderophore. These molecules are used by fungi to acquire iron from the environment, which is necessary for survival. However, GR-2397 is a unique cyclic hexapeptide with a chelated aluminum ion. Fungi take up GR-2397 using the iron-transporter Sit1, resulting in significant intracellular accumulation. Human cells lack this transporter and cannot take up GR-2397, resulting in a low propensity for human toxicity.

Gravitas plans to initially develop GR-2397 for a Limited Use Indication (LUI) under LPAD for the treatment of invasive aspergillosis. The FDA granted Orphan Drug, Qualified Infectious Disease Product (QIDP) and Fast Track designations to GR-2397 for the treatment of invasive aspergillosis. GR-2397's IND remains active with the FDA.