Medically reviewed by Drugs.com. Last updated on May 20, 2020.
(tel OH tri state ETH il)
- Telotristat Etiprate
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Xermelo: 250 mg
Brand Names: U.S.
- Tryptophan Hydroxylase Inhibitor
Telotristat ethyl is a small molecule inhibitor of tryptophan hydroxylase (TPH). TPH converts tryptophan to 5-hydroxytryptophan and ultimately to serotonin, and is the rate-limiting enzyme in serotonin synthesis (Kulke 2017). Decreased production of peripheral serotonin by telotristat ethyl results in a reduction in the frequency of carcinoid syndrome diarrhea.
The high molecular weight and acidic moieties of telotristat ethyl inhibit the compound from crossing the blood brain barrier (Kulke 2017).
Telotristat ethyl is hydrolyzed via carboxylesterases to the metabolite telotristat (active); telotristat is further metabolized.
Feces (~93%); urine (<1%)
Time to Peak
Telotristat ethyl: 0.5 to 2 hours; Telotristat: 1 to 3 hours
Telotristat ethyl: ~0.6 hours; Telotristat: ~5 hours
Use: Labeled Indications
Carcinoid syndrome diarrhea: Treatment of carcinoid syndrome diarrhea (in combination with somatostatin analog therapy) in adults with symptoms inadequately controlled by somatostatin analog therapy
There are no contraindications listed within the manufacturer's labeling.
Carcinoid syndrome diarrhea: Oral: 250 mg 3 times daily
Missed dose: If a dose is missed, administer the next dose at the regularly scheduled time; do not take 2 doses at the same time.
Refer to adult dosing.
Dosing: Adjustment for Toxicity
Gastrointestinal toxicity: Discontinue for severe constipation or for development of severe, persistent or worsening abdominal pain
Administer with food. If used in combination with short-acting octreotide, administer octreotide at least 30 minutes after telotristat ethyl. Rescue octreotide (short-acting) and antidiarrheals were allowed and unrestricted in a clinical study (Kulke 2017).
Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).
CloZAPine: CYP3A4 Inducers (Weak) may decrease the serum concentration of CloZAPine. Monitor therapy
NiMODipine: CYP3A4 Inducers (Weak) may decrease the serum concentration of NiMODipine. Monitor therapy
Octreotide: May decrease the serum concentration of Telotristat Ethyl. Management: Administer short-acting octreotide at least 30 minutes after administration of telotristat ethyl and monitor for decreased telotristat ethyl efficacy. Consider therapy modification
Selpercatinib: CYP3A4 Inducers (Weak) may decrease the serum concentration of Selpercatinib. Monitor therapy
Tacrolimus (Systemic): CYP3A4 Inducers (Weak) may decrease the serum concentration of Tacrolimus (Systemic). Monitor therapy
Ubrogepant: CYP3A4 Inducers (Weak) may decrease the serum concentration of Ubrogepant. Management: Use an initial ubrogepant dose of 100 mg and second dose (if needed) of 100 mg when used with a weak CYP3A4 inducer. Consider therapy modification
Central nervous system: Headache (11%)
Gastrointestinal: Nausea (13%)
1% to 10%:
Cardiovascular: Peripheral edema (7%)
Central nervous system: Depression (9%)
Endocrine & metabolic: Increased gamma-glutamyl transferase (9%)
Gastrointestinal: Decreased appetite (7%), flatulence (7%), abdominal pain (≥5%), constipation (≥5%)
Hepatic: Increased serum alkaline phosphatase (<5%), increased serum ALT (<5%), increased serum AST (<5%)
Miscellaneous: Fever (7%)
Concerns related to adverse effects:
• Gastrointestinal toxicity: Constipation has been reported in clinical trials. Although rarely serious, some events resulted in hospitalization, intestinal perforation or bowel obstruction (these events occurred at a dose higher than the recommended dose). Patients with advanced carcinoid tumors may be at risk for altered gastrointestinal tract wall integrity; monitor closely for constipation and/or severe, persistent, or worsening abdominal pain. Discontinue for severe constipation and/or the development of severe persistent or worsening abdominal pain.
Monitor for symptoms of constipation and/or severe, persistent, or worsening abdominal pain
Adverse events were observed in some animal reproduction studies.
What is this drug used for?
• It is used to treat carcinoid syndrome diarrhea.
All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:
• Passing gas
• Lack of appetite
WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:
• Severe constipation
• Severe abdominal pain
• Swelling in the arms or legs
• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.
Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine’s uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.
Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.
More about telotristat
- Side Effects
- During Pregnancy
- Dosage Information
- Drug Interactions
- En Español
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- Drug class: miscellaneous GI agents
Other brands: Xermelo