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

Stem definition	Drug id	CAS RN
enzyme inhibitors	5214	1033805-22-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: telotristat ethyl xermelo telotristat etiprate LX1606 LX 1606	Telotristat, the active metabolite of telotristat ethyl, is an inhibitor of tryptophan hydroxylase, which mediates the rate limiting step in serotonin biosynthesis. The in vitro inhibitory potency of telotristat towards tryptophan hydroxylase is 29 times higher than that of telotristat ethyl. Serotonin plays a role in mediating secretion, motility, inflammation, and sensation of the gastrointestinal tract, and is over-produced in patients with carcinoid syndrome. Through inhibition of tryptophan hydroxylase, telotristat and telotristat ethyl reduce the production of peripheral serotonin, and the frequency of carcinoid syndrome diarrhea. Molecular weight: 574.99 Formula: C27H26ClF3N6O3 CLOGP: 6.03 LIPINSKI: 2 HAC: 9 HDO: 2 TPSA: 131.17 ALOGS: -5.29 ROTB: 11 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

telotristat ethyl
xermelo
telotristat etiprate
LX1606
LX 1606

Telotristat, the active metabolite of telotristat ethyl, is an inhibitor of tryptophan hydroxylase, which mediates the rate limiting step in serotonin biosynthesis. The in vitro inhibitory potency of telotristat towards tryptophan hydroxylase is 29 times higher than that of telotristat ethyl. Serotonin plays a role in mediating secretion, motility, inflammation, and sensation of the gastrointestinal tract, and is over-produced in patients with carcinoid syndrome. Through inhibition of tryptophan hydroxylase, telotristat and telotristat ethyl reduce the production of peripheral serotonin, and the frequency of carcinoid syndrome diarrhea.

Molecular weight: 574.99
Formula: C27H26ClF3N6O3
CLOGP: 6.03
LIPINSKI: 2
HAC: 9
HDO: 2
TPSA: 131.17
ALOGS: -5.29
ROTB: 11

Status: ONP

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

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Feb. 28, 2017	FDA	LEXICON PHARMA INC
Sept. 18, 2017	EMA	Ipsen Pharma

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
Constipation	52.25	36.56	37	1013	224906	63263066
Abdominal pain	45.59	36.56	38	1012	293418	63194554
Flushing	39.82	36.56	21	1029	75066	63412906
Disease progression	37.54	36.56	24	1026	122734	63365238

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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
Flushing	74.27	42.38	30	1018	32390	34923493
Abdominal pain	69.63	42.38	49	999	163569	34792314
Diarrhoea	57.85	42.38	64	984	389848	34566035
Serum serotonin increased	47.75	42.38	7	1041	87	34955796
Blood chromogranin A increased	46.89	42.38	8	1040	273	34955610
Constipation	46.75	42.38	36	1012	136946	34818937

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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
Flushing	49.36	37.98	24	1059	88244	79655061
Death	46.48	37.98	47	1036	566467	79176838
Disease progression	44.87	37.98	29	1054	184333	79558972
Abdominal pain	44.73	37.98	39	1044	389530	79353775

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

None

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

Disease	Relation	SNOMED_ID	DOID
Diarrhea	indication	62315008

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	7.14	Basic
pKa2	2.78	Basic

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
EQ 250MG BASE	XERMELO	TERSERA	N208794	Feb. 28, 2017	RX	TABLET	ORAL	7968559	Dec. 11, 2027	THE TREATMENT OF CARCINOID SYNDROME DIARRHEA IN COMBINATION WITH SOMATOSTATIN ANALOG (SSA) THERAPY IN ADULTS INADEQUATELY CONTROLLED BY SSA THERAPY
EQ 250MG BASE	XERMELO	TERSERA	N208794	Feb. 28, 2017	RX	TABLET	ORAL	8653094	Dec. 19, 2028	THE TREATMENT OF CARCINOID SYNDROME DIARRHEA IN COMBINATION WITH SOMATOSTATIN ANALOG (SSA) THERAPY IN ADULTS INADEQUATELY CONTROLLED BY SSA THERAPY
EQ 250MG BASE	XERMELO	TERSERA	N208794	Feb. 28, 2017	RX	TABLET	ORAL	7709493	Feb. 28, 2031	THE TREATMENT OF CARCINOID SYNDROME DIARRHEA IN COMBINATION WITH SOMATOSTATIN ANALOG (SSA) THERAPY IN ADULTS INADEQUATELY CONTROLLED BY SSA THERAPY

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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
EQ 250MG BASE	XERMELO	TERSERA	N208794	Feb. 28, 2017	RX	TABLET	ORAL	Feb. 28, 2024	TREATMENT OF CARCINOID SYNDROME DIARRHEA IN COMBINATION WITH SOMATOSTATIN ANALOG (SSA) THERAPY IN ADULTS INADEQUATELY CONTROLLED BY SSA THERAPY

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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
Tryptophan 5-hydroxylase 1	Enzyme	P17752	TPH1_HUMAN	INHIBITOR	IC50	7.80		SCIENTIFIC LITERATURE	DRUG LABEL

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External reference:

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ID	Source
017120	NDDF
017121	NDDF
1137608-69-5	SECONDARY_CAS_RN
1872441	RXNORM
25181577	PUBCHEM_CID
252423	MMSL
32389	MMSL
4036470	VANDF
733879005	SNOMEDCT_US
8G388563M7	UNII

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Xermelo	HUMAN PRESCRIPTION DRUG LABEL	1	70183-125	TABLET	250 mg	ORAL	NDA	24 sections
Xermelo	HUMAN PRESCRIPTION DRUG LABEL	1	70183-125	TABLET	250 mg	ORAL	NDA	24 sections
Xermelo	HUMAN PRESCRIPTION DRUG LABEL	1	70183-125	TABLET	250 mg	ORAL	NDA	24 sections
Xermelo	HUMAN PRESCRIPTION DRUG LABEL	1	70183-125	TABLET	250 mg	ORAL	NDA	24 sections
Xermelo	HUMAN PRESCRIPTION DRUG LABEL	1	70720-125	TABLET	250 mg	ORAL	NDA	25 sections
Xermelo	HUMAN PRESCRIPTION DRUG LABEL	1	70720-125	TABLET	250 mg	ORAL	NDA	25 sections

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