New drug for nerve pain after shingles! New powerful AAK1 inhibitor LX9211 enters Phase II clinical: penetration of the nervous system, no risk of addiction!

December 31, 2020 // -- Lexicon Pharmaceuticals has announced that a Phase II RELIEF-PHN-1 clinical study evaluating LX9211 for the treatment of post-herpes nerve pain (post-herpetic neuralgia, PHN) 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 showed that in neurogenic pain models, LX9211 showed central nervous system penetration and reduced pain behavior without affecting opioid pathps.
based on preclinical data, LX9211 has the potential to significantly reduce pain response without addiction, while providing a new treatment for neuropathic pain by inhibiting AAK1.
, LX9211 also has the potential to be developed for the treatment of other neurogenic pain, based on promising results and favorable Phase I clinical safety in multiple preclinical models.
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-PHN-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 for the treatment of post-shingles nerve pain (PHN).
the study aims to recruit about 74 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).
early September this year, a Phase II RELIEF-DPN-1 clinical study evaluating LX9211's treatment of nerve pain around diabetes also began treating patients.
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 is the 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 begin the treatment of patients in the second proof-of-concept study of LX9211.
patients with shingles usually experience pain that lasts from months to years after the rash subsides, with limited treatment options.
believe that LX9211 has the potential to provide a new treatment for post-shingles nerve pain.
look forward to completing this study by the end of next year and another Phase 2 proof-of-concept study of LX9211 in nerve pain around diabetes.
": Lexicon Pharmaceuticals Announces Commencement of Dosing in Phase 2 Clinical Study of LX9211 in Post-Herpetic Neuralgia