School of Medicine, Louisiana State University Health Sciences Center at Shreveport, Shreveport, LA, USA.
School of Medicine, Ross University School of Medicine, Miramar, FL, USA.
Expert Opin Investig Drugs. 2024 Aug;33(8):829-837. doi: 10.1080/13543784.2024.2376570. Epub 2024 Jul 8.
LX-9211 is a drug designed to treat neuropathic pain conditions. It functions by inhibiting the adaptor-associated kinase 1 (AAK1) enzyme which promotes clathrin-dependent endocytosis. Preclinical studies have shown that LX-9211 does produce a reduction in nociceptive related behaviors and produces no major adverse effects in rats. Thus, LX-9211 has advanced to clinical trials to assess its safety and efficacy in humans. So far, phase 1 and phase 2 clinical trials involving patients with postherpetic neuralgia and diabetic peripheral neuropathic pain have been conducted with phase 3 trials planned in the future.
This paper highlights preclinical studies involving LX-9211 in rodents. Additionally, phase 1 clinical trials examining the safety of LX-9211 in healthy subjects as well as phase 2 studies looking at the safety and efficacy of LX-9211 compared to placebo in patients with diabetic peripheral neuropathic pain and postherpetic neuralgia are also discussed.
In phase 1 and phase 2 clinical trials conducted so far, LX-9211 has been shown to produce few adverse effects as well as cause a significantly greater reduction in pain compared to placebo. However, more clinical studies are needed to further assess its effects in humans to ensure its safety.
LX-9211 是一种旨在治疗神经性疼痛病症的药物。它通过抑制衔接相关激酶 1(AAK1)酶来发挥作用,该酶促进网格蛋白依赖性内吞作用。临床前研究表明,LX-9211 确实能减少与疼痛相关的行为,且在大鼠中没有产生重大不良反应。因此,LX-9211 已进入临床试验,以评估其在人类中的安全性和疗效。到目前为止,已经进行了涉及带状疱疹后神经痛和糖尿病周围神经性疼痛患者的 1 期和 2 期临床试验,并计划进行 3 期临床试验。
本文重点介绍了 LX-9211 在啮齿动物中的临床前研究。此外,还讨论了 1 期临床试验,该试验检查了 LX-9211 在健康受试者中的安全性,以及 2 期研究,该研究比较了 LX-9211 与安慰剂在糖尿病周围神经性疼痛和带状疱疹后神经痛患者中的安全性和疗效。
到目前为止进行的 1 期和 2 期临床试验表明,与安慰剂相比,LX-9211 产生的不良反应较少,且能显著更大程度地减轻疼痛。然而,需要更多的临床研究来进一步评估其在人类中的效果,以确保其安全性。