Literature DB >> 27509102

Treatment of Fabry's Disease with the Pharmacologic Chaperone Migalastat.

Dominique P Germain1, Derralynn A Hughes1, Kathleen Nicholls1, Daniel G Bichet1, Roberto Giugliani1, William R Wilcox1, Claudio Feliciani1, Suma P Shankar1, Fatih Ezgu1, Hernan Amartino1, Drago Bratkovic1, Ulla Feldt-Rasmussen1, Khan Nedd1, Usama Sharaf El Din1, Charles M Lourenco1, Maryam Banikazemi1, Joel Charrow1, Majed Dasouki1, David Finegold1, Pilar Giraldo1, Ozlem Goker-Alpan1, Nicola Longo1, C Ronald Scott1, Roser Torra1, Ahmad Tuffaha1, Ana Jovanovic1, Stephen Waldek1, Seymour Packman1, Elizabeth Ludington1, Christopher Viereck1, John Kirk1, Julie Yu1, Elfrida R Benjamin1, Franklin Johnson1, David J Lockhart1, Nina Skuban1, Jeff Castelli1, Jay Barth1, Carrolee Barlow1, Raphael Schiffmann1.   

Abstract

BACKGROUND: Fabry's disease, an X-linked disorder of lysosomal α-galactosidase deficiency, leads to substrate accumulation in multiple organs. Migalastat, an oral pharmacologic chaperone, stabilizes specific mutant forms of α-galactosidase, increasing enzyme trafficking to lysosomes.
METHODS: The initial assay of mutant α-galactosidase forms that we used to categorize 67 patients with Fabry's disease for randomization to 6 months of double-blind migalastat or placebo (stage 1), followed by open-label migalastat from 6 to 12 months (stage 2) plus an additional year, had certain limitations. Before unblinding, a new, validated assay showed that 50 of the 67 participants had mutant α-galactosidase forms suitable for targeting by migalastat. The primary end point was the percentage of patients who had a response (≥50% reduction in the number of globotriaosylceramide inclusions per kidney interstitial capillary) at 6 months. We assessed safety along with disease substrates and renal, cardiovascular, and patient-reported outcomes.
RESULTS: The primary end-point analysis, involving patients with mutant α-galactosidase forms that were suitable or not suitable for migalastat therapy, did not show a significant treatment effect: 13 of 32 patients (41%) who received migalastat and 9 of 32 patients (28%) who received placebo had a response at 6 months (P=0.30). Among patients with suitable mutant α-galactosidase who received migalastat for up to 24 months, the annualized changes from baseline in the estimated glomerular filtration rate (GFR) and measured GFR were -0.30±0.66 and -1.51±1.33 ml per minute per 1.73 m(2) of body-surface area, respectively. The left-ventricular-mass index decreased significantly from baseline (-7.7 g per square meter; 95% confidence interval [CI], -15.4 to -0.01), particularly when left ventricular hypertrophy was present (-18.6 g per square meter; 95% CI, -38.2 to 1.0). The severity of diarrhea, reflux, and indigestion decreased.
CONCLUSIONS: Among all randomly assigned patients (with mutant α-galactosidase forms that were suitable or not suitable for migalastat therapy), the percentage of patients who had a response at 6 months did not differ significantly between the migalastat group and the placebo group. (Funded by Amicus Therapeutics; ClinicalTrials.gov numbers, NCT00925301 [study AT1001-011] and NCT01458119 [study AT1001-041].).

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Year:  2016        PMID: 27509102     DOI: 10.1056/NEJMoa1510198

Source DB:  PubMed          Journal:  N Engl J Med        ISSN: 0028-4793            Impact factor:   91.245


  123 in total

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Authors:  Thomas Gaisl; Albina Nowak; Noriane A Sievi; Nicolas Gerard; Christian F Clarenbach; Malcolm Kohler; Daniel Franzen
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Review 5.  Enzyme replacement therapy and beyond-in memoriam Roscoe O. Brady, M.D. (1923-2016).

Authors:  Markus Ries
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Review 6.  Emptying the stores: lysosomal diseases and therapeutic strategies.

Authors:  Frances M Platt
Journal:  Nat Rev Drug Discov       Date:  2017-11-17       Impact factor: 84.694

7.  Fabry disease: A pharmacological chaperone on the horizon.

Authors:  Martina Gaggl; Gere Sunder-Plassmann
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Review 8.  Pharmacoperones as Novel Therapeutics for Diverse Protein Conformational Diseases.

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Review 10.  Lysosomal storage diseases.

Authors:  Frances M Platt; Alessandra d'Azzo; Beverly L Davidson; Elizabeth F Neufeld; Cynthia J Tifft
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