tasimelteon 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	4820	609799-22-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: tasimelteon hetlioz VEC-162 BMS-214778	an agonist at melatonin MT1 and MT2 receptors, these receptors are thought to be involved in the control of circadian rhythms Molecular weight: 245.32 Formula: C15H19NO2 CLOGP: 1.89 LIPINSKI: 0 HAC: 3 HDO: 1 TPSA: 38.33 ALOGS: -3.81 ROTB: 4 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

tasimelteon
hetlioz
VEC-162
BMS-214778

an agonist at melatonin MT1 and MT2 receptors, these receptors are thought to be involved in the control of circadian rhythms

Molecular weight: 245.32
Formula: C15H19NO2
CLOGP: 1.89
LIPINSKI: 0
HAC: 3
HDO: 1
TPSA: 38.33
ALOGS: -3.81
ROTB: 4

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
CL (Clearance)	9.04 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	0.75 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.33 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.12 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

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Approvals:

Date	Agency	Company	Orphan
Jan. 31, 2014	FDA	VANDA PHARMS INC

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Insomnia	355.67	43.91	169	2255	215083	63271515
Middle insomnia	335.78	43.91	81	2343	12562	63474036
Drug ineffective	330.44	43.91	286	2138	1044479	62442119
Product dose omission issue	246.47	43.91	136	2288	234177	63252421
Incorrect product administration duration	211.51	43.91	55	2369	11491	63475107
Abnormal dreams	177.70	43.91	47	2377	10469	63476129
Nightmare	175.20	43.91	53	2371	19141	63467457
Somnolence	147.83	43.91	89	2335	178596	63308002
Initial insomnia	130.62	43.91	33	2391	6124	63480474
Therapeutic product effect delayed	98.86	43.91	22	2402	2369	63484229

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Drug ineffective	456.77	58.94	278	1487	456473	34498693
Middle insomnia	402.61	58.94	88	1677	6714	34948452
Insomnia	267.87	58.94	121	1644	103786	34851380
Incorrect product administration duration	233.46	58.94	53	1712	4758	34950408
Nightmare	202.12	58.94	59	1706	14332	34940834
Product dose omission issue	161.14	58.94	90	1675	119621	34835545
Abnormal dreams	151.50	58.94	41	1724	7537	34947629
Somnolence	134.42	58.94	78	1687	111038	34844128
Therapeutic product effect decreased	116.55	58.94	49	1716	34694	34920472
Initial insomnia	107.08	58.94	26	1739	3098	34952068

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Drug ineffective	448.22	48.31	321	2210	1080592	78661265
Middle insomnia	409.15	48.31	96	2435	15973	79725884
Incorrect product administration duration	370.90	48.31	84	2447	11938	79729919
Insomnia	333.14	48.31	159	2372	245011	79496846
Nightmare	265.54	48.31	75	2456	25786	79716071
Product dose omission issue	245.67	48.31	130	2401	247407	79494450
Abnormal dreams	217.18	48.31	54	2477	11358	79730499
Somnolence	159.40	48.31	97	2434	238884	79502973
Initial insomnia	122.77	48.31	31	2500	6907	79734950
Therapeutic product effect decreased	97.50	48.31	62	2469	163801	79578056

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N05CH03	NERVOUS SYSTEM PSYCHOLEPTICS HYPNOTICS AND SEDATIVES Melatonin receptor agonists
CHEBI has role	CHEBI:79046	melatonin receptor agonists
FDA EPC	N0000175743	Melatonin Receptor Agonist
FDA MoA	N0000000250	Melatonin Receptor Agonists

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Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Non-24 hour sleep-wake cycle	indication	230496009

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	13.05	acidic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
20MG	HETLIOZ	VANDA PHARMS INC	N205677	Jan. 31, 2014	RX	CAPSULE	ORAL	10149829	Jan. 25, 2033	TREATMENT OF NIGHTTIME SLEEP DISTURBANCES IN SMITH-MAGENIS SYNDROME NON-24 HOUR SLEEP-WAKE DISORDER BY AVOIDING THE USE OF TASIMELTEON IN COMBINATION WITH CYP1A2 STRONG INHIBITORS
20MG	HETLIOZ	VANDA PHARMS INC	N205677	Jan. 31, 2014	RX	CAPSULE	ORAL	10149829	Jan. 25, 2033	TREATMENT OF NON-24 HOUR SLEEP-WAKE DISORDER BY AVOIDING THE USE OF TASIMELTEON IN COMBINATION WITH CYP1A2 STRONG INHIBITORS
20MG	HETLIOZ	VANDA PHARMS INC	N205677	Jan. 31, 2014	RX	CAPSULE	ORAL	10449176	Jan. 25, 2033	TREATMENT OF NON-24 HOUR SLEEP-WAKE DISORDER BY ADMINISTERING TASIMELTEON
20MG	HETLIOZ	VANDA PHARMS INC	N205677	Jan. 31, 2014	RX	CAPSULE	ORAL	10610510	Jan. 25, 2033	TREATMENT OF NIGHTTIME SLEEP DISTURBANCES IN SMITH-MAGENIS SYNDROME BY ADMINISTERING TASIMELTEON TO PATIENTS WITH A SMOKING HISTORY
20MG	HETLIOZ	VANDA PHARMS INC	N205677	Jan. 31, 2014	RX	CAPSULE	ORAL	10610510	Jan. 25, 2033	TREATMENT OF NON-24 HOUR SLEEP-WAKE DISORDER BY ADMINISTERING TASIMELTEON TO PATIENTS WITH A SMOKING HISTORY
20MG	HETLIOZ	VANDA PHARMS INC	N205677	Jan. 31, 2014	RX	CAPSULE	ORAL	10945988	Jan. 25, 2033	TREATMENT OF NON-24 HOUR SLEEP-WAKE DISORDER BY ADMINISTERING TASIMELTEON
20MG	HETLIOZ	VANDA PHARMS INC	N205677	Jan. 31, 2014	RX	CAPSULE	ORAL	10980770	Jan. 25, 2033	TREATMENT OF NIGHTTIME SLEEP DISTURBANCES IN SMITH-MAGENIS SYNDROME BY AVOIDING THE ADMINISTRATION OF TASIMELTEON TO SMOKERS OR TO PATIENTS BEING TREATED WITH A CYP1A2 INHIBITOR
20MG	HETLIOZ	VANDA PHARMS INC	N205677	Jan. 31, 2014	RX	CAPSULE	ORAL	10980770	Jan. 25, 2033	TREATMENT OF NON-24 HOUR SLEEP-WAKE DISORDER BY AVOIDING THE ADMINISTRATION OF TASIMELTEON TO SMOKERS OR TO PATIENTS BEING TREATED WITH A CYP1A2 INHIBITOR
20MG	HETLIOZ	VANDA PHARMS INC	N205677	Jan. 31, 2014	RX	CAPSULE	ORAL	11285129	Jan. 25, 2033	TREATMENT OF NIGHTTIME SLEEP DISTURBANCES IN SMITH-MAGENIS SYNDROME BY AVOIDING THE ADMINISTRATION OF TASIMELTEON WITH BETA-ADRENERGIC RECEPTOR ANTAGONISTS
20MG	HETLIOZ	VANDA PHARMS INC	N205677	Jan. 31, 2014	RX	CAPSULE	ORAL	11285129	Jan. 25, 2033	TREATMENT OF NON-24-HOUR SLEEP-WAKE DISORDER BY AVOIDING THE ADMINISTRATION OF TASIMELTEON WITH BETA-ADRENERGIC RECEPTOR ANTAGONISTS

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
20MG	TASIMELTEON	APOTEX	A211607	Dec. 20, 2022	RX	CAPSULE	ORAL	June 27, 2023	PATENT CHALLENGE
20MG	HETLIOZ	VANDA PHARMS INC	N205677	Jan. 31, 2014	RX	CAPSULE	ORAL	Dec. 1, 2023	TREATMENT OF NIGHTTIME SLEEP DISTURBANCES IN SMITH-MAGENIS SYNDROME (SMS) IN PATIENTS 16 YEARS OF AGE AND OLDER
20MG	HETLIOZ	VANDA PHARMS INC	N205677	Jan. 31, 2014	RX	CAPSULE	ORAL	Dec. 1, 2027	THE TREATMENT OF NIGHTTIME SLEEP DISTURBANCES IN SMITH-MAGENIS SYNDROME (SMS) IN PATIENTS 16 YEARS OF AGE AND OLDER
4MG/ML	HETLIOZ LQ	VANDA PHARMS INC	N214517	Dec. 1, 2020	RX	SUSPENSION	ORAL	Dec. 1, 2023	NEW PRODUCT
4MG/ML	HETLIOZ LQ	VANDA PHARMS INC	N214517	Dec. 1, 2020	RX	SUSPENSION	ORAL	Dec. 1, 2027	FOR THE TREATMENT OF NIGHTTIME SLEEP DISTURBANCES IN SMITH-MAGENIS SYNDROME (SMS) IN PEDIATRIC PATIENTS 3 TO 15 YEARS OF AGE

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Melatonin receptor type 1A	GPCR	P48039	MTR1A_HUMAN	AGONIST	Ki	9.45		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Melatonin receptor type 1B	GPCR	P49286	MTR1B_HUMAN	AGONIST	Ki	9.80		SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE

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External reference:

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ID	Source
015295	NDDF
10220503	PUBCHEM_CID
1490468	RXNORM
211275	MMSL
30166	MMSL
364462	MMSL
4033173	VUID
4033173	VANDF
702394009	SNOMEDCT_US
704468000	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Hetlioz	HUMAN PRESCRIPTION DRUG LABEL	1	43068-220	CAPSULE	20 mg	ORAL	NDA	34 sections
Hetlioz	HUMAN PRESCRIPTION DRUG LABEL	1	43068-220	CAPSULE	20 mg	ORAL	NDA	34 sections
HetliozLQ	HUMAN PRESCRIPTION DRUG LABEL	1	43068-304	SUSPENSION	4 mg	ORAL	NDA	34 sections
HetliozLQ	HUMAN PRESCRIPTION DRUG LABEL	1	43068-304	SUSPENSION	4 mg	ORAL	NDA	34 sections
Tasimelteon	HUMAN PRESCRIPTION DRUG LABEL	1	0480-4490	CAPSULE, GELATIN COATED	20 mg	ORAL	ANDA	27 sections
Tasimelteon	HUMAN PRESCRIPTION DRUG LABEL	1	69238-2548	CAPSULE	20 mg	ORAL	ANDA	31 sections

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