RNA therapeutics and their delivery methods: a paradigm for haemophilia management

Haemophilia management is currently undergoing a paradigm shift from traditional protein replacement to RNA modalities and their delivery. This review provides a critical analysis of RNA-based therapeutics (specifically small interfering RNA (siRNA), mRNA and CRISPR/Cas9) as a versatile paradigm distinct from DNA ones. We synthesise clinical and preclinical data to contrast these modalities: siRNA strategies (e.g. fitusiran) have indicated ∼90% reductions in bleeding rates by rebalancing haemostasis independent of factor deficiency; lipid nanoparticles (LNPs)-mRNA platforms offer tuneable, transient factor production without genomic integration risks; and CRISPR-based editing aims for permanent correction (up to 170% coagulation factor IX, FIX expression in preclinical studies) but necessitates rigorous monitoring for off-target effects. Crucially, this article dissects the non-viral delivery landscape determining the clinical viability of these cargos. We evaluate LNPs as the current clinical gold standard for hepatic delivery, contrasting them against emerging polymeric systems, aptamer conjugates and exosomes designed to overcome rate-limiting barriers such as endosomal entrapment and renal clearance. By juxtaposing the immunogenic limitations of viral vectors, we conclude that next-generation RNA therapeutics, enabled by LNPs and GalNAc-conjugation, offer a strategic pathway to overcome the durability gap observed in haemophilia A and expand treatment access to patients currently excluded by viral seroprevalence.

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Publication Details

Journal
Journal of drug targeting
Published
2026-05-11
DOI
https://doi.org/10.1080/1061186x.2026.2638330
Primary Topic
RNA Interference and Gene Delivery
Type
article
Field-Weighted Citation Impact
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article

RNA therapeutics and their delivery methods: a paradigm for haemophilia management

Ali Rajabi Zangi, Hamid Reza Heidari, Pouya Pazooki, Yousef Javadzadeh et al.
Journal of drug targeting
RNA Interference and Gene Delivery
article

RNA therapeutics and their delivery methods: a paradigm for haemophilia management

Ali Rajabi Zangi, Hamid Reza Heidari, Pouya Pazooki, Yousef Javadzadeh, Ala Amiri, Hamed Hamishehkar, Fatemeh Eskandari
article en

Abstract

Haemophilia management is currently undergoing a paradigm shift from traditional protein replacement to RNA modalities and their delivery. This review provides a critical analysis of RNA-based therapeutics (specifically small interfering RNA (siRNA), mRNA and CRISPR/Cas9) as a versatile paradigm distinct from DNA ones. We synthesise clinical and preclinical data to contrast these modalities: siRNA strategies (e.g. fitusiran) have indicated ∼90% reductions in bleeding rates by rebalancing haemostasis independent of factor deficiency; lipid nanoparticles (LNPs)-mRNA platforms offer tuneable, transient factor production without genomic integration risks; and CRISPR-based editing aims for permanent correction (up to 170% coagulation factor IX, FIX expression in preclinical studies) but necessitates rigorous monitoring for off-target effects. Crucially, this article dissects the non-viral delivery landscape determining the clinical viability of these cargos. We evaluate LNPs as the current clinical gold standard for hepatic delivery, contrasting them against emerging polymeric systems, aptamer conjugates and exosomes designed to overcome rate-limiting barriers such as endosomal entrapment and renal clearance. By juxtaposing the immunogenic limitations of viral vectors, we conclude that next-generation RNA therapeutics, enabled by LNPs and GalNAc-conjugation, offer a strategic pathway to overcome the durability gap observed in haemophilia A and expand treatment access to patients currently excluded by viral seroprevalence.

Journal of drug targeting
Tabriz University of Medical Sciences (IR), University of Calgary (CA), University of Tabriz (IR), Advanced Tissue (United States) (US), Pharmaceutical Biotechnology (Czechia) (CZ), Alzahra University (IR)
Openalex Percentile: Top 10%
RNA Interference and Gene Delivery
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