Drug intelligence / Profile preview

GR-2397

Development stage
Discontinued
Lead developer
Basilea Pharmaceutica
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules, Peptides
Administration
Intravenous
01

Overview

GR-2397 is a first-in-class antifungal agent developed for the treatment of invasive aspergillosis and other serious fungal infections. Structurally, it is a cyclic hexapeptide that resembles the siderophore ferrichrome but features three amino acid substitutions and an aluminum chelate instead of iron. Its unique mechanism involves uptake into fungal cells via the Sit1 transporter—a protein absent in humans—resulting in high fungal specificity and low human toxicity. Although its precise intracellular target remains unclear, GR-2397 demonstrates rapid fungicidal activity against Aspergillus species (including azole-resistant strains), Fusarium solani, Candida glabrata, Cryptococcus neoformans, and other difficult-to-treat fungi. The drug has shown efficacy in animal models and completed phase 1 clinical trials with favorable safety and pharmacokinetic profiles. It has received Orphan Drug, Qualified Infectious Disease Product (QIDP), and Fast Track designations from the FDA for invasive aspergillosis[1][3][5][6].

Other names
BAL 2062BAL2062BAL-2062ASP 2397ASP2397ASP-2397VL 2397VL2397VL-2397GR 2397GR2397GR-2397
02

Targets

SIT1 (Sodium/imino acid transporter 1)

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