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 2678		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 2678		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 8429	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 1737	substrate 1037 inhibitor 1767 inducer 389	substrate 1217 inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 1524 CYP2B6 810 CYP2C8 911 CYP2C19 1478 CYP3A4/5 278 OATP1B1 788 OATP1B3 706 OAT1 599 BCRP 699 OCT2 647 OAT3 642 P-gp 1461	CYP1A2 1054 CYP1A1 349 CYP2C19 991 OATP1B1 406 OATP1B3 350 P-gp 1537	CYP3A4/5 124 CYP2C8 168 CYP1A2 701 CYP2B6 547 CYP2C19 293

Drug as perpetrator

Target	Modality	Activity	Metabolite	Clinical evidence
BCRP 773	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
BCRP 773	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
BCRP 773	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
BCRP 773	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
CYP1A2 1692	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
CYP2B6 1001	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no
CYP2B6 1001	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
CYP2B6 1001	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
CYP2B6 1001	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
CYP2B6 1001	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
CYP2C19 1553	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
CYP2C8 965	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
CYP2C8 965	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
CYP2C8 965	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
CYP2C8 965	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
CYP2C9 1819	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
CYP3A4/5 335	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
CYP3A4/5 335	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
CYP3A4/5 335	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
CYP3A4/5 335	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
OAT1 603	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
OAT1 603	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
OAT1 603	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
OAT1 603	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
OAT3 644	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
OAT3 644	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
OAT3 644	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
OAT3 644	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
OATP1B1 803	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
OATP1B1 803	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
OATP1B1 803	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
OATP1B1 803	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
OATP1B3 715	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
OATP1B3 715	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
OATP1B3 715	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
OATP1B3 715	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
OCT2 648	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no
OCT2 648	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M12 1
OCT2 648	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M13 2
OCT2 648	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=7 Page: 7.0	no	M9 2
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no	M12 1
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no	M13 2
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no	M9 2
CYP2C8 965	inducer 1573 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
CYP3A4/5 335	inducer 1573 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 1054	substrate 3367 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 1737	substrate 3367 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 349	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=5 Page: 5.0	minor
CYP2C19 991	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=5 Page: 5.0	minor
CYP2C9 1037	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=5 Page: 5.0	minor
CYP2D6 1217	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=5 Page: 5.0	minor
OATP1B1 406	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no
OATP1B1 406	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no	M12 1
OATP1B1 406	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no	M13 2
OATP1B1 406	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no	M9 2
OATP1B3 350	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no
OATP1B3 350	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no	M12 1
OATP1B3 350	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no	M13 2
OATP1B3 350	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no	M9 2
P-gp 1537	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no
P-gp 1537	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no	M12 1
P-gp 1537	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205677Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	no	M13 2
P-gp 1537	substrate 3367 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 1647	inhibitor 1626 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
Preclinical pharmacokinetics and metabolism of BMS-214778, a novel melatonin receptor agonist.	2003 Apr	12661062
Melatonin and its agonists: an update.	2008 Oct	18827285
Melatonin agonist tasimelteon (VEC-162) for transient insomnia after sleep-time shift: two randomised controlled multicentre trials.	2009 Feb 7	19054552
Tasimelteon, a melatonin agonist for the treatment of insomnia and circadian rhythm sleep disorders.	2009 Jul	19579175
Sleep-promoting action of IIK7, a selective MT2 melatonin receptor agonist in the rat.	2009 Jun 26	19429170
Melatonin agonists and insomnia.	2010 Feb	20136385
Investigational melatonin receptor agonists.	2010 Jun	20408738
A systematic, updated review on the antidepressant agomelatine focusing on its melatonergic modulation.	2010 Sep	21358978
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 `Fri Dec 15 15:58:06 UTC 2023` Edited by `admin` on `Fri Dec 15 15:58:06 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