Telotristat ethyl
Pronunciation: tel-OH-tri-stat-ETH-il
Brand name: Xermelo
Dosage form: tablet (250mg)
Drug class: Miscellaneous GI agents
What is Telotristat ethyl?
Telotristat ethyl is an FDA-approved medication used to treat carcinoid syndrome diarrhea in combination with somatostatin analog (SSA) therapy when SSA therapy alone does not provide adequate relief. Carcinoid syndrome diarrhea is due to carcinoid tumors producing excess serotonin which causes frequent diarrhea and other symptoms.
Telotristat ethyl works by blocking the enzyme responsible for producing serotonin, thereby reducing serotonin levels in the body. This reduction helps control diarrhea associated with carcinoid syndrome.
Telotristat ethyl brand name is Xermelo.
Telotristat ethyl FDA approval indication is for the treatment of carcinoid syndrome diarrhea in combination with SSA therapy for adults whose symptoms remain uncontrolled by SSA therapy alone. FDA approval was granted on February 28, 2017, for Lexicon Pharmaceuticals, Inc.
How telotristat ethyl works
Telotristat ethyl mechanism of action is as a tryptophan hydroxylase inhibitor
- Carcinoid tumors release serotonin, which stimulates rapid gut contractions, preventing proper water absorption and causing diarrhea.
- Telotristat ethyl inhibits the enzyme tryptophan hydroxylase, reducing serotonin production and directly targeting the underlying cause of carcinoid syndrome diarrhea.
- When used with SSA therapy, which blocks serotonin release, telotristat ethyl further decreases serotonin levels, improving symptom control.
This medication is not a chemotherapy drug and does not treat the tumor itself. Instead, it manages symptoms associated with carcinoid syndrome.
Clinical trials: How effective is telotristat ethyl?
Phase III Study Results
A placebo-controlled phase III study (TELESTAR) evaluated telotristat ethyl in 135 carcinoid syndrome patients who experienced 4 or more bowel movements (BM) per day despite taking somatostatin analog therapy. Telotristat dose was three times daily.
Key Findings (12-Week Double-Blind Study):
- BM Frequency Reduction:
- Telotristat ethyl 250 mg: 1.7 fewer bowel movements per day
- Telotristat ethyl 500 mg: 2.1 fewer bowel movements per day
- Placebo group: 0.9 fewer bowel movements per day
- Urinary 5-HIAA Reduction: Both telotristat ethyl dosages significantly lowered 5-hydroxyindole acetic acid (5-HIAA) levels (a marker of serotonin production), confirming the drug's effectiveness.
Conclusion: The study demonstrated that telotristat ethyl effectively reduces diarrhea symptoms in patients with carcinoid syndrome, when SSAs alone are insufficient.
Telotristat ethyl side effects
Common telotristat side effects:
- Nausea (13%)
- Loss of appetite (7%)
- Gas (7%)
- Headache (11%)
- Depressed mood (9%)
- Swelling in hands or feet (7%)
- Fever; (7%)
- Increased GGT levels (9%)
These common side effects occurred in at least 5% of patients taking Telotristat 250 mg three times a day in the double-blind, placebo-controlled clinical trial of 90 patients with metastatic neuroendocrine tumors and carcinoid syndrome diarrhea.
Serious telotristat side effects
- Signs of an allergic reaction (hives, difficulty breathing, swelling of the face, lips, tongue, or throat)
- Severe constipation
- Severe or worsening stomach pain
This is not a comprehensive list of side effects. Consult your doctor for medical advice, or report side effects to the FDA at 1-800-FDA-1088.
Related/similar drugs
Warnings
- Use only as directed by your doctor.
- Inform your doctor about any medications, allergies, or pre-existing conditions.
- Discontinue use if you experience severe constipation or persistent abdominal pain.
Before taking this medicine
Tell your doctor if you have:
- Have ever had liver disease
- Pregnancy or breastfeeding concerns
This medication is not approved for individuals under 18 years old.
Telotristat ethyl dosage
Recommended telotristat ethyl adult dose
- 250 mg tablet, taken three times a day with food.
- The medication is packaged in a monthly case containing four weekly boxes, with seven daily doses per week.
- Short-acting octreotide should be administered at least 30 minutes after taking telotristat ethyl.
Missed Dose
- If you miss a dose, skip it and take the next dose at the regular time.
- Do not double the dose to make up for a missed one.
Overdose
- In case of overdose, seek emergency medical help or call the Poison Help Line at 1-800-222-1222.
Drug interactions
Sometimes it is not safe to use certain medications at the same time. Some drugs can affect your blood levels of other drugs you take, which may increase side effects or make the medications less effective.
- CYP3A4 substrates, such as midazolam, may have reduced effectiveness when taken with telotristat ethyl.
- Always inform your doctor about all medications you are taking, including:
- Prescription drugs
- Over-the-counter medicines
- Vitamins and supplements
- Herbal products
You can use the Drug Interaction Checker or consult your healthcare provider to verify potential interactions.
Telotristat Ethyl Package Insert
HCPs and patients often use the Telotristat Ethyl Package Insert (PI) - Xermelo brand - for more detailed information about this medicine. The Telotristat Ethyl Package Insert (prescribing information) contains more comprehensive information on Indications and Usage, Dosage and Administration, Clinical Pharmacology, Clinical Studies, Drug Interaction, and more. Discuss any medical questions you have with your HCP (health care professional). This is not all the information you need to know about this medicine for safe and effective use, and it does not take the place of talking to your doctor about your treatment.
The Package Insert is sometimes called Prescribing Information (PI) or FDA label.
Additional information
Storage
- Store at 25°C (77°F).
- Permitted temperature excursions: 15°C to 30°C (59°F to 86°F).
Ingredients
- Active ingredient: 250 mg of telotristat ethyl (free base), equivalent to 328 mg telotristat etiprate.
- Inactive ingredients: colloidal silicon dioxide, croscarmellose sodium, hydroxypropyl cellulose, lactose anhydrous, macrogol/PEG, magnesium stearate, polyvinyl alcohol (partially hydrolyzed), talc, and titanium dioxide.
Manufacturer
Telotristat ethyl is produced by Lexicon Pharmaceuticals, Inc., located in The Woodlands, TX 77381.
Popular FAQ
How long does it take for Xermelo to start working?
In studies conducted for the FDA approval of Xermelo, most patients saw a significant improvement in their diarrhea frequency in 12 weeks, and some patients saw results as soon as 3 weeks. Xermelo targets the overproduction of serotonin inside mNET cells to lessen carcinoid syndrome diarrhea.
What type of diarrhea does Xermelo treat?
Xermelo (telotristat ethyl) is a tablet used to treat carcinoid syndrome diarrhea. This is a type of diarrhea that develops in people with carcinoid tumors. Continue reading
References
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