RQ-00466479

RQ-00466479 is a small molecule antagonist of the P2X7 purinergic receptor, developed through a collaboration between RaQualia Pharma and Asahi Kasei Pharma, and later sublicensed to Eli Lilly. Also known as AK1780 and LY3857210, the compound was designed to treat chronic and neuropathic pain by inhibiting the P2X7 receptor, an ATP-gated ion channel involved in the release of pro-inflammatory cytokines like IL-1β from immune cells. Preclinical studies demonstrated high central nervous system penetration and analgesic efficacy in rat models. However, as of late 2025, Eli Lilly discontinued the development of the compound for pain indications, although the licensing agreement remains active.

Other names

AK1780AK-1780AK 1780AKP-23494954AKP23494954AKP 23494954RQ-00466479RQ00466479RQ 00466479