Details of the Drug

General Information of Drug (ID: DMDIYFZ)

• Drug Name: Telotristat ethyl
• Synonyms: Telotristat; Telotristat etiprate; LP-778902; LX-1032; LX-1606; Serotonin modulator (oral, GI disorder/hypertension/carcinoid syndrome), Lexicon; Tryptophan hydroxylase inhibitor (oral, GI disorder/hypertension/carcinoid syndrome), Lexicon

Indication

Disease Entry	ICD 11	Status	REF
Carcinoid syndrome	5B10	Approved	[1]
Carcinoid syndrome diarrhea	DA90.0	Approved	[2]

• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 3:
  Molecular Weight (mw); 575
  Logarithm of the Partition Coefficient (xlogp); 5.1
  Rotatable Bond Count (rotbonds); 10
  Hydrogen Bond Donor Count (hbonddonor); 2
  Hydrogen Bond Acceptor Count (hbondacc); 11
• ADMET Property:
  Half-life: The concentration or amount of drug in body reduced by one-half in 4C12 hours [3]
  Metabolism: The drug is metabolized via the liver []
• Chemical Identifiers:
  Formula: C27H26ClF3N6O3
  IUPAC Name: ethyl (2S)-2-amino-3-[4-[2-amino-6-[(1R)-1-[4-chloro-2-(3-methylpyrazol-1-yl)phenyl]-2,2,2-trifluoroethoxy]pyrimidin-4-yl]phenyl]propanoate
  Canonical SMILES: CCOC(=O)[C@H](CC1=CC=C(C=C1)C2=CC(=NC(=N2)N)O[C@H](C3=C(C=C(C=C3)Cl)N4C=CC(=N4)C)C(F)(F)F)N
  InChI: InChI=1S/C27H26ClF3N6O3/c1-3-39-25(38)20(32)12-16-4-6-17(7-5-16)21-14-23(35-26(33)34-21)40-24(27(29,30)31)19-9-8-18(28)13-22(19)37-11-10-15(2)36-37/h4-11,13-14,20,24H,3,12,32H2,1-2H3,(H2,33,34,35)/t20-,24+/m0/s1
  InChIKey: MDSQOJYHHZBZKA-GBXCKJPGSA-N
• Cross-matching ID:
  PubChem CID: 25181577
  CAS Number: 1033805-22-9
  DrugBank ID: DB12095
  TTD ID: D0RE6T
  ACDINA ID: D00658
• Repurposed Drugs (RPD): Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Tryptophan hydroxylase (TPH)	TTDJBV3	TPH1_HUMAN ; TPH2_HUMAN	Modulator	[4]

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Telotristat ethyl (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Oliceridine	DM6MDCF	Major	Increased metabolism of Telotristat ethyl caused by Oliceridine mediated induction of CYP450 enzyme.	Acute pain [MG31]	[5]
Erdafitinib	DMI782S	Major	Increased metabolism of Telotristat ethyl caused by Erdafitinib mediated induction of CYP450 enzyme.	Bladder cancer [2C94]	[6]
Pexidartinib	DMS2J0Z	Moderate	Increased metabolism of Telotristat ethyl caused by Pexidartinib mediated induction of CYP450 enzyme.	Bone/articular cartilage neoplasm [2F7B]	[7]
Bay 80-6946	DMLOS5R	Moderate	Increased metabolism of Telotristat ethyl caused by Bay 80-6946 mediated induction of CYP450 enzyme.	Follicular lymphoma [2A80]	[8]
Tazemetostat	DMWP1BH	Major	Increased metabolism of Telotristat ethyl caused by Tazemetostat mediated induction of CYP450 enzyme.	Follicular lymphoma [2A80]	[9]
Ripretinib	DM958QB	Moderate	Increased metabolism of Telotristat ethyl caused by Ripretinib mediated induction of CYP450 enzyme.	Gastrointestinal stromal tumour [2B5B]	[10]
Avapritinib	DMK2GZX	Moderate	Increased metabolism of Telotristat ethyl caused by Avapritinib mediated induction of CYP450 enzyme.	Gastrointestinal stromal tumour [2B5B]	[11]
MK-1439	DM215WE	Major	Increased metabolism of Telotristat ethyl caused by MK-1439 mediated induction of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[11]
Pemigatinib	DM819JF	Moderate	Increased metabolism of Telotristat ethyl caused by Pemigatinib mediated induction of CYP450 enzyme.	Liver cancer [2C12]	[12]
Brigatinib	DM7W94S	Major	Increased metabolism of Telotristat ethyl caused by Brigatinib mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[10]
Lurbinectedin	DMEFRTZ	Major	Decreased metabolism of Telotristat ethyl caused by Lurbinectedin mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[13]
PF-06463922	DMKM7EW	Major	Increased metabolism of Telotristat ethyl caused by PF-06463922 mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[11]
Pralsetinib	DMWU0I2	Moderate	Increased metabolism of Telotristat ethyl caused by Pralsetinib mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[14]
Selpercatinib	DMZR15V	Moderate	Increased metabolism of Telotristat ethyl caused by Selpercatinib mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[15]
Ubrogepant	DM749I3	Moderate	Increased metabolism of Telotristat ethyl caused by Ubrogepant mediated induction of CYP450 enzyme.	Migraine [8A80]	[16]
Rimegepant	DMHOAUG	Major	Increased metabolism of Telotristat ethyl caused by Rimegepant mediated induction of CYP450 enzyme.	Migraine [8A80]	[17]
Fedratinib	DM4ZBK6	Moderate	Increased metabolism of Telotristat ethyl caused by Fedratinib mediated induction of CYP450 enzyme.	Myeloproliferative neoplasm [2A20]	[11]
Macimorelin	DMQYJIR	Moderate	Increased metabolism of Telotristat ethyl caused by Macimorelin mediated induction of CYP450 enzyme.	Pituitary gland disorder [5A60-5A61]	[15]
Lefamulin	DME6G97	Moderate	Increased metabolism of Telotristat ethyl caused by Lefamulin mediated induction of CYP450 enzyme.	Pneumonia [CA40]	[15]
Darolutamide	DMV7YFT	Moderate	Increased metabolism of Telotristat ethyl caused by Darolutamide mediated induction of CYP450 enzyme.	Prostate cancer [2C82]	[18]
Upadacitinib	DM32B5U	Moderate	Increased metabolism of Telotristat ethyl caused by Upadacitinib mediated induction of CYP450 enzyme.	Rheumatoid arthritis [FA20]	[11]
Larotrectinib	DM26CQR	Moderate	Increased metabolism of Telotristat ethyl caused by Larotrectinib mediated induction of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[10]

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Beta-D-lactose	E00099	6134	Diluent; Dry powder inhaler carrier; Lyophilization aid
Carmellose sodium	E00625	Not Available	Disintegrant
Magnesium stearate	E00208	11177	lubricant
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Telotristat ethyl 250 mg tablet	250 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

• [1] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [2] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2018
• [3] Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
• [4] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [5] Product Information. Mycobutin (rifabutin). Pharmacia and Upjohn, Kalamazoo, MI.
• [6] Cronk GA, Wheatley WB, Fellers GF, Albright H "The relationship of food intake to the absorption of potassium alpha-phenoxyethyl penicillin and potassium phenoxymethyl penicillin from the gastrointestinal tract." Am J Med Sci 240 (1960): 219-25. [PMID: 13812969]
• [7] Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
• [8] Product Information. Aliqopa (copanlisib). Bayer Pharmaceutical Inc, West Haven, CT.
• [9] Product Information. Tazverik (tazemetostat). Epizyme, Inc, Cambridge, MA.
• [10] Cerner Multum, Inc. "Australian Product Information.".
• [11] Cerner Multum, Inc. "UK Summary of Product Characteristics.".
• [12] Product Information. Pemazyre (pemigatinib). Incyte Corporation, Wilmington, DE.
• [13] Product Information. Xermelo (telotristat ethyl). Lexicon Pharmaceuticals, Inc., The Woodlands, TX.
• [14] Product Information. Gavreto (pralsetinib). Blueprint Medicines Corporation, Cambridge, MA.
• [15] Product Information. Diabinese (chlorpropamide). Pfizer US Pharmaceuticals, New York, NY.
• [16] Product Information. Ubrelvy (ubrogepant). Allergan Inc, Irvine, CA.
• [17] Product Information. Nurtec ODT (rimegepant). Biohaven Pharmaceuticals, New Haven, CT.
• [18] Jerntorp P, Almer LO "Chlorpropamide-alcohol flushing in relation to macroangiopathy and peripheral neuropathy in non-insulin dependent diabetes." Acta Med Scand 656 (1981): 33-6. [PMID: 6953748]