telotristat ethyl (Rx)

Brand and Other Names:Xermelo
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 250mg

Carcinoid Syndrome Diarrhea

Indicated for carcinoid syndrome diarrhea in combination with somatostatin analog (SSA) therapy in adults inadequately controlled by SSA therapy

250 mg PO TID

Also see Administration

Safety and efficacy not established

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Interactions

Interaction Checker

and telotristat ethyl

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    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Nausea (13%)

            Headache (11%)

            1-10%

            Increased GGT (9%)

            Depression (9%)

            Peripheral edema (7%)

            Flatulence (7%)

            Decreased appetite (7%)

            Pyrexia (7%)

            Abdominal pain (5%)

            Constipation (5%)

            Increased alkaline phosphatase (<5%)

            Increased ALT and AST (<5%)

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            Warnings

            Contraindications

            None

            Cautions

            Reduces bowel movement frequency; monitor for development of constipation and/or severe, persistent, or worsening abdominal pain; discontinue if severe constipation or severe persistent or worsening abdominal pain develops

            Drug interaction overview

            • Telotristat ethyl induces CYP3A4 and may reduce systemic exposure of sensitive CYP3A4 substrates
            • Short-acting octreotide decreases telotristat Cmax and AUC by 79% and 68%, respectively; administer octreotide at least 30 minutes after telotristat ethyl (also see Administration)
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            Pregnancy

            Pregnancy

            There are no human data in pregnant women to inform a drug-associated risk

            Animal studies

            • No effects on embryo-fetal development were observed with administration of telotristat ethyl to rats during organogenesis at doses up to 750 mg/kg/day (~9 times the exposure at recommended human dose [RHD])
            • Treatment of pregnant rabbits during organogenesis produced maternal toxicity and postimplantation loss at doses of ≥250 mg/kg/day (~15 times the exposure at the RHD), and reduced fetal weight at 500 mg/kg/day (~33 times the exposure at the RHD)

            Lactation

            Unknown if distributed in human breast milk

            Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for the drug, and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition

            If administered to a breastfeeding woman, monitor infant for constipation

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Telotristat, the active metabolite of telotristat ethyl, inhibits tryptophan hydroxylase, which mediates the rate-limiting step in serotonin biosynthesis

            Serotonin plays a role in mediating secretion, motility, inflammation, and sensation of the GI tract, and is overproduced in patients with carcinoid syndrome

            In vitro inhibitory potency of telotristat towards tryptophan hydroxylase is 29 times higher than that of telotristat ethyl

            Absorption

            Peak plasma time: 1 hr (telotristat ethyl); 2 hr (telotristat)

            Peak plasma concentration: 7 ng/mL (telotristat ethyl); 900 ng/mL (telotristat)

            AUC: 22 ng·hr/mL (telotristat ethyl); 3000 ng·hr/mL (telotristat)

            Administration with food significantly increases systemic exposure of telotristat ethyl and telotristat

            Distribution

            Protein bound: >99% (both telotristat ethyl and telotristat)

            P-gp substrate

            Metabolism

            Telotristat ethyl undergoes hydrolysis via carboxylesterases to telotristat, its active metabolite

            Telotristat is further metabolized

            Telotristat ethyl and telotristat are not substrates for CYP enzymes

            Elimination

            Half-life: 0.6 hr (telotristat ethyl); 5 hr (telotristat)

            Total clearance: 2.7 L/hr (telotristat ethyl); 152 L/hr (telotristat)

            Excretion: <0.4% urine; 92.8% feces

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            Administration

            Oral Administration

            Take with food

            When used in combination with short-acting octreotide, administer short-acting octreotide at least 30 minutes after telotristat ethyl

            Discontinue if severe constipation develops

            Missed dose

            • 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

            Storage

            Store at controlled room temperature (25°C [77°F])

            Excursions permitted to 15-30°C (59-86°F)

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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