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Accession NumberDB08842
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionAcetylcarnitine is an investigational drug in the United states, Italy, United Kingdom, China, Israel, and Norway, and it is approved in Italy, Portugal, Argentina, Chile, Philippines, Australia, and India. Acetylcarnitine can be synthesized, but it is also naturally found in adequate amounts in healthy humans. In human plasma and tissues, acetylcarnitine is the most predominant acylated ester of carnitine, which is an amino acid derivative that is made in the kidney, liver, and brain from lysine and methionine. The main role of acetylcarnitine is to help transport fatty acids into the mitochondrial matrix where fatty acid metabolism occurs.
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
AcilenIFI (Italy)
ActigeronBago (Chile)
BranigenSigma-Tau (Italy)
BranitilOFF (Italy)
CeredorIRBI (Italy)
FertilixFortbenton (Argentina)
LacetilinaPentafarma (Portugal)
LaremideLafedar (Argentina)
LevocetileKorea United (Philippines)
MaxozaSun (India)
Memorx IQ PlusGruppo Medica (Philippines)
MemovigorEuro-Pharma (Italy)
NeurexBeta (Argentina)
Neuroactil Bago (Argentina)
NicetileSigma-Tau (Italy)
NormobrenMedosan (Italy)
PhototropTubilux (Italy)
ZibrenSigma-Tau (Italy)
Brand mixturesNot Available
SaltsNot Available
CAS number3040-38-8
WeightAverage: 204.2435
Monoisotopic: 204.123583069
Chemical FormulaC9H18NO4
CC(=O)O[[email protected]](CC(O)=O)C[N+](C)(C)C
IndicationAcetylcarnitine is not approved for any indication in the United states and Canada, but it is approved and indicated in Italy for cerebrovascular disorders, mental function disorders, peripheral nerve disorders, diabetic neuropathy, and nutritional supplementation; Portugal for mental function disorders; Argentina for cerebral vasculopathy, nutritional supplementation, and peripheral neuropathy; Chile for dementia; Philippines for cerebrovascular disorders and mental function disorders; Australia for nutritional supplementation; and India for nutritional supplementation to increase sperm count. Acetylcarnitine also has several potential therapeutic indications for which it is still being investigated: in Norway, acetylcarnitine is in a phase IV trial for prophylactic treatment of migraines; in Italy acetylcarnitine is in a phase II trial for use in patients with type 2 Diabetes Mellitus, a phase III trial for alleviating fatigue in patients with chronic hepatitis C, and for use in patients with Minimal Hepatic Encephalopathy; in the United States acetylcarnitine is in a phase II trial for the neurodegenerative disorder Progressive Supranuclear Palsy, a phase II and III trial for reducing peripheral neuropathy in cancer patients as an adjunct to chemotherapy, a phase I and II trial for treating patients in septic shock, a phase II trial for bipolar depression, a phase II trial to reduce oxidative stress in patients with Sickle Cell disease, a phase I and II trial for chronic fatigue syndrome, and a study for preventing nerve damage in HIV patients; in China acetylcarnitine is in a phase III trial for reducing peripheral neuropathy in cancer patients as an adjunct to chemotherapy; in the United Kingdom acetylcarnitine is being investigated for preventing nerve damage in HIV patients; and in Israel acetylcarnitine is being studied for the treatment of male infertility.
Structured Indications Not Available
PharmacodynamicsThe complete physiological effects of acetycarnitine are still being studied. What has been discovered so far is that acetylcarinitine has positive effects on mental fatigue, neurodegenerative disorders, cognitive functions, peripheral neuropathy, and sperm motility. Specifically, in one study involving patients with HIV, patients on acetylcarnitine supplementation had increased CD4 cells, decreased lymphocyte apoptosis, improved polyneuropathy and cardiovascular damage, and decreased triglyceride and TNF alpha levels in the blood. Another study showed that acetylcarnitine increased glucose disposal in type 2 diabetic patients through possibly increasing the activity of glycogen synthase.
Mechanism of actionThe mechanisms of action of acetylcarnitine have not been fully elucidated, but it seems that the main role of acetylcarnitine is to donate an acetyl group during fatty acid metabolism to help transport fatty acids, such as acetyl CoA, into the mitochondrial matrix where fatty acid metabolism occurs. Additionally several studies have found that separate from its metabolic role, acetylcarnitine has neuromodulatory, neurotrophic, and neuroprotective effects that most likely are involved in its positive effects in neurological diseases. In its role in treating male infertility, acetylcarnitine increases the active movement of sperm cells. One study has also mentioned a role for acetylcarnitine as an antioxidant. The study found that through the receptor, tyrosine kinase A, acetylcarnitine was able to decrease the production of free radicals, peroxidation of lipids, and oxidation of proteins as well as decrease glutathione levels and increase thioredoxin.
Related Articles
AbsorptionAcetylcarnitine supplements are absorbed in a similar manner to L-carnitine.
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationAcetylcarnitine is eliminated in a similar manner as L-carnitine. Both of which are eliminated by the kidneys and involve tubular secretion.
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Drug InteractionsNot Available
Food InteractionsNot Available
Synthesis Reference

Gu, Heng-da; Shi, Shuang; Yang, Ying; Shi, Zhao-xin; Yu, Zhan-long. Synthesis of acetyl-L-carnitine by direct acylation method. Shenyang Huagong Xueyuan Xuebao (2006), 20(2), 154-155, 160.

General References
  1. Vermeulen RC, Scholte HR: Exploratory open label, randomized study of acetyl- and propionylcarnitine in chronic fatigue syndrome. Psychosom Med. 2004 Mar-Apr;66(2):276-82. [PubMed:15039515 ]
  2. Ilias I, Manoli I, Blackman MR, Gold PW, Alesci S: L-Carnitine and acetyl-L-carnitine in the treatment of complications associated with HIV infection and antiretroviral therapy. Mitochondrion. 2004 Jul;4(2-3):163-8. [PubMed:16120381 ]
  3. Salvioli G, Neri M: L-acetylcarnitine treatment of mental decline in the elderly. Drugs Exp Clin Res. 1994;20(4):169-76. [PubMed:7813389 ]
  4. Rebouche CJ: Kinetics, pharmacokinetics, and regulation of L-carnitine and acetyl-L-carnitine metabolism. Ann N Y Acad Sci. 2004 Nov;1033:30-41. [PubMed:15591001 ]
  5. Virmani A, Binienda Z: Role of carnitine esters in brain neuropathology. Mol Aspects Med. 2004 Oct-Dec;25(5-6):533-49. [PubMed:15363640 ]
  6. Giancaterini A, De Gaetano A, Mingrone G, Gniuli D, Liverani E, Capristo E, Greco AV: Acetyl-L-carnitine infusion increases glucose disposal in type 2 diabetic patients. Metabolism. 2000 Jun;49(6):704-8. [PubMed:10877193 ]
  7. Barhwal K, Hota SK, Jain V, Prasad D, Singh SB, Ilavazhagan G: Acetyl-l-carnitine (ALCAR) prevents hypobaric hypoxia-induced spatial memory impairment through extracellular related kinase-mediated nuclear factor erythroid 2-related factor 2 phosphorylation. Neuroscience. 2009 Jun 30;161(2):501-14. doi: 10.1016/j.neuroscience.2009.02.086. Epub 2009 Mar 24. [PubMed:19318118 ]
  8. Wilson AD, Hart A, Brannstrom T, Wiberg M, Terenghi G: Delayed acetyl-L-carnitine administration and its effect on sensory neuronal rescue after peripheral nerve injury. J Plast Reconstr Aesthet Surg. 2007;60(2):114-8. Epub 2006 Jul 24. [PubMed:17223507 ]
  9. Ruggenenti P, Cattaneo D, Loriga G, Ledda F, Motterlini N, Gherardi G, Orisio S, Remuzzi G: Ameliorating hypertension and insulin resistance in subjects at increased cardiovascular risk: effects of acetyl-L-carnitine therapy. Hypertension. 2009 Sep;54(3):567-74. doi: 10.1161/HYPERTENSIONAHA.109.132522. Epub 2009 Jul 20. [PubMed:19620516 ]
  10. Brayfield, Alison (2014). Martindale : The Complete Drug Reference (38th ed.). Pharmaceutical Press. [ISBN:978-0857111395 ]
  11. O'Neil, Maryadele J. (2013). The Merck Index : An Encyclopedia of Chemicals, Drugs, and Biologicals (15th ed.). Royal Society of Chemistry, The. [ISBN:978-1849736701 ]
External Links
ATC CodesN06BX12
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (39.8 KB)
Predicted ADMET features
Human Intestinal Absorption-0.9965
Blood Brain Barrier+0.8614
Caco-2 permeable+0.5175
P-glycoprotein substrateNon-substrate0.5593
P-glycoprotein inhibitor INon-inhibitor0.9272
P-glycoprotein inhibitor IINon-inhibitor0.6465
Renal organic cation transporterNon-inhibitor0.916
CYP450 2C9 substrateNon-substrate0.8267
CYP450 2D6 substrateNon-substrate0.8471
CYP450 3A4 substrateSubstrate0.5303
CYP450 1A2 substrateNon-inhibitor0.9367
CYP450 2C9 inhibitorNon-inhibitor0.9236
CYP450 2D6 inhibitorNon-inhibitor0.9355
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8818
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9761
Ames testNon AMES toxic0.8217
CarcinogenicityCarcinogens 0.5207
BiodegradationReady biodegradable0.8743
Rat acute toxicity2.3717 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9728
hERG inhibition (predictor II)Non-inhibitor0.9018
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Experimental Properties
melting point145°CFrom The Merck Index.
water solubilityVery soluble in water and alcohol.From The Merck Index.
Predicted Properties
Water Solubility0.429 mg/mLALOGPS
pKa (Strongest Acidic)4.09ChemAxon
pKa (Strongest Basic)-7ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area63.6 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity61.8 m3·mol-1ChemAxon
Polarizability21.17 Å3ChemAxon
Number of Rings0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Mass Spec (NIST)Not Available
Spectrum TypeDescriptionSplash Key
Predicted GC-MSPredicted GC-MS Spectrum - GC-MSNot Available
DescriptionThis compound belongs to the class of organic compounds known as acyl cholines. These are acylated derivatives of choline. Choline or 2-Hydroxy-N,N,N-trimethylethanaminium is a quaternary ammonium salt with the chemical formula (CH3)3N+(CH2)2OH.
KingdomOrganic compounds
Super ClassOrganonitrogen compounds
ClassQuaternary ammonium salts
Sub ClassCholines
Direct ParentAcyl cholines
Alternative Parents
  • Acyl choline
  • Fatty acid
  • Dicarboxylic acid or derivatives
  • Acetate salt
  • Carboxylic acid ester
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Carbonyl group
  • Amine
  • Organic cation
  • Aliphatic acyclic compound
Molecular FrameworkAliphatic acyclic compounds
External Descriptors


Pharmacological action
General Function:
Symporter activity
Specific Function:
Sodium-ion dependent, high affinity carnitine transporter. Involved in the active cellular uptake of carnitine. Transports one sodium ion with one molecule of carnitine. Also transports organic cations such as tetraethylammonium (TEA) without the involvement of sodium. Also relative uptake activity ratio of carnitine to TEA is 11.3.
Gene Name:
Uniprot ID:
Molecular Weight:
62751.08 Da
  1. Ohashi R, Tamai I, Yabuuchi H, Nezu JI, Oku A, Sai Y, Shimane M, Tsuji A: Na(+)-dependent carnitine transport by organic cation transporter (OCTN2): its pharmacological and toxicological relevance. J Pharmacol Exp Ther. 1999 Nov;291(2):778-84. [PubMed:10525100 ]
  2. Kobayashi D, Tamai I, Sai Y, Yoshida K, Wakayama T, Kido Y, Nezu J, Iseki S, Tsuji A: Transport of carnitine and acetylcarnitine by carnitine/organic cation transporter (OCTN) 2 and OCTN3 into epididymal spermatozoa. Reproduction. 2007 Nov;134(5):651-8. [PubMed:17965255 ]
Pharmacological action
General Function:
Cation:cation antiporter activity
Specific Function:
Sodium-ion independent, medium affinity carnitine transporter. Also transports organic cations such as tetraethylammonium (TEA) without the involvement of sodium. Relative uptake activity ratio of carnitine to TEA is 746.
Gene Name:
Uniprot ID:
Molecular Weight:
63320.215 Da
  1. Kobayashi D, Tamai I, Sai Y, Yoshida K, Wakayama T, Kido Y, Nezu J, Iseki S, Tsuji A: Transport of carnitine and acetylcarnitine by carnitine/organic cation transporter (OCTN) 2 and OCTN3 into epididymal spermatozoa. Reproduction. 2007 Nov;134(5):651-8. [PubMed:17965255 ]
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Drug created on February 27, 2013 14:42 / Updated on August 17, 2016 12:24