Echinomycin
Also known as: AM-65, Levomycin, NSC-526417, Quinomycin A
Summary
Echinomycin is a naturally occurring cyclic depsipeptide produced by Streptomyces echinatus. It is a potent bisintercalating agent that binds preferentially to CpG-containing DNA sequences, inhibiting transcription. It has demonstrated anticancer activity in preclinical and early clinical studies but has not achieved regulatory approval due to toxicity and limited efficacy in trials. Current research investigates its role as a HIF-1alpha inhibitor for oncology applications.
Mechanism of Action
Bisintercalation into DNA at CpG sequences, causing double-stranded DNA unwinding and inhibition of DNA-dependent RNA synthesis; also inhibits HIF-1alpha transcriptional activity by binding to hypoxia response elements
Routes of Administration
Goals & Uses
- Pediatric leukemia treatmentOncologyLow
- Antimicrobial activityAnti InfectiveLow
- Anticancer activity (leukemia, lymphoma)OncologyLow
- HIF-1alpha inhibition in solid tumorsOncology / Hypoxia TargetingLow
Contraindications
- Severe hepatic impairmentOrganHighLiver function concerns
- PregnancyPopulationHighPotential fetal risk or insufficient safety data
- Severe myelosuppressionHematologicHigh
Adverse Effects
- HepatotoxicityHepaticUncommonLiver injury or dysfunction
- HypotensionCardiovascularUncommonLow blood pressure
- Nausea and vomitingGastrointestinalCommon
- MucositisGastrointestinal / MucosalUncommon
- MyelosuppressionHematologicCommon
Drug Interactions
- Other myelosuppressive agentsHigh
- DNA-intercalating agents (e.g., anthracyclines)High
Population Constraints
- Pediatric patientsAgeRelative
- Patients with pre-existing bone marrow suppressionHematologicAbsolute
- Pregnant womenReproductiveAbsolute
Regulatory Status
- European UnionUnapprovedNo EMA approval; research compound only
- United StatesUnapprovedInvestigated under IND in Phase I/II trials; not approved by FDA; available for research use only
- United KingdomUnapprovedNo MHRA approval; used only in research or historical clinical trials
Not approved by FDA, EMA, or other major regulatory agencies. Investigated in Phase I/II oncology trials in the 1980s–1990s. Currently used only in preclinical and early-phase research settings.
Evidence & Sources
No sources recorded yet.