GE-2270A
Also known as: Antibiotic GE-2270A, GE-2270A, GE2270A, MDL 62,879, MDL-62879
Source GE-2270A at Peptiology
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Summary
GE-2270A (also known as MDL 62,879) is a naturally occurring thiopeptide antibiotic produced by Planobispora rosea. It exhibits potent activity against Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE), by targeting bacterial EF-Tu. It has not advanced to clinical approval, but has served as a scaffold for semi-synthetic derivatives such as LFF571 that have entered clinical investigation.
Mechanism of Action
Inhibits bacterial protein synthesis by binding to elongation factor Tu (EF-Tu), preventing the EF-Tu·GTP·aminoacyl-tRNA ternary complex from interacting with the ribosomal A site, thereby blocking translocation and halting translation.
Routes of Administration
Goals & Uses
- Antimicrobial therapyInfectionModerate
- Scaffold for antibiotic drug discoveryDrug DiscoveryHigh
- Treatment of MRSA infectionsAntimicrobialModerate
- Treatment of Clostridioides difficile infectionAntimicrobialLow
- Treatment of Gram-positive bacterial infectionsAntimicrobialModerate
Contraindications
- Gram-negative bacterial infectionsSpectrum LimitationModerate
- Known hypersensitivity to thiopeptide antibioticsAllergyHigh
Adverse Effects
- HepatotoxicityHepaticUnknownLiver injury or dysfunction
- Injection site reactionsLocalUnknown
- Gastrointestinal intoleranceGastrointestinalUnknown
Drug Interactions
- Other EF-Tu targeting agentsLow
- CYP3A4 substratesLow
Population Constraints
- Pediatric patientsAgeRelative
- Patients with hepatic impairmentOrgan FunctionRelative
- Pregnant womenReproductiveRelative
Regulatory Status
- European UnionInvestigationalNo EMA approval
- United StatesInvestigationalNo FDA approval; used only in preclinical studies
- United KingdomUnapprovedNo MHRA approval; research use only.
GE-2270A itself has not received regulatory approval in any jurisdiction. It has been primarily used as a research tool and chemical scaffold. Its semi-synthetic derivative LFF571 was evaluated in Phase II clinical trials for Clostridioides difficile infection.
Evidence & Sources
- Journal ArticleUngradedTavecchia P, et al.1994-01-01T00:00:00.000000Z
Frequently Asked Questions
What is GE-2270A?
GE-2270A (also known as MDL 62,879) is a naturally occurring thiopeptide antibiotic produced by Planobispora rosea. It exhibits potent activity against Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE), by targeting bacterial EF-Tu. It has not advanced to clinical approval, but has served as a scaffold for semi-synthetic derivatives such as LFF571 that have entered clinical investigation.
What is GE-2270A used for?
GE-2270A is educationally associated with: Antimicrobial therapy, Scaffold for antibiotic drug discovery, Treatment of MRSA infections, Treatment of Clostridioides difficile infection, Treatment of Gram-positive bacterial infections. Educational only — not medical advice.
How is GE-2270A administered?
Recorded routes of administration: Intravenous, Oral.
What are the potential side effects of GE-2270A?
Reported adverse effects include: Hepatotoxicity, Injection site reactions, Gastrointestinal intolerance. This list is not exhaustive — consult a qualified clinician.
Who should avoid GE-2270A?
Recorded contraindications: Gram-negative bacterial infections, Known hypersensitivity to thiopeptide antibiotics. Consult a qualified clinician before use.