Safety and tolerability of topical polyhexamethylene biguanide: a randomised clinical trial in healthy adult volunteers.


Journal

The British journal of ophthalmology
ISSN: 1468-2079
Titre abrégé: Br J Ophthalmol
Pays: England
ID NLM: 0421041

Informations de publication

Date de publication:
02 2022
Historique:
received: 27 08 2020
revised: 01 10 2020
accepted: 21 10 2020
pubmed: 27 11 2020
medline: 23 4 2022
entrez: 26 11 2020
Statut: ppublish

Résumé

Polyhexamethyl biguanide (PHMB), a widely used topical treatment for A prospective, randomised, double-masked controlled trial in 90 healthy volunteers. Subjects were treated with topical 0.04%, 0.06%, 0.08% PHMB or placebo (vehicle) 12× daily for 7 days, then 6× daily for 7 days. The rates of dose-limiting adverse events (DLAEs) leading to interruption of dosing, mild adverse events (AEs) (not dose limiting) and incidental AEs (unrelated to treatment) were compared. The primary outcome was the difference between treatments for DLAE rates. 5/90 subjects developed DLAE within <1-4 days of starting treatment; 2/5 using PHMB 0.06% and 3/5 PHMB 0.08%. These resolved within 1-15 days. There were no significant differences in DLAE between treatment groups. Mild AEs occurred in 48/90 subjects (including placebo). There was no trend for an increased incidence of any AE with increasing concentrations of PHMB, except for corneal punctate keratopathy with PHMB 0.08%, which fully resolved within 7-14 days. These findings are reassuring for PHMB 0.02% users. They also suggest that higher PHMB concentrations may show acceptable levels of tolerance and toxicity in AK subjects, whose susceptibility to AE may be greater than for the normal eyes in this study. Given the potential benefits of higher PHMB concentrations for treating deep stromal invasion in AK, we think that the use of PHMB 0.08% is justified in treatment trials. NCT02506257.

Sections du résumé

BACKGROUND AND AIMS
Polyhexamethyl biguanide (PHMB), a widely used topical treatment for
METHODS
A prospective, randomised, double-masked controlled trial in 90 healthy volunteers. Subjects were treated with topical 0.04%, 0.06%, 0.08% PHMB or placebo (vehicle) 12× daily for 7 days, then 6× daily for 7 days. The rates of dose-limiting adverse events (DLAEs) leading to interruption of dosing, mild adverse events (AEs) (not dose limiting) and incidental AEs (unrelated to treatment) were compared. The primary outcome was the difference between treatments for DLAE rates.
RESULTS
5/90 subjects developed DLAE within <1-4 days of starting treatment; 2/5 using PHMB 0.06% and 3/5 PHMB 0.08%. These resolved within 1-15 days. There were no significant differences in DLAE between treatment groups. Mild AEs occurred in 48/90 subjects (including placebo). There was no trend for an increased incidence of any AE with increasing concentrations of PHMB, except for corneal punctate keratopathy with PHMB 0.08%, which fully resolved within 7-14 days.
CONCLUSION
These findings are reassuring for PHMB 0.02% users. They also suggest that higher PHMB concentrations may show acceptable levels of tolerance and toxicity in AK subjects, whose susceptibility to AE may be greater than for the normal eyes in this study. Given the potential benefits of higher PHMB concentrations for treating deep stromal invasion in AK, we think that the use of PHMB 0.08% is justified in treatment trials.
TRIAL REGISTRATION NUMBER
NCT02506257.

Identifiants

pubmed: 33239413
pii: bjophthalmol-2020-317848
doi: 10.1136/bjophthalmol-2020-317848
doi:

Substances chimiques

Biguanides 0
polihexanide 322U039GMF

Banques de données

ClinicalTrials.gov
['NCT02506257']

Types de publication

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

Langues

eng

Sous-ensembles de citation

IM

Pagination

190-196

Subventions

Organisme : Department of Health
Pays : United Kingdom

Informations de copyright

© Author(s) (or their employer(s)) 2022. No commercial re-use. See rights and permissions. Published by BMJ.

Déclaration de conflit d'intérêts

Competing interests: Vincenzo Papa and Antonino Asero are employees of SIFI S.p.A. who manufacture and supply PHMB eye drops in Italy, and who are carrying out studies to develop it as a licenced therapy for the treatment of Acanthamoeba keratitis in Europe. John Dart and Darwin Minassian are consultants to SIFI SpA. The remaining authors have no proprietary or commercial interest in any materials discussed in this article.

Auteurs

Vincenzo Papa (V)

SIFI S.p.A., 36, via Ercole Patti, 95025 Lavinaio (Catania), Italy, Lavinaio, Italy.

Ivanka van der Meulen (I)

Amsterdam UMC Locatie AMC, Amsterdam, Netherlands.

Sylvie Rottey (S)

DRUG Research Unit, Ghent, Belgium.

Guy Sallet (G)

Ooginstituut, Aalst, Belgium.

Jolanda Overweel (J)

PSR Group BV, Hoofddorp, Netherlands.

Nino Asero (N)

SIFI SpA, Catania, Italy.

Darwin C Minassian (DC)

Epivision Ophthalmic Epidemiology Consultants, Penn, UK.

John K G Dart (JKG)

Corneal & External Disease, Moorfields Eye Hospital NHS Foundation Trust, London, UK j.dart@ucl.ac.uk.
Ocular Biology & Therapeutics, UCL Institute of Ophthalmology, London, UK.

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Classifications MeSH