Sirpiglenastat

DB17536InvestigationalSmall molecule

Sirpiglenastat, also known as DRP-104, is a prodrug of 6-diazo-5-oxo-L-norleucine (DON), which is a broad-acting glutamine antagonist. It is under investigation in clinical trial NCT04471415 (Study to Investigate DRP-104 in...

Mechanism: Pharmacologically active on Glutaminase liver isoform, mitochondrial and Glutaminase kidney isoform, mitochondrial
Curator reviewed
Formula / weight: C₂₂H₂₇N₅O₅ · 441.488 g/mol (avg)
Also known as: (-)-sirpiglenastat · (s)-isopropyl 2-((s)-2-acetamido-3-(1h-indol-3-yl)propanamido)-6-diazo-5-oxohexanoate · L-norleucine, n-acetyl-l-tryptophyl-6-diazo-5-oxo-, 1-methylethyl ester · Propan-2-yl (2s)-2-((n-acetyl-l-tryptophyl)amino)-6-diazo-5-oxohexanoate
Code names: DRP-104

Resolves to

Compound

UNII9GGE6A0ZMKCAS2079939-05-0ChEMBLCHEMBL4650367

Structure

InChIKeyLQNMCWOJACNQQM-PMACEKPBSA-NSMILESCC(C)OC(=O)[C@H](CCC(=O)C=[N+]=[N-])NC(=O)[C@H](CC1=CNC2=CC=CC=C12)NC(C)=O

Targets

Q9UI32GLS2O94925GLS

What you can answer from here — as of July 08, 2026

2Protein targetsEach mapped to UniProt, with action and pharmacological action

Listed above

4Clinical trialsPhase, status and sponsor resolved per trial

8+ReferencesStructured and connected to the statements they support

Which drugs share a target with Sirpiglenastat, and which of those have an active Phase 3 trial?

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