Meldonium
PharmaceuticalApproved (Latvia)Also known as: Mildronate, Meldonium dihydrate, MET-88, Quaterin, 3-(2,2,2-trimethylhydrazinium)propionate, THP
Meldonium, sold as Mildronate, was developed at the Latvian Institute of Organic Synthesis (PMID: 12242052) and is a licensed cardiovascular medicine in Latvia and a number of eastern European and post-Soviet countries. It has never been approved in the United States or the European Union as a whole.
Overview
At A Glance
Meldonium is a structural analog of gamma-butyrobetaine, the precursor of carnitine. It inhibits gamma-butyrobetaine hydroxylase, reducing carnitine biosynthesis, and it is the most potent clinically used inhibitor of the organic cation transporter OCTN2 (SLC22A5), which handles …
Overview
Meldonium, sold as Mildronate, was developed at the Latvian Institute of Organic Synthesis (PMID: 12242052) and is a licensed cardiovascular medicine in Latvia and a number of eastern European and post-Soviet countries. It has never been approved in the United States or the European Union as a whole. Most English-speaking readers first heard of it in 2016, when it appeared on the WADA prohibited list and a wave of positive tests followed. Its mechanism is unusual and worth understanding. Meldonium is the most potent clinically used inhibitor of the carnitine transporter OCTN2, and it also inhibits gamma-butyrobetaine hydroxylase, the enzyme that makes carnitine. Blocking both lowers tissue carnitine, and since carnitine is the shuttle that carries long-chain fatty acids into mitochondria, the cell shifts from burning fat toward burning glucose (PMID: 12242052; PMID: 26850121). Under low-oxygen conditions glucose oxidation needs less oxygen per unit of ATP, which is the basis for the anti-ischemic claim. The best human trial is MILSS I, a randomized, double-blind, placebo-controlled study of 512 patients with stable angina across 72 centers in four countries, testing four daily doses against placebo on top of standard therapy over twelve weeks. The primary endpoint was change in bicycle exercise time. Two lower dose groups did not separate from placebo. The 1000 mg group increased total exercise time by a mean of 35 seconds compared with a 7 second decrease on placebo, and the highest dose group did worse than the middle one (PMID: 22186118). That is a real but modest effect in patients whose exercise was limited by cardiac ischemia. Whether it helps healthy athletes is a different question, and the sports medicine reviews are not encouraging. A narrative review concluded that the performance benefit is speculative and discussed without sound scientific evidence (PMID: 27465696), and a 2026 review revisiting the ergogenic evidence reached similar conclusions (PMID: 42344756). The pharmacokinetics are the strangest part. Because meldonium competes with carnitine for OCTN2-mediated transport, it accumulates in muscle during treatment and then leaves slowly by diffusion. In 32 healthy athlete volunteers given oral meldonium for three weeks, plasma steady state took several days and urinary elimination continued for months after the last dose (PMID: 30328291). In mice, giving carnitine or gamma-butyrobetaine speeds elimination by competing for the same transporter (PMID: 27983775). This is why athletes tested positive long after they stopped, and it is also why meldonium residues have been found in milk as a possible inadvertent doping route (PMID: 34448364). Capsules sold as meldonium dihydrate are a foreign prescription drug being distributed outside any prescribing system.
Potential Research Fields
Chemical Information
IUPAC Name
Not yet available
CAS Number
76144-81-5
Molecular Formula
C6H14N2O2
Molecular Mass
146.19 g/mol
Dosing & Protocols
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Interactions
Contraindications
Regulatory rather than pharmacological in most cases: meldonium is prohibited at all times in tested sport and its months-long elimination window means stopping before competition does not clear it (PMID: 30328291). Mechanism-based caution applies to anyone with a carnitine deficiency disorder or on carnitine supplementation, since the drug directly opposes carnitine transport and biosynthesis (PMID: 27983775). It is not an approved medicine in the United States or the European Union, so no prescriber-supervised use exists there. No adequate pregnancy, lactation or pediatric data have been published in English-language literature.
Research Disclaimer
This interaction data is compiled from published research and community reports. It may not be exhaustive. Always consult a healthcare professional before combining compounds.
$69.99
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1
1
capsule
| Vendor | Product | Form | Qty | Price | $/mg | Coupon | |
|---|---|---|---|---|---|---|---|
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Meldonium dihydrate capsules (60) | capsule | 60 capsules● In Stock | $69.99BEST | — | — |
Tracking since Sep 7, 2026 · 1 data point
Vendors Selling Meldonium
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Protocols, calculator & safety for Meldonium
Research Score
0 PubMed studies
Quality Indicators
Data Completeness
63%Quick Facts
Half-Life
Not a single simple value: in 32 healthy athlete volunteers taking oral meldonium for three weeks, plasma took several days to reach steady state and urinary elimination continued for several months after the last dose, because tissue clearance depends on slow diffusion rather than transport (PMID: 30328291)
Molecular Weight
146.19 g/mol
Administration
Oral, Intravenous injection
CAS Number
76144-81-5
Trial Phase
Approved (Latvia)
Research Disclaimer
This information is for educational and research purposes only. Not intended as medical advice. Consult a healthcare professional before use.
Frequently Asked Questions
What is Meldonium used for in research?
Meldonium, sold as Mildronate, was developed at the Latvian Institute of Organic Synthesis (PMID: 12242052) and is a licensed cardiovascular medicine in Latvia and a number of eastern European and post-Soviet countries. It has never been approved in the United States or the European Union as a whole. Most English-speaking readers first heard of it in 2016, when it appeared on the WADA prohibited list and a wave of positive tests followed.
Its mechanism is unusual and worth understanding. Meldonium is the most potent clinically used inhibitor of the carnitine transporter OCTN2, and it also inhibits gamma-butyrobetaine hydroxylase, the enzyme that makes carnitine. Blocking both lowers tissue carnitine, and since carnitine is the shuttle that carries long-chain fatty acids into mitochondria, the cell shifts from burning fat toward burning glucose (PMID: 12242052; PMID: 26850121). Under low-oxygen conditions glucose oxidation needs less oxygen per unit of ATP, which is the basis for the anti-ischemic claim.
The best human trial is MILSS I, a randomized, double-blind, placebo-controlled study of 512 patients with stable angina across 72 centers in four countries, testing four daily doses against placebo on top of standard therapy over twelve weeks. The primary endpoint was change in bicycle exercise time. Two lower dose groups did not separate from placebo. The 1000 mg group increased total exercise time by a mean of 35 seconds compared with a 7 second decrease on placebo, and the highest dose group did worse than the middle one (PMID: 22186118). That is a real but modest effect in patients whose exercise was limited by cardiac ischemia.
Whether it helps healthy athletes is a different question, and the sports medicine reviews are not encouraging. A narrative review concluded that the performance benefit is speculative and discussed without sound scientific evidence (PMID: 27465696), and a 2026 review revisiting the ergogenic evidence reached similar conclusions (PMID: 42344756).
The pharmacokinetics are the strangest part. Because meldonium competes with carnitine for OCTN2-mediated transport, it accumulates in muscle during treatment and then leaves slowly by diffusion. In 32 healthy athlete volunteers given oral meldonium for three weeks, plasma steady state took several days and urinary elimination continued for months after the last dose (PMID: 30328291). In mice, giving carnitine or gamma-butyrobetaine speeds elimination by competing for the same transporter (PMID: 27983775). This is why athletes tested positive long after they stopped, and it is also why meldonium residues have been found in milk as a possible inadvertent doping route (PMID: 34448364).
Capsules sold as meldonium dihydrate are a foreign prescription drug being distributed outside any prescribing system.
What forms does Meldonium come in?
Meldonium is available in capsule form.
How much does Meldonium cost?
Prices start at $69.99 across 1 verified vendor.
How do I compare Meldonium vendors?
Compare prices, payment methods, shipping, and COA scores across 1 vendor.
Research Tools
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View AllAlbuterol (salbutamol)
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Clascoterone
PharmaceuticalPreclinicalClascoterone (brand name Winlevi; development codes CB-03-01 and, for the alopecia formulation, Breezula) is a first-in-class topical androgen receptor (AR) antagonist approved by the U.S.
Finasteride
PharmaceuticalPreclinicalFinasteride is an orally-active selective type II 5α-reductase inhibitor that blocks the conversion of testosterone to dihydrotestosterone (DHT), the primary androgenic driver of both benign prostatic hyperplasia (BPH) and androgenetic alopecia (male-pattern hair loss).
Mirabegron
PharmaceuticalFDA ApprovedMirabegron is an approved prescription drug, not a research chemical.
Tropisetron
PharmaceuticalApproved (Japan)Tropisetron, coded ICS 205-930 during development and marketed as Navoban, is a serotonin 5-HT3 receptor antagonist approved as an antiemetic in Japan and in many other countries outside the United States, with ATC code A04AA03 (KEGG DRUG D02041, D02130).
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