The PROGRESS study marks initiation of the late-stage development program for AAK1 inhibitor LX9211, with potential to become the first new, non-opioid drug therapy in high-unmet need neuropathic pain in more than 20 years

LX9211 has previously received Fast Track designation from the U.S. Food and Drug Administration (FDA) for DPNP

THE WOODLANDS, TX, USA I November 30, 2023 I Lexicon Pharmaceuticals, Inc. (Nasdaq: LXRX) today announced that it has enrolled the first patient in PROGRESS (A Phase 2b, Dose-ranging, Randomized, Double-blind, PlacebO-controlled, Parallel-GRoup, MulticEnter Study with an Open-label Extension in PatientS with Diabetic Peripheral Neuropathic Pain) studying LX9211, a potent, orally-delivered, selective, investigational small molecule inhibitor of adaptor-associated kinase 1 (AAK1).

PROGRESS will enroll adult patients with a diagnosis of type 1 diabetes mellitus (T1DM) or type 2 diabetes mellitus (T2DM) with moderate to severe DPNP. The primary endpoint of PROGRESS is a reduction of Average Daily Pain Score (ADPS), consistent with the primary endpoint achieved in the successful RELIEF-DPN-1 Phase 2a proof-of-concept study and, informed by regulatory feedback, the primary endpoint planned for Phase 3 studies of LX9211 in DPNP. The placebo-controlled treatment period of PROGRESS is intended to identify the optimal dosing for Phase 3 studies. The open-label extension is expected to run in parallel with planned next-stage Phase 3 studies, supporting long-term safety requirements for regulatory approval.

“We are excited about the potential for LX9211 to become a safe and effective treatment for DPNP and pleased to be moving this promising drug candidate into late-stage development with the initiation of PROGRESS,” said Craig Granowitz, M.D., Ph.D., Lexicon’s senior vice president and chief medical officer. “With no new, non-opioid drugs having been approved for the treatment of neuropathic pain in over two decades, this is an area where novel treatment options are urgently needed. We thank the study sites and especially the patients for their participation in this important scientific endeavor.”

Topline data from PROGRESS is expected to be announced in Q2 2025.

LX9211 has previously received Fast Track designation from the FDA for development in DPNP.

About Lexicon Pharmaceuticals

Lexicon is a biopharmaceutical company with a mission of pioneering medicines that transform patients’ lives. Through its Genome5000™ program, Lexicon scientists studied the role and function of nearly 5,000 genes and 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 treat diseases safely and effectively. Lexicon has advanced multiple medicines to market and has a pipeline of promising drug candidates in heart failure, neuropathic pain, diabetes and metabolism and other indications. For additional information, please visit

About LX9211

Discovered using Lexicon’s unique approach to gene science, LX9211 is a potent, orally delivered, selective, investigational small molecule inhibitor of adaptor-associated kinase 1 (AAK1). Lexicon identified AAK1 in its 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 Lexicon holds exclusive development and commercialization rights. Preclinical studies of LX9211 demonstrated central nervous system penetration and reduction in pain behavior in models of neuropathic pain without affecting opiate pathways. LX9211 has received Fast Track designation from the U.S. Food and Drug Administration for development in diabetic peripheral neuropathic pain.

SOURCE: Lexicon Pharmaceuticals