Generic name: telotristat ethyl [ tel-OH-tri-stat-ETH-il ]
Dosage form: tablet (250 mg)
Drug class: Miscellaneous GI agents

Medically reviewed by Melisa Puckey, BPharm. Last updated on Mar 4, 2024.

What is Xermelo?

Xermelo tablets are used to treat carcinoid syndrome diarrhea in adults, Xermelo works by blocking the enzyme that helps make serotonin which reduces the amount of serotonin being made to help prevent diarrhea. Xermelo (telotristat ethyl) is a tryptophan hydroxylase inhibitor that specifically targets the underlying cause of carcinoid syndrome diarrhea, which is high serotonin levels. Xermelo is not a chemotherapy.

Carcinoid syndrome diarrhea is caused by carcinoid tumors releasing too much serotonin, which increases wave-like contractions in the gut (peristalsis). These contractions reduce how much water and electrolyte is absorbed from the gut, which leads to diarrhea. Carcinoid syndrome is a rare condition that affects people with metastatic neuroendocrine tumors (mNETs).

Xermelo is used together with medications such as octreotide (Sandostatin), which is a somatostatin analog (SSA) therapy; Xermelo is used with SSA therapy when the SSA therapy has not effectively controlled the diarrhea on its own.

Medications like octreotide work by blocking the release of serotonin. When Xermelo is combined with SSA therapy, they work well together as Xermelo reduces how much serotonin is made, and SSA therapy decreases the amount of serotonin released, leading to an improvement in carcinoid syndrome diarrhea symptoms.

Xermelo received FDA approval on February 28, 2017. Xermelo is indicated for treating carcinoid syndrome diarrhea in combination with somatostatin analog (SSA) therapy, such as octreotide in adults whose carcinoid syndrome diarrhea has not been controlled by SSA therapy.

Xermelo side effects

Common Xermelo side effects 

Common Xermelo side effects may include nausea, loss of appetite, gas, headache, depressed mood, swelling in your hands or feet, fever; or abnormal liver function tests.

Serious Xermelo side effects

Get emergency medical help if you have signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Xermelo may cause serious side effects. Stop using Xermelo and call your doctor at once if you have:

• severe constipation; or
• severe or worsening stomach pain.

This is not a complete list of side effects, and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Warnings

Use only as directed. Tell your doctor if you use other medicines or have other medical conditions or allergies.

Discontinue this medicine if severe constipation or severe persistent or worsening abdominal pain develops.

Before taking this medicine

Tell your doctor if you have ever had liver disease.

Tell your doctor if you are pregnant or breastfeeding.

Not approved for use by anyone younger than 18 years old.

Xermelo Dosing Information

Usual Xermelo Adult Dose: 250 mg tablet orally 3 times a day with food.

Xermelo comes in a monthly case that contains 4 weekly boxes; 1 box of 7 daily doses for use each week. Keep each tablet in the package until you are ready to take a dose.

Short-acting Octreotide is usually given at least 30 minutes after taking this medicine.

Follow all directions on your prescription label and read all medication guides or instruction sheets. Use the medicine exactly as directed.

This medicine is only part of a complete treatment program that may also include other medications. Do not change your doses or medication schedule without your doctor's advice.

Available as Xermelo 250mg tablets,

What happens if I miss a dose?

Skip the missed dose and use your next dose at the regular time. Do not use two doses at one time.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What should I avoid while taking Xermelo?

Follow your doctor's instructions about any restrictions on food, beverages, or activity.

What other drugs will affect Xermelo?

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.  Using Xermelo with medicines that are CYP3A4 substrates (e.g., midazolam) may decrease their effectiveness. Tell your doctor about all other medicines you use.

Other drugs may affect Xermelo, including prescription and over-the-counter medicines, vitamins, and herbal products.

Click on the link below to check for interactions with Xermelo.

Xermelo Package Insert

Review the Xermelo Package Insert for more detailed information about this medication. Discuss any medical questions you have with your doctor or other healthcare provider. This is not all the information you need to know about this medication.

Storage

Store at 25°C (77°F) with excursions permitted to 15°C to 30°C (59°F to 86°F) 

Ingredients

Active ingredients: 250 mg of telotristat ethyl (free base) which is equivalent to 328 mg telotristat etiprate. 

Inactive ingredients: colloidal silicon dioxide, croscarmellose sodium, hydroxypropyl cellulose, lactose anhydrous, macrogol/PEG, magnesium stearate, polyvinyl alcohol [part hydrolyzed], talc, and titanium dioxide.

Company

Xermelo by Lexicon Pharmaceuticals, Inc. The Woodlands, TX 77381.

Popular FAQ

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Medical Disclaimer

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