New drug for nerve pain around diabetes! New powerful AAK1 inhibitor LX9211 enters Phase II clinical: permeable nervous system, no risk of addiction!

September 07, 2020 // -- Lexicon Pharmaceuticals has announced that a Phase II RELIEF-DPN-1 clinical study evaluating LX9211 for the treatment of nerve pain around diabetes has begun to treat patients.
LX9211 is a powerful, oral, selective small molecule inhibitor that targets adapter-related kinase 1 (Adaptor associated kinase 1, AAK1).
the target was discovered and widely indicated by a alliance between Lexicon and BMS.
preclinical studies have shown that in neurogenic pain models, LX9211 shows central nervous system penetration and reduced pain behavior without affecting opioid pathps.
LX9211 (BMS-986176) Chemical Structure (Photo: chemicalbook.com) In 2016, Lexicon acquired exclusive research, development and commercial rights to LX9211 and other compounds discovered under the alliance through AAK1, and BMS will receive $115.5 million from the acquisition.
RELIEF-DPN-1 is a randomized, double-blind, placebo-controlled, parallel group, multi-center Phase 2 study that is evaluating the efficacy, safety, and pharmacodynamics of LX9211 in treating nerve pain around diabetes.
the study aims to recruit about 300 patients at about 30 clinical sites in the United States.
end point of the assessment was a change in the average daily pain score (ADPS) from baseline check (day 1) to week 6 based on the 11-point Numeric Score Scale (NRS).
Praveen Tyle, Executive Vice President of Research and Development at
Lexicon, said, "We are pleased to advance the LX9211 clinical program to treat patients with peripheral nerve pain in the first proof-of-concept study.
based on preclinical data, we believe LX9211 has the potential to significantly reduce pain response without addiction, while providing a new treatment for neuropathic pain by inhibiting AAK1.
we are preparing for another Phase 2 study on herpes sequelae nerve pain, which is expected to start later this year.
, based on promising results and favorable Phase I clinical safety in multiple preclinical models, we will explore opportunities for LX9211 in other areas of neurogenic pain.
Origin: Lexicon Pharmaceuticals Announces Company of Patient Dosing IN RELIEF-DPN-1 Phase 2 Clinical Study of LX9211 in Patients With Diabetic Perennity Neuropathic Pain.