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Identification
NameTasimelteon
Accession NumberDB09071
TypeSmall Molecule
GroupsApproved
Description

Tasimelteon is a selective dual melatonin receptor agonist indicated for the treatment of Non-24-Hour Sleep-Wake Disorder (N24HSWD). Occurring commonly in blind individuals without light perception, this condition is often characterized by periods of night-time insomnia and day-time sleepiness. In blind individuals, a lack of light stimulation causes an extension of the 24-hour circadian cycle and can lead to progressively delayed sleep onset. By activating melatonin receptors MT1 and MT2 in the suprachiasmatic nucleus of the brain, tasimelteon has been shown to improve sleep by resynchronizing the circadian rhythm through its “non-photic” mechanism. Tasimelteon is currently the only drug available for the treatment of N24HSWD and was granted orphan drug status by the FDA in 2010.

Structure
Thumb
Synonyms
N-{[(1R,2R)-2-(2,3-dihydro-1-benzofuran-4-yl)cyclopropyl]methyl}propanamide
tasimeltéon
External Identifiers
  • BMS 214778
  • BMS-214778
  • BMS214778
  • VEC 162
  • VEC-162
  • VEC162
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Hetliozcapsule20 mg/1oralVanda Pharmaceuticals Inc.2014-04-04Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIISHS4PU80D9
CAS number609799-22-6
WeightAverage: 245.322
Monoisotopic: 245.141578856
Chemical FormulaC15H19NO2
InChI KeyPTOIAAWZLUQTIO-GXFFZTMASA-N
InChI
InChI=1S/C15H19NO2/c1-2-15(17)16-9-10-8-13(10)11-4-3-5-14-12(11)6-7-18-14/h3-5,10,13H,2,6-9H2,1H3,(H,16,17)/t10-,13+/m0/s1
IUPAC Name
N-{[(1R,2R)-2-(2,3-dihydro-1-benzofuran-4-yl)cyclopropyl]methyl}propanimidic acid
SMILES
[H][C@@]1(CN=C(O)CC)C[C@@]1([H])C1=C2CCOC2=CC=C1
Taxonomy
ClassificationNot classified
Pharmacology
IndicationTasimelteon is indicated for the treatment of Non-24-Hour Sleep-Wake Disorder (N24HSWD).
PharmacodynamicsNot Available
Mechanism of actionTasimelteon is a selective dual agonist of the melatonin receptors MT1 and MT2.
Related Articles
AbsorptionNot Available
Volume of distribution

The apparent oral volume of distribution of tasimelteon at steady state in young healthy subjects is approximately 56 – 126 L.

Protein bindingAt therapeutic concentrations, tasimelteon is about 90% bound to proteins.
Metabolism

Tasimelteon is extensively metabolized. Metabolism of tasimelteon consists primarily of oxidation at multiple sites and oxidative dealkylation resulting in opening of the dihydrofuran ring followed by further oxidation to give a carboxylic acid. CYP1A2 and CYP3A4 are the major isozymes involved in the metabolism of tasimelteon. Phenolic glucuronidation is the major phase II metabolic route.

Route of eliminationFollowing oral administration of radiolabeled tasimelteon, 80% of total radioactivity was excreted in urine and approximately 4% in feces, resulting in a mean recovery of 84%. Less than 1% of the dose was excreted in urine as the parent compound.
Half lifeThe observed mean elimination half-life for tasimelteon is 1.3 ± 0.4 hours.
ClearanceNot Available
ToxicityThe most common adverse reactions are headache, increased alanine aminotransferase, nightmares or unusual dreams, and upper respiratory or urinary tract infections. There are currently no adequate or well-controlled studies that suggest that tasimelteon is safe to use during pregnancy. In animal studies, administration of tasimelteon during pregnancy resulted in developmental toxicity (embryofetal mortality, neurobehavioral impairment, and decreased growth and development in offspring) at doses greater than those used clinically. During clinical trials, rats did not self-administer tasimelteon, suggesting that the drug does not have a potential for abuse.
Affected organismsNot Available
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal AbsorptionNot AvailableNot Available
Blood Brain BarrierNot AvailableNot Available
Caco-2 permeableNot AvailableNot Available
P-glycoprotein substrateNot AvailableNot Available
P-glycoprotein inhibitor INot AvailableNot Available
P-glycoprotein inhibitor IINot AvailableNot Available
Renal organic cation transporterNot AvailableNot Available
CYP450 2C9 substrateNot AvailableNot Available
CYP450 2D6 substrateNot AvailableNot Available
CYP450 3A4 substrateNot AvailableNot Available
CYP450 1A2 substrateNot AvailableNot Available
CYP450 2C9 inhibitorNot AvailableNot Available
CYP450 2D6 inhibitorNot AvailableNot Available
CYP450 2C19 inhibitorNot AvailableNot Available
CYP450 3A4 inhibitorNot AvailableNot Available
CYP450 inhibitory promiscuityNot AvailableNot Available
Ames testNot AvailableNot Available
CarcinogenicityNot AvailableNot Available
BiodegradationNot AvailableNot Available
Rat acute toxicityNot AvailableNot applicable
hERG inhibition (predictor I)Not AvailableNot Available
hERG inhibition (predictor II)Not AvailableNot Available
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Capsuleoral20 mg/1
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5856529 No1997-12-092017-12-09Us
US8785492 No2013-01-252033-01-25Us
US9060995 No2013-01-252033-01-25Us
USUS5856529 A No1997-12-092017-12-09Us
USUS8785492 B2 No2013-01-252033-01-25Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
boiling point442.553°CMSDS
water solubility1.1 mg/mLMSDS
logP2.43MSDS
Predicted Properties
PropertyValueSource
Water Solubility0.0216 mg/mLALOGPS
logP3.35ALOGPS
logP2.22ChemAxon
logS-4.1ALOGPS
pKa (Strongest Acidic)4.41ChemAxon
pKa (Strongest Basic)6.46ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area41.82 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity70.87 m3·mol-1ChemAxon
Polarizability27.91 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceNot Available
General References
  1. Lavedan C, Forsberg M, Gentile AJ: Tasimelteon: a selective and unique receptor binding profile. Neuropharmacology. 2015 Apr;91:142-7. doi: 10.1016/j.neuropharm.2014.12.004. Epub 2014 Dec 19. [PubMed:25534555 ]
  2. Neubauer DN: Tasimelteon for the treatment of non-24-hour sleep-wake disorder. Drugs Today (Barc). 2015 Jan;51(1):29-35. doi: 10.1358/dot.2015.51.1.2258364. [PubMed:25685859 ]
  3. Stahl SM: Mechanism of action of tasimelteon in non-24 sleep-wake syndrome: treatment for a circadian rhythm disorder in blind patients. CNS Spectr. 2014 Dec;19(6):475-8. doi: 10.1017/S1092852914000637. [PubMed:25422900 ]
  4. Vachharajani NN, Yeleswaram K, Boulton DW: Preclinical pharmacokinetics and metabolism of BMS-214778, a novel melatonin receptor agonist. J Pharm Sci. 2003 Apr;92(4):760-72. [PubMed:12661062 ]
External Links
ATC CodesN05CH03
AHFS Codes
  • 28:24.92
PDB EntriesNot Available
FDA labelDownload (249 KB)
MSDSDownload (203 KB)
Interactions
Drug Interactions
Drug
7-NitroindazoleThe risk or severity of adverse effects can be increased when 7-Nitroindazole is combined with Tasimelteon.
AbirateroneThe serum concentration of Tasimelteon can be increased when it is combined with Abiraterone.
AcepromazineThe risk or severity of adverse effects can be increased when Acepromazine is combined with Tasimelteon.
AceprometazineThe risk or severity of adverse effects can be increased when Aceprometazine is combined with Tasimelteon.
adipiplonThe risk or severity of adverse effects can be increased when adipiplon is combined with Tasimelteon.
AgomelatineThe risk or severity of adverse effects can be increased when Agomelatine is combined with Tasimelteon.
AlfaxaloneThe risk or severity of adverse effects can be increased when Alfaxalone is combined with Tasimelteon.
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Tasimelteon.
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Alphacetylmethadol is combined with Tasimelteon.
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Tasimelteon.
AmiodaroneThe serum concentration of Tasimelteon can be increased when it is combined with Amiodarone.
AmisulprideThe risk or severity of adverse effects can be increased when Amisulpride is combined with Tasimelteon.
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Tasimelteon.
AmobarbitalThe risk or severity of adverse effects can be increased when Amobarbital is combined with Tasimelteon.
AmoxapineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Amoxapine.
AmperozideThe risk or severity of adverse effects can be increased when Amperozide is combined with Tasimelteon.
AripiprazoleThe risk or severity of adverse effects can be increased when Aripiprazole is combined with Tasimelteon.
ArticaineThe risk or severity of adverse effects can be increased when Articaine is combined with Tasimelteon.
AsenapineThe risk or severity of adverse effects can be increased when Asenapine is combined with Tasimelteon.
AtazanavirThe serum concentration of Tasimelteon can be increased when it is combined with Atazanavir.
AzaperoneThe risk or severity of adverse effects can be increased when Azaperone is combined with Tasimelteon.
AzelastineTasimelteon may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
AzelastineThe risk or severity of adverse effects can be increased when Azelastine is combined with Tasimelteon.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Tasimelteon.
BarbitalThe risk or severity of adverse effects can be increased when Barbital is combined with Tasimelteon.
BenzocaineThe risk or severity of adverse effects can be increased when Benzocaine is combined with Tasimelteon.
Benzyl alcoholThe risk or severity of adverse effects can be increased when Benzyl alcohol is combined with Tasimelteon.
BoceprevirThe serum concentration of Tasimelteon can be increased when it is combined with Boceprevir.
BrexpiprazoleThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Brexpiprazole.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.
BrimonidineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Brimonidine.
BromazepamThe risk or severity of adverse effects can be increased when Bromazepam is combined with Tasimelteon.
BrompheniramineThe risk or severity of adverse effects can be increased when Brompheniramine is combined with Tasimelteon.
BrotizolamThe risk or severity of adverse effects can be increased when Brotizolam is combined with Tasimelteon.
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with Tasimelteon.
BuprenorphineThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Tasimelteon.
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Tasimelteon.
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Tasimelteon.
ButacaineThe risk or severity of adverse effects can be increased when Butacaine is combined with Tasimelteon.
ButalbitalThe risk or severity of adverse effects can be increased when Butalbital is combined with Tasimelteon.
ButambenThe risk or severity of adverse effects can be increased when Butamben is combined with Tasimelteon.
ButethalThe risk or severity of adverse effects can be increased when Butethal is combined with Tasimelteon.
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Tasimelteon.
CarbamazepineThe serum concentration of Tasimelteon can be decreased when it is combined with Carbamazepine.
CarbamazepineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Carbamazepine.
CarbinoxamineThe risk or severity of adverse effects can be increased when Carbinoxamine is combined with Tasimelteon.
CarfentanilThe risk or severity of adverse effects can be increased when Carfentanil is combined with Tasimelteon.
CarisoprodolThe risk or severity of adverse effects can be increased when Carisoprodol is combined with Tasimelteon.
CeritinibThe serum concentration of Tasimelteon can be increased when it is combined with Ceritinib.
CetirizineThe risk or severity of adverse effects can be increased when Cetirizine is combined with Tasimelteon.
Chloral hydrateThe risk or severity of adverse effects can be increased when Chloral hydrate is combined with Tasimelteon.
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Tasimelteon.
ChlormezanoneThe risk or severity of adverse effects can be increased when Chlormezanone is combined with Tasimelteon.
ChloroprocaineThe risk or severity of adverse effects can be increased when Chloroprocaine is combined with Tasimelteon.
ChlorphenamineThe risk or severity of adverse effects can be increased when Chlorphenamine is combined with Tasimelteon.
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Tasimelteon.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Chlorprothixene is combined with Tasimelteon.
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Chlorzoxazone is combined with Tasimelteon.
CinchocaineThe risk or severity of adverse effects can be increased when Cinchocaine is combined with Tasimelteon.
CitalopramThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Citalopram.
ClarithromycinThe serum concentration of Tasimelteon can be increased when it is combined with Clarithromycin.
ClemastineThe risk or severity of adverse effects can be increased when Clemastine is combined with Tasimelteon.
ClidiniumThe risk or severity of adverse effects can be increased when Clidinium is combined with Tasimelteon.
ClobazamThe risk or severity of adverse effects can be increased when Clobazam is combined with Tasimelteon.
clomethiazoleThe risk or severity of adverse effects can be increased when clomethiazole is combined with Tasimelteon.
ClomipramineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Clomipramine.
ClonazepamThe risk or severity of adverse effects can be increased when Clonazepam is combined with Tasimelteon.
ClonidineThe risk or severity of adverse effects can be increased when Clonidine is combined with Tasimelteon.
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Tasimelteon.
ClozapineThe risk or severity of adverse effects can be increased when Clozapine is combined with Tasimelteon.
CobicistatThe serum concentration of Tasimelteon can be increased when it is combined with Cobicistat.
CocaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Tasimelteon.
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Tasimelteon.
CyclizineThe risk or severity of adverse effects can be increased when Cyclizine is combined with Tasimelteon.
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Tasimelteon.
CyproheptadineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Tasimelteon.
DantroleneThe risk or severity of adverse effects can be increased when Dantrolene is combined with Tasimelteon.
DapiprazoleThe risk or severity of adverse effects can be increased when Dapiprazole is combined with Tasimelteon.
DapoxetineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Dapoxetine.
DarunavirThe serum concentration of Tasimelteon can be increased when it is combined with Darunavir.
deramciclaneThe risk or severity of adverse effects can be increased when deramciclane is combined with Tasimelteon.
DesfluraneThe risk or severity of adverse effects can be increased when Desflurane is combined with Tasimelteon.
DesipramineThe risk or severity of adverse effects can be increased when Desipramine is combined with Tasimelteon.
DesloratadineThe risk or severity of adverse effects can be increased when Desloratadine is combined with Tasimelteon.
DetomidineThe risk or severity of adverse effects can be increased when Detomidine is combined with Tasimelteon.
DexbrompheniramineThe risk or severity of adverse effects can be increased when Dexbrompheniramine is combined with Tasimelteon.
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Tasimelteon.
DextromoramideThe risk or severity of adverse effects can be increased when Dextromoramide is combined with Tasimelteon.
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Tasimelteon.
DezocineThe risk or severity of adverse effects can be increased when Dezocine is combined with Tasimelteon.
DiazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Tasimelteon.
DifenoxinThe risk or severity of adverse effects can be increased when Difenoxin is combined with Tasimelteon.
DihydrocodeineThe risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Tasimelteon.
DihydroetorphineThe risk or severity of adverse effects can be increased when Dihydroetorphine is combined with Tasimelteon.
DihydromorphineThe risk or severity of adverse effects can be increased when Dihydromorphine is combined with Tasimelteon.
DimenhydrinateThe risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Tasimelteon.
DiphenhydramineThe risk or severity of adverse effects can be increased when Diphenhydramine is combined with Tasimelteon.
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with Tasimelteon.
DoramectinThe risk or severity of adverse effects can be increased when Doramectin is combined with Tasimelteon.
DoxepinThe risk or severity of adverse effects can be increased when Doxepin is combined with Tasimelteon.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.
DoxylamineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Doxylamine.
DPDPEThe risk or severity of adverse effects can be increased when DPDPE is combined with Tasimelteon.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.
DroperidolThe risk or severity of adverse effects can be increased when Droperidol is combined with Tasimelteon.
DrotebanolThe risk or severity of adverse effects can be increased when Drotebanol is combined with Tasimelteon.
DyclonineThe risk or severity of adverse effects can be increased when Dyclonine is combined with Tasimelteon.
EcgonineThe risk or severity of adverse effects can be increased when Ecgonine is combined with Tasimelteon.
ECGONINE METHYL ESTERThe risk or severity of adverse effects can be increased when ECGONINE METHYL ESTER is combined with Tasimelteon.
EfavirenzThe risk or severity of adverse effects can be increased when Efavirenz is combined with Tasimelteon.
EnfluraneThe risk or severity of adverse effects can be increased when Enflurane is combined with Tasimelteon.
EntacaponeThe risk or severity of adverse effects can be increased when Entacapone is combined with Tasimelteon.
EnzalutamideThe serum concentration of Tasimelteon can be decreased when it is combined with Enzalutamide.
EscitalopramThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Escitalopram.
EstazolamThe risk or severity of adverse effects can be increased when Estazolam is combined with Tasimelteon.
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Tasimelteon.
EthanolTasimelteon may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
EthanolThe risk or severity of adverse effects can be increased when Ethanol is combined with Tasimelteon.
EthchlorvynolThe risk or severity of adverse effects can be increased when Ethchlorvynol is combined with Tasimelteon.
EthosuximideThe risk or severity of adverse effects can be increased when Ethosuximide is combined with Tasimelteon.
EthotoinThe risk or severity of adverse effects can be increased when Ethotoin is combined with Tasimelteon.
Ethyl carbamateThe risk or severity of adverse effects can be increased when Ethyl carbamate is combined with Tasimelteon.
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Ethyl loflazepate is combined with Tasimelteon.
EthylmorphineThe risk or severity of adverse effects can be increased when Ethylmorphine is combined with Tasimelteon.
EtidocaineThe risk or severity of adverse effects can be increased when Etidocaine is combined with Tasimelteon.
EtifoxineThe risk or severity of adverse effects can be increased when Etifoxine is combined with Tasimelteon.
EtizolamThe risk or severity of adverse effects can be increased when Etizolam is combined with Tasimelteon.
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with Tasimelteon.
EtoperidoneThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Etoperidone.
EtorphineThe risk or severity of adverse effects can be increased when Etorphine is combined with Tasimelteon.
EzogabineThe risk or severity of adverse effects can be increased when Ezogabine is combined with Tasimelteon.
FelbamateThe risk or severity of adverse effects can be increased when Felbamate is combined with Tasimelteon.
FencamfamineThe risk or severity of adverse effects can be increased when Fencamfamine is combined with Tasimelteon.
FenfluramineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Fenfluramine.
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Tasimelteon.
FexofenadineThe risk or severity of adverse effects can be increased when Fexofenadine is combined with Tasimelteon.
FlibanserinThe risk or severity of adverse effects can be increased when Flibanserin is combined with Tasimelteon.
FludiazepamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Tasimelteon.
FlumazenilFlumazenil may decrease the sedative activities of Tasimelteon.
FlunarizineThe risk or severity of adverse effects can be increased when Flunarizine is combined with Tasimelteon.
FlunitrazepamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Tasimelteon.
FluoxetineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Fluoxetine.
FlupentixolThe risk or severity of adverse effects can be increased when Flupentixol is combined with Tasimelteon.
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Tasimelteon.
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Tasimelteon.
FluspirileneThe risk or severity of adverse effects can be increased when Fluspirilene is combined with Tasimelteon.
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Fluticasone Propionate is combined with Tasimelteon.
FluvoxamineThe serum concentration of Tasimelteon can be increased when it is combined with Fluvoxamine.
FluvoxamineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Fluvoxamine.
FosphenytoinThe serum concentration of Tasimelteon can be decreased when it is combined with Fosphenytoin.
FosphenytoinThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Fosphenytoin.
FospropofolThe risk or severity of adverse effects can be increased when Fospropofol is combined with Tasimelteon.
GabapentinThe risk or severity of adverse effects can be increased when Gabapentin is combined with Tasimelteon.
gabapentin enacarbilThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Tasimelteon.
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Gamma Hydroxybutyric Acid is combined with Tasimelteon.
GlutethimideThe risk or severity of adverse effects can be increased when Glutethimide is combined with Tasimelteon.
GuanfacineThe risk or severity of adverse effects can be increased when Guanfacine is combined with Tasimelteon.
HalazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Tasimelteon.
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with Tasimelteon.
HalothaneThe risk or severity of adverse effects can be increased when Halothane is combined with Tasimelteon.
HeroinThe risk or severity of adverse effects can be increased when Heroin is combined with Tasimelteon.
HexobarbitalThe risk or severity of adverse effects can be increased when Hexobarbital is combined with Tasimelteon.
HydrocodoneThe risk or severity of adverse effects can be increased when Hydrocodone is combined with Tasimelteon.
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Tasimelteon.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.
HydroxyzineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Hydroxyzine.
IdelalisibThe serum concentration of Tasimelteon can be increased when it is combined with Idelalisib.
IloperidoneThe risk or severity of adverse effects can be increased when Iloperidone is combined with Tasimelteon.
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Tasimelteon.
IndalpineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Indalpine.
IndinavirThe serum concentration of Tasimelteon can be increased when it is combined with Indinavir.
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Tasimelteon.
ItraconazoleThe serum concentration of Tasimelteon can be increased when it is combined with Itraconazole.
KetamineThe risk or severity of adverse effects can be increased when Ketamine is combined with Tasimelteon.
KetazolamThe risk or severity of adverse effects can be increased when Ketazolam is combined with Tasimelteon.
KetobemidoneThe risk or severity of adverse effects can be increased when Ketobemidone is combined with Tasimelteon.
KetoconazoleThe serum concentration of Tasimelteon can be increased when it is combined with Ketoconazole.
LamotrigineThe risk or severity of adverse effects can be increased when Lamotrigine is combined with Tasimelteon.
LevetiracetamThe risk or severity of adverse effects can be increased when Levetiracetam is combined with Tasimelteon.
LevobupivacaineThe risk or severity of adverse effects can be increased when Levobupivacaine is combined with Tasimelteon.
LevocabastineThe risk or severity of adverse effects can be increased when Levocabastine is combined with Tasimelteon.
LevocetirizineThe risk or severity of adverse effects can be increased when Levocetirizine is combined with Tasimelteon.
LevodopaThe risk or severity of adverse effects can be increased when Levodopa is combined with Tasimelteon.
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Levomethadyl Acetate is combined with Tasimelteon.
LevomilnacipranThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Levomilnacipran.
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Tasimelteon.
LidocaineThe risk or severity of adverse effects can be increased when Lidocaine is combined with Tasimelteon.
LithiumThe risk or severity of adverse effects can be increased when Lithium is combined with Tasimelteon.
LofentanilThe risk or severity of adverse effects can be increased when Lofentanil is combined with Tasimelteon.
LopinavirThe serum concentration of Tasimelteon can be increased when it is combined with Lopinavir.
LoratadineThe risk or severity of adverse effects can be increased when Loratadine is combined with Tasimelteon.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Tasimelteon.
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Tasimelteon.
Lu AA21004The risk or severity of adverse effects can be increased when Tasimelteon is combined with Lu AA21004.
LurasidoneThe risk or severity of adverse effects can be increased when Lurasidone is combined with Tasimelteon.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.
Magnesium SulfateThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Magnesium Sulfate.
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with Tasimelteon.
MeclizineThe risk or severity of adverse effects can be increased when Meclizine is combined with Tasimelteon.
MedetomidineThe risk or severity of adverse effects can be increased when Medetomidine is combined with Tasimelteon.
MelatoninThe risk or severity of adverse effects can be increased when Melatonin is combined with Tasimelteon.
MelperoneThe risk or severity of adverse effects can be increased when Melperone is combined with Tasimelteon.
MepivacaineThe risk or severity of adverse effects can be increased when Mepivacaine is combined with Tasimelteon.
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Tasimelteon.
MesoridazineThe risk or severity of adverse effects can be increased when Mesoridazine is combined with Tasimelteon.
MetaxaloneThe risk or severity of adverse effects can be increased when Metaxalone is combined with Tasimelteon.
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Tasimelteon.
Methadyl AcetateThe risk or severity of adverse effects can be increased when Methadyl Acetate is combined with Tasimelteon.
MethapyrileneThe risk or severity of adverse effects can be increased when Methapyrilene is combined with Tasimelteon.
MethaqualoneThe risk or severity of adverse effects can be increased when Methaqualone is combined with Tasimelteon.
MethocarbamolThe risk or severity of adverse effects can be increased when Methocarbamol is combined with Tasimelteon.
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with Tasimelteon.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Methotrimeprazine is combined with Tasimelteon.
MethoxyfluraneThe risk or severity of adverse effects can be increased when Methoxyflurane is combined with Tasimelteon.
MethsuximideThe risk or severity of adverse effects can be increased when Methsuximide is combined with Tasimelteon.
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Methylphenobarbital is combined with Tasimelteon.
MetyrosineTasimelteon may increase the sedative activities of Metyrosine.
MexiletineThe serum concentration of Tasimelteon can be increased when it is combined with Mexiletine.
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Tasimelteon.
MilnacipranThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Milnacipran.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.
MirtazapineTasimelteon may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MirtazapineThe risk or severity of adverse effects can be increased when Mirtazapine is combined with Tasimelteon.
MitotaneThe serum concentration of Tasimelteon can be decreased when it is combined with Mitotane.
MolindoneThe risk or severity of adverse effects can be increased when Molindone is combined with Tasimelteon.
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Tasimelteon.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.
NabiloneThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Nabilone.
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Tasimelteon.
NefazodoneThe serum concentration of Tasimelteon can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Tasimelteon can be increased when it is combined with Nelfinavir.
NevirapineThe serum concentration of Tasimelteon can be decreased when it is combined with Nevirapine.
NitrazepamThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Tasimelteon.
Nitrous oxideThe risk or severity of adverse effects can be increased when Nitrous oxide is combined with Tasimelteon.
NormethadoneThe risk or severity of adverse effects can be increased when Normethadone is combined with Tasimelteon.
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Tasimelteon.
OlanzapineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Olanzapine.
OlopatadineThe risk or severity of adverse effects can be increased when Olopatadine is combined with Tasimelteon.
OndansetronThe risk or severity of adverse effects can be increased when Ondansetron is combined with Tasimelteon.
OpiumThe risk or severity of adverse effects can be increased when Opium is combined with Tasimelteon.
OrphenadrineTasimelteon may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
OrphenadrineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Tasimelteon.
OsanetantThe risk or severity of adverse effects can be increased when Osanetant is combined with Tasimelteon.
OxazepamThe risk or severity of adverse effects can be increased when Oxazepam is combined with Tasimelteon.
OxprenololThe risk or severity of adverse effects can be increased when Oxprenolol is combined with Tasimelteon.
OxybuprocaineThe risk or severity of adverse effects can be increased when Oxybuprocaine is combined with Tasimelteon.
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Tasimelteon.
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Tasimelteon.
PaliperidoneThe risk or severity of adverse effects can be increased when Paliperidone is combined with Tasimelteon.
ParaldehydeTasimelteon may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParaldehydeThe risk or severity of adverse effects can be increased when Paraldehyde is combined with Tasimelteon.
ParoxetineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Paroxetine.
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Tasimelteon.
PentobarbitalThe serum concentration of Tasimelteon can be decreased when it is combined with Pentobarbital.
PentobarbitalThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Pentobarbital.
PerampanelThe risk or severity of adverse effects can be increased when Perampanel is combined with Tasimelteon.
PerospironeThe risk or severity of adverse effects can be increased when Perospirone is combined with Tasimelteon.
PerphenazineThe risk or severity of adverse effects can be increased when Perphenazine is combined with Tasimelteon.
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Tasimelteon.
PhenobarbitalThe serum concentration of Tasimelteon can be decreased when it is combined with Phenobarbital.
PhenobarbitalThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Phenobarbital.
PhenoxyethanolThe risk or severity of adverse effects can be increased when Phenoxyethanol is combined with Tasimelteon.
PhenytoinThe serum concentration of Tasimelteon can be decreased when it is combined with Phenytoin.
PhenytoinThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Phenytoin.
PimozideThe risk or severity of adverse effects can be increased when Pimozide is combined with Tasimelteon.
PipamperoneThe risk or severity of adverse effects can be increased when Pipamperone is combined with Tasimelteon.
PipotiazineThe risk or severity of adverse effects can be increased when Pipotiazine is combined with Tasimelteon.
PizotifenThe risk or severity of adverse effects can be increased when Pizotifen is combined with Tasimelteon.
PomalidomideThe risk or severity of adverse effects can be increased when Pomalidomide is combined with Tasimelteon.
PosaconazoleThe serum concentration of Tasimelteon can be increased when it is combined with Posaconazole.
PramipexoleTasimelteon may increase the sedative activities of Pramipexole.
PramocaineThe risk or severity of adverse effects can be increased when Pramocaine is combined with Tasimelteon.
PrazepamThe risk or severity of adverse effects can be increased when Prazepam is combined with Tasimelteon.
PregabalinThe risk or severity of adverse effects can be increased when Pregabalin is combined with Tasimelteon.
PrilocaineThe risk or severity of adverse effects can be increased when Prilocaine is combined with Tasimelteon.
PrimidoneThe serum concentration of Tasimelteon can be decreased when it is combined with Primidone.
PrimidoneThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Primidone.
ProcaineThe risk or severity of adverse effects can be increased when Procaine is combined with Tasimelteon.
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Tasimelteon.
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Tasimelteon.
PromethazineThe risk or severity of adverse effects can be increased when Promethazine is combined with Tasimelteon.
ProparacaineThe risk or severity of adverse effects can be increased when Proparacaine is combined with Tasimelteon.
PropofolThe risk or severity of adverse effects can be increased when Propofol is combined with Tasimelteon.
PropoxycaineThe risk or severity of adverse effects can be increased when Propoxycaine is combined with Tasimelteon.
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Tasimelteon.
PSD502The risk or severity of adverse effects can be increased when PSD502 is combined with Tasimelteon.
QuazepamThe risk or severity of adverse effects can be increased when Quazepam is combined with Tasimelteon.
QuetiapineThe risk or severity of adverse effects can be increased when Quetiapine is combined with Tasimelteon.
RamelteonThe risk or severity of adverse effects can be increased when Ramelteon is combined with Tasimelteon.
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Tasimelteon.
RemoxiprideThe risk or severity of adverse effects can be increased when Remoxipride is combined with Tasimelteon.
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Tasimelteon.
RifabutinThe serum concentration of Tasimelteon can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Tasimelteon can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Tasimelteon can be decreased when it is combined with Rifapentine.
RisperidoneThe risk or severity of adverse effects can be increased when Risperidone is combined with Tasimelteon.
RitonavirThe serum concentration of Tasimelteon can be increased when it is combined with Ritonavir.
RomifidineThe risk or severity of adverse effects can be increased when Romifidine is combined with Tasimelteon.
RopiniroleTasimelteon may increase the sedative activities of Ropinirole.
RopivacaineThe risk or severity of adverse effects can be increased when Ropivacaine is combined with Tasimelteon.
RotigotineTasimelteon may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Tasimelteon.
S-EthylisothioureaThe risk or severity of adverse effects can be increased when S-Ethylisothiourea is combined with Tasimelteon.
SaquinavirThe serum concentration of Tasimelteon can be increased when it is combined with Saquinavir.
ScopolamineThe risk or severity of adverse effects can be increased when Scopolamine is combined with Tasimelteon.
SecobarbitalThe risk or severity of adverse effects can be increased when Secobarbital is combined with Tasimelteon.
SertindoleThe risk or severity of adverse effects can be increased when Sertindole is combined with Tasimelteon.
SertralineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Sertraline.
SevofluraneThe risk or severity of adverse effects can be increased when Sevoflurane is combined with Tasimelteon.
Sodium oxybateTasimelteon may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Sodium oxybateThe risk or severity of adverse effects can be increased when Sodium oxybate is combined with Tasimelteon.
StiripentolThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Stiripentol.
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Tasimelteon.
SulpirideThe risk or severity of adverse effects can be increased when Sulpiride is combined with Tasimelteon.
SuvorexantThe risk or severity of adverse effects can be increased when Suvorexant is combined with Tasimelteon.
TapentadolThe risk or severity of adverse effects can be increased when Tapentadol is combined with Tasimelteon.
TelaprevirThe serum concentration of Tasimelteon can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Tasimelteon can be increased when it is combined with Telithromycin.
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Tasimelteon.
TetrabenazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Tasimelteon.
TetracaineThe risk or severity of adverse effects can be increased when Tetracaine is combined with Tasimelteon.
TetrodotoxinThe risk or severity of adverse effects can be increased when Tetrodotoxin is combined with Tasimelteon.
ThalidomideTasimelteon may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ThalidomideThe risk or severity of adverse effects can be increased when Thalidomide is combined with Tasimelteon.
ThiamylalThe risk or severity of adverse effects can be increased when Thiamylal is combined with Tasimelteon.
ThiopentalThe risk or severity of adverse effects can be increased when Thiopental is combined with Tasimelteon.
ThioridazineThe risk or severity of adverse effects can be increased when Thioridazine is combined with Tasimelteon.
ThiothixeneThe risk or severity of adverse effects can be increased when Thiothixene is combined with Tasimelteon.
TiagabineThe risk or severity of adverse effects can be increased when Tiagabine is combined with Tasimelteon.
TiletamineThe risk or severity of adverse effects can be increased when Tiletamine is combined with Tasimelteon.
TizanidineThe risk or severity of adverse effects can be increased when Tizanidine is combined with Tasimelteon.
TolcaponeThe risk or severity of adverse effects can be increased when Tolcapone is combined with Tasimelteon.
TopiramateThe risk or severity of adverse effects can be increased when Topiramate is combined with Tasimelteon.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Tasimelteon.
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Trans-2-Phenylcyclopropylamine is combined with Tasimelteon.
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Tasimelteon.
TrazodoneThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Trazodone.
TriazolamThe risk or severity of adverse effects can be increased when Triazolam is combined with Tasimelteon.
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Tasimelteon.
TriflupromazineThe risk or severity of adverse effects can be increased when Triflupromazine is combined with Tasimelteon.
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Tasimelteon.
TriprolidineThe risk or severity of adverse effects can be increased when Triprolidine is combined with Tasimelteon.
Valproic AcidThe risk or severity of adverse effects can be increased when Valproic Acid is combined with Tasimelteon.
VigabatrinThe risk or severity of adverse effects can be increased when Vigabatrin is combined with Tasimelteon.
VilazodoneThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Vilazodone.
VoriconazoleThe serum concentration of Tasimelteon can be increased when it is combined with Voriconazole.
VortioxetineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Vortioxetine.
XylazineThe risk or severity of adverse effects can be increased when Xylazine is combined with Tasimelteon.
ZaleplonThe risk or severity of adverse effects can be increased when Zaleplon is combined with Tasimelteon.
ZiconotideThe risk or severity of adverse effects can be increased when Ziconotide is combined with Tasimelteon.
ZimelidineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Zimelidine.
ZiprasidoneThe risk or severity of adverse effects can be increased when Ziprasidone is combined with Tasimelteon.
ZolazepamThe risk or severity of adverse effects can be increased when Zolazepam is combined with Tasimelteon.
ZolpidemThe risk or severity of adverse effects can be increased when Zolpidem is combined with Tasimelteon.
ZonisamideThe risk or severity of adverse effects can be increased when Zonisamide is combined with Tasimelteon.
ZopicloneThe risk or severity of adverse effects can be increased when Zopiclone is combined with Tasimelteon.
ZotepineThe risk or severity of adverse effects can be increased when Zotepine is combined with Tasimelteon.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Zuclopenthixol is combined with Tasimelteon.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Organic cyclic compound binding
Specific Function:
High affinity receptor for melatonin. Likely to mediates the reproductive and circadian actions of melatonin. The activity of this receptor is mediated by pertussis toxin sensitive G proteins that inhibit adenylate cyclase activity.
Gene Name:
MTNR1A
Uniprot ID:
P48039
Molecular Weight:
39374.315 Da
References
  1. Lavedan C, Forsberg M, Gentile AJ: Tasimelteon: a selective and unique receptor binding profile. Neuropharmacology. 2015 Apr;91:142-7. doi: 10.1016/j.neuropharm.2014.12.004. Epub 2014 Dec 19. [PubMed:25534555 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Melatonin receptor activity
Specific Function:
High affinity receptor for melatonin. Likely to mediates the reproductive and circadian actions of melatonin. The activity of this receptor is mediated by pertussis toxin sensitive G proteins that inhibit adenylate cyclase activity.
Gene Name:
MTNR1B
Uniprot ID:
P49286
Molecular Weight:
40187.895 Da
References
  1. Lavedan C, Forsberg M, Gentile AJ: Tasimelteon: a selective and unique receptor binding profile. Neuropharmacology. 2015 Apr;91:142-7. doi: 10.1016/j.neuropharm.2014.12.004. Epub 2014 Dec 19. [PubMed:25534555 ]
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Drug created on May 14, 2015 10:07 / Updated on August 31, 2016 02:14