Translating promising preclinical pain relief data for novel molecules from drug discovery to positive clinical trial outcomes is challenging. The angiotensin II type 2 (AT₂) receptor is a clinically-validated target based upon positive proof-of-concept clinical trial data in patients with post-herpetic neuralgia. This trial was conducted because AT₂ receptor antagonists evoked pain relief in rodent models of neuropathic pain. EMA401 was selected as the drug candidate based upon its suitable preclinical toxicity and safety profile and good pharmacokinetics. Herein, we provide an overview of the discovery, preclinical and clinical development of EMA401, for the alleviation of peripheral neuropathic pain.

将新分子有前景的临床前疼痛缓解数据从药物发现转化为积极的临床试验结果具有挑战性。血管紧张素 II 2 型 (AT ₂ ) 受体是一个经过临床验证的靶点，基于带状疱疹后神经痛患者的积极概念验证临床试验数据。进行这项试验是因为 AT ₂受体拮抗剂可以在啮齿动物神经性疼痛模型中引起疼痛缓解。基于其合适的临床前毒性和安全性以及良好的药代动力学，选择 EMA401 作为候选药物。在此，我们概述了用于缓解周围神经病理性疼痛的 EMA401 的发现、临床前和临床开发。