We are developing LX9211, an orally-delivered small molecule drug candidate, as a treatment for neuropathic pain. We identified the target of LX9211, adapter-associated kinase 1, or AAK1, in our target discovery efforts as a promising approach for the treatment of neuropathic pain, and identified LX9211 and another development candidate in a neuroscience drug discovery alliance with Bristol-Myers Squibb from which we hold exclusive development and commercialization rights. In preclinical studies, LX9211 demonstrated central nervous system penetration and reduction in pain behavior in multiple models of neuropathic pain, and has been demonstrated not to affect opiate pathways. We have reported top-line results from two Phase 1 clinical trials of LX9211, and are now conducting a Phase 2 clinical trial of LX9211 in diabetic peripheral neuropathic pain and preparing to initiate a second Phase 2 clinical trial of LX9211 in post-herpetic neuralgia.

Phase 1 Clinical Trials

We reported top-line data in December 2018 and December 2019 from two Phase 1 clinical trials evaluating the safety, tolerability and pharmacokinetics of LX9211. The first trial enrolled ten cohorts of healthy volunteers in a randomized, double-blind, placebo-controlled, ascending single dose study of daily doses of LX9211. The second trial enrolled five cohorts of healthy volunteers in a randomized, double-blind, placebo-controlled, ascending multiple dose study of daily doses of LX9211, followed by a maintenance dose for 14 days. In both trials, LX9211 demonstrated a safety, tolerability and pharmacokinetics profile identifying the maximum tolerated dose and supportive of once-daily dosing, while exhibiting dose proportional pharmacokinetics. The most common adverse events were headache and dizziness, and there were no drug-related serious adverse events.

RELIEF-DPN-1 Phase 2 Clinical Trial

RELIEF-DPN-1 is a Phase 2 randomized, double-blind, placebo-controlled, parallel-group, multicenter study evaluating the efficacy, safety and pharmacokinetics of LX9211 in the treatment of diabetic peripheral neuropathic pain. The study is designed to enroll approximately 300 patients at approximately 30 U.S. clinical sites. The primary efficacy endpoint under evaluation is the change from baseline (Day 1) to Week 6 in Average Daily Pain Score (ADPS), based on the 11-point numerical rating scale (NRS).

RELIEF-PHN1 Phase 2 Clinical Trial

RELIEF-PHN1 is a Phase 2 randomized, double-blind, placebo-controlled, parallel-group, multicenter study evaluating the efficacy, safety and pharmacokinetics of LX9211 in the treatment of post-herpetic neuralgia. The study is designed to enroll approximately 74 patients at approximately 30 clinical sites worldwide. The primary efficacy endpoint under evaluation is the change from baseline (Day 1) to Week 6 in ADPS, based on the 11-point NRS.