THE WOODLANDS, TX, USA I December 18, 2018 I Lexicon Pharmaceuticals, Inc. (Nasdaq: LXRX), today announced positive topline results from its Phase 1a study of LX9211, a potent oral small molecule inhibitor of adaptor associated kinase 1, or AAK1, in development for the treatment of neuropathic pain.
“We are pleased that the initial clinical data for LX9211 confirms the drug candidate’s preclinical profile,” said Praveen Tyle, Ph.D., executive vice president of Research and Development at Lexicon. “LX9211 was well tolerated with predictable pharmacokinetics. At doses tested, drug levels of LX9211 were at biologically relevant concentrations and support the therapeutic potential of this highly selective inhibitor of AAK1. We look forward to initiating a multiple ascending dose study for LX9211 in the first quarter of 2019.”
The Phase 1a study met its primary objectives, demonstrating a favorable safety and tolerability profile in healthy human subjects and identifying the maximum tolerated dose.
The randomized, double-blind, placebo-controlled, ascending single dose Phase 1a study was performed to evaluate the safety, tolerability and pharmacokinetics of orally administered LX9211 in healthy volunteers. The study was comprised of 10 cohorts over a wide daily dose range of 5 mg to 200 mg. LX9211 demonstrated a favorable safety and pharmacokinetics profile supportive of once-daily, or less frequent, dosing. Pharmacokinetics were dose proportional over virtually all of the dose range and exhibited a minimal food effect. The most common adverse event was headache, and there were no drug-related serious adverse events.
About LX9211
LX9211 is a potent, orally delivered, selective small molecule inhibitor of AAK1, a target discovered and extensively characterized in an alliance with Bristol Myers Squibb. Preclinical data demonstrated central nervous system penetration and reduction in pain behavior in models of neuropathic pain. Lexicon has exclusive research, development and commercialization rights to LX9211 and additional compounds acting through AAK1.
About Lexicon Pharmaceuticals
Lexicon is a fully integrated biopharmaceutical company that is applying a unique approach to gene science based on Nobel Prize-winning technology to discover and develop precise medicines for patients with serious, chronic conditions. Through its Genome5000™ program, Lexicon scientists have studied the role and function of nearly 5,000 genes over the last 20 years and have identified more than 100 protein targets with significant therapeutic potential in a range of diseases. Through the precise targeting of these proteins, Lexicon is pioneering the discovery and development of innovative medicines to safely and effectively treat disease. In addition to its first commercial product, XERMELO® (telotristat ethyl), Lexicon has a pipeline of promising drug candidates in clinical and pre-clinical development in diabetes and metabolism and neuropathic pain. For additional information please visit www.lexpharma.com.
SOURCE: Lexicon Pharmaceuticals
Post Views: 42
THE WOODLANDS, TX, USA I December 18, 2018 I Lexicon Pharmaceuticals, Inc. (Nasdaq: LXRX), today announced positive topline results from its Phase 1a study of LX9211, a potent oral small molecule inhibitor of adaptor associated kinase 1, or AAK1, in development for the treatment of neuropathic pain.
“We are pleased that the initial clinical data for LX9211 confirms the drug candidate’s preclinical profile,” said Praveen Tyle, Ph.D., executive vice president of Research and Development at Lexicon. “LX9211 was well tolerated with predictable pharmacokinetics. At doses tested, drug levels of LX9211 were at biologically relevant concentrations and support the therapeutic potential of this highly selective inhibitor of AAK1. We look forward to initiating a multiple ascending dose study for LX9211 in the first quarter of 2019.”
The Phase 1a study met its primary objectives, demonstrating a favorable safety and tolerability profile in healthy human subjects and identifying the maximum tolerated dose.
The randomized, double-blind, placebo-controlled, ascending single dose Phase 1a study was performed to evaluate the safety, tolerability and pharmacokinetics of orally administered LX9211 in healthy volunteers. The study was comprised of 10 cohorts over a wide daily dose range of 5 mg to 200 mg. LX9211 demonstrated a favorable safety and pharmacokinetics profile supportive of once-daily, or less frequent, dosing. Pharmacokinetics were dose proportional over virtually all of the dose range and exhibited a minimal food effect. The most common adverse event was headache, and there were no drug-related serious adverse events.
About LX9211
LX9211 is a potent, orally delivered, selective small molecule inhibitor of AAK1, a target discovered and extensively characterized in an alliance with Bristol Myers Squibb. Preclinical data demonstrated central nervous system penetration and reduction in pain behavior in models of neuropathic pain. Lexicon has exclusive research, development and commercialization rights to LX9211 and additional compounds acting through AAK1.
About Lexicon Pharmaceuticals
Lexicon is a fully integrated biopharmaceutical company that is applying a unique approach to gene science based on Nobel Prize-winning technology to discover and develop precise medicines for patients with serious, chronic conditions. Through its Genome5000™ program, Lexicon scientists have studied the role and function of nearly 5,000 genes over the last 20 years and have identified more than 100 protein targets with significant therapeutic potential in a range of diseases. Through the precise targeting of these proteins, Lexicon is pioneering the discovery and development of innovative medicines to safely and effectively treat disease. In addition to its first commercial product, XERMELO® (telotristat ethyl), Lexicon has a pipeline of promising drug candidates in clinical and pre-clinical development in diabetes and metabolism and neuropathic pain. For additional information please visit www.lexpharma.com.
SOURCE: Lexicon Pharmaceuticals
Post Views: 42
