Telotristat ethyl
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Black Box Warning
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Warning Title
See full prescribing information for complete Boxed Warning.
Condition Name: (Content)
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Overview
Telotristat ethyl is a Acetylcholine release inhibitor, Adrenergic receptor agonist that is FDA approved for the (type of indication of drug) of a list of indications, separated by commas.. There is a Black Box Warning for this drug as shown here. Common adverse reactions include a list of adverse reactions, separated by commas..
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
Condition 1
- Dosing Information
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Condition 2
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Off-Label Use and Dosage (Adult)
Guideline-Supported Use
Condition 1
- Developed by: (Organisation)
- Class of Recommendation: (Class) (Link)
- Strength of Evidence: (Category A/B/C) (Link)
- Dosing Information/Recommendation
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Condition 2
- Developed by: (Organisation)
- Class of Recommendation: (Class) (Link)
- Strength of Evidence: (Category A/B/C) (Link)
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Non–Guideline-Supported Use
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Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
Condition 1
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Condition 2
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Off-Label Use and Dosage (Pediatric)
Guideline-Supported Use
Condition 1
- Developed by: (Organisation)
- Class of Recommendation: (Class) (Link)
- Strength of Evidence: (Category A/B/C) (Link)
- Dosing Information/Recommendation
- (Dosage)
Condition 2
- Developed by: (Organisation)
- Class of Recommendation: (Class) (Link)
- Strength of Evidence: (Category A/B/C) (Link)
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Non–Guideline-Supported Use
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Contraindications
CONTRAINDICATIONS
Warnings
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Warning Title
See full prescribing information for complete Boxed Warning.
Condition Name: (Content)
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Conidition 1
(Description)
Conidition 2
(Description)
Conidition 3
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Adverse Reactions
Clinical Trials Experience
Central Nervous System
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Cardiovascular
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Respiratory
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Gastrointestinal
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Hypersensitive Reactions
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Miscellaneous
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Condition 2
Central Nervous System
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Cardiovascular
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Respiratory
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Gastrointestinal
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Hypersensitive Reactions
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Miscellaneous
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Postmarketing Experience
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Drug Interactions
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Drug 1
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Drug 4
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Drug 5
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Use in Specific Populations
Pregnancy
Pregnancy Category (FDA):
(Description)
Pregnancy Category (AUS):
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Telotristat ethyl in women who are pregnant.
Labor and Delivery
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Nursing Mothers
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Pediatric Use
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Geriatic Use
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Gender
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Race
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Renal Impairment
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Hepatic Impairment
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Females of Reproductive Potential and Males
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Immunocompromised Patients
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Others
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Administration and Monitoring
Administration
(Oral/Intravenous/etc)
Monitoring
Condition 1
(Description regarding monitoring, from Warnings section)
Condition 2
(Description regarding monitoring, from Warnings section)
Condition 3
(Description regarding monitoring, from Warnings section)
IV Compatibility
There is limited information regarding the compatibility of Telotristat ethyl and IV administrations.
Overdosage
Acute Overdose
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Management
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Chronic Overdose
Signs and Symptoms
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Management
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Pharmacology
Telotristat ethyl
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Mechanism of Action
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Structure
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Pharmacodynamics
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Pharmacokinetics
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Nonclinical Toxicology
Carcinogenesis, Mutagenesis, Impairment of Fertility
- In a 26-week study in transgenic (Tg.rasH2) mice, telotristat ethyl was not tumorigenic at oral doses up to 300 mg/kg/day.
- Telotristat ethyl was negative in the in vitro Ames test, the in vitro chromosomal aberration test using Chinese hamster ovary cells, and the in vivo rat micronucleus test.
- Telotristat ethyl at oral doses up to 500 mg/kg/day (approximately 5 times the AUC for the active metabolite at the RHD) was found to have no effect on fertility and reproductive performance of male or female rats.
Clinical Studies
- A 12-week double-blind, placebo-controlled, randomized, multicenter trial of Xermelo was conducted in adult patients with a well-differentiated metastatic neuroendocrine tumor and carcinoid syndrome diarrhea who were having between 4 to 12 daily bowel movements despite the use of SSA therapy at a stable dose for at least 3 months. Patients were randomized to placebo or treatment with Xermelo 250 mg three times daily.
- Study medication was administered within 15 minutes before or within 1 hour after a meal or snack. All patients were required to stay on their baseline SSA regimen and were allowed to use rescue medication (short-acting octreotide) and antidiarrheals (e.g., loperamide) for symptomatic relief. A total of 90 patients were evaluated for efficacy. The mean age of the population was 63 years of age (range 37 to 83 years), 50% were male, and 90% were White.
- The primary efficacy endpoint was the change from baseline in the number of daily bowel movements averaged over the 12-week treatment period. The analysis results can be found in TABLE 2 below. The average was based on the number of days with valid, non-missing data. When a patient had more than 6 weeks of missing data, the change from baseline was considered equal to zero. A week of missing data was defined as a patient missing at least 4 days of diary data in that week.
- In the 12-week study, a difference in average weekly reductions in bowel movement frequency between Xermelo and placebo was observed as early as 1 to 3 weeks, and persisted for the remaining 9 weeks of the study.
- To aid in the interpretation of the bowel movement reduction results, the proportion of patients reporting any particular level of reduction in overall average bowel movement frequency is depicted in Figure 1 below. For example, 33% of patients randomized to Xermelo and 4% of patients randomized to placebo experienced a reduction in overall average bowel movements from baseline of at least 2 bowel movements per day.
- Other symptoms of carcinoid syndrome (abdominal pain or flushing) did not show improvement in the comparison of Xermelo to placebo.
- The average number of daily short-acting octreotide injections used for rescue therapy over the 12-week double-blind treatment period was 0.3 and 0.7 in the Xermelo and placebo groups, respectively. In the subgroup of patients who received short-acting octreotide injections, observed reductions in the number of bowel movements per day and treatment differences were generally consistent with the reductions and differences observed in patients who did not receive rescue therapy, and were similar to the overall data presented in TABLE 2 above.
- A third randomized treatment arm of Xermelo 500 mg three times daily did not demonstrate additional treatment benefit on the primary endpoint and had a greater incidence of adverse reactions than Xermelo 250 mg three times daily. Therefore, Xermelo 500 mg three times daily is not recommended.
How Supplied
- 250 mg tablet: white to off-white coated oval tablet with “T-E” debossed on one side and “250” debossed on the other side.
- Xermelo is dispensed in a monthly case for a total of 28 days of therapy. Each monthly case contains four weekly boxes. Each weekly box contains seven daily dose packs (day pack).
- NDC 70183-125-84: Monthly case of 84 tablets. Each child resistant daily dose pack (day pack) contains three 250 mg tablets.
Storage
- Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).
Images
Drug Images
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Package and Label Display Panel
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Patient Counseling Information
- Advise patients:
- If they experience severe constipation or severe persistent or worsening abdominal pain, to discontinue Xermelo and contact their healthcare provider.
- To take Xermelo with food.
- When short-acting octreotide is used in combination with Xermelo, administer short-acting octreotide at least 30 minutes after administering Xermelo.
- If a dose is missed, take the next dose at the regular time. Do not take 2 doses at the same time to make up for a missed dose.
Precautions with Alcohol
Alcohol-Telotristat ethyl interaction has not been established. Talk to your doctor regarding the effects of taking alcohol with this medication.
Brand Names
- Xermelo
Look-Alike Drug Names
There is limited information regarding Telotristat ethyl Look-Alike Drug Names in the drug label.
Drug Shortage Status
Drug Shortage
Price
References
The contents of this FDA label are provided by the National Library of Medicine.