Eliglustat

Eliglustat Brand Name– CERDELGA

What is Eliglustat

Eliglustat is an oral glucosylceramide synthase inhibitor indicated for the long-term treatment of adult patients with Gaucher disease type 1 (GD1).

Unlike enzyme replacement therapies, which break down fatty deposits that build up in cells of patients with Gaucher disease, eliglustat slows the accumulation of the fatty deposits by inhibiting the metabolic process that forms them.

Although ease of oral administration provides substantial benefit over intravenous enzyme replacement therapy, eliglustat use is somewhat limited by cytochrome P450 (CYP450) 2D6 genotype.

Eliglustat is primarily metabolized via CYP2D6 and, to a lesser extent, CYP3A. Patient selection should take into account CYP2D6 metabolizer status, as established by a FDA-cleared test.

Patients who are CYP2D6 ultra-rapid metabolizers may not achieve therapeutic concentrations of eliglustat.

Poor metabolizers require dosage reduction. In addition, depending on the patient’s CYP2D6 metabolizer status, concomitant administration of some CYP2D6 and CYP3A inhibitors may be contraindicated or require dosage adjustment to reduce the risk of potentially significant ECG changes.

Eliglustat was approved by the FDA in August 2014.

Indications

  • Gaucher disease

Side Effects

  1. abdominal pain
  2. arrhythmia exacerbation
  3. arthralgia
  4. asthenia
  5. back pain
  6. constipation
  7. cough
  8. diarrhea
  9. dizziness
  10. dyspepsia
  11. fatigue
  12. flatulence
  13. gastroesophageal reflux
  14. headache
  15. migraine
  16. nausea
  17. palpitations
  18. QT prolongation
  19. rash

Monitoring Parameters

  • LFTs

Contraindications

  • apheresis
  • AV block
  • bradycardia
  • breast-feeding
  • cardiomyopathy
  • celiac disease
  • females
  • fever
  • geriatric
  • heart failure
  • hepatic disease
  • human immunodeficiency virus (HIV) infection
  • hyperparathyroidism
  • hypocalcemia
  • hypokalemia
  • hypomagnesemia
  • hypothermia
  • hypothyroidism
  • long QT syndrome
  • myocardial infarction
  • pheochromocytoma
  • pregnancy
  • QT prolongation
  • renal failure
  • renal impairment
  • rheumatoid arthritis
  • sickle cell disease
  • sleep deprivation
  • stroke
  • systemic lupus erythematosus (SLE)

Interactions

  • Abiraterone
  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Acetaminophen; Caffeine; Dihydrocodeine
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine
  • Acetaminophen; Chlorpheniramine; Phenylephrine; Phenyltoloxamine
  • Acetaminophen; Codeine
  • Acetaminophen; Dextromethorphan
  • Acetaminophen; Dextromethorphan; Doxylamine
  • Acetaminophen; Dextromethorphan; Guaifenesin; Phenylephrine
  • Acetaminophen; Dextromethorphan; Phenylephrine
  • Acetaminophen; Dextromethorphan; Pseudoephedrine
  • Acetaminophen; Diphenhydramine
  • Acetaminophen; Hydrocodone
  • Acetaminophen; Oxycodone
  • Acetaminophen; Tramadol
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  • Chlorpheniramine; Hydrocodone
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  • grapefruit juice
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