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Telotristat Etiprate

FDA-approved product (tablet, oral), marketed as Xermelo.

Registered studies
27
Lab records
0
Pathogens at ≥40%
3 of 4

Chemical structure

Chemical structure of Telotristat Etiprate
A drawing shows what the molecule is, not what it does.

Existing / approved use

Documented · FDA, WHO, ChEMBL

Approved for

  • Carcinoid tumor
  • Diarrhea
  • Neuroendocrine neoplasm

Indications ChEMBL records as approved, from FDA and DailyMed labels. Label ↗

WHO therapeutic group
Various alimentary tract and metabolism products
Anti-infective classification
Not classified as an anti-infective.

Repurposing investigation

This medicine is being investigated here for AI-predicted antimicrobial activity against M. tuberculosis, MRSA and E. coli. It was surfaced computationally for further investigation; it is not an established treatment for these infections.

AI-predicted activity

AI prediction · nothing measured
  • MRSA54.0% AI-predicted activityAt or above the ≥40% mark this site uses to surface candidates.
  • E. coli54.9% AI-predicted activityAt or above the ≥40% mark this site uses to surface candidates.
  • K. pneumoniae34.7% AI-predicted activityBelow the ≥40% mark this site uses to surface candidates.
  • M. tuberculosis60.0% AI-predicted activityAt or above the ≥40% mark this site uses to surface candidates.

A model’s estimate of laboratory activity against each pathogen species. It is not clinical effectiveness.

Evidence

Clinical and experimental

Documented evidence

Clinical

27registered studies name this medicine, for any condition. See them below.

Experimental

No evidence found

No laboratory measurement against the four pathogens in the ChEMBL records loaded here.

Docking

Computational · nothing measured

Dihydrofolate reductase ↗ (E. coli)

Not yet docked: queued in the docking rundetails

KPC-2 carbapenemase ↗ (K. pneumoniae)

Not yet docked: queued in the docking rundetails

Enoyl-ACP reductase (InhA) ↗ (M. tuberculosis)

Not yet docked: queued in the docking rundetails

Dihydrofolate reductase ↗ (MRSA)

Not yet docked: queued in the docking rundetails

AutoDock Vina, one experimentally solved protein per pathogen. This project’s screening target is -7.0 kcal/mol, its own mark rather than a universal cutoff. A docking score is a structural hypothesis, not proof of binding, and requires experimental validation.

Other medicines to investigate

AI prediction · nothing measured

Other repurposing candidates: approved medicines besides Telotristat Etiprate with AI-predicted activity ≥40% against the chosen pathogen, leaving out existing antimicrobials. They are computational candidates for further investigation, not alternatives and not recommendations.

Sorted by AI-predicted activity, high to low. The order is not a ranking of which medicine is better.

Registered studies

A registration describes a study; it does not establish a positive result.

  • Telotristat Ethyl for Reducing Intraoperative Carcinoid Crisis in Patients With Neuroendocrine Tumors

    NCT04672876 · start 2022-01

    Registered record
    Registry ID
    NCT04672876
    Conditions
    Neuroendocrine Tumors
    Interventions
    Telotristat Ethyl Oral Tablet
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Withdrawn
    Start
    2022-01
    Completion
    2023-10-01
    Enrolment
    0

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionNeuroendocrine Tumors
    InterventionTelotristat Ethyl Oral Tablet
    PhasePhase 2
    Registry statusWithdrawn
  • Telotristat With Lutathera in Neuroendocrine Tumors

    NCT04543955 · start 2021-09-13

    Registered record
    Registry ID
    NCT04543955
    Conditions
    Neuroendocrine Tumors
    Interventions
    Telotristat (Low-Dose); Telotristat (High-Dose)
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Terminated
    Start
    2021-09-13
    Completion
    2022-06-03
    Enrolment
    1

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionNeuroendocrine Tumors
    InterventionTelotristat (Low-Dose); Telotristat (High-Dose)
    PhasePhase 2
    Registry statusTerminated
  • Telotristat Ethyl for the Treatment of Carcinoid Heart Disease in Patients With Metastatic Neuroendocrine Tumor

    NCT04810091 · start 2021-05-18

    Registered record
    Registry ID
    NCT04810091
    Conditions
    Locally Advanced Neuroendocrine Neoplasm; Metastatic Neuroendocrine Neoplasm
    Interventions
    Placebo Administration; Questionnaire Administration; Telotristat Ethyl
    Study type
    INTERVENTIONAL
    Phase
    Phase 3
    Registry status
    Active not recruiting
    Start
    2021-05-18
    Completion
    2026-08-03
    Enrolment
    79

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionLocally Advanced Neuroendocrine Neoplasm; Metastatic Neuroendocrine Neoplasm
    InterventionPlacebo Administration; Questionnaire Administration; Telotristat Ethyl
    PhasePhase 3
    Registry statusActive not recruiting
  • Prospective Assessment of Patients With Neuroendocrine Tumors and Current or Prior History of Carcinoid Syndrome or Diarrhea Undergoing Peptide Receptor Radionuclide Therapy With or Without Telotristat Ethyl

    NCT04713202 · start 2021-03-03

    Registered record
    Registry ID
    NCT04713202
    Conditions
    Neuroendocrine Tumors; Carcinoid Syndrome; Diarrhea
    Interventions
    Telotristat ethyl; Peptide Receptor Radionuclide Therapy; Placebo
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Withdrawn
    Start
    2021-03-03
    Completion
    2024-02
    Enrolment
    0

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionNeuroendocrine Tumors; Carcinoid Syndrome; Diarrhea
    InterventionTelotristat ethyl; Peptide Receptor Radionuclide Therapy; Placebo
    PhasePhase 2
    Registry statusWithdrawn
  • Retifanlimab (INCMGA00012) and Telotristat Ethyl for the Treatment of Advanced Neuroendocrine Tumors and Carcinoid Syndrome

    NCT04776876 · start 2021-03-01

    Registered record
    Registry ID
    NCT04776876
    Conditions
    Advanced Neuroendocrine Neoplasm; Carcinoid Syndrome
    Interventions
    Retifanlimab; Telotristat Ethyl
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Withdrawn
    Start
    2021-03-01
    Completion
    2021-09-02
    Enrolment
    0

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionAdvanced Neuroendocrine Neoplasm; Carcinoid Syndrome
    InterventionRetifanlimab; Telotristat Ethyl
    PhasePhase 2
    Registry statusWithdrawn
  • Open Label Study to Analyze the Effect of Telotristat Ethyl on Weight Regulation/Gain

    NCT04034745 · start 2020-10

    Registered record
    Registry ID
    NCT04034745
    Conditions
    Pancreatic Cancer; Neuroendocrine Tumors; Cachexia; Cancer
    Interventions
    telotristat ethyl
    Study type
    OBSERVATIONAL
    Phase
    Not recorded
    Registry status
    Withdrawn
    Start
    2020-10
    Completion
    2023-11
    Enrolment
    0

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionPancreatic Cancer; Neuroendocrine Tumors; Cachexia; Cancer
    Interventiontelotristat ethyl
    PhaseNot recorded
    Registry statusWithdrawn
  • Lanreotide Combined With Telotristat Ethyl or Placebo for the First-line Treatment in Patients With Advanced Well Differentiated Small Intestinal Neuroendocrine Tumours (siNET) With Highly-functioning Carcinoid Syndrome

    NCT04065165 · start 2020-04

    Registered record
    Registry ID
    NCT04065165
    Conditions
    Small Intestinal NET; Carcinoid Heart Disease
    Interventions
    Telotristat Ethyl; Lanreotide
    Study type
    INTERVENTIONAL
    Phase
    Phase 3
    Registry status
    Withdrawn
    Start
    2020-04
    Completion
    2027-10
    Enrolment
    0

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionSmall Intestinal NET; Carcinoid Heart Disease
    InterventionTelotristat Ethyl; Lanreotide
    PhasePhase 3
    Registry statusWithdrawn
  • Telotristat Ethyl to Promote Weight Stability in Patients With Advanced Stage Pancreatic Cancer

    NCT03910387 · start 2019-04-17

    Registered record
    Registry ID
    NCT03910387
    Conditions
    Locally Advanced Unresectable Pancreatic Adenocarcinoma; Metastatic Pancreatic Adenocarcinoma; Recurrent Pancreatic Adenocarcinoma; Stage III Pancreatic Cancer AJCC v8; Stage IV Pancreatic Cancer AJCC v8
    Interventions
    Gemcitabine; Nab-paclitaxel; Telotristat Ethyl
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Completed
    Start
    2019-04-17
    Completion
    2022-06-29
    Enrolment
    23

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionLocally Advanced Unresectable Pancreatic Adenocarcinoma; Metastatic Pancreatic Adenocarcinoma; Recurrent Pancreatic Adenocarcinoma; Stage III Pancreatic Cancer AJCC v8 +1 more
    InterventionGemcitabine; Nab-paclitaxel; Telotristat Ethyl
    PhasePhase 2
    Registry statusCompleted
  • A Safety and Efficacy Study of XERMELO® + First-line Chemotherapy in Patients With Advanced Biliary Tract Cancer

    NCT03790111 · start 2019-03-13

    Registered record
    Registry ID
    NCT03790111
    Conditions
    Biliary Tract Cancer (BTC)
    Interventions
    telotristat ethyl
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Terminated
    Start
    2019-03-13
    Completion
    2022-01-13
    Enrolment
    53

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionBiliary Tract Cancer (BTC)
    Interventiontelotristat ethyl
    PhasePhase 2
    Registry statusTerminated
  • AMT-PET in Monitoring Telotristat Etiprate Treatment in Participants With MetastaticNeuroendocrine Neoplasm

    NCT03453489 · start 2018-06-20

    Registered record
    Registry ID
    NCT03453489
    Conditions
    Carcinoid Syndrome; Metastatic Nonfunctional Well Differentiated Neuroendocrine Neoplasm
    Interventions
    Carbon C 11 Alpha-methyltryptophan; Laboratory Biomarker Analysis; Positron Emission Tomography; Telotristat Etiprate
    Study type
    INTERVENTIONAL
    Phase
    Phase 2
    Registry status
    Completed
    Start
    2018-06-20
    Completion
    2020-10-15
    Enrolment
    4

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionCarcinoid Syndrome; Metastatic Nonfunctional Well Differentiated Neuroendocrine Neoplasm
    InterventionCarbon C 11 Alpha-methyltryptophan; Laboratory Biomarker Analysis; Positron Emission Tomography; Telotristat Etiprate
    PhasePhase 2
    Registry statusCompleted
  • Study to Compare a Dose of Telotristat Etiprate in Subjects With Renal Impairment With Matched Subjects With Normal Renal Function

    NCT03442725 · start 2018-02-09

    Registered record
    Registry ID
    NCT03442725
    Conditions
    Renal Impairment
    Interventions
    Telotristat etiprate
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2018-02-09
    Completion
    2018-05-13
    Enrolment
    16

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionRenal Impairment
    InterventionTelotristat etiprate
    PhasePhase 1
    Registry statusCompleted
  • Study to Evaluate the Pharmacokinetics of Telotristat Ethyl in Subjects With Severe Hepatic Impairment

    NCT03423446 · start 2017-11-28

    Registered record
    Registry ID
    NCT03423446
    Conditions
    Hepatic Impairment
    Interventions
    Telotristat Ethyl
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2017-11-28
    Completion
    2018-06-15
    Enrolment
    16

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionHepatic Impairment
    InterventionTelotristat Ethyl
    PhasePhase 1
    Registry statusCompleted
  • A Phase 1 Study to Evaluate the Effects of Omeprazole and Famotidine on the Absorption of Telotristat Ethyl in Healthy Subjects

    NCT03302845 · start 2017-09-21

    Registered record
    Registry ID
    NCT03302845
    Conditions
    Drug-drug Interaction
    Interventions
    Omeprazole 40 MG; Famotidine 40 mg; Telotristat ethyl 250 mg
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2017-09-21
    Completion
    2017-11-07
    Enrolment
    32

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionDrug-drug Interaction
    InterventionOmeprazole 40 MG; Famotidine 40 mg; Telotristat ethyl 250 mg
    PhasePhase 1
    Registry statusCompleted
  • Real-world Evidence Study EvaLuating PAtient-Reported Outcomes With XERMELO

    NCT03223428 · start 2017-06-22

    Registered record
    Registry ID
    NCT03223428
    Conditions
    Carcinoid Syndrome
    Interventions
    Xermelo
    Study type
    OBSERVATIONAL
    Phase
    Not recorded
    Registry status
    Completed
    Start
    2017-06-22
    Completion
    2022-01-14
    Enrolment
    223

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionCarcinoid Syndrome
    InterventionXermelo
    PhaseNot recorded
    Registry statusCompleted
  • Study to Evaluate a Dose of Telotristat Etiprate in Male and Female With Mild, Moderate and Severe Hepatic Insufficiency and Matched Healthy Subjects

    NCT02683577 · start 2016-02

    Registered record
    Registry ID
    NCT02683577
    Conditions
    Hepatic Impairment
    Interventions
    telotristat etiprate
    Study type
    INTERVENTIONAL
    Phase
    Phase 1
    Registry status
    Completed
    Start
    2016-02
    Completion
    2016-07
    Enrolment
    24

    As stored from ClinicalTrials.gov. Registration describes a study; it does not mean the study worked.

    ConditionHepatic Impairment
    Interventiontelotristat etiprate
    PhasePhase 1
    Registry statusCompleted