You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameTasimelteon
Accession NumberDB09071
TypeSmall Molecule
GroupsApproved
DescriptionTasimelteon 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
HetliozCapsule20 mgOralVanda Pharmaceuticals Ltd2015-07-03Not applicableEu
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
Pharmacology
IndicationTasimelteon is indicated for the treatment of Non-24-Hour Sleep-Wake Disorder (N24HSWD).
Structured Indications
PharmacodynamicsNot Available
Mechanism of actionTasimelteon is a selective dual agonist of the melatonin receptors MT1 and MT2.
TargetKindPharmacological actionActionsOrganismUniProt ID
Melatonin receptor type 1AProteinyes
agonist
HumanP48039 details
Melatonin receptor type 1BProteinyes
agonist
HumanP49286 details
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
Interactions
Drug Interactions
DrugInteractionDrug group
1,1,1,2 TetrafluoroethaneThe risk or severity of adverse effects can be increased when Tasimelteon is combined with 1,1,1,2 Tetrafluoroethane.Investigational
7-NitroindazoleThe risk or severity of adverse effects can be increased when 7-Nitroindazole is combined with Tasimelteon.Experimental
AbirateroneThe serum concentration of Tasimelteon can be increased when it is combined with Abiraterone.Approved
AcepromazineThe risk or severity of adverse effects can be increased when Acepromazine is combined with Tasimelteon.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Aceprometazine is combined with Tasimelteon.Approved
adipiplonThe risk or severity of adverse effects can be increased when adipiplon is combined with Tasimelteon.Investigational
AgomelatineThe risk or severity of adverse effects can be increased when Agomelatine is combined with Tasimelteon.Approved, Investigational
AlfaxaloneThe risk or severity of adverse effects can be increased when Alfaxalone is combined with Tasimelteon.Vet Approved
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Tasimelteon.Approved, Illicit
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Alphacetylmethadol is combined with Tasimelteon.Experimental, Illicit
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Tasimelteon.Approved, Illicit, Investigational
AmiodaroneThe serum concentration of Tasimelteon can be increased when it is combined with Amiodarone.Approved, Investigational
AmisulprideThe risk or severity of adverse effects can be increased when Amisulpride is combined with Tasimelteon.Approved, Investigational
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Tasimelteon.Approved
AmobarbitalThe risk or severity of adverse effects can be increased when Amobarbital is combined with Tasimelteon.Approved, Illicit
AmoxapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Tasimelteon.Approved
AmperozideThe risk or severity of adverse effects can be increased when Amperozide is combined with Tasimelteon.Experimental
AripiprazoleThe risk or severity of adverse effects can be increased when Aripiprazole is combined with Tasimelteon.Approved, Investigational
ArticaineThe risk or severity of adverse effects can be increased when Articaine is combined with Tasimelteon.Approved
AsenapineThe risk or severity of adverse effects can be increased when Asenapine is combined with Tasimelteon.Approved
AtazanavirThe serum concentration of Tasimelteon can be increased when it is combined with Atazanavir.Approved, Investigational
AzaperoneThe risk or severity of adverse effects can be increased when Azaperone is combined with Tasimelteon.Vet Approved
AzelastineTasimelteon may increase the central nervous system depressant (CNS depressant) activities of Azelastine.Approved
AzelastineThe risk or severity of adverse effects can be increased when Azelastine is combined with Tasimelteon.Approved
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Tasimelteon.Approved
BarbitalThe risk or severity of adverse effects can be increased when Barbital is combined with Tasimelteon.Illicit
BenperidolThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Benperidol.Investigational
BenzocaineThe risk or severity of adverse effects can be increased when Benzocaine is combined with Tasimelteon.Approved
Benzyl alcoholThe risk or severity of adverse effects can be increased when Benzyl alcohol is combined with Tasimelteon.Approved
BoceprevirThe serum concentration of Tasimelteon can be increased when it is combined with Boceprevir.Approved
BrexpiprazoleThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Brexpiprazole.Approved
BrimonidineThe risk or severity of adverse effects can be increased when Brimonidine is combined with Tasimelteon.Approved
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.Approved
BromazepamThe risk or severity of adverse effects can be increased when Bromazepam is combined with Tasimelteon.Approved, Illicit
BrompheniramineThe risk or severity of adverse effects can be increased when Brompheniramine is combined with Tasimelteon.Approved
BrotizolamThe risk or severity of adverse effects can be increased when Brotizolam is combined with Tasimelteon.Approved, Withdrawn
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with Tasimelteon.Approved, Investigational
BuprenorphineTasimelteon may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Tasimelteon.Approved, Investigational
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Tasimelteon.Approved, Illicit
ButacaineThe risk or severity of adverse effects can be increased when Butacaine is combined with Tasimelteon.Vet Approved
ButalbitalThe risk or severity of adverse effects can be increased when Butalbital is combined with Tasimelteon.Approved, Illicit
ButambenThe risk or severity of adverse effects can be increased when Butamben is combined with Tasimelteon.Approved
ButethalThe risk or severity of adverse effects can be increased when Butethal is combined with Tasimelteon.Approved, Illicit
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Tasimelteon.Approved, Illicit, Vet Approved
CarbamazepineThe serum concentration of Tasimelteon can be decreased when it is combined with Carbamazepine.Approved, Investigational
CarbinoxamineThe risk or severity of adverse effects can be increased when Carbinoxamine is combined with Tasimelteon.Approved
CarfentanilThe risk or severity of adverse effects can be increased when Carfentanil is combined with Tasimelteon.Illicit, Vet Approved
CarisoprodolThe risk or severity of adverse effects can be increased when Carisoprodol is combined with Tasimelteon.Approved
CeritinibThe serum concentration of Tasimelteon can be increased when it is combined with Ceritinib.Approved
CetirizineThe risk or severity of adverse effects can be increased when Cetirizine is combined with Tasimelteon.Approved
Chloral hydrateThe risk or severity of adverse effects can be increased when Chloral hydrate is combined with Tasimelteon.Approved, Illicit, Vet Approved
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Tasimelteon.Approved, Illicit
ChlormezanoneThe risk or severity of adverse effects can be increased when Chlormezanone is combined with Tasimelteon.Approved, Withdrawn
ChloroprocaineThe risk or severity of adverse effects can be increased when Chloroprocaine is combined with Tasimelteon.Approved
ChlorphenamineThe risk or severity of adverse effects can be increased when Chlorphenamine is combined with Tasimelteon.Approved
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Tasimelteon.Approved, Vet Approved
ChlorprothixeneThe risk or severity of adverse effects can be increased when Chlorprothixene is combined with Tasimelteon.Approved, Withdrawn
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Chlorzoxazone is combined with Tasimelteon.Approved
CinchocaineThe risk or severity of adverse effects can be increased when Cinchocaine is combined with Tasimelteon.Approved, Vet Approved
CitalopramThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Citalopram.Approved
ClarithromycinThe serum concentration of Tasimelteon can be increased when it is combined with Clarithromycin.Approved
ClemastineThe risk or severity of adverse effects can be increased when Clemastine is combined with Tasimelteon.Approved
ClidiniumThe risk or severity of adverse effects can be increased when Clidinium is combined with Tasimelteon.Approved
ClobazamThe risk or severity of adverse effects can be increased when Clobazam is combined with Tasimelteon.Approved, Illicit
clomethiazoleThe risk or severity of adverse effects can be increased when clomethiazole is combined with Tasimelteon.Investigational
ClomipramineThe risk or severity of adverse effects can be increased when Clomipramine is combined with Tasimelteon.Approved, Vet Approved
ClonazepamThe risk or severity of adverse effects can be increased when Clonazepam is combined with Tasimelteon.Approved, Illicit
ClonidineThe risk or severity of adverse effects can be increased when Clonidine is combined with Tasimelteon.Approved
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Tasimelteon.Approved, Illicit
ClozapineThe risk or severity of adverse effects can be increased when Clozapine is combined with Tasimelteon.Approved
CobicistatThe serum concentration of Tasimelteon can be increased when it is combined with Cobicistat.Approved
CocaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Tasimelteon.Approved, Illicit
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Tasimelteon.Approved, Illicit
CyclizineThe risk or severity of adverse effects can be increased when Cyclizine is combined with Tasimelteon.Approved
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Tasimelteon.Approved
CyproheptadineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Tasimelteon.Approved
DantroleneThe risk or severity of adverse effects can be increased when Dantrolene is combined with Tasimelteon.Approved
DapiprazoleThe risk or severity of adverse effects can be increased when Dapiprazole is combined with Tasimelteon.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Dapoxetine.Investigational
DarunavirThe serum concentration of Tasimelteon can be increased when it is combined with Darunavir.Approved
deramciclaneThe risk or severity of adverse effects can be increased when deramciclane is combined with Tasimelteon.Investigational
DesfluraneThe risk or severity of adverse effects can be increased when Desflurane is combined with Tasimelteon.Approved
DesipramineThe risk or severity of adverse effects can be increased when Desipramine is combined with Tasimelteon.Approved
DesloratadineThe risk or severity of adverse effects can be increased when Desloratadine is combined with Tasimelteon.Approved, Investigational
DesvenlafaxineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Desvenlafaxine.Approved
DetomidineThe risk or severity of adverse effects can be increased when Detomidine is combined with Tasimelteon.Vet Approved
DexbrompheniramineThe risk or severity of adverse effects can be increased when Dexbrompheniramine is combined with Tasimelteon.Approved
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Tasimelteon.Approved, Vet Approved
DextromoramideThe risk or severity of adverse effects can be increased when Dextromoramide is combined with Tasimelteon.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Tasimelteon.Approved, Illicit, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Dezocine is combined with Tasimelteon.Approved
DiazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Tasimelteon.Approved, Illicit, Vet Approved
DifenoxinThe risk or severity of adverse effects can be increased when Difenoxin is combined with Tasimelteon.Approved, Illicit
DihydrocodeineThe risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Tasimelteon.Approved, Illicit
DihydroetorphineThe risk or severity of adverse effects can be increased when Dihydroetorphine is combined with Tasimelteon.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Dihydromorphine is combined with Tasimelteon.Experimental, Illicit
DimenhydrinateThe risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Tasimelteon.Approved
DiphenhydramineThe risk or severity of adverse effects can be increased when Diphenhydramine is combined with Tasimelteon.Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with Tasimelteon.Approved, Illicit
DoramectinThe risk or severity of adverse effects can be increased when Doramectin is combined with Tasimelteon.Vet Approved
DoxepinThe risk or severity of adverse effects can be increased when Doxepin is combined with Tasimelteon.Approved
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.Approved, Vet Approved
DPDPEThe risk or severity of adverse effects can be increased when DPDPE is combined with Tasimelteon.Investigational
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.Approved, Illicit
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.Approved, Vet Approved
DrotebanolThe risk or severity of adverse effects can be increased when Drotebanol is combined with Tasimelteon.Experimental, Illicit
DuloxetineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Duloxetine.Approved
DyclonineThe risk or severity of adverse effects can be increased when Dyclonine is combined with Tasimelteon.Approved
EcgonineThe risk or severity of adverse effects can be increased when Ecgonine is combined with Tasimelteon.Experimental, Illicit
ECGONINE METHYL ESTERThe risk or severity of adverse effects can be increased when ECGONINE METHYL ESTER is combined with Tasimelteon.Experimental
EcopipamThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Ecopipam.Investigational
EfavirenzThe risk or severity of adverse effects can be increased when Efavirenz is combined with Tasimelteon.Approved, Investigational
EnfluraneThe risk or severity of adverse effects can be increased when Enflurane is combined with Tasimelteon.Approved, Vet Approved
EntacaponeThe risk or severity of adverse effects can be increased when Entacapone is combined with Tasimelteon.Approved, Investigational
EnzalutamideThe serum concentration of Tasimelteon can be decreased when it is combined with Enzalutamide.Approved
EscitalopramThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Escitalopram.Approved, Investigational
EstazolamThe risk or severity of adverse effects can be increased when Estazolam is combined with Tasimelteon.Approved, Illicit
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Tasimelteon.Approved
EthanolTasimelteon may increase the central nervous system depressant (CNS depressant) activities of Ethanol.Approved
EthchlorvynolThe risk or severity of adverse effects can be increased when Ethchlorvynol is combined with Tasimelteon.Approved, Illicit, Withdrawn
EthosuximideThe risk or severity of adverse effects can be increased when Ethosuximide is combined with Tasimelteon.Approved
EthotoinThe risk or severity of adverse effects can be increased when Ethotoin is combined with Tasimelteon.Approved
Ethyl carbamateThe risk or severity of adverse effects can be increased when Ethyl carbamate is combined with Tasimelteon.Withdrawn
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Ethyl loflazepate is combined with Tasimelteon.Approved, Illicit
EthylmorphineThe risk or severity of adverse effects can be increased when Ethylmorphine is combined with Tasimelteon.Approved, Illicit
EtidocaineThe risk or severity of adverse effects can be increased when Etidocaine is combined with Tasimelteon.Approved
EtifoxineThe risk or severity of adverse effects can be increased when Etifoxine is combined with Tasimelteon.Withdrawn
EtizolamThe risk or severity of adverse effects can be increased when Etizolam is combined with Tasimelteon.Approved
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with Tasimelteon.Approved
EtoperidoneThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Etoperidone.Approved
EtorphineThe risk or severity of adverse effects can be increased when Etorphine is combined with Tasimelteon.Illicit, Vet Approved
EzogabineThe risk or severity of adverse effects can be increased when Ezogabine is combined with Tasimelteon.Approved
FelbamateThe risk or severity of adverse effects can be increased when Felbamate is combined with Tasimelteon.Approved
FencamfamineThe risk or severity of adverse effects can be increased when Fencamfamine is combined with Tasimelteon.Approved, Illicit, Withdrawn
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Tasimelteon.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe risk or severity of adverse effects can be increased when Fexofenadine is combined with Tasimelteon.Approved
FlibanserinThe risk or severity of adverse effects can be increased when Flibanserin is combined with Tasimelteon.Approved
FludiazepamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Tasimelteon.Approved, Illicit
FlumazenilFlumazenil may decrease the sedative activities of Tasimelteon.Approved
FlunarizineThe risk or severity of adverse effects can be increased when Flunarizine is combined with Tasimelteon.Approved
FlunitrazepamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Tasimelteon.Approved, Illicit
FluoxetineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe risk or severity of adverse effects can be increased when Flupentixol is combined with Tasimelteon.Approved, Withdrawn
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Tasimelteon.Approved
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Tasimelteon.Approved, Illicit
FluspirileneThe risk or severity of adverse effects can be increased when Fluspirilene is combined with Tasimelteon.Approved
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Fluticasone Propionate is combined with Tasimelteon.Approved
FluvoxamineThe serum concentration of Tasimelteon can be increased when it is combined with Fluvoxamine.Approved, Investigational
FosphenytoinThe serum concentration of Tasimelteon can be decreased when it is combined with Fosphenytoin.Approved
FospropofolThe risk or severity of adverse effects can be increased when Fospropofol is combined with Tasimelteon.Approved, Illicit
GabapentinThe risk or severity of adverse effects can be increased when Gabapentin is combined with Tasimelteon.Approved, Investigational
gabapentin enacarbilThe risk or severity of adverse effects can be increased when gabapentin enacarbil is combined with Tasimelteon.Approved
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Gamma Hydroxybutyric Acid is combined with Tasimelteon.Approved, Illicit
GepironeThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Gepirone.Investigational
GlutethimideThe risk or severity of adverse effects can be increased when Glutethimide is combined with Tasimelteon.Approved, Illicit
GuanfacineThe risk or severity of adverse effects can be increased when Guanfacine is combined with Tasimelteon.Approved, Investigational
HalazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Tasimelteon.Approved, Illicit, Withdrawn
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with Tasimelteon.Approved
HalothaneThe risk or severity of adverse effects can be increased when Halothane is combined with Tasimelteon.Approved, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Heroin is combined with Tasimelteon.Approved, Illicit
HexobarbitalThe risk or severity of adverse effects can be increased when Hexobarbital is combined with Tasimelteon.Approved
HydrocodoneTasimelteon may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.Approved, Illicit
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Tasimelteon.Approved, Illicit
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.Approved
IdelalisibThe serum concentration of Tasimelteon can be increased when it is combined with Idelalisib.Approved
IloperidoneThe risk or severity of adverse effects can be increased when Iloperidone is combined with Tasimelteon.Approved
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Tasimelteon.Approved
IndalpineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Indalpine.Investigational, Withdrawn
IndinavirThe serum concentration of Tasimelteon can be increased when it is combined with Indinavir.Approved
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Tasimelteon.Approved, Vet Approved
ItraconazoleThe serum concentration of Tasimelteon can be increased when it is combined with Itraconazole.Approved, Investigational
KetamineThe risk or severity of adverse effects can be increased when Ketamine is combined with Tasimelteon.Approved, Vet Approved
KetazolamThe risk or severity of adverse effects can be increased when Ketazolam is combined with Tasimelteon.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Ketobemidone is combined with Tasimelteon.Approved
KetoconazoleThe serum concentration of Tasimelteon can be increased when it is combined with Ketoconazole.Approved, Investigational
LamotrigineThe risk or severity of adverse effects can be increased when Lamotrigine is combined with Tasimelteon.Approved, Investigational
LevetiracetamThe risk or severity of adverse effects can be increased when Levetiracetam is combined with Tasimelteon.Approved, Investigational
LevobupivacaineThe risk or severity of adverse effects can be increased when Levobupivacaine is combined with Tasimelteon.Approved
LevocabastineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Levocabastine.Approved
LevocetirizineThe risk or severity of adverse effects can be increased when Levocetirizine is combined with Tasimelteon.Approved
LevodopaThe risk or severity of adverse effects can be increased when Levodopa is combined with Tasimelteon.Approved
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Levomethadyl Acetate is combined with Tasimelteon.Approved
LevomilnacipranThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Levomilnacipran.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Tasimelteon.Approved
LidocaineThe risk or severity of adverse effects can be increased when Lidocaine is combined with Tasimelteon.Approved, Vet Approved
LithiumThe risk or severity of adverse effects can be increased when Lithium is combined with Tasimelteon.Approved
LofentanilThe risk or severity of adverse effects can be increased when Lofentanil is combined with Tasimelteon.Illicit
LopinavirThe serum concentration of Tasimelteon can be increased when it is combined with Lopinavir.Approved
LoratadineThe risk or severity of adverse effects can be increased when Loratadine is combined with Tasimelteon.Approved
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Tasimelteon.Approved
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Tasimelteon.Approved
Lu AA21004The risk or severity of adverse effects can be increased when Lu AA21004 is combined with Tasimelteon.Investigational
LumacaftorThe serum concentration of Tasimelteon can be decreased when it is combined with Lumacaftor.Approved
LurasidoneThe risk or severity of adverse effects can be increased when Lurasidone is combined with Tasimelteon.Approved
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.Approved, Vet Approved
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with Tasimelteon.Approved
MeclizineThe risk or severity of adverse effects can be increased when Meclizine is combined with Tasimelteon.Approved
MedetomidineThe risk or severity of adverse effects can be increased when Medetomidine is combined with Tasimelteon.Vet Approved
MelatoninThe risk or severity of adverse effects can be increased when Melatonin is combined with Tasimelteon.Approved, Nutraceutical, Vet Approved
MelperoneThe risk or severity of adverse effects can be increased when Melperone is combined with Tasimelteon.Approved
MepivacaineThe risk or severity of adverse effects can be increased when Mepivacaine is combined with Tasimelteon.Approved, Vet Approved
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Tasimelteon.Approved, Illicit
MesoridazineThe risk or severity of adverse effects can be increased when Mesoridazine is combined with Tasimelteon.Approved
MetaxaloneThe risk or severity of adverse effects can be increased when Metaxalone is combined with Tasimelteon.Approved
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Tasimelteon.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Methadyl Acetate is combined with Tasimelteon.Approved, Illicit
MethapyrileneThe risk or severity of adverse effects can be increased when Methapyrilene is combined with Tasimelteon.Withdrawn
MethaqualoneThe risk or severity of adverse effects can be increased when Methaqualone is combined with Tasimelteon.Illicit, Withdrawn
MethocarbamolThe risk or severity of adverse effects can be increased when Methocarbamol is combined with Tasimelteon.Approved, Vet Approved
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with Tasimelteon.Approved
MethotrimeprazineTasimelteon may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.Approved
MethoxyfluraneThe risk or severity of adverse effects can be increased when Methoxyflurane is combined with Tasimelteon.Approved, Vet Approved
MethsuximideThe risk or severity of adverse effects can be increased when Methsuximide is combined with Tasimelteon.Approved
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Methylphenobarbital is combined with Tasimelteon.Approved
MetyrosineTasimelteon may increase the sedative activities of Metyrosine.Approved
MexiletineThe serum concentration of Tasimelteon can be increased when it is combined with Mexiletine.Approved
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Tasimelteon.Approved, Illicit
MilnacipranThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Milnacipran.Approved
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.Approved, Investigational
MirtazapineTasimelteon may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.Approved
MitotaneThe serum concentration of Tasimelteon can be decreased when it is combined with Mitotane.Approved
MolindoneThe risk or severity of adverse effects can be increased when Molindone is combined with Tasimelteon.Approved
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Tasimelteon.Approved, Investigational
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.Approved, Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Tasimelteon.Approved
NefazodoneThe serum concentration of Tasimelteon can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Tasimelteon can be increased when it is combined with Nelfinavir.Approved
NevirapineThe serum concentration of Tasimelteon can be decreased when it is combined with Nevirapine.Approved
NitrazepamThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Tasimelteon.Approved
Nitrous oxideThe risk or severity of adverse effects can be increased when Nitrous oxide is combined with Tasimelteon.Approved, Vet Approved
NormethadoneThe risk or severity of adverse effects can be increased when Normethadone is combined with Tasimelteon.Approved, Illicit
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Tasimelteon.Approved
OlanzapineThe risk or severity of adverse effects can be increased when Olanzapine is combined with Tasimelteon.Approved, Investigational
OlopatadineThe risk or severity of adverse effects can be increased when Olopatadine is combined with Tasimelteon.Approved
OndansetronThe risk or severity of adverse effects can be increased when Ondansetron is combined with Tasimelteon.Approved
OpiumThe risk or severity of adverse effects can be increased when Opium is combined with Tasimelteon.Approved, Illicit
OrphenadrineTasimelteon may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OsanetantThe risk or severity of adverse effects can be increased when Osanetant is combined with Tasimelteon.Investigational
OxazepamThe risk or severity of adverse effects can be increased when Oxazepam is combined with Tasimelteon.Approved
OxetacaineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Oxetacaine.Investigational
OxprenololThe risk or severity of adverse effects can be increased when Oxprenolol is combined with Tasimelteon.Approved
OxybuprocaineThe risk or severity of adverse effects can be increased when Oxybuprocaine is combined with Tasimelteon.Approved
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Tasimelteon.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Tasimelteon.Approved, Investigational, Vet Approved
PaliperidoneThe risk or severity of adverse effects can be increased when Paliperidone is combined with Tasimelteon.Approved
ParaldehydeTasimelteon may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.Approved
ParoxetineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Paroxetine.Approved, Investigational
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Tasimelteon.Approved, Vet Approved
PentobarbitalThe serum concentration of Tasimelteon can be decreased when it is combined with Pentobarbital.Approved, Vet Approved
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.Approved
PerazineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Perazine.Investigational
PerospironeThe risk or severity of adverse effects can be increased when Perospirone is combined with Tasimelteon.Approved
PerphenazineThe risk or severity of adverse effects can be increased when Perphenazine is combined with Tasimelteon.Approved
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Tasimelteon.Approved
PhenobarbitalThe serum concentration of Tasimelteon can be decreased when it is combined with Phenobarbital.Approved
PhenoxyethanolThe risk or severity of adverse effects can be increased when Phenoxyethanol is combined with Tasimelteon.Approved
PhenytoinThe serum concentration of Tasimelteon can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PimozideThe risk or severity of adverse effects can be increased when Pimozide is combined with Tasimelteon.Approved
PipamperoneThe risk or severity of adverse effects can be increased when Pipamperone is combined with Tasimelteon.Approved
PipotiazineThe risk or severity of adverse effects can be increased when Pipotiazine is combined with Tasimelteon.Approved
PiritramideThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Piritramide.Investigational
PizotifenThe risk or severity of adverse effects can be increased when Pizotifen is combined with Tasimelteon.Approved
PomalidomideThe risk or severity of adverse effects can be increased when Pomalidomide is combined with Tasimelteon.Approved
PosaconazoleThe serum concentration of Tasimelteon can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PramipexoleTasimelteon may increase the sedative activities of Pramipexole.Approved, Investigational
PramocaineThe risk or severity of adverse effects can be increased when Pramocaine is combined with Tasimelteon.Approved
PrazepamThe risk or severity of adverse effects can be increased when Prazepam is combined with Tasimelteon.Approved, Illicit
PregabalinThe risk or severity of adverse effects can be increased when Pregabalin is combined with Tasimelteon.Approved, Illicit, Investigational
PregnanoloneThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Pregnanolone.Investigational
PrilocaineThe risk or severity of adverse effects can be increased when Prilocaine is combined with Tasimelteon.Approved
PrimidoneThe serum concentration of Tasimelteon can be decreased when it is combined with Primidone.Approved, Vet Approved
ProcaineThe risk or severity of adverse effects can be increased when Procaine is combined with Tasimelteon.Approved, Investigational, Vet Approved
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Tasimelteon.Approved, Vet Approved
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Tasimelteon.Approved, Vet Approved
PromethazineThe risk or severity of adverse effects can be increased when Promethazine is combined with Tasimelteon.Approved
ProparacaineThe risk or severity of adverse effects can be increased when Proparacaine is combined with Tasimelteon.Approved, Vet Approved
PropofolThe risk or severity of adverse effects can be increased when Propofol is combined with Tasimelteon.Approved, Investigational, Vet Approved
PropoxycaineThe risk or severity of adverse effects can be increased when Propoxycaine is combined with Tasimelteon.Approved
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Tasimelteon.Approved
PSD502The risk or severity of adverse effects can be increased when PSD502 is combined with Tasimelteon.Investigational
QuazepamThe risk or severity of adverse effects can be increased when Quazepam is combined with Tasimelteon.Approved, Illicit
QuetiapineThe risk or severity of adverse effects can be increased when Quetiapine is combined with Tasimelteon.Approved
RacloprideThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Raclopride.Investigational
RamelteonThe risk or severity of adverse effects can be increased when Ramelteon is combined with Tasimelteon.Approved, Investigational
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Tasimelteon.Approved
RemoxiprideThe risk or severity of adverse effects can be increased when Remoxipride is combined with Tasimelteon.Approved, Withdrawn
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Tasimelteon.Approved
RifabutinThe serum concentration of Tasimelteon can be decreased when it is combined with Rifabutin.Approved
RifampicinThe serum concentration of Tasimelteon can be decreased when it is combined with Rifampicin.Approved
RifapentineThe serum concentration of Tasimelteon can be decreased when it is combined with Rifapentine.Approved
RisperidoneThe risk or severity of adverse effects can be increased when Risperidone is combined with Tasimelteon.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Ritanserin.Investigational
RitonavirThe serum concentration of Tasimelteon can be increased when it is combined with Ritonavir.Approved, Investigational
RomifidineThe risk or severity of adverse effects can be increased when Romifidine is combined with Tasimelteon.Vet Approved
RopiniroleTasimelteon may increase the sedative activities of Ropinirole.Approved, Investigational
RopivacaineThe risk or severity of adverse effects can be increased when Ropivacaine is combined with Tasimelteon.Approved
RotigotineTasimelteon may increase the sedative activities of Rotigotine.Approved
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Tasimelteon.Approved
S-EthylisothioureaThe risk or severity of adverse effects can be increased when S-Ethylisothiourea is combined with Tasimelteon.Experimental
Sage 547The risk or severity of adverse effects can be increased when Tasimelteon is combined with Sage 547.Investigational
SaquinavirThe serum concentration of Tasimelteon can be increased when it is combined with Saquinavir.Approved, Investigational
ScopolamineThe risk or severity of adverse effects can be increased when Scopolamine is combined with Tasimelteon.Approved
SecobarbitalThe risk or severity of adverse effects can be increased when Secobarbital is combined with Tasimelteon.Approved, Vet Approved
SertindoleThe risk or severity of adverse effects can be increased when Sertindole is combined with Tasimelteon.Approved, Withdrawn
SertralineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Sertraline.Approved
SevofluraneThe risk or severity of adverse effects can be increased when Sevoflurane is combined with Tasimelteon.Approved, Vet Approved
Sodium oxybateTasimelteon may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.Approved
St. John's WortThe serum concentration of Tasimelteon can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Stiripentol.Approved
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Tasimelteon.Approved, Investigational
SulpirideThe risk or severity of adverse effects can be increased when Sulpiride is combined with Tasimelteon.Approved
SuvorexantTasimelteon may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.Approved
TandospironeThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Tandospirone.Investigational
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Tasimelteon.Approved
TelaprevirThe serum concentration of Tasimelteon can be increased when it is combined with Telaprevir.Approved
TelithromycinThe serum concentration of Tasimelteon can be increased when it is combined with Telithromycin.Approved
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Tasimelteon.Approved
TetrabenazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Tasimelteon.Approved
TetracaineThe risk or severity of adverse effects can be increased when Tetracaine is combined with Tasimelteon.Approved, Vet Approved
TetrodotoxinThe risk or severity of adverse effects can be increased when Tetrodotoxin is combined with Tasimelteon.Investigational
ThalidomideTasimelteon may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.Approved, Investigational, Withdrawn
ThiamylalThe risk or severity of adverse effects can be increased when Thiamylal is combined with Tasimelteon.Approved, Vet Approved
ThiopentalThe risk or severity of adverse effects can be increased when Thiopental is combined with Tasimelteon.Approved, Vet Approved
ThioridazineThe risk or severity of adverse effects can be increased when Thioridazine is combined with Tasimelteon.Approved
ThiothixeneThe risk or severity of adverse effects can be increased when Thiothixene is combined with Tasimelteon.Approved
TiagabineThe risk or severity of adverse effects can be increased when Tiagabine is combined with Tasimelteon.Approved
TiaprideThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Tiapride.Investigational
TiletamineThe risk or severity of adverse effects can be increased when Tiletamine is combined with Tasimelteon.Vet Approved
TizanidineThe risk or severity of adverse effects can be increased when Tizanidine is combined with Tasimelteon.Approved
TolcaponeThe risk or severity of adverse effects can be increased when Tolcapone is combined with Tasimelteon.Approved, Withdrawn
TopiramateThe risk or severity of adverse effects can be increased when Topiramate is combined with Tasimelteon.Approved
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Tasimelteon.Approved, Investigational
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Trans-2-Phenylcyclopropylamine is combined with Tasimelteon.Experimental
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Tasimelteon.Approved
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Tasimelteon.Approved, Investigational
TriazolamThe risk or severity of adverse effects can be increased when Triazolam is combined with Tasimelteon.Approved
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Tasimelteon.Approved
TriflupromazineThe risk or severity of adverse effects can be increased when Triflupromazine is combined with Tasimelteon.Approved, Vet Approved
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Tasimelteon.Approved
TriprolidineThe risk or severity of adverse effects can be increased when Triprolidine is combined with Tasimelteon.Approved
Uc1010The risk or severity of adverse effects can be increased when Tasimelteon is combined with Uc1010.Investigational
Valproic AcidThe risk or severity of adverse effects can be increased when Valproic Acid is combined with Tasimelteon.Approved, Investigational
VenlafaxineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Venlafaxine.Approved
VigabatrinThe risk or severity of adverse effects can be increased when Vigabatrin is combined with Tasimelteon.Approved
VoriconazoleThe serum concentration of Tasimelteon can be increased when it is combined with Voriconazole.Approved, Investigational
VortioxetineThe risk or severity of adverse effects can be increased when Vortioxetine is combined with Tasimelteon.Approved
XylazineThe risk or severity of adverse effects can be increased when Xylazine is combined with Tasimelteon.Vet Approved
ZaleplonThe risk or severity of adverse effects can be increased when Zaleplon is combined with Tasimelteon.Approved, Illicit, Investigational
ZiconotideThe risk or severity of adverse effects can be increased when Ziconotide is combined with Tasimelteon.Approved
ZimelidineThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Zimelidine.Withdrawn
ZiprasidoneThe risk or severity of adverse effects can be increased when Ziprasidone is combined with Tasimelteon.Approved
ZolazepamThe risk or severity of adverse effects can be increased when Zolazepam is combined with Tasimelteon.Vet Approved
ZolpidemTasimelteon may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.Approved
ZonisamideThe risk or severity of adverse effects can be increased when Zonisamide is combined with Tasimelteon.Approved, Investigational
ZopicloneThe risk or severity of adverse effects can be increased when Zopiclone is combined with Tasimelteon.Approved
ZotepineThe risk or severity of adverse effects can be increased when Zotepine is combined with Tasimelteon.Approved
ZuclopenthixolThe risk or severity of adverse effects can be increased when Zuclopenthixol is combined with Tasimelteon.Approved, Investigational
Food InteractionsNot 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)
ADMET
Predicted ADMET featuresNot Available
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
CapsuleOral20 mg/1
CapsuleOral20 mg
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
Taxonomy
ClassificationNot classified

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 ]
Comments
comments powered by Disqus
Drug created on May 14, 2015 10:07 / Updated on December 02, 2016 02:44