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

Stem definitionDrug idCAS RN
enzyme inhibitors 5214 1033805-22-9

Description:

MoleculeDescription

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:

DateAgencyCompanyOrphan
Sept. 18, 2017 EMA Ipsen Pharma
Feb. 28, 2017 FDA LEXICON PHARMA INC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Constipation 51.27 34.37 37 1007 185671 50418409
Abdominal pain 45.45 34.37 38 1006 236190 50367890
Disease progression 38.12 34.37 24 1020 95842 50508238
Flushing 37.70 34.37 21 1023 66994 50537086
Hospice care 34.47 34.37 10 1034 5762 50598318

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Flushing 73.46 41.29 30 990 28962 29544545
Abdominal pain 71.85 41.29 49 971 135308 29438199
Diarrhoea 57.10 41.29 63 957 332635 29240872
Blood chromogranin A increased 48.37 41.29 8 1012 195 29573312
Constipation 48.12 41.29 36 984 114124 29459383
Serum serotonin increased 46.84 41.29 7 1013 86 29573421

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Flushing 47.91 39.04 24 1024 78624 64419060
Abdominal pain 46.16 39.04 39 1009 312336 64185348
Disease progression 44.58 39.04 28 1020 141652 64356032
Death 43.93 39.04 46 1002 482659 64015025

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

None

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

DiseaseRelationSNOMED_IDDOID
Diarrhea indication 62315008




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.14 Basic
pKa2 2.78 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 250MG BASE XERMELO TERSERA N208794 Feb. 28, 2017 RX TABLET ORAL 7709493 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 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

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 250MG BASE XERMELO TERSERA N208794 Feb. 28, 2017 RX TABLET ORAL Feb. 28, 2022 NEW CHEMICAL ENTITY
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

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Tryptophan 5-hydroxylase 1 Enzyme INHIBITOR IC50 7.80 SCIENTIFIC LITERATURE DRUG LABEL

External reference:

IDSource
8G388563M7 UNII
C4317559 UMLSCUI
CHEMBL2105695 ChEMBL_ID
25181577 PUBCHEM_CID
DB12095 DRUGBANK_ID
D09974 KEGG_DRUG
CHEMBL3348963 ChEMBL_ID
C000592493 MESH_SUPPLEMENTAL_RECORD_UI
9490 IUPHAR_LIGAND_ID
1872441 RXNORM
252423 MMSL
32389 MMSL
d08528 MMSL
733879005 SNOMEDCT_US
4036470 VANDF
017120 NDDF
017121 NDDF
C000621725 MESH_SUPPLEMENTAL_RECORD_UI
1137608-69-5 SECONDARY_CAS_RN

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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 24 sections