Telotristat ethyl

Identification

Summary

Telotristat ethyl is a tryptophan hydroxylase inhibitor that is used to treat carcinoid syndrome diarrhea.

Brand Names

Xermelo

Generic Name

Telotristat ethyl

DrugBank Accession Number

DB12095

Background

Telotristat ethyl is a prodrug of telotristat that was approved by the FDA in March 2017 as Xermelo.⁸ It was previously referred to as telotristat etiprate, the hippurate salt form; however, the FDA recommends the use of the name of the neutral form rather than that of the salt.^4,5 Currently, telotristat ethyl is used to treat carcinoid syndrome diarrhea from neuroendocrine tumors that are inadequately controlled by short-acting somatostatin analog (SSA) treatment.⁸

Neuroendocrine cells are cells that secrete regulatory peptides and biogenic amines in response to chemical, neural, or other types of stimuli.⁶ Neuroendocrine tumors (NET) arising from these cells can therefore secrete chemical mediators into the bloodstream to cause side effects in distant sites, a phenomenon called carcinoid syndrome.⁶ The most common peptides and amines secreted by NET are histamines, tachykinins, kallikrein, and serotonin.¹² Overexposure to serotonin can cause severe diarrhea, one of the main clinical symptoms of carcinoid syndrome.⁴ Serotonin is metabolized in the urinary metabolite 5-hydroxy indole acetic acid (u5-HIAA), and high levels of u5-HIAA is associated with poor survival outcome in patients with NET.⁴ The first line treatment of carcinoid syndrome diarrhea is SSA, but symptoms still reoccur over the course of the disease.⁴

Type

Small Molecule

Groups

Approved, Investigational

Structure

3D

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MOLSDF3D-SDFPDBSMILESInChI

Similar Structures

Structure for Telotristat ethyl (DB12095)

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Weight

Average: 574.99
Monoisotopic: 574.1707009

Chemical Formula

C₂₇H₂₆ClF₃N₆O₃

Synonyms

• Telotristat ethyl

External IDs

• LX 1032
• LX 1606
• LX-1032
• LX-1606
• LX1032
• LX1606

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Pharmacology

Indication

Xermelo is indicated for the treatment of carcinoid syndrome diarrhea in combination with somatostatin analog (SSA) therapy in adults inadequately controlled by SSA therapy.⁸

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Age Group	Patient Characteristics	Dose Form
Used in combination to manage	Carcinoid syndrome diarrhea	Regimen in combination with: Octreotide (DB00104), Lanreotide (DB06791), Somatostatin (DB09099), Pasireotide (DB06663)	••••••••••••		••• •••••••••• •••••••••• •••• •••••••••••• •••••• ••••• •••••••	••••••

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Pharmacodynamics

In normal mice, telotristat etiprate (administered once daily for 4 days at doses of 15–300 mg/kg/day) was found to reduce serotonin levels throughout the gastrointestinal tract.^1,2 These reductions occurred in a dose dependent fashion with maximal effects observed with doses of telotristat etiprate ≥150 mg/kg. No significant change in brain serotonin or 5-hydroxyindoleacetic acid (5-HIAA, a serotonin metabolite) was observed.^1,2 Similar findings were seen in Sprague-Dawley rats. Gastrointestinal motility studies were conducted in rats using the charcoal meal test.^1,2 There was a significant dose-related delay in both gastrointestinal transit and gastric emptying, associated with a reduction in blood serotonin levels and proximal colon serotonin.^1,2

A quantitative whole-body autoradiography study was conducted to assess the absorption, distribution and excretion of radioactivity in rats following a single oral dose of telotristat etiprate labeled with carbon 14.^1,2 Rats were administered either 30 mg/kg or 100 mg/kg of the compound. The distribution of radioactivity was limited to tissues of the hepatic and renal system and the contents of the GI tract. There was no measurable radioactivity in the brain at any dose tested.^1,2

Mechanism of action

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.⁸

Target	Actions	Organism
ATryptophan 5-hydroxylase 2	antagonist	Humans
ATryptophan 5-hydroxylase 1	antagonist	Humans

Absorption

After a single oral dose of telotristat ethyl to healthy subjects, telotristat ethyl was absorbed and metabolized to its active metabolite, telotristat. Peak plasma concentrations of telotristat ethyl were achieved within 0.5 to 2 hours, and those of telotristat within 1 to 3 hours. Plasma concentrations thereafter declined in a biphasic manner. Following administration of a single 500 mg dose of telotristat ethyl (twice the recommended dosage) under fasted conditions in healthy subjects, the mean C_max and AUC_0-inf were 4.4 ng/mL and 6.23 ng•hr/mL, respectively for telotristat ethyl. The mean C_max and AUC_0-inf were 610 ng/mL and 2320 ng•hr/mL, respectively for telotristat. Peak plasma concentrations and AUC of telotristat ethyl and telotristat appeared to be dose proportional following administration of a single dose of telotristat ethyl in the range of 100 mg (0.4 times the lowest recommended dose to 1000 mg [4 times the highest recommended dose]) under fasted conditions.⁸

Following multiple-dose administration of telotristat ethyl 500 mg three times daily, there was negligible accumulation at steady state for both telotristat ethyl and telotristat.⁸

In patients with metastatic neuroendocrine tumors and carcinoid syndrome diarrhea treated with SSA therapy, the median T_max for telotristat ethyl and telotristat was approximately 1 and 2 hours, respectively. Following administration of 500 mg telotristat ethyl three times daily, with meals in patients, the mean C_max and AUC_0-6hr were approximately 7 ng/mL and 22 ng•hr/mL, respectively, for telotristat ethyl. The mean C_max and AUC_0-6hr were approximately 900 ng/mL and 3000 ng•hr/mL, respectively for telotristat. The pharmacokinetic parameters for both telotristat ethyl and telotristat were highly variable with about 55% coefficient of variation.⁸

Volume of distribution

The estimated apparent total volume of distribution for the active metabolite from the Population PK model of 428.1 L in a typical healthy fasted subject and 348.7 L in patients with carcinoid syndrome.¹¹

Protein binding

Both telotristat ethyl and telotristat are greater than 99% bound to human plasma proteins.⁸

Metabolism

After oral administration, telotristat ethyl undergoes hydrolysis via carboxylesterases to telotristat, its active metabolite. Telotristat is further metabolized.⁸ Among the metabolites of telotristat, the systemic exposure to an acid metabolite of oxidative deaminated decarboxylated telotristat was about 35% of that of telotristat.⁸ In vitro data suggest that telotristat ethyl and telotristat are not substrates for CYP enzymes.⁸

Hover over products below to view reaction partners

• Telotristat ethyl
  • Telotristat
    • M1 telotristat
      • M2 telotristat
        • LP-951757

Route of elimination

Following a single 500 mg oral dose of ¹⁴C-telotristat ethyl, 93.2% of the dose was recovered over 240 hours: 92.8% was recovered in the feces, with less than 0.4% being recovered in the urine.⁸

Half-life

Following a single 500 mg oral dose of telotristat ethyl in healthy subjects, the apparent half-life was approximately 0.6 hours for telotristat ethyl and 5 hours for telotristat.⁸

Clearance

The apparent total clearance at steady state (CL/F_ss) following oral dosing with telotristat ethyl 500 mg three times daily for 14 days (twice the recommended dosage) in healthy subjects was 2.7 and 152 L/hr for telotristat ethyl and telotristat, respectively.⁸

Adverse Effects

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Toxicity

An embryo-fetal development study performed in rats with oral telotristat ethyl at doses up to 750 mg/kg/day (approximately 9 times the AUC [area under the plasma concentration-time curve] for the active metabolite at the RHD) during organogenesis produced no harm to embryo-fetal development.⁸

In pregnant rabbits treated orally with telotristat ethyl during organogenesis, an increased incidence of post-implantation loss at doses of 250 and 500 mg/kg/day (approximately 15 times the AUC for the active metabolite at RHD) and a decrease in fetal weight at 500 mg/kg/day (approximately 33 times the AUC for the active metabolite at the RHD) was observed. The adverse effects on embryo-fetal development were associated with maternal toxicity (impaired weight gain and/or mortality) at 250 and 500 mg/kg/day. No adverse effects on embryo-fetal development were observed at 125 mg/kg/day (approximately 5 times the AUC for the active metabolite at the RHD).⁸

A pre-/postnatal development study was conducted in rats using oral administration of 100, 200, and 500 mg/kg/day telotristat ethyl during organogenesis through lactation. An increased incidence of pup mortality was observed during postnatal days 0 to 4 at the maternal dose of 500 mg/kg/day (approximately 5 times the AUC for the active metabolite at the RHD). No developmental abnormalities or effects on growth, learning, memory or reproductive performance were observed through the maturation of offspring at maternal doses of up to 500 mg/kg/day in surviving offspring.⁸

In a 26-week study in transgenic (Tg.rasH2) mice, telotristat ethyl was not tumorigenic at oral doses up to 300 mg/kg/day (approximately 12 to 19 times the AUC for the active metabolite at the RHD).⁸

In a 2-year carcinogenicity study in Sprague-Dawley rats, telotristat ethyl was not tumorigenic at oral doses up to 170 mg/kg/day (approximately 2 to 5 times the AUC for the active metabolite at the RHD).⁸

Telotristat ethyl was negative in the in vitro Ames test, the in vitro chromosomal aberration test using Chinese hamster ovary cells, and the in vivo rat micronucleus test.⁸

Telotristat ethyl at oral doses up to 500 mg/kg/day (approximately 5 times the AUC for the active metabolite at the RHD) was found to have no effect on the fertility and reproductive performance of male or female rats.⁸

Pathways

Not Available

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Interactions

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This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
Integrate drug-drug interactions in your software
1,2-Benzodiazepine	The serum concentration of 1,2-Benzodiazepine can be decreased when it is combined with Telotristat ethyl.
Abemaciclib	The serum concentration of Abemaciclib can be decreased when it is combined with Telotristat ethyl.
Abiraterone	The serum concentration of Abiraterone can be decreased when it is combined with Telotristat ethyl.
Abrocitinib	The serum concentration of Telotristat ethyl can be increased when it is combined with Abrocitinib.
Acalabrutinib	The serum concentration of Acalabrutinib can be decreased when it is combined with Telotristat ethyl.

Food Interactions

• Take with a high fat meal. High fat food increases the bioavailability of telotristat ethyl.
• Take with food. Food increases the bioavailability of telotristat ethyl.

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Product Ingredients

Ingredient	UNII	CAS	InChI Key
Telotristat etiprate	3T25U84H4U	1137608-69-5	XSFPZBUIBYMVEA-CELUQASASA-N

Active Moieties

Name	Kind	UNII	CAS	InChI Key
Telotristat	prodrug	381V4FCV2Z	1033805-28-5	NCLGDOBQAWBXRA-PGRDOPGGSA-N

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Xermelo	Tablet	250 mg	Oral	Serb Sas	2018-12-07	Not applicable
Xermelo	Tablet, film coated	250 mg	Oral	Serb Sas	2020-12-16	Not applicable
Xermelo	Tablet	250 mg/1	Oral	Tersera Therapeutics Llc	2020-10-05	Not applicable
Xermelo	Tablet, film coated	250 mg	Oral	Serb Sas	2020-12-16	Not applicable
Xermelo	Tablet	250 mg/1	Oral	Lexicon Pharmaceuticals, Inc.	2017-03-01	Not applicable

Categories

Drug Categories

• Antidiarrheals
• Cytochrome P-450 CYP2B6 Inducers
• Cytochrome P-450 CYP2B6 Inducers (strength unknown)
• Cytochrome P-450 CYP2C19 Inhibitors
• Cytochrome P-450 CYP2C19 inhibitors (strength unknown)
• Cytochrome P-450 CYP2C8 Inhibitors
• Cytochrome P-450 CYP2C8 Inhibitors (strength unknown)
• Cytochrome P-450 CYP2C9 Inhibitors
• Cytochrome P-450 CYP2C9 Inhibitors (strength unknown)
• Cytochrome P-450 CYP2D6 Inhibitors
• Cytochrome P-450 CYP2D6 Inhibitors (strength unknown)
• Cytochrome P-450 CYP3A Inducers
• Cytochrome P-450 CYP3A Inhibitors
• Cytochrome P-450 CYP3A4 Inducers
• Cytochrome P-450 CYP3A4 Inducers (strength unknown)
• Cytochrome P-450 CYP3A4 Inhibitors
• Cytochrome P-450 CYP3A4 Inhibitors (strength unknown)
• Cytochrome P-450 Enzyme Inducers
• Cytochrome P-450 Enzyme Inhibitors
• P-glycoprotein inhibitors
• P-glycoprotein substrates
• Tryptophan Hydroxylase Inhibitor
• UGT2B7 inducers

Chemical TaxonomyProvided by Classyfire

Description

This compound belongs to the class of organic compounds known as phenylalanine and derivatives. These are compounds containing phenylalanine or a derivative thereof resulting from reaction of phenylalanine at the amino group or the carboxy group, or from the replacement of any hydrogen of glycine by a heteroatom.

Kingdom

Organic compounds

Super Class

Organic acids and derivatives

Class

Carboxylic acids and derivatives

Sub Class

Amino acids, peptides, and analogues

Direct Parent

Phenylalanine and derivatives

Alternative Parents

Alpha amino acid esters / Phenylpyrimidines / Phenylpyrazoles / Amphetamines and derivatives / Alkyl aryl ethers / Aminopyrimidines and derivatives / Aralkylamines / Chlorobenzenes / Fatty acid esters / Aryl chlorides / Heteroaromatic compounds / Carboxylic acid esters / Azacyclic compounds / Monocarboxylic acids and derivatives / Organochlorides / Alkyl fluorides / Carbonyl compounds / Organofluorides / Hydrocarbon derivatives / Monoalkylamines / Organic oxides

show 11 more

Substituents

4-phenylpyrimidine / Alkyl aryl ether / Alkyl fluoride / Alkyl halide / Alpha-amino acid ester / Amine / Aminopyrimidine / Amphetamine or derivatives / Aralkylamine / Aromatic heteromonocyclic compound / Aryl chloride / Aryl halide / Azacycle / Azole / Benzenoid / Carbonyl group / Carboxylic acid ester / Chlorobenzene / Ether / Fatty acid ester / Fatty acyl / Halobenzene / Heteroaromatic compound / Hydrocarbon derivative / Monocarboxylic acid or derivatives / Monocyclic benzene moiety / Organic nitrogen compound / Organic oxide / Organic oxygen compound / Organochloride / Organofluoride / Organohalogen compound / Organoheterocyclic compound / Organonitrogen compound / Organooxygen compound / Phenylalanine or derivatives / Phenylpyrazole / Primary aliphatic amine / Primary amine / Pyrazole / Pyrimidine

show 31 more

Molecular Framework

Aromatic heteromonocyclic compounds

External Descriptors

Not Available

Affected organisms

• Humans and other mammals

Chemical Identifiers

UNII

8G388563M7

CAS number

1033805-22-9

InChI Key

MDSQOJYHHZBZKA-GBXCKJPGSA-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

IUPAC Name

ethyl (2S)-2-amino-3-(4-{2-amino-6-[(1R)-1-[4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl]-2,2,2-trifluoroethoxy]pyrimidin-4-yl}phenyl)propanoate

SMILES

CCOC(=O)[C@@H](N)CC1=CC=C(C=C1)C1=NC(N)=NC(O[C@H](C2=CC=C(Cl)C=C2N2C=CC(C)=N2)C(F)(F)F)=C1

References

General References

1. Lamarca A, Barriuso J, McNamara MG, Hubner RA, Valle JW: Telotristat ethyl: a new option for the management of carcinoid syndrome. Expert Opin Pharmacother. 2016 Dec;17(18):2487-2498. Epub 2016 Nov 16. [Article]
2. Kulke MH, O'Dorisio T, Phan A, Bergsland E, Law L, Banks P, Freiman J, Frazier K, Jackson J, Yao JC, Kvols L, Lapuerta P, Zambrowicz B, Fleming D, Sands A: Telotristat etiprate, a novel serotonin synthesis inhibitor, in patients with carcinoid syndrome and diarrhea not adequately controlled by octreotide. Endocr Relat Cancer. 2014 Oct;21(5):705-14. doi: 10.1530/ERC-14-0173. Epub 2014 Jul 10. [Article]
3. Tian DD, Leonowens C, Cox EJ, Gonzalez-Perez V, Frederick KS, Scarlett YV, Fisher MB, Paine MF: Indinavir Increases Midazolam N-Glucuronidation in Humans: Identification of an Alternate CYP3A Inhibitor Using an In Vitro to In Vivo Approach. Drug Metab Dispos. 2019 Jul;47(7):724-731. doi: 10.1124/dmd.119.087007. Epub 2019 Apr 26. [Article]
4. Pavel M, Gross DJ, Benavent M, Perros P, Srirajaskanthan R, Warner RRP, Kulke MH, Anthony LB, Kunz PL, Horsch D, Weickert MO, Lapuerta P, Jiang W, Kassler-Taub K, Wason S, Fleming R, Fleming D, Garcia-Carbonero R: Telotristat ethyl in carcinoid syndrome: safety and efficacy in the TELECAST phase 3 trial. Endocr Relat Cancer. 2018 Mar;25(3):309-322. doi: 10.1530/ERC-17-0455. Epub 2018 Jan 12. [Article]
5. Kulke MH, Horsch D, Caplin ME, Anthony LB, Bergsland E, Oberg K, Welin S, Warner RR, Lombard-Bohas C, Kunz PL, Grande E, Valle JW, Fleming D, Lapuerta P, Banks P, Jackson S, Zambrowicz B, Sands AT, Pavel M: Telotristat Ethyl, a Tryptophan Hydroxylase Inhibitor for the Treatment of Carcinoid Syndrome. J Clin Oncol. 2017 Jan;35(1):14-23. doi: 10.1200/JCO.2016.69.2780. Epub 2016 Oct 28. [Article]
6. Dillon JS, Chandrasekharan C: Telotristat ethyl: a novel agent for the therapy of carcinoid syndrome diarrhea. Future Oncol. 2018 May;14(12):1155-1164. doi: 10.2217/fon-2017-0340. Epub 2018 Jan 19. [Article]
7. FDA Review- Telotristat [Link]
8. FDA Approved Drug Products: XERMELO® (telotristat ethyl) tablets, for oral use 2022 [Link]
9. FDA Approved Drug Products: Xermelo (telotristat ethyl) tablets for oral use [Link]
10. CLINICAL PHARMACOLOGY AND BIOPHARMACEUTICS REVIEW(S) [Link]
11. Assessment Report: Xermelo (International non-proprietary name telotristat ethyl) [Link]
12. Carcinoid Syndrome [Link]

External Links

PubChem Compound

25025298

PubChem Substance

347828399

ChemSpider

28189674

BindingDB

445704

RxNav

1872441

ChEMBL

CHEMBL2105695

ZINC

ZINC000043205655

Wikipedia

Telotristat_ethyl

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">

Phase	Status	Purpose	Conditions	Count
3	Completed	Treatment	Carcinoid Syndrome	3
3	Recruiting	Treatment	Locally Advanced Neuroendocrine Neoplasm / Metastatic Neuroendocrine Neoplasm	1
3	Withdrawn	Treatment	Carcinoid Heart Disease / Small Intestinal Neuroendocrine Tumor	1
2	Active Not Recruiting	Supportive Care	Locally Advanced Unresectable Pancreatic Adenocarcinoma / Pancreatic Adenocarcinoma Metastatic / Recurrent Pancreatic Adenocarcinoma / Stage III Pancreatic Cancer AJCC v8 / Stage IV Pancreatic Cancer AJCC v8	1
2	Completed	Treatment	Carcinoid Syndrome	2

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Tablet	Oral	250 mg
Tablet	Oral	250 mg/1
Tablet, film coated	Oral	250 MG

Prices

Not Available

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
US7553840	No	2009-06-30	2027-12-11
US8193204	No	2012-06-05	2031-02-27
US7968559	No	2011-06-28	2027-12-11
US8653094	No	2014-02-18	2028-12-19
US7709493	No	2010-05-04	2027-12-11

Properties

State

Solid

Experimental Properties

Property	Value	Source
water solubility	71 mg/mL	L43342

Predicted Properties

Property	Value	Source
Water Solubility	0.00294 mg/mL	ALOGPS
logP	5.35	ALOGPS
logP	5.54	Chemaxon
logS	-5.3	ALOGPS
pKa (Strongest Acidic)	16.06	Chemaxon
pKa (Strongest Basic)	6.94	Chemaxon
Physiological Charge	1	Chemaxon
Hydrogen Acceptor Count	7	Chemaxon
Hydrogen Donor Count	2	Chemaxon
Polar Surface Area	131.17 Å2	Chemaxon
Rotatable Bond Count	11	Chemaxon
Refractivity	144.98 m3·mol-1	Chemaxon
Polarizability	55.38 Å3	Chemaxon
Number of Rings	4	Chemaxon
Bioavailability	0	Chemaxon
Rule of Five	No	Chemaxon
Ghose Filter	No	Chemaxon
Veber's Rule	No	Chemaxon
MDDR-like Rule	Yes	Chemaxon

Predicted ADMET Features

Not Available

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	splash10-004i-0000090000-c90e91b91d25f596be6f
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	splash10-05i0-3000190000-b5f226787f16d87e674e
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	splash10-01si-0000290000-69ee12a8ab51910338d8
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	splash10-03di-3020190000-fd1f60402493936541f0
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	splash10-05br-5280890000-8be17c601154f2b1d3f6
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	splash10-00g1-9020640000-e1afc225a69583e6e6c9

Chromatographic Properties

Collision Cross Sections (CCS)

Adduct	CCS Value (Å2)	Source type	Source
[M-H]-	224.68744	predicted	DeepCCS 1.0 (2019)
[M+H]+	226.64502	predicted	DeepCCS 1.0 (2019)
[M+Na]+	232.38544	predicted	DeepCCS 1.0 (2019)

Targets

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Details1. Tryptophan 5-hydroxylase 2

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Antagonist

General Function

Tryptophan 5-monooxygenase activity

Specific Function

Not Available

Gene Name

TPH2

Uniprot ID

Q8IWU9

Uniprot Name

Tryptophan 5-hydroxylase 2

Molecular Weight

56056.295 Da

References

1. Kulke MH, O'Dorisio T, Phan A, Bergsland E, Law L, Banks P, Freiman J, Frazier K, Jackson J, Yao JC, Kvols L, Lapuerta P, Zambrowicz B, Fleming D, Sands A: Telotristat etiprate, a novel serotonin synthesis inhibitor, in patients with carcinoid syndrome and diarrhea not adequately controlled by octreotide. Endocr Relat Cancer. 2014 Oct;21(5):705-14. doi: 10.1530/ERC-14-0173. Epub 2014 Jul 10. [Article]

Details2. Tryptophan 5-hydroxylase 1

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Antagonist

General Function

Tryptophan 5-monooxygenase activity

Specific Function

Not Available

Gene Name

TPH1

Uniprot ID

P17752

Uniprot Name

Tryptophan 5-hydroxylase 1

Molecular Weight

50984.725 Da

References

1. Kulke MH, O'Dorisio T, Phan A, Bergsland E, Law L, Banks P, Freiman J, Frazier K, Jackson J, Yao JC, Kvols L, Lapuerta P, Zambrowicz B, Fleming D, Sands A: Telotristat etiprate, a novel serotonin synthesis inhibitor, in patients with carcinoid syndrome and diarrhea not adequately controlled by octreotide. Endocr Relat Cancer. 2014 Oct;21(5):705-14. doi: 10.1530/ERC-14-0173. Epub 2014 Jul 10. [Article]

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Drug created at October 20, 2016 21:20 / Updated at February 15, 2023 07:39