Efficacy and safety of BH4 before the age of 4 years in patients with mild phenylketonuria

J Inherit Metab Dis. 2012 Nov;35(6):975-81. doi: 10.1007/s10545-012-9464-3. Epub 2012 Mar 3.

Abstract

Background: Sapropterin dihydrochloride, an EMEA-approved synthetic formulation of BH4, has been available in Europe since 2009 for PKU patients older than 4 years, but its use with younger children is allowed in France based on an expert recommendation. We report the cases of 15 patients treated under the age of 4 years and demonstrate the safety and efficacy of this treatment for patients in this age group.

Patients and method: We report the use of BH4 in 15 PKU patients treated before the age of 4 years.

Results: Fifteen patients were enrolled in this retrospective study. Mean phenylalaninemia at diagnosis was 542 ± 164 μM and all patients had mild PKU (maximal phenylalaninemia: 600-1200 μM). BH4 responsiveness was assessed using a 24-hour BH4 loading test (20 mg/kg), performed during the neonatal period (n = 11) or before 18 months of age (n = 4). During the test, these patients exhibited an 80 ± 12% decrease in phenylalaninemia. Long-term BH4 therapy was initiated during the neonatal period (n = 7) or at the age of 13 ± 12 months (n = 8). The median duration of treatment was 23 months [min 7; max 80]. BH4 therapy drastically improved dietary phenylalanine tolerance (456 ± 181 vs 1683 ± 627 mg/day, p < 0.0001) and allowed a phenylalanine-free amino acid mixture to be discontinued or not introduced in 14 patients. Additionally, in the eight patients treated after a few months of diet therapy, BH4 treatment significantly decreased mean phenylalaninemia (352 ± 85 vs 254 ± 64 μM, p < 0.05), raised the percentage of phenylalaninemia tests within therapeutic targets [120-300 μM] (35 ± 25 vs 64 ± 16%, p < 0.05), and reduced phenylalaninemia variance (130 ± 21 vs 93 ± 27 μM, p < 0.05). No side effects were reported.

Conclusion: BH4-therapy is efficient and safe before the age of 4 years in mild PKU, BH4-responsive patients.

Publication types

  • Multicenter Study

MeSH terms

  • Age Factors
  • Biopterins / administration & dosage
  • Biopterins / analogs & derivatives*
  • Biopterins / therapeutic use
  • Child, Preschool
  • Female
  • France
  • Genotype
  • Humans
  • Infant
  • Infant, Newborn
  • Male
  • Mutation
  • Phenylalanine / administration & dosage
  • Phenylalanine / blood
  • Phenylalanine Hydroxylase / genetics
  • Phenylketonurias / blood
  • Phenylketonurias / diagnosis
  • Phenylketonurias / diet therapy
  • Phenylketonurias / drug therapy*
  • Retrospective Studies
  • Treatment Outcome

Substances

  • Biopterins
  • Phenylalanine
  • Phenylalanine Hydroxylase
  • sapropterin