CYP3A4 Induction by Rifampin: An Alternative Pathway for Vitamin D Inactivation in Patients With CYP24A1 Mutations

J Clin Endocrinol Metab. 2017 May 1;102(5):1440-1446. doi: 10.1210/jc.2016-4048.

Abstract

Context: The P450 enzyme CYP24A1 is the principal inactivator of vitamin D metabolites. Biallelic loss-of-function mutations in CYP24A1 are associated with elevated serum levels of 1,25-dihydroxyvitamin D3 with consequent hypercalcemia and hypercalciuria and represent the most common form of idiopathic infantile hypercalcemia (IIH). Current management strategies for this condition include a low-calcium diet, reduced dietary vitamin D intake, and limited sunlight exposure. CYP3A4 is a P450 enzyme that inactivates many drugs and xenobiotics and may represent an alternative pathway for inactivation of vitamin D metabolites.

Objective: Our goal was to determine if rifampin, a potent inducer of CYP3A4, can normalize mineral metabolism in patients with IIH due to mutations in CYP24A1.

Methods: We treated two patients with IIH with daily rifampin (10 mg/kg/d, up to a maximum of 600 mg). Serum calcium, phosphorus, parathyroid hormone (PTH), liver, and adrenal function and vitamin D metabolites, as well as urinary calcium excretion, were monitored during treatment of up to 13 months.

Results: Prior to treatment, both patients had hypercalcemia, hypercalciuria, and nephrocalcinosis with elevated serum 1,25-dihydroxyvitamin D3 and suppressed serum PTH. Daily treatment with rifampin was well tolerated and led to normalization or improvement in all clinical and biochemical parameters.

Conclusion: These observations suggest that rifampin-induced overexpression of CYP3A4 provides an alternative pathway for inactivation of vitamin D metabolites in patients who lack CYP24A1 function.

Publication types

  • Case Reports
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Calcitriol / blood
  • Calcium / blood
  • Calcium / urine
  • Child
  • Cytochrome P-450 CYP3A Inducers / therapeutic use*
  • Female
  • Humans
  • Hypercalcemia / blood
  • Hypercalcemia / complications
  • Hypercalcemia / drug therapy*
  • Hypercalcemia / genetics
  • Hypercalciuria / etiology
  • Infant, Newborn, Diseases / blood
  • Infant, Newborn, Diseases / drug therapy*
  • Infant, Newborn, Diseases / genetics
  • Male
  • Metabolism, Inborn Errors / blood
  • Metabolism, Inborn Errors / complications
  • Metabolism, Inborn Errors / drug therapy*
  • Metabolism, Inborn Errors / genetics
  • Mutation
  • Nephrocalcinosis / etiology
  • Parathyroid Hormone / blood
  • Phosphorus / blood
  • Rifampin / therapeutic use*
  • Treatment Outcome
  • Vitamin D / blood
  • Vitamin D3 24-Hydroxylase / genetics

Substances

  • Cytochrome P-450 CYP3A Inducers
  • Parathyroid Hormone
  • Vitamin D
  • Phosphorus
  • CYP24A1 protein, human
  • Vitamin D3 24-Hydroxylase
  • Calcitriol
  • Calcium
  • Rifampin

Supplementary concepts

  • Hypercalcemia, Idiopathic, of Infancy