eliglustat (Rx)

Brand and Other Names:Cerdelga
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

capsule

  • 84mg
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Gaucher Disease

Indicated for the long-term treatment of adults with Gaucher disease type 1 who are CYP2D6 extensive metabolizers (EM), intermediate metabolizers (IM), or poor metabolizers (PM) as detected by an FDA-cleared test for genotype

Dose is based on patient's CYP2D6 metabolizer status

CYP2D6 EMs or IMs: 84 mg PO BID

CYP2D6 PMs: 84 mg PO qDay

Dosage Modifications

Drugs that inhibit CYP2D6 and CYP3A pathways may significantly increase systemic exposure to eliglustat and result in prolongation of the PR, QTc, and/or QRS cardiac interval, which could result in cardiac arrhythmias

Some CYP2D6 and CYP3A inhibitors are contraindicated with eliglustat, depending on the patient’s metabolizer status

Coadministration of eliglustat with other CYP2D6 and CYP3A inhibitors may require dose reduction of eliglustat, depending on the patient’s CYP2D6 metabolizer status, to reduce the exposure to eliglustat

Hepatic impairment (all stages): Use not recommended

Renal impairment

  • Mild: No dosage adjustment required
  • Moderate-to-severe or end-stage renal disease: Has not been studied and use is not recommended

Dosing Considerations

Patients who are CYP2D6 ultra-rapid metabolizers (URMs) may not achieve adequate serum concentrations to achieve a therapeutic effect

CYP2D6 genotype not determined: Specific dosage cannot be recommended for indeterminate metabolizers

Administration

Swallow capsules whole, do not crush, dissolve, or open capsules

May take with or without food

Avoid eating grapefruit or drinking grapefruit juice

Safety and efficacy not established

Studies did not include sufficient numbers of subjects aged ≥65 yr to determine whether they respond differently from younger subjects

Clinical experience has not identified differences in responses between elderly and younger patients

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Interactions

Interaction Checker

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            Adverse Effects

            >10%

            Arthralgia (45%)

            Headache (13-40%)

            Fatigue (14%)

            Nausea (10-12%)

            Diarrhea (12%)

            Back pain (12%)

            Extremity pain (11%)

            1-10%

            Upper abdominal pain (10%)

            Migraine (10%)

            Flatulence (10%)

            Oropharyngeal pain (10%)

            Dizziness (8%)

            Asthenia (8%)

            Cough (7%)

            Dyspepsia (7%)

            GERD (7%)

            Constipation (5%)

            Palpitations (5%)

            Rash (5%)

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            Warnings

            Contraindications

            Extensive/intermediate metabolizers taking a strong or moderate CYP2D6 inhibitor with a strong or moderate CYP3A inhibitor

            Intermediate/poor metabolizers taking a strong CYP3A inhibitor

            Cautions

            CYP2D6 and CYP3A substrate; drugs that inhibit CYP2D6 and CYP3A metabolism may significantly increase eliglustat systemic exposure and result in prolongation of the PR, QTc, and/or QRS cardiac intervals

            Some CYP2D6 and CYP3A inhibitors are contraindicated with eliglustat, depending on the patient’s CYP2D6 metabolizer status

            Eliglustat inhibits P-gp and CYP2D6; coadministration with P-gp or CYP2D6 substrates may result in increased concentrations of the concomitant drug

            Increases in ECG intervals (PR, QTc, and QRS) occurs at substantially elevated eliglustat plasma concentrations; avoid use in patients with pre-existing cardiac conditions (eg, CHF, recent acute MI, bradycardia, heart block, ventricular arrhythmia), long QT syndrome, and in combination with class IA (eg, quinidine, procainamide) and class III (eg, amiodarone, sotalol) antiarrhythmics

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            Pregnancy & Lactation

            Pregnancy Category: C

            Women with Gaucher disease type 1 have an increased risk of spontaneous abortion, especially if disease symptoms are not treated and controlled preconception and during a pregnancy

            In animal reproduction studies, a spectrum of anomalies at doses 6 times the recommended human dose were observed in orally dosed rats; no fetal harm was observed with oral administration to pregnant rabbits at dose levels 10 times the recommended human dose

            Use during pregnancy only if the potential benefit justifies the potential risk to the fetus

            Lactation: Unknown if distributed in human breast milk; not recommended; a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the lactating woman

            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

            Gaucher disease is caused by a deficiency of the lysosomal enzyme acid β-glucosidase (ie, glucocerebrosidase), which catalyzes the conversion of the sphingolipid glucocerebroside into glucose and ceramide

            The enzymatic deficiency causes an accumulation of glucosylceramide (GL-1), primarily in the lysosomal compartment of macrophages, giving rise to foam cells or "Gaucher cells"

            Eliglustat is a specific inhibitor of glucosylceramide synthase, thereby reducing production of glucosylceramide

            Absorption

            Peak plasma concentration, peak plasma time, and AUC dependent on CYP2D6 phenotype

            CYP2D6 EM

            • Bioavailability: <5% (single dose, significant first-pass metabolism)
            • Peak plasma time: 1.5-2 hr
            • Peak plasma concentration: 12.1-25 ng/mL
            • AUC: 76.3-143 hr•ng/mL

            CYP2D6 IM

            • Peak plasma concentration: 44.6 ng/mL
            • AUC: 306 hr•ng/mL

            CYP2D6 PM

            • Peak plasma time: 3 hr (BID dosing)
            • Peak plasma concentration: 113-137 ng/mL (BID dose); 75 ng/mL (predicted for once-daily dose)
            • AUC: 922-1057 hr•ng/mL (BID dose); 956 hr•ng/mL (predicted for once-daily dose)

            Distribution

            Protein bound: 76-83%

            In the blood, it is mainly distributed in plasma and not RBCs

            Vd: 835 L

            Metabolism

            Extensively metabolized in the liver with high clearance, mainly by CYP2D6 and to a lesser extent CYP3A4

            No active metabolites have been identified

            Elimination

            Half-life: 6.5 hr (EM); 8.9 hr (PM)

            Total body clearance: 88 L/hr

            Excretion: 51.4% feces; 41.8% urine

            Excreted mainly as metabolites

            Pharmacogenomics

            Dosage is based the patient’s CYP2D6 metabolizer status

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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.
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