Meldonium

Overview

Meldonium (Mildronate) is a small-molecule carnitine-biosynthesis inhibitor and anti-ischemic metabolic modulator — not a peptide. It is an approved prescription cardiovascular drug in several ex-Soviet states but is not FDA- or EMA-approved, and it is WADA-prohibited (added January 2016). It is also sold as a gray-market research chemical.

Mechanism of Action

Meldonium competitively inhibits γ-butyrobetaine hydroxylase (the L-carnitine-synthesizing enzyme) and the carnitine transporter OCTN2, lowering intracellular L-carnitine. That suppresses long-chain fatty-acid β-oxidation and shifts metabolism toward glycolysis — the proposed anti-ischemic mechanism (Dambrova et al., 2016).

Research Summary

In rat ischemia-reperfusion models, meldonium (100–200 mg/kg) reduced myocardial infarct size ~30% and protected liver, brain, and endothelial function. In humans it is used clinically (in approving markets) for chronic heart failure and angina at 500 mg twice daily, but there is no FDA/EMA-registered pivotal efficacy trial. Urinary detection persists for weeks-to-months, central to doping cases. Not FDA/EMA-approved; not a peptide.

Reported Side Effects

• Not FDA- or EMA-approved; long-term/high-dose safety outside approved markets is limited
• WADA-prohibited since 1 Jan 2016; detectable in urine for weeks-to-months
• No primary LD50/toxicology data located
• Do not treat vendor or forum dosing claims as validated

Compare Meldonium with Others

Research References

• Dambrova M, et al. Pharmacological effects of meldonium: mechanisms and biomarkers. Pharmacol Res. 2016. PMID 26850121.
• Görgens C, et al. Meldonium long-term excretion and pharmacokinetics in healthy athletes. 2018. PMID 30328291.
• Stuart M, et al. Meldonium and the Prohibited List. 2016. PMC4919179.

Frequently asked questions

Has Meldonium been independently lab-tested?

Disclosed Labs has collected 2 Certificates of Analysis (COA) for Meldonium from 2 independent testing labs. 1 vendor has submitted material for testing. Products average 99.9% tested purity across the corpus. Full testing data is available at https://www.disclosedlabs.com/peptides/meldonium/testing.

How does Meldonium work?

Meldonium competitively inhibits γ-butyrobetaine hydroxylase (the L-carnitine-synthesizing enzyme) and the carnitine transporter OCTN2, lowering intracellular L-carnitine. That suppresses long-chain fatty-acid β-oxidation and shifts metabolism toward glycolysis — the proposed anti-ischemic mechanism (Dambrova et al., 2016).

What does the research say about Meldonium?

In rat ischemia-reperfusion models, meldonium (100–200 mg/kg) reduced myocardial infarct size ~30% and protected liver, brain, and endothelial function. In humans it is used clinically (in approving markets) for chronic heart failure and angina at 500 mg twice daily, but there is no FDA/EMA-registered pivotal efficacy trial. Urinary detection persists for weeks-to-months, central to doping cases. Not FDA/EMA-approved; not a peptide.