Efficacy and pharmacokinetics of betaine in CBS and cblC deficiencies: a cross-over randomized controlled trial.


Journal

Orphanet journal of rare diseases
ISSN: 1750-1172
Titre abrégé: Orphanet J Rare Dis
Pays: England
ID NLM: 101266602

Informations de publication

Date de publication:
14 11 2022
Historique:
received: 01 07 2022
accepted: 30 10 2022
entrez: 15 11 2022
pubmed: 16 11 2022
medline: 18 11 2022
Statut: epublish

Résumé

Betaine is an "alternate" methyl donor for homocysteine remethylation catalyzed by betaine homocysteine methyltransferase (BHMT), an enzyme mainly expressed in the liver and kidney. Betaine has been used for more than 30 years in pyridoxine non-responsive cystathionine beta-synthase (pnrCBS) and cobalamin C (cblC) deficiencies to lower the hyperhomocysteinemia, although little is known about the optimal therapeutic dosage and its pharmacokinetic in these patients. We compared 2 betaine doses (100 mg/kg/day vs. 250 mg/kg/day) in children affected by pnrCBS or cblC deficiencies. We also measured the pharmacokinetics parameters after a single dose of betaine (100 or 250 mg/kg) in these patients. We conducted a prospective, randomized, crossover clinical trial with blinded evaluation. The primary outcome was the equivalence of total plasma homocysteine (tHcy) concentrations upon one-month oral treatment with betaine at 100 versus 250 mg/kg/day. Eleven patients completed the study (5 pnrCBS and 6 cblC). tHcy concentrations were equivalent after a one-month treatment period for the two betaine dosages. Multivariate analysis showed a significant effect of betaine dose on methionine (Met) (p = 0.01) and S-adenosylmethionine (SAM) concentrations (p = 0.006). Our analysis shows that there is no overt benefit to increasing betaine dosage higher than 100 mg/kg/day to lower tHcy concentrations in pnrCBS and cblC deficiencies. However, increasing betaine up to 250 mg/kg/d could benefit cblC patients through the increase of methionine and SAM concentrations, as low Met and SAM concentrations are involved in the pathophysiology of this disease. In contrast, in pnrCBS deficiency, betaine doses higher than 100 mg/kg/day could be harmful to these patients with pre-existing hypermethioninemia. Clinical Trials, NCT02404337. Registered 23 May 2015-prospectively registered, https://clinicaltrials.gov .

Sections du résumé

BACKGROUND
Betaine is an "alternate" methyl donor for homocysteine remethylation catalyzed by betaine homocysteine methyltransferase (BHMT), an enzyme mainly expressed in the liver and kidney. Betaine has been used for more than 30 years in pyridoxine non-responsive cystathionine beta-synthase (pnrCBS) and cobalamin C (cblC) deficiencies to lower the hyperhomocysteinemia, although little is known about the optimal therapeutic dosage and its pharmacokinetic in these patients.
AIMS
We compared 2 betaine doses (100 mg/kg/day vs. 250 mg/kg/day) in children affected by pnrCBS or cblC deficiencies. We also measured the pharmacokinetics parameters after a single dose of betaine (100 or 250 mg/kg) in these patients.
METHODS
We conducted a prospective, randomized, crossover clinical trial with blinded evaluation. The primary outcome was the equivalence of total plasma homocysteine (tHcy) concentrations upon one-month oral treatment with betaine at 100 versus 250 mg/kg/day.
RESULTS
Eleven patients completed the study (5 pnrCBS and 6 cblC). tHcy concentrations were equivalent after a one-month treatment period for the two betaine dosages. Multivariate analysis showed a significant effect of betaine dose on methionine (Met) (p = 0.01) and S-adenosylmethionine (SAM) concentrations (p = 0.006).
CONCLUSIONS
Our analysis shows that there is no overt benefit to increasing betaine dosage higher than 100 mg/kg/day to lower tHcy concentrations in pnrCBS and cblC deficiencies. However, increasing betaine up to 250 mg/kg/d could benefit cblC patients through the increase of methionine and SAM concentrations, as low Met and SAM concentrations are involved in the pathophysiology of this disease. In contrast, in pnrCBS deficiency, betaine doses higher than 100 mg/kg/day could be harmful to these patients with pre-existing hypermethioninemia.
TRIAL REGISTRATION
Clinical Trials, NCT02404337. Registered 23 May 2015-prospectively registered, https://clinicaltrials.gov .

Identifiants

pubmed: 36376887
doi: 10.1186/s13023-022-02567-4
pii: 10.1186/s13023-022-02567-4
pmc: PMC9664596
doi:

Substances chimiques

Betaine 3SCV180C9W
Cystathionine beta-Synthase EC 4.2.1.22
Methionine AE28F7PNPL
S-Adenosylmethionine 7LP2MPO46S
Homocysteine 0LVT1QZ0BA

Banques de données

ClinicalTrials.gov
['NCT02404337']

Types de publication

Randomized Controlled Trial Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

417

Informations de copyright

© 2022. The Author(s).

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Auteurs

Apolline Imbard (A)

Laboratoire de Biochimie-Hormonologie, Hôpital Robert Debré, APHP, Filière G2M, Paris, France. apolline.imbard@aphp.fr.
Laboratoire de Biochimie Métabolique, Hôpital Necker-Enfants-Malades, APHP, 149 Rue de Sèvres, Filière G2M, Paris, France. apolline.imbard@aphp.fr.
LYPSIS2, Faculté de Pharmacie de Chatenay-Malabry, Université Paris-Saclay, Paris, France. apolline.imbard@aphp.fr.

Artemis Toumazi (A)

Unité d'Epidémiologie Clinique, Unité de Recherche Clinique, Hôpital Robert Debré, Paris, France.
Inserm CIC-EC 1426, Paris, France.

Sophie Magréault (S)

UF de Pharmacologie | Service de Microbiologie, Hôpital Jean Verdier, Paris, France.
UMR 1137, Inserm, Paris, France.

Nuria Garcia-Segarra (N)

Centre de Référence Maladies Héréditaires du Métabolisme, Hôpital Robert Debré, APHP, Filière G2M, Paris, France.
Center for Molecular Diseases, Lausanne University Hospital, Lausanne, Switzerland.

Dimitri Schlemmer (D)

Laboratoire de Biochimie-Hormonologie, Hôpital Robert Debré, APHP, Filière G2M, Paris, France.

Florentia Kaguelidou (F)

Inserm CIC-EC 1426, Paris, France.
Centre d'Investigations Cliniques, Hôpital Robert Debré, APHP, Paris, France.

Isabelle Perronneau (I)

Laboratoire de Biochimie-Hormonologie, Hôpital Robert Debré, APHP, Filière G2M, Paris, France.

Jérémie Haignere (J)

Unité d'Epidémiologie Clinique, Unité de Recherche Clinique, Hôpital Robert Debré, Paris, France.

Hélène Ogier de Baulny (HO)

Centre de Référence Maladies Héréditaires du Métabolisme, Hôpital Robert Debré, APHP, Filière G2M, Paris, France.

Alice Kuster (A)

Centre de Compétence Maladies Héréditaires du Métabolisme, Centre Hospitalo-Universitaire de Nantes, Filière G2M, Nantes, France.

François Feillet (F)

Centre de Référence des Maladies Métaboliques, Inserm U1256 NGERE, Centre Hospitalo-Universitaire Brabois Enfants, Filière G2M, Vandoeuvre-Les-Nancy, France.

Corinne Alberti (C)

Unité d'Epidémiologie Clinique, Unité de Recherche Clinique, Hôpital Robert Debré, Paris, France.

Sophie Guilmin-Crépon (S)

Unité d'Epidémiologie Clinique, Unité de Recherche Clinique, Hôpital Robert Debré, Paris, France.
Inserm CIC-EC 1426, Paris, France.

Jean-François Benoist (JF)

Laboratoire de Biochimie-Hormonologie, Hôpital Robert Debré, APHP, Filière G2M, Paris, France.
Laboratoire de Biochimie Métabolique, Hôpital Necker-Enfants-Malades, APHP, 149 Rue de Sèvres, Filière G2M, Paris, France.
LYPSIS2, Faculté de Pharmacie de Chatenay-Malabry, Université Paris-Saclay, Paris, France.

Manuel Schiff (M)

Centre de Référence Maladies Héréditaires du Métabolisme, Hôpital Robert Debré, APHP, Filière G2M, Paris, France.
Centre de Référence Maladies Héréditaires du Métabolisme, Hôpital Necker-Enfants-Malades, APHP, Filière G2M, Paris, France.
Inserm UMR_S1163, Institut Imagine, Université Paris Cité, Paris, France.

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