TASIMELTEON

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C15H19NO2
Molecular Weight	245.3169
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCC(=O)NC[C@@H]1C[C@H]1C2=C3CCOC3=CC=C2

InChI

InChIKey=PTOIAAWZLUQTIO-GXFFZTMASA-N

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

HIDE SMILES / InChI

Molecular Formula	C15H19NO2
Molecular Weight	245.3169
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	2 / 2
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205677s000lbledt.pdf
Curator's Comment: description was created based on several sources, including http://www.ncbi.nlm.nih.gov/pubmed/?term=19579175

Tasimelteon, developed by Vanda Pharmaceuticals Inc under license from Bristol-Myers Squibb Co, is a melatonin receptor agonist. Tasimelteon differs structurally from melatonin and drugs with known melatonin agonist activity, in particular by its distinct aromatic group and linker. Tasimelteon bears also no structural relationship to any other approved active substance. Tasimelteon is presumably acts through activation of MT1 and MT2 G-protein coupled receptors, which are involved primarily in inhibition of neuronal firing and phase shift of circadian rhythms. Tasimelteon is approved for the treatment of Non24-Hour Sleep-Wake Disorder.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Melatonin receptor type 1B 4 Target ID: P49286 Gene ID: 4544.0 Gene Symbol: MTNR1B Target Organism: Homo sapiens (Human) Sources: http://www.pbm.va.gov/PBM/clinicalguidance/drugmonographs/Tasimelteon_Drug_Monograph.pdf	Agonist 2662		0.0692 nM [Ki]
Melatonin receptor type 1A 3 Target ID: P48039 Gene ID: 4543.0 Gene Symbol: MTNR1A Target Organism: Homo sapiens (Human) Sources: http://www.pbm.va.gov/PBM/clinicalguidance/drugmonographs/Tasimelteon_Drug_Monograph.pdf	Agonist 2662		0.304 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Sleep disorders, circadian rhythm 3 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205677s000lbledt.pdf	Primary		Approved 8360	HETLIOZ Approved Use Indicated for the treatment of Non-24-Hour Sleep-Wake Disorder (Non-24). Launch Date 1.39112638E12

C_max

Value	Dose	Analyte	Population
12 ng/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	1 mg 1 times / day steady-state, oral dose: 1 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
394 ng/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
873 ng/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	150 mg 1 times / day steady-state, oral dose: 150 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
173 ng/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
33 ng/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
261 ng/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
5 ng/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
51 ng/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
786 ng/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
445 ng/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: HIGH-FAT

AUC

Value	Dose	Analyte	Population
17 ng × h/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	1 mg 1 times / day steady-state, oral dose: 1 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1823 ng × h/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
3797 ng × h/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	150 mg 1 times / day steady-state, oral dose: 150 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
426 ng × h/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
59 ng × h/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
611 ng × h/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
8 ng × h/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
96 ng × h/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2269 ng × h/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2304 ng × h/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: HIGH-FAT

T_1/2

Value	Dose	Analyte	Population
1.49 h OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	1 mg 1 times / day steady-state, oral dose: 1 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.78 h OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.63 h OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	150 mg 1 times / day steady-state, oral dose: 150 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.37 h OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.29 h OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.57 h OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.75 h OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.44 h OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.75 h OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2.06 h OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	TASIMELTEON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: HIGH-FAT

Doses

Dose	Population	Adverse events
20 mg 1 times / day multiple, oral Recommended Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.81	unhealthy, 18 - 92 years n = 1346 Health Status: unhealthy Condition: 24-Hour Sleep-Wake Disorder Age Group: 18 - 92 years Sex: M+F Population Size: 1346 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.81	Disc. AE: Supraventricular extrasystoles, Tachycardia... AEs leading to discontinuation/dose reduction: Supraventricular extrasystoles (0.07%) Tachycardia (0.07%) Constipation (0.07%) Fatigue (0.07%) Oedema peripheral (0.07%) Cholestasis (0.07%) ALT increased (0.07%) AST increased (0.07%) GGT increased (0.07%) Blood creatine increased (0.07%) Hyperglycaemia (0.07%) Headache (0.07%) Loss of consciousness (0.07%) Syncope (0.07%) Transient ischaemic attack (0.07%) Insomnia (0.14%) Nightmare (0.14%) Renal pain (0.07%) Rash (0.07%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.81
20 mg 1 times / day multiple, oral Recommended Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.84	unhealthy, 18 - 92 years n = 151 Health Status: unhealthy Condition: 24-Hour Sleep-Wake Disorder Age Group: 18 - 92 years Sex: M+F Population Size: 151 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.84	Disc. AE: Supraventricular extrasystoles, Vomiting... AEs leading to discontinuation/dose reduction: Supraventricular extrasystoles (0.7%) Vomiting (0.7%) Headache (0.7%) Syncope (0.7%) Insomnia (0.7%) Nightmare (1.3%) Anger (0.7%) Depression (0.7%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.84
1 mg 1 times / day multiple, oral Studied dose Dose: 1 mg, 1 times / day Route: oral Route: multiple Dose: 1 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.81	unhealthy, 18 - 92 years n = 1346 Health Status: unhealthy Condition: 24-Hour Sleep-Wake Disorder Age Group: 18 - 92 years Sex: M+F Population Size: 1346 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.81	Disc. AE: Local swelling, Disorientation... AEs leading to discontinuation/dose reduction: Local swelling (0.07%) Disorientation (0.07%) Rash (0.07%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.81
10 mg 1 times / day multiple, oral Studied dose Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.81	unhealthy, 18 - 92 years n = 1346 Health Status: unhealthy Condition: 24-Hour Sleep-Wake Disorder Age Group: 18 - 92 years Sex: M+F Population Size: 1346 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.81	Disc. AE: Diarrhoea, Gastritis... AEs leading to discontinuation/dose reduction: Diarrhoea (0.07%) Gastritis (0.07%) Dizziness (0.07%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.81
100 mg 1 times / day multiple, oral Studied dose Dose: 100 mg, 1 times / day Route: oral Route: multiple Dose: 100 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.81	unhealthy, 18 - 92 years n = 1346 Health Status: unhealthy Condition: 24-Hour Sleep-Wake Disorder Age Group: 18 - 92 years Sex: M+F Population Size: 1346 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.81	Disc. AE: Vomiting... AEs leading to discontinuation/dose reduction: Vomiting (0.07%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.81
150 mg 1 times / day multiple, oral Studied dose Dose: 150 mg, 1 times / day Route: oral Route: multiple Dose: 150 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.81	unhealthy, 18 - 92 years n = 1346 Health Status: unhealthy Condition: 24-Hour Sleep-Wake Disorder Age Group: 18 - 92 years Sex: M+F Population Size: 1346 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.81	Disc. AE: Rash... AEs leading to discontinuation/dose reduction: Rash (0.07%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.81
20 mg 1 times / day multiple, oral (max) Studied dose Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.84	unhealthy, 18 - 92 years n = 114 Health Status: unhealthy Condition: 24-Hour Sleep-Wake Disorder Age Group: 18 - 92 years Sex: M+F Population Size: 114 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.84	Disc. AE: Ventricular arrhythmia, Gastritis... AEs leading to discontinuation/dose reduction: Ventricular arrhythmia (0.9%) Gastritis (0.9%) Local swelling (0.9%) Electrocardiogram ST segment elevation (0.9%) Ataxia (0.9%) Dizziness (0.9%) Confusional state (0.9%) Disorientation (0.9%) Rash (0.9%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.84
25 mg 1 times / day multiple, oral (mean) Studied dose Dose: 25 mg, 1 times / day Route: oral Route: multiple Dose: 25 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.84	unhealthy, 18 - 92 years n = 429 Health Status: unhealthy Condition: 24-Hour Sleep-Wake Disorder Age Group: 18 - 92 years Sex: M+F Population Size: 429 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.84	Disc. AE: Supraventricular extrasystoles, Ventricular arrhythmia... AEs leading to discontinuation/dose reduction: Supraventricular extrasystoles (0.2%) Ventricular arrhythmia (0.2%) Diarrhoea (0.2%) Dyspepsia (0.2%) Gastritis (0.2%) Hypoaesthesia oral (0.2%) Vomiting (0.2%) Local swelling (0.2%) Somnolence (0.5%) Ataxia (0.2%) Dizziness (0.2%) Headache (0.2%) Syncope (0.2%) Insomnia (0.5%) Nightmare (0.5%) Anger (0.2%) Confusional state (0.2%) Depression (0.2%) Disorientation (0.2%) Rash (0.2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.84
50 mg 1 times / day multiple, oral Studied dose Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.81	unhealthy, 18 - 92 years n = 1346 Health Status: unhealthy Condition: 24-Hour Sleep-Wake Disorder Age Group: 18 - 92 years Sex: M+F Population Size: 1346 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.81	Disc. AE: Dyspepsia, Blood creatine increased... AEs leading to discontinuation/dose reduction: Dyspepsia (0.07%) Blood creatine increased (0.07%) Somnolence (0.07%) Insomnia (0.07%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.81
50 mg 1 times / day multiple, oral Studied dose Dose: 50 mg, 1 times / day Route: oral Route: multiple Dose: 50 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.84	unhealthy, 18 - 92 years n = 164 Health Status: unhealthy Condition: 24-Hour Sleep-Wake Disorder Age Group: 18 - 92 years Sex: M+F Population Size: 164 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.84	Disc. AE: Diarrhoea, Dyspepsia... AEs leading to discontinuation/dose reduction: Diarrhoea (0.6%) Dyspepsia (0.6%) Hypoaesthesia oral (0.6%) Blood creatine phosphokinase increased (0.6%) Somnolence (1.2%) Insomnia (0.6%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.84
300 mg 1 times / day multiple, oral Highest studied dose Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.20	healthy, 18-44 years n = 11 Health Status: healthy Age Group: 18-44 years Sex: M+F Population Size: 11 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.20	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000MedR.pdf Page: nda/2014/205677Orig1s000MedR.pdf - p.20

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1709	substrate 1010 inhibitor 1752 inducer 383	substrate 1193 inhibitor 1837	inhibitor 1599

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 1509 CYP2B6 799 CYP2C8 901 CYP2C19 1463 CYP3A4/5 273 OATP1B1 781 OATP1B3 700 OAT1 595 BCRP 691 OCT2 638 OAT3 636 P-gp 1437	CYP1A2 1032 CYP1A1 348 CYP2C19 985 OATP1B1 403 OATP1B3 347 P-gp 1527	CYP3A4/5 120 CYP2C8 168 CYP1A2 689 CYP2B6 538 CYP2C19 290

Drug as perpetrator

Target	Modality	Activity	Metabolite	Clinical evidence
BCRP 765	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
BCRP 765	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
BCRP 765	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
BCRP 765	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
CYP1A2 1673	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no
CYP1A2 1673	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
CYP1A2 1673	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
CYP1A2 1673	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
CYP1A2 1673	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
CYP2B6 985	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no
CYP2B6 985	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
CYP2B6 985	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
CYP2B6 985	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
CYP2B6 985	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
CYP2C19 1537	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no
CYP2C19 1537	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
CYP2C19 1537	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
CYP2C19 1537	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
CYP2C19 1537	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
CYP2C8 955	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
CYP2C8 955	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
CYP2C8 955	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
CYP2C8 955	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
CYP2C9 1803	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no
CYP2C9 1803	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
CYP2C9 1803	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
CYP2C9 1803	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
CYP2C9 1803	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
CYP2D6 1875	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
CYP2D6 1875	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
CYP2D6 1875	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
CYP2D6 1875	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
CYP3A4/5 330	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
CYP3A4/5 330	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
CYP3A4/5 330	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
CYP3A4/5 330	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
OAT1 599	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
OAT1 599	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
OAT1 599	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
OAT1 599	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
OAT3 638	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
OAT3 638	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
OAT3 638	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
OAT3 638	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
OATP1B1 796	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
OATP1B1 796	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
OATP1B1 796	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
OATP1B1 796	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
OATP1B3 709	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
OATP1B3 709	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
OATP1B3 709	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
OATP1B3 709	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
OCT2 639	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
OCT2 639	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
OCT2 639	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
OCT2 639	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
P-gp 1626	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no
P-gp 1626	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no	M12 1
P-gp 1626	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no	M13 2
P-gp 1626	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no	M9 2
CYP2C8 955	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	yes		yes (co-administration study) Comment: Rifampin, a strong CYP3A4 and moderate CYP2C8, CYP2C9/2C19 inducer, decreased the exposure of tasimelteon by approximately 90%. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0
CYP3A4/5 330	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	yes		yes (co-administration study) Comment: Rifampin, a strong CYP3A4 and moderate CYP2C8, CYP2C9/2C19 inducer, decreased the exposure of tasimelteon by approximately 90%. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
CYP1A2 1032	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=5 Page: 5.0	major		yes (co-administration study) Comment: Drug interaction studies with CY1A2 inhibitor, fluvoxamine and CYP3A4 inducer, rifampin resulted in 6.5 fold increase and 90% decrease in tasimelteon exposure respectively. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=5 Page: 5.0
CYP3A4 1709	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=5 Page: 5.0	major		yes (co-administration study) Comment: Drug interaction studies with CY1A2 inhibitor, fluvoxamine and CYP3A4 inducer, rifampin resulted in 6.5 fold increase and 90% decrease in tasimelteon exposure respectively. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=5 Page: 5.0
CYP1A1 348	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=5 Page: 5.0	minor
CYP2C19 985	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=5 Page: 5.0	minor
CYP2C9 1010	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=5 Page: 5.0	minor
CYP2D6 1193	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=5 Page: 5.0	minor
OATP1B1 403	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no
OATP1B1 403	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no	M12 1
OATP1B1 403	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no	M13 2
OATP1B1 403	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no	M9 2
OATP1B3 347	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no
OATP1B3 347	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no	M12 1
OATP1B3 347	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no	M13 2
OATP1B3 347	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no	M9 2
P-gp 1527	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no
P-gp 1527	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no	M12 1
P-gp 1527	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no	M13 2
P-gp 1527	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no	M9 2

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1632	inhibitor 1613 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000PharmR.pdf#page=28 Page: 28.0

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:79042	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:79042
ChemicalBook	CB41518537	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB41518537
MolPort	MolPort-028-600-027	https://www.molport.com/shop/molecule-link/MolPort-028-600-027
ZINC	ZINC000004392649	http://zinc15.docking.org/substances/ZINC000004392649
eMolecules	28326483	https://www.emolecules.com/cgi-bin/more?vid=28326483

PubMed

Title	Date	PubMed

New approaches in the management of insomnia: weighing the advantages of prolonged-release melatonin and synthetic melatoninergic agonists.	2009	19557144
Melatonin agonists and insomnia.	2010 Feb	20136385
Gateways to clinical trials.	2010 Jan-Feb	20383346
Investigational melatonin receptor agonists.	2010 Jun	20408738
Jet lag, circadian rhythm sleep disturbances, and depression: the role of melatonin and its analogs.	2010 Nov	20827520
A systematic, updated review on the antidepressant agomelatine focusing on its melatonergic modulation.	2010 Sep	21358978
[The newer sedative-hypnotics].	2010 Sep	20945020
Mechanism of action of tasimelteon in non-24 sleep-wake syndrome: treatment for a circadian rhythm disorder in blind patients.	2014 Dec	25422900
Tasimelteon: a selective and unique receptor binding profile.	2015 Apr	25534555
Tasimelteon for the treatment of non-24-hour sleep-wake disorder.	2015 Jan	25685859

Patents

Sample Use Guides

In Vivo Use Guide

The recommended dosage of HETLIOZ is 20 mg per day taken before bedtime, at the same time every night. Because of individual differences in circadian rhythms, drug effect may not occur for weeks or months. HETLIOZ should be taken without food.

Route of Administration: Oral

In Vitro Use Guide

Unknown

Substance Class	Chemical Created by `admin` on `Wed Jul 05 23:26:24 UTC 2023` Edited by `admin` on `Wed Jul 05 23:26:24 UTC 2023`
Record UNII	SHS4PU80D9
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

TASIMELTEON

Official Name

English

TASIMELTEON [USAN]

Common Name

English

HETLIOZ

Brand Name

English

Tasimelteon [WHO-DD]

Common Name

English

PROPANAMIDE, N-(((1R,2R)-2-(2,3-DIHYDRO-4-BENZOFURANYL)CYCLOPROPYL)METHYL)-

Systematic Name

English

BMS-214778

Code

English

VEC-162

Code

English

BMS-214,778

Code

English

HETLIOZ LQ

Brand Name

English

N-[[(1R,2R)-2-(2,3-Dihydro-1-benzofuran-4-yl)cyclopropyl]methyl]propanamide

Systematic Name

English

TASIMELTEON [VANDF]

Common Name

English

TASIMELTEON [MI]

Common Name

English

TASIMELTEON [MART.]

Common Name

English

TASIMELTEON [ORANGE BOOK]

Common Name

English

tasimelteon [INN]

Common Name

English

Classification Tree Code System Code

WHO-ATC

N05CH03