Omberacetam
Also known as: GVS-111, N-phenylacetyl-L-prolylglycine ethyl ester, Noopept, Noopeptide
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Summary
Omberacetam, also known as Noopept, GVS‑111, or N‑phenylacetyl‑L‑prolylglycine ethyl ester, is a synthetic dipeptide marketed as a prescription nootropic. It is classified with racetams but has a distinct structure. The drug is approved for clinical use in some jurisdictions and is administered orally, intranasally, or sublingually to support cognitive function and provide neuroprotective effects.
Mechanism of Action
Omberacetam’s pharmacology is described as multifaceted, influencing several neurotransmitter systems in the brain, though specific pathways are not detailed in the cited literature. In vitro studies show that at high concentrations it increases the cellular content of organic anion‑transporting polypeptides OATP1B1 and OATP1B3, modestly reducing uptake of substrates such as atorvastatin, an effect judged clinically insignificant. Overall, its neuroprotective and cognition‑enhancing actions are attributed to broad modulation of neuronal signaling.
What the Research Shows
Three peer‑reviewed papers provide the current evidence base. A 2025 analytical study characterized omberacetam’s physicochemical properties, confirming it as an orally bioavailable API with neuroprotective claims, but offered no efficacy data. A 2023 cellular investigation in HepG2 cells demonstrated that 500 µM omberacetam up‑regulates OATP1B1 and OATP1B3 transporter levels and reduces substrate penetration, yet FDA‑based calculations deemed the effect clinically irrelevant. A 2021 survey of over‑the‑counter supplements revealed that many products labeled for cognitive enhancement contain undeclared omberacetam at doses up to four times the typical pharmacologic amount, highlighting regulatory and safety concerns. No human clinical trials are cited.
Reported Benefits
Preclinical work suggests omberacetam may exert neuroprotective activity and modulate neurotransmitter systems, supporting its intended use as a cognition‑enhancing agent. The physicochemical analysis confirms its stability and oral availability, which are favorable for therapeutic formulation. However, direct evidence of cognitive benefit in humans is not presented in the available abstracts.
Limitations of the Evidence
The literature lacks randomized clinical trials or human efficacy studies, limiting confidence in claimed cognitive benefits. Cellular findings on OATP transporters were observed only at supratherapeutic concentrations and judged clinically insignificant. Additionally, the presence of undeclared omberacetam in dietary supplements underscores the difficulty of ensuring product purity and dosage consistency.
Safety Considerations
No adverse‑event data are reported in the cited papers. The supplement analysis warns that consumers may ingest pharmaceutical‑level doses without medical supervision, raising potential for unknown toxicity or drug interactions. In vitro transporter effects appear negligible at therapeutic levels, but the overall safety profile in humans remains inadequately characterized, warranting clinician oversight.
How It Is Administered
Omberacetam is approved for prescription use and can be delivered orally, intranasally, or sublingually. Formulations are typically presented as tablets, capsules, or nasal sprays, though specific product details are not provided in the cited literature.
Routes of Administration
Goals & Uses
- Memory consolidationCognitiveModerate
- NeuroprotectionNeurologyModerate
- Alzheimer's disease symptomatic treatmentNeurodegenerationLow
- Anxiety reductionNeuropsychiatricLow
- Post-traumatic cognitive recoveryRehabilitationModerate
- Cognitive enhancementNootropicModerate
Contraindications
- Hypersensitivity to omberacetam or excipientsAllergyHigh
- Severe hepatic impairmentOrganModerateLiver function concerns
- Age under 18PediatricModerate
- Severe renal impairmentOrganModerateKidney function concerns
- PregnancyPopulationHighPotential fetal risk or insufficient safety data
- LactationReproductiveHigh
Adverse Effects
- HeadacheNeurologicUncommonPain in the head or upper neck
- InsomniaPsychiatricUncommonDifficulty sleeping
- Increased blood pressureCardiovascularUncommon
- NauseaGastrointestinalUncommonFeeling of sickness or urge to vomit
- Psychomotor agitationNeuropsychiatricRare
- IrritabilityPsychiatricUncommonIncreased agitation or short temper
Drug Interactions
- Psychostimulants (amphetamine, modafinil)Moderate
- Cholinergic agentsLow
- AlcoholModerate
- AntihypertensivesLowMay potentiate hypotensive effects in some contexts
Population Constraints
- Patients with hypertensionCardiovascularRelative
- Patients with epilepsyNeurologicalRelative
- Elderly patientsAgeRelative
- Pediatric population (<18 years)PediatricAbsolute
Regulatory Status
- European UnionUnapprovedNot approved by EMA; regulatory status varies by member state; generally sold as a supplement or research compound
- United StatesUnapprovedNot FDA approved; sold as a research chemical or unscheduled dietary supplement; no IND or NDA on record
- United KingdomUnapprovedNot MHRA approved; sold as unregulated supplement; not a controlled substance under UK law as of last review
Approved as a pharmaceutical drug in Russia (Novartis/Grunethal licensed to JSC Lekko Pharmaceuticals) for cognitive impairment associated with organic brain diseases and post-traumatic stress. Not approved by the FDA, EMA, or MHRA. Sold as an unregulated dietary supplement or research chemical in many Western markets.
Evidence & Sources
- Journal ArticleLowCohen PA, et al.2021-01-01T00:00:00.000000Z
- Journal ArticleLowAraj SK, et al.2025-01-01T00:00:00.000000Z
- Journal ArticleLowErokhina PD, et al.2023-01-01T00:00:00.000000Z
Frequently Asked Questions
Is omberacetam approved for medical use?
According to the structured data, omberacetam holds prescription status and is listed as an approved compound, though the abstracts do not specify the regulatory agencies or indications for which it is approved.
How does omberacetam differ from piracetam?
While both belong to the racetam family, omberacetam is a synthetic dipeptide with a distinct chemical scaffold and is described as having a broader, multifaceted modulation of neurotransmitter systems compared with piracetam’s more limited profile.
Can I find omberacetam in over‑the‑counter supplements?
A 2021 study found that many cognitive‑enhancement supplements contain undeclared omberacetam, sometimes at doses up to four times the typical pharmacologic amount, indicating that such products are not regulated and may expose users to unmonitored drug levels.
What are the known side effects of omberacetam?
The abstracts do not report specific adverse effects. However, the presence of high, unregulated doses in supplements suggests a potential risk of toxicity or interactions, emphasizing the need for medical supervision when using the drug.
Does omberacetam affect drug metabolism?
In vitro experiments showed that high concentrations of omberacetam increase OATP1B1 and OATP1B3 transporter levels, modestly reducing substrate uptake, but FDA‑based calculations concluded that this effect is clinically insignificant at therapeutic concentrations.
What is Omberacetam?
Omberacetam, also known as Noopept, GVS‑111, or N‑phenylacetyl‑L‑prolylglycine ethyl ester, is a synthetic dipeptide marketed as a prescription nootropic. It is classified with racetams but has a distinct structure. The drug is approved for clinical use in some jurisdictions and is administered orally, intranasally, or sublingually to support cognitive function and provide neuroprotective effects.
What is Omberacetam used for?
Omberacetam is educationally associated with: Memory consolidation, Neuroprotection, Alzheimer's disease symptomatic treatment, Anxiety reduction, Post-traumatic cognitive recovery, Cognitive enhancement. Educational only — not medical advice.
How is Omberacetam administered?
Recorded routes of administration: Intranasal, Oral, Sublingual.
What are the potential side effects of Omberacetam?
Reported adverse effects include: Headache, Insomnia, Increased blood pressure, Nausea, Psychomotor agitation, Irritability. This list is not exhaustive — consult a qualified clinician.
Who should avoid Omberacetam?
Recorded contraindications: Hypersensitivity to omberacetam or excipients, Severe hepatic impairment, Age under 18, Severe renal impairment, Pregnancy, Lactation. Consult a qualified clinician before use.