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Acivicin is a natural glutamine antagonist, originally isolated from Streptomyces sviceus, that was investigated as an antineoplastic (anticancer) agent for its ability to irreversibly block glutamine-dependent enzymes.
- Studied as an anticancer agent that starves tumor cells of glutamine needed for growth
- Used as a laboratory research tool to study glutamine metabolism in cancer biology
- Dose-limiting neurotoxicity halted clinical development
- Readily crosses the blood-brain barrier due to its amino-acid-like structure, raising CNS toxicity risk regardless of tumor location
- Associated with myelosuppression and other adverse effects in trials
Overview
A genuinely interesting cancer-metabolism idea that got shut down by its own side effect; it crosses into the brain and causes neurotoxicity.
Mechanism
Acivicin covalently and irreversibly inhibits glutamine amidotransferases and gamma-glutamyl transpeptidase (GGT), enzymes that use glutamine as a nitrogen source for nucleotide and amino acid biosynthesis. By blocking these enzymes, it reduces intracellular glutamine availability, starving rapidly dividing cells (including tumor cells) of building blocks needed for growth.
receptor fingerprint
Glutamine amidotransferaseInhibitor
Gamma-glutamyl transpeptidase (GGT)Inhibitor
Dosingtypical ranges, not medical advice
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Safetyrisks and cautions, not medical advice
Clinical development of acivicin was halted primarily due to dose-limiting neurotoxicity. Because it structurally resembles a large neutral amino acid, it crosses the blood-brain barrier via the large neutral amino acid transporter, producing central nervous system side effects even when the tumor being treated is elsewhere in the body. Trials also reported myelosuppression and other adverse effects.
Subjective profileweighing the evidence above
Dead as a drug for a concrete reason: dose-limiting neurotoxicity ended development, because its amino-acid-like shape carries it straight into the brain whatever the tumor is doing. What remains is a useful lab tool for studying glutamine metabolism.
Resources
This entry is here for reference.
Research
1 listed here; entry last updated July 2026
Reviews
My notesprivate to this device
FAQ
What is Acivicin used for?
It has no approved medical use. It was studied as an experimental anticancer drug that blocks glutamine metabolism, but trials were discontinued due to neurotoxicity.
How does Acivicin work?
It irreversibly inhibits enzymes (glutamine amidotransferases and gamma-glutamyl transpeptidase) that cells need to use glutamine for building nucleotides and other molecules, which slows the growth of rapidly dividing cells like tumor cells.
Is Acivicin well-researched?
It went through Phase I human cancer trials, so there is real clinical data, but development stopped there due to dose-limiting neurotoxicity.
Adverse effects
- Dose-limiting neurotoxicity halted clinical development
- Readily crosses the blood-brain barrier due to its amino-acid-like structure, raising CNS toxicity risk regardless of tumor location
- Associated with myelosuppression and other adverse effects in trials