Compton David R, DeMarco Steven J, Yalamanchili Padmaja
7404PTC Therapeutics, Inc., South Plainfield, NJ, USA.
Int J Toxicol. 2023 Mar-Apr;42(2):135-145. doi: 10.1177/10915818221144424. Epub 2022 Dec 5.
Aromatic L-amino acid decarboxylase deficiency is a genetic disorder of enzyme loss with decreased neurotransmitter synthesis, and it is characterized by symptoms of impaired motor development and cognitive function, hypotonia, dystonia, and oculogyric crises. Though symptomatic severity varies, the majority of patients experience severe motor impairments, including an inability to sit, stand, or walk. One approved therapy for Aromatic L-amino acid decarboxylase deficiency involves intraputaminal delivery of an adeno-associated virus packaging the human Aromatic L-amino acid decarboxylase enzyme (hAADC) cDNA. The objective of this study in monkeys was to determine the acceptability of ICV/IT as minimally invasive dosing options by evaluating hAADC biodistribution and expression following intraputaminal, intracerebroventricular (ICV), or intrathecal (IT, lumbar) administration. Results show that all routes produced comparable CSF transgene levels and were well-tolerated. The intraputaminal route yielded the highest levels of transgene-derived mRNA expression in the putamen, caudate, and globus pallidus, while expression levels in the spinal cord and dorsal root ganglia (DRG, a target of special toxicological concern) were undetectable. In contrast, the highest transgene levels in ICV/IT groups were observed in the spinal cord and DRG, but levels were too low to result in expression in the putamen, caudate, and globus pallidus. Unlike ICV/IT, the intraputaminal route produced no transgene in blood, suggesting a lower likelihood of off-target toxicities. Additionally, intraputaminal dosing resulted in the lowest anti-AAV2 antibody (anti-drug antibody) levels. Together, these data demonstrate the superiority of intraputaminal administration over ICV/IT routes in achieving AAV2-hAADC transgene DNA distribution and mRNA expression in target therapeutic areas while minimizing risk of toxicity.
芳香族L-氨基酸脱羧酶缺乏症是一种因酶缺失导致神经递质合成减少的遗传性疾病,其特征为运动发育和认知功能受损、肌张力减退、肌张力障碍和动眼危象。尽管症状严重程度各不相同,但大多数患者都有严重的运动障碍,包括无法坐立或行走。一种已获批用于治疗芳香族L-氨基酸脱羧酶缺乏症的疗法是通过脑内注射携带人芳香族L-氨基酸脱羧酶(hAADC)cDNA的腺相关病毒。本研究在猴子身上的目的是通过评估脑内、脑室内(ICV)或鞘内(IT,腰椎)给药后hAADC的生物分布和表达,来确定ICV/IT作为微创给药方案的可接受性。结果表明,所有给药途径产生的脑脊液转基因水平相当,且耐受性良好。脑内注射途径在壳核、尾状核和苍白球中产生的转基因衍生mRNA表达水平最高,而在脊髓和背根神经节(DRG,一个特别受毒理学关注的靶点)中的表达水平则无法检测到。相比之下,ICV/IT组在脊髓和DRG中观察到的转基因水平最高,但水平过低,无法在壳核、尾状核和苍白球中表达。与ICV/IT不同的是,脑内注射途径在血液中未产生转基因,表示脱靶毒性的可能性较低。此外,脑内注射给药导致的抗AAV2抗体(抗药物抗体)水平最低。总之,这些数据证明了在实现AAV2-hAADC转基因DNA在目标治疗区域的分布和mRNA表达方面,脑内注射给药优于ICV/IT途径,同时将毒性风险降至最低。