FDA批准的抗癫痫药物有望逆转骨关节炎软骨损伤

耶鲁医学院研究人员发现，FDA批准的抗癫痫药物拉考酰胺可能具有逆转骨关节炎软骨破坏的效果1。该药物通过阻断Nav1.7蛋白发挥作用，而这种蛋白既参与疼痛信号传递，也参与软骨破坏过程，因此拉考酰胺能同时实现缓解关节疼痛和修复软骨损伤的双重功效1。这种方法填补了现有医学的空白，目前尚无其他治疗手段能够同时阻止骨关节炎进展并缓解疼痛1。

在临床前研究中，研究人员采用第二型胶原蛋白制成的水凝胶作为递送系统，该水凝胶在体温下可变成凝胶状，能够持续释放药物超过一个月1。研究发现，每四周注射一次含拉考酰胺的凝胶比每日口服药物更能有效防止软骨丧失1。此外，药物的最佳浓度处于一个精细调节的范围，在低浓度下效果最好1。值得注意的是，Nav1.7蛋白在健康关节中活性较低，但在骨关节炎患者的关节中活性显著增加1。相关研究成果已发表在《生物活性材料》期刊2026年第61卷第640页1。

Researchers at Yale School of Medicine have discovered that lacosamide, an FDA-approved antiepileptic medication, may help reverse cartilage damage caused by osteoarthritis 1. The drug works through a dual mechanism by blocking the Nav1.7 protein, which plays a role in both pain signaling and cartilage destruction, offering a novel approach to addressing a significant gap in current treatment options 1. Existing therapies can either slow disease progression or relieve pain, but typically cannot achieve both objectives simultaneously 1.

In preclinical studies, lacosamide demonstrated particular effectiveness when delivered through a specialized hydrogel formulation made from type II collagen 1. This hydrogel transforms into a gel-like state at body temperature and provides sustained drug release over several weeks 1. The Nav1.7 protein shows notably lower activity in healthy joints compared to those affected by osteoarthritis 1. Injections of the lacosamide-containing gel administered once every four weeks proved more effective at preventing cartilage loss than daily oral dosing 1. The hydrogel serves as a local reservoir, slowly releasing the medication for more than a month, while the drug's optimal concentration range represents a carefully calibrated therapeutic window that performs best at lower doses 1.

The findings were published in Bioactive Materials, Volume 61, page 640, in 2026 1.