LX9211 for Diabetic Neuropathy

(RELIEF-DPN 1 Trial)

No longer recruiting at 55 trial locations

Overseen By Christopher Warner, PhD

Age: 18+

Sex: Any

Trial Phase: Phase 2

Sponsor: Lexicon Pharmaceuticals

Must not be taking: Opioids, NSAIDs

Disqualifiers: Other painful conditions, Major depression, Drug/alcohol disorder, others

Prior Safety Data This treatment has passed at least one previous human trial

Compensation: Varies

Number of Visits: Unknown

Duration: 6 weeks

What You Need to Know Before You Apply

What is the purpose of this trial?

This trial examines the effectiveness of a new drug, LX9211, in reducing pain from diabetic peripheral neuropathy (nerve pain caused by diabetes). Participants will receive either a low or high dose of LX9211, or a placebo (inactive pill), to determine which is most effective over 11 weeks. The trial suits individuals who have experienced diabetic nerve pain for at least six months and are on a stable diabetes treatment plan. As a Phase 2 trial, this research focuses on assessing the treatment's effectiveness in an initial, smaller group of people.

Will I have to stop taking my current medications?

The trial does not specify if you need to stop taking your current medications, but you cannot use opioid medications for DPNP within 2 months before the screening or NSAIDs less than 2 weeks before the screening.

Is there any evidence suggesting that LX9211 is likely to be safe for humans?

Research has shown that LX9211 is safe and well tolerated in people. In early studies, participants took doses ranging from 5 to 300 mg, experiencing only minor side effects. Most participants did not have serious reactions, suggesting that LX9211 is generally safe for humans at the tested doses.

The current trial is in a later stage, indicating that earlier studies have already demonstrated its safety. This should provide reassurance about its safety. However, it is important to remember that all medications can affect people differently, so researchers will continue to monitor participants during the trial. ^{1 2 3 4 5}

Why do researchers think this study treatment might be promising for diabetic peripheral neuropathy?

Researchers are excited about LX9211 because it offers a fresh approach to tackling diabetic peripheral neuropathic pain. Unlike standard treatments, which often involve medications like gabapentin or duloxetine that modulate nerve signals, LX9211 targets a novel mechanism by inhibiting a specific enzyme involved in pain pathways. This could potentially provide more effective pain relief with fewer side effects. Furthermore, LX9211 is administered orally, making it easy to incorporate into daily routines. These factors give hope that LX9211 could become a game-changer in managing neuropathic pain for diabetic patients.

What evidence suggests that LX9211 could be effective for reducing pain related to diabetic peripheral neuropathy?

Research has shown that LX9211 can help reduce pain in people with diabetic peripheral neuropathy (DPNP). One study found that participants taking a high dose of LX9211 reported a greater reduction in pain levels compared to those taking a placebo, with pain scores decreasing by 1.27 points versus 0.72 points for the placebo group. Another study demonstrated that even a lower 10 mg dose of LX9211 helped reduce pain in patients. In this trial, participants will receive either a 100 mg/10 mg or 200 mg/20 mg dose of LX9211, or a placebo. These results suggest that LX9211 might provide significant relief for those experiencing nerve pain due to diabetes. ^{1 2 6 7 8}

Who Is on the Research Team?

Suma Gopinathan, PhD

Principal Investigator

Lexicon Pharmaceuticals

Are You a Good Fit for This Trial?

Inclusion Criteria

Patient has given written informed consent to participate in the study in accordance with local regulations

Body mass index ≥18.0 to ≤40.0 kg/m2 at Screening

Diagnosis of DPNP at Screening

Timeline for a Trial Participant

Screening

Participants are screened for eligibility to participate in the trial

2-4 weeks

Treatment

Participants receive either a low or high dose of LX9211 or placebo once daily

6 weeks

Follow-up

Participants are monitored for safety and effectiveness after treatment

4-5 weeks

What Are the Treatments Tested in This Trial?

Interventions

• LX9211

How Is the Trial Designed?

Group I: LX9211 200 mg/20 mg Experimental Treatment 1 Intervention

Following a 2-week run-in period, participants were randomized to receive a single loading dose of LX9211, 200 mg orally on Day 1, followed by maintenance doses of LX9211, 20 mg, orally, QD from Day 2 up to Week 6. Following completion of the 6-week treatment, all participants were followed for safety and received single oral tablet of LX9211 matching placebo, QD, for 5 weeks during safety follow-up.

Group II: LX9211 100 mg/10 mg Experimental Treatment 1 Intervention

Following a 2-week run-in period, participants were randomized to receive a single loading dose of LX9211, 100 milligrams (mg), tablet, orally, on Day 1, followed by maintenance doses of LX9211 10 mg tablets, orally, QD from Day 2 up to Week 6. Following completion of the 6-week treatment, all participants were followed for safety and received single oral tablet of LX9211 matching placebo, QD, for 5 weeks during safety follow-up.

Group III: Placebo Placebo Group 1 Intervention

Following a 2-week run-in period, participants were randomized to LX9211 matching placebo received as a single loading dose, orally, on Day 1, followed by maintenance doses of LX9211 matching placebo tablets, orally, once daily (QD) from Day 2 up to Week 6. Following completion of the 6-week treatment, all participants were followed for safety and received single oral tablet of LX9211 matching placebo, QD, for 5 weeks during the safety follow-up.

Who Is Running the Clinical Trial?

Lexicon Pharmaceuticals

Lead Sponsor

Trials

67

Recruited

24,400+

Dr. Mike Exton

Lexicon Pharmaceuticals

Chief Executive Officer

PhD in Neuroscience from the University of Newcastle and PhD in Immunology from the University of Essen, Germany

Dr. Craig Granowitz

Lexicon Pharmaceuticals

Chief Medical Officer since 2021

MD

Citations

1. diabetesjournals.org diabetesjournals.org/care/article/47/8/1325/154530/Efficacy-and-Safety-of-LX9211-for-Relief-of

Efficacy and Safety of LX9211 for Relief of Diabetic Peripheral ... Results for high-dose LX9211 demonstrated improvement in pain severity versus placebo (−1.27 vs. −0.72 points, respectively).

2. pmc.ncbi.nlm.nih.gov pmc.ncbi.nlm.nih.gov/articles/PMC11272977/

Efficacy and Safety of LX9211 for Relief of Diabetic Peripheral ... Results for high-dose LX9211 demonstrated improvement in pain severity versus placebo (−1.27 vs. −0.72 points, respectively).

3. onlinelibrary.wiley.com onlinelibrary.wiley.com/doi/full/10.1111/jdi.14342

LX9211, a rising star for relieving of diabetic peripheral ... In a multicenter trial, LX9211 significantly reduced pain in diabetic peripheral neuropathy (DPN) patients, with the 10 mg dose showing notable ...

4. pubmed.ncbi.nlm.nih.gov pubmed.ncbi.nlm.nih.gov/38895916/

Efficacy and Safety of LX9211 for Relief of Diabetic Peripheral ... Results for high-dose LX9211 demonstrated improvement in pain severity versus placebo (-1.27 vs. -0.72 points, respectively).

5. investors.lexpharma.com investors.lexpharma.com/news-releases/news-release-details/lexicon-pharmaceuticals-announces-topline-results-phase-2b

Release Details - Investor Relations | Lexicon Pharmaceuticals Pilavapadin achieved meaningful pain reduction versus placebo and was well-tolerated in the 10 mg dose, meeting the Company's objectives for the study.

6. tandfonline.com tandfonline.com/doi/abs/10.1080/13543784.2024.2376570

An overview of the safety and efficacy of LX-9211 ... Phase 1 studies involving LX-9211 showed it is safe as the adverse effects reported were minimal. Phase 2 studies with LX-9211 were conducted on patients with ...

7. sciencedirect.com sciencedirect.com/science/article/pii/S0149291821002095

Results of two Phase 1, Randomized, Double-blind ... These studies found that LX9211 was safe and well tolerated in healthy participants. These findings suggest it is appropriate to take LX9211 forward into Phase ...

8. clinicaltrials.gov clinicaltrials.gov/study/NCT04662281

Study Details | NCT04662281 | Efficacy and Safety of ... Also called a data safety and monitoring board, or DSMB. Early Phase 1 ... Safety of LX9211 in the Treatment of Postherpetic Neuralgia (RELIEF-PHN1).