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Tryptophan hydroxylase inhibitor

Xermelo (telotrisat ethyl) is a prescription medicine used to treat diarrhea caused by carcinoid syndrome in adults. It is used alongside somatostatin analog (SSA) therapy when that therapy alone does not control the diarrhea well enough.

How it worksXermelo works as a tryptophan hydroxylase inhibitor to help manage symptoms of carcinoid syndrome.

Brand names:Xermelo

Used for
Carcinoid syndrome diarrhea
Conditions
Carcinoid syndrome
Class
Tryptophan hydroxylase inhibitorGastrointestinal

How to take

FormsOral
RoutesOral

The usual dose for adults is 250 mg taken three times every day.

You should take Xermelo with food. If you miss a dose, take it at your regular time, but do not take two doses at once to make up for a missed one.

Missed dose: Take the missed dose at your regular time. Do not take two doses at once.

Key warnings

  • ·Xermelo can cause constipation and reduce how often you have bowel movements. You should monitor for severe constipation or worsening abdominal pain and stop taking the medicine if these occur.

Do not use if

  • ·Do not use Xermelo if you have had an allergic reaction to telotrisat, such as a rash, itching, or swelling (angioedema).

Side effects

Common

NauseaHeadacheIncreased GGT (liver enzyme)DepressionFlatulenceDecreased appetiteSwelling in the limbs (peripheral edema)Fever (pyrexia)

Serious

  • ·Constipation
  • ·Severe or worsening abdominal pain
  • ·Intestinal perforation
  • ·Intestinal obstruction
  • ·Fecaloma
  • ·Allergic reactions (swelling, rash, or itching)

Seek help if

  • ·Severe constipation
  • ·Severe or worsening abdominal pain
  • ·Allergic reaction symptoms like rash or swelling

Interactions

  • ·Drugs that use the CYP3A4 pathway (like midazolam) may be less effective when taken with Xermelo.
  • ·Drugs that use the CYP2B6 pathway (like bupropion or efavirans) may be less effective when taken with Xermelo.
  • ·If you use short-acting octreotide, wait at least 30 minutes after taking Xermelo before taking the octreotide.
FoodTake Xermelo with food.

Special populations

PregnancyThere is no data on how Xermelo affects pregnant women. In animal studies, very high doses caused issues like pregnancy loss and reduced fetal weight, but the risks for humans are not yet known.

PediatricThe safety and effectiveness of Xermelo for children have not been studied.

GeriatricIn clinical trials, older adults (65 and older) used the drug similarly to younger adults, though older people might be more sensitive to some side effects.

Talk to your doctor

Monitor

  • ·Bowel movement frequency
  • ·Abdominal pain
  • ·Liver enzymes (GGT)
  • ·Signs of allergic reaction

Questions to ask

  • ·Can I take Xermelo if I have liver or kidney issues?
  • ·How will Xermelo interact with my other medications?
  • ·What should I do if I experience severe constipation?
  • ·Is it safe to take Xermelo with my current SSA therapy?

Pharmacokinetics

MetabolismSystemic exposure of telotrisat ethyl and its active metabolite, telotrisat, increases in patients with moderate or severe hepatic impairment.

Educational summary derived from FDA labeling, AI-assisted. Not medical advice — consult a healthcare professional. Updated 2026-04-26.