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CompletedNCT04455633RELIEF-DPN 1Updated Jun 25, 2025Results posted

Efficacy, Safety, and PK of LX9211 in Participants With Diabetic Peripheral Neuropathic Pain

A Phase 2 interventional study of LX9211 and LX9211 Matching Placebo in Diabetic Peripheral Neuropathy and Diabetes, sponsored by Lexicon Pharmaceuticals. Completed at 44 sites in United States. Open to participants aged 18 Years and older. Per ClinicalTrials.gov, last updated 2025-06-25.

Sponsored by Lexicon Pharmaceuticals · Phase 2, Interventional, and Treatment

Phase
Phase 2
Study type
Interventional
Enrollment
319
Allocation
Randomized
Ages
18 Years and older
Sex
All
01

Study summary

Evaluation of the efficacy of a low and high dose of LX9211 compared to placebo in reducing pain related to diabetic peripheral neuropathy (DPNP) over an 11 week assessment period.

02

Conditions studied

  • Diabetic Peripheral Neuropathy
  • Diabetes

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03

Who can participate

Ages eligible
18 Years and older
Sexes eligible
All
Accepts healthy volunteers
No

Inclusion criteria

  • Participant has given written informed consent to participate in the study in accordance with local regulations
  • Adult male and female participants ≥18 years of age at the time of screening
  • Body mass index ≥18.0 to ≤40.0 kg/m2 at Screening
  • Diagnosis of diabetic peripheral neuropathic pain (DPNP) at Screening
  • Pain from DPN present for at least 6 months
  • Haemoglobin A1C ≤11% at screening
  • Stable regimen for the treatment of type 1 diabetes mellitus (T1DM) or type 2 diabetes mellitus (T2DM) for ≥1 month prior to Screening

Exclusion criteria

Exclusion Criteria:

  • Presence of other painful conditions that may confound assessment or self-evaluation of DPNP
  • History of major depressive episode, active, significant psychiatric disorders
  • History of clinically significant drug or alcohol use disorder
  • History of neurolytic or neurosurgical therapy for DPNP
  • Use of opioid medications for management of DPNP within the 2 months prior to Screening Visit
  • Use of non-steroidal anti-inflammatory drugs (NSAIDs) less than 2 weeks prior to the Screening Visit
04

Study design

Phase
Phase 2
Primary purpose
Treatment
Allocation
Randomized
Intervention model
Parallel assignment
Masking
Quadruple (Participant, Care provider, Investigator, Outcomes assessor)
Enrollment
319 participants (actual)

Study arms

  • Placebo comparator
    Placebo

    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.

    Drug: LX9211 Matching Placebo

  • Experimental
    LX9211 100 mg/10 mg

    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.

    Drug: LX9211

  • Experimental
    LX9211 200 mg/20 mg

    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.

    Drug: LX9211

Interventions

  • DrugLX9211

    Oral Tablets

  • DrugLX9211 Matching Placebo

    Oral Tablets

05

What researchers measure

Primary outcomes

  1. Change From Baseline to Week 6 in ADPS as Measured by the Numerical Rating Scale

    ADPS is based on question 5 of Brief Pain Inventory (BPI)-short form for Diabetic Peripheral Neuropathy (BPI-DPN) and is assessed on an 11-point numerical rating scale. Participants were asked to rate their average pain over the past 24 hours, by answering the question 5 "Please rate your pain due to your diabetes by indicating the one number that best describes your pain on the average." on a scale of 0 to 10: 0=no pain, and 10=pain as bad as you can imagine. Higher ADPS scores indicate higher pain intensity. Negative change from baseline indicates improvement.

    Time frame: Baseline (Week 2 of the Run-in period) to Week 6

Secondary outcomes

  1. Percentage of Participants With ≥30% Reduction in Pain Intensity in ADPS From Baseline to Week 6

    ADPS is based on question 5 of BPI-DPN and assessed on an 11-point numerical rating scale. Participants were asked to rate their average pain over the past 24 hours, by answering the question 5 "Please rate your pain due to your diabetes by indicating the one number that best describes your pain on the average." on a scale of 0 to 10 where 0 = No Pain and 10 = pain as bad as you can imagine. If % change from Baseline ≤ (-30) then participant was considered a Responder and if missing % change from Baseline or \>(-30) participant is considered a Non-responder. Percentage of participants who were responders (who achieved ≥30% reduction in pain intensity in ADPS from Baseline to Week 6) are reported.

    Time frame: Baseline (Week 2 of the Run-in period) to Week 6

  2. Percentage of Participants With ≥50% Reduction in Pain Intensity in ADPS From Baseline at Week 6

    ADPS is based on question 5 of BPI-DPN and assessed on an 11-point numerical rating scale. Participants were asked to rate their average pain over the past 24 hours, by answering the question 5 "Please rate your pain due to your diabetes by indicating the one number that best describes your pain on the average." on a scale of 0 to 10 where 0 = No Pain and 10 = pain as bad as you can imagine. If % change from Baseline ≤ (-50) then participant is considered a Responder and if missing % change from Baseline or \>(-50) then participant is considered a Non-responder. Percentage of participants who were responders (who achieved ≥50% reduction in pain intensity in ADPS from Baseline to Week 6) are reported.

    Time frame: Baseline (Week 2 of the Run-in period) to Week 6

  3. Change From Baseline to Week 6 in Severity of Pain and Interference of Pain With Sleep and Other Aspects of the Participant's Life Based on the BPI-DPN

    BPI-DPN: questionnaire that assesses severity of pain \& its impact on functioning in participants with DPN. It consists of 4 questions that measure pain at its "worst,"least","average","now"(current pain) on 11-point numerical scale 0=no pain;10=worst pain.Score range:0-10 for each of these pain questions, higher scores=greater pain severity. Other 7 questions of BPI evaluate level of interference of pain on daily functioning (general activity,walking,work ability,mood,enjoyment of life,relations,sleep) on 11-point numerical scale, 0=does not interfere;10=completely interferes.Score range:0-10 for each of these intensity questions, higher scores=greater interference. Pain severity \& pain interference factors are reported as separate categories. Average interference score= mean of 7 interference categories collected in Questions 9A-G, only if 50% (ie at least 4 of 7) of scores were non-missing. Negative change from baseline=improvement. Score range for average interference score: 0-70.

    Time frame: Baseline (Week 2 of the Run-in period) to Week 6

  4. Percentage of Participants Discontinuing Treatment Due to Lack of Efficacy

    Lack of efficacy was defined as an increase of 30% from baseline in ADPS based on question 5 of the BPI-DPN. Baseline was defined as the average of the Week 2 Run-in period data collected by participants in the daily pain diary of BPI-DPN. ADPS is based on question 5 of BPI-DPN and assessed on an 11-point numerical rating scale where 0 = No Pain to 10 = pain as bad as you can imagine, higher score indicates higher pain intensity.

    Time frame: Baseline (Week 2 of the Run-in period) to Week 6

  5. Patient Global Impression of Change (PGIC) Scale Score at Week 6

    PGIC is a 7-point rating scale that assesses participant's belief about the overall improvement experienced after the end of treatment, where 1= very much improved to 7 = very much worse. Higher score indicates worsening.

    Time frame: Baseline (Week 2 of the Run-in period) to Week 6

  6. Time to Loss of Efficacy From Week 6 to Week 11 Among Participants Achieving a ≥30% Reduction in Pain Intensity at Week 6

    For participants who achieved ≥30% reduction in ADPS based on Question 5 of the BPI-DPN at Week 6, the time to loss of efficacy was defined as the time from the date of Week 6 visit to the date of termination of safety follow-up due to lack of efficacy. ADPS is based on question 5 of BPI-DPN and assessed on an 11-point numerical rating scale where, 0 = No Pain to 10 = pain as bad as you can imagine.

    Time frame: Weeks 6 to 11

  7. Number of Participants With Treatment-emergent Adverse Events (TEAEs)

    Adverse Events (AE) is defined as any sign, symptom, or diagnosis/disease that is unfavorable or unintended, that is new, or if pre-existing, worsens in participants administered a pharmaceutical product and that does not necessarily have a causal relationship with this treatment. Treatment-emergent AEs are defined as any AEs that occur or worsen after the first dose of study medication.

    Time frame: First dose of study drug after randomization up to the end of study (up to Week 11)

06

Results

Posted Jun 25, 2025

Participant flow

Participants took part in the study at multiple investigative sites in the United States from 03 Sep 2020 to 28 Jun 2022.

Double-Blind Period (Up to Week 6)
Participant flow — Double-Blind Period (Up to Week 6)
MilestonePlaceboLX9211 100 mg/10 mgLX9211 200 mg/20 mg
Started107106106
Completed1018570
Not completed62136
Withdrew: Adverse event41728
Withdrew: Subject choice unrelated to adverse event/serious adverse event226
Withdrew: Other, not specified022
Follow up Period (Weeks 7 to 11)
Participant flow — Follow up Period (Weeks 7 to 11)
MilestonePlaceboLX9211 100 mg/10 mgLX9211 200 mg/20 mg
Started1049992
Completed1039992
Not completed100
Withdrew: Other, not specified100

Outcome measures

PrimaryChange From Baseline to Week 6 in ADPS as Measured by the Numerical Rating Scale

ADPS is based on question 5 of Brief Pain Inventory (BPI)-short form for Diabetic Peripheral Neuropathy (BPI-DPN) and is assessed on an 11-point numerical rating scale. Participants were asked to rate their average pain over the past 24 hours, by answering the question 5 "Please rate your pain due to your diabetes by indicating the one number that best describes your pain on the average." on a scale of 0 to 10: 0=no pain, and 10=pain as bad as you can imagine. Higher ADPS scores indicate higher pain intensity. Negative change from baseline indicates improvement.

Time frame:
Baseline (Week 2 of the Run-in period) to Week 6
Reported as:
Least squares mean · score on a scale
Change From Baseline to Week 6 in ADPS as Measured by the Numerical Rating Scale
score on a scalePlaceboLX9211 100 mg/10 mgLX9211 200 mg/20 mg
Change From Baseline to Week 6 in ADPS as Measured by the Numerical Rating Scale-0.72 (-1.08 to -0.36)-1.39 (-1.77 to -1.01)-1.27 (-1.66 to -0.88)
Statistical analysis
  • Placebo vs LX9211 100 mg/10 mg · MMRM model · p = 0.007 · Ls mean difference: -0.67 · 95% CI -1.16 to -0.18
  • Placebo vs LX9211 200 mg/20 mg · MMRM model · p = 0.030 · Ls mean difference: -0.55 · 95% CI -1.06 to -0.05
SecondaryPercentage of Participants With ≥30% Reduction in Pain Intensity in ADPS From Baseline to Week 6

ADPS is based on question 5 of BPI-DPN and assessed on an 11-point numerical rating scale. Participants were asked to rate their average pain over the past 24 hours, by answering the question 5 "Please rate your pain due to your diabetes by indicating the one number that best describes your pain on the average." on a scale of 0 to 10 where 0 = No Pain and 10 = pain as bad as you can imagine. If % change from Baseline ≤ (-30) then participant was considered a Responder and if missing % change from Baseline or \>(-30) participant is considered a Non-responder. Percentage of participants who were responders (who achieved ≥30% reduction in pain intensity in ADPS from Baseline to Week 6) are reported.

Time frame:
Baseline (Week 2 of the Run-in period) to Week 6
Reported as:
Number · percentage of participants
Percentage of Participants With ≥30% Reduction in Pain Intensity in ADPS From Baseline to Week 6
percentage of participantsPlaceboLX9211 100 mg/10 mgLX9211 200 mg/20 mg
Percentage of Participants With ≥30% Reduction in Pain Intensity in ADPS From Baseline to Week 617.827.417.0
Statistical analysis
  • Placebo vs LX9211 100 mg/10 mg · Cochran-Mantel-Haenszel · p = 0.091 · Difference in percentage of responders: 9.6 · 95% CI -1.55 to 20.76
  • Placebo vs LX9211 200 mg/20 mg · Cochran-Mantel-Haenszel · p = 0.883 · Difference in percentage of responders: -0.8 · 95% CI -10.95 to 9.40
SecondaryPercentage of Participants With ≥50% Reduction in Pain Intensity in ADPS From Baseline at Week 6

ADPS is based on question 5 of BPI-DPN and assessed on an 11-point numerical rating scale. Participants were asked to rate their average pain over the past 24 hours, by answering the question 5 "Please rate your pain due to your diabetes by indicating the one number that best describes your pain on the average." on a scale of 0 to 10 where 0 = No Pain and 10 = pain as bad as you can imagine. If % change from Baseline ≤ (-50) then participant is considered a Responder and if missing % change from Baseline or \>(-50) then participant is considered a Non-responder. Percentage of participants who were responders (who achieved ≥50% reduction in pain intensity in ADPS from Baseline to Week 6) are reported.

Time frame:
Baseline (Week 2 of the Run-in period) to Week 6
Reported as:
Number · percentage of participants
Percentage of Participants With ≥50% Reduction in Pain Intensity in ADPS From Baseline at Week 6
percentage of participantsPlaceboLX9211 100 mg/10 mgLX9211 200 mg/20 mg
Percentage of Participants With ≥50% Reduction in Pain Intensity in ADPS From Baseline at Week 610.315.19.4
Statistical analysis
  • Placebo vs LX9211 100 mg/10 mg · Cochran-Mantel-Haenszel · p = 0.289 · Difference in percentage of responders: 4.8 · 95% CI -4.11 to 13.73
  • Placebo vs LX9211 200 mg/20 mg · Cochran-Mantel-Haenszel · p = 0.837 · Difference in percentage of responders: -0.8 · 95% CI -8.85 to 7.16
SecondaryChange From Baseline to Week 6 in Severity of Pain and Interference of Pain With Sleep and Other Aspects of the Participant's Life Based on the BPI-DPN

BPI-DPN: questionnaire that assesses severity of pain \& its impact on functioning in participants with DPN. It consists of 4 questions that measure pain at its "worst,"least","average","now"(current pain) on 11-point numerical scale 0=no pain;10=worst pain.Score range:0-10 for each of these pain questions, higher scores=greater pain severity. Other 7 questions of BPI evaluate level of interference of pain on daily functioning (general activity,walking,work ability,mood,enjoyment of life,relations,sleep) on 11-point numerical scale, 0=does not interfere;10=completely interferes.Score range:0-10 for each of these intensity questions, higher scores=greater interference. Pain severity \& pain interference factors are reported as separate categories. Average interference score= mean of 7 interference categories collected in Questions 9A-G, only if 50% (ie at least 4 of 7) of scores were non-missing. Negative change from baseline=improvement. Score range for average interference score: 0-70.

Time frame:
Baseline (Week 2 of the Run-in period) to Week 6
Reported as:
Least squares mean · score on a scale
Change From Baseline to Week 6 in Severity of Pain and Interference of Pain With Sleep and Other Aspects of the Participant's Life Based on the BPI-DPN
score on a scalePlaceboLX9211 100 mg/10 mgLX9211 200 mg/20 mg
Pain at its Worst-0.69 (-1.11 to -0.26)-1.42 (-1.87 to -0.97)-1.38 (-1.81 to -0.96)
Pain at its Least-0.69 (-1.13 to -0.26)-1.43 (-1.89 to -0.98)-1.38 (-1.81 to -0.95)
Pain Right Now-0.55 (-1.00 to -0.10)-1.42 (-1.89 to -0.95)-1.03 (-1.47 to -0.59)
Interference Score Averaged Over Questions 9A - G-0.74 (-1.17 to -0.30)-1.00 (-1.46 to -0.53)-0.97 (-1.41 to -0.53)
General Activity-0.77 (-1.25 to -0.28)-0.96 (-1.48 to -0.44)-0.82 (-1.31 to -0.33)
Mood-0.71 (-1.22 to -0.19)-0.72 (-1.27 to -0.16)-0.65 (-1.18 to -0.13)
Walking Ability-0.74 (-1.24 to -0.24)-1.36 (-1.89 to -0.83)-1.22 (-1.73 to -0.72)
Normal Work-1.01 (-1.50 to -0.53)-1.07 (-1.58 to -0.55)-1.05 (-1.54 to -0.56)
Relations with Other People-0.29 (-0.79 to 0.20)0.14 (-0.39 to 0.67)-0.09 (-0.59 to 0.41)
Sleep-0.48 (-0.96 to -0.01)-1.45 (-1.96 to -0.94)-1.52 (-2.00 to -1.04)
Enjoyment of Life-1.03 (-1.53 to -0.52)-1.05 (-1.59 to -0.50)-1.13 (-1.64 to -0.61)
Statistical analysis
  • Placebo vs LX9211 100 mg/10 mg · MMRM model · p = 0.014 · Ls mean difference: -0.73 · 95% CI -1.32 to -0.15
  • Placebo vs LX9211 200 mg/20 mg · MMRM model · p = 0.017 · Ls mean difference: -0.70 · 95% CI -1.27 to -0.13
  • Placebo vs LX9211 100 mg/10 mg · MMRM model · p = 0.015 · Ls mean difference: -0.74 · 95% CI -1.33 to -0.15
  • Placebo vs LX9211 200 mg/20 mg · MMRM model · p = 0.020 · Ls mean difference: -0.69 · 95% CI -1.27 to -0.11
  • Placebo vs LX9211 100 mg/10 mg · MMRM model · p = 0.005 · Ls mean difference: -0.87 · 95% CI -1.48 to -0.27
  • Placebo vs LX9211 200 mg/20 mg · MMRM model · p = 0.111 · Ls mean difference: -0.48 · 95% CI -1.07 to 0.11
  • Placebo vs LX9211 100 mg/10 mg · MMRM model · p = 0.399 · Ls mean difference: -0.26 · 95% CI -0.87 to 0.35
  • Placebo vs LX9211 200 mg/20 mg · MMRM model · p = 0.441 · Ls mean difference: -0.23 · 95% CI -0.83 to 0.36
  • Placebo vs LX9211 100 mg/10 mg · MMRM model · p = 0.575 · Ls mean difference: -0.19 · 95% CI -0.87 to 0.49
  • Placebo vs LX9211 200 mg/20 mg · MMRM model · p = 0.880 · Ls mean difference: -0.05 · 95% CI -0.71 to 0.61
  • Placebo vs LX9211 100 mg/10 mg · MMRM model · p = 0.978 · Ls mean difference: -0.01 · 95% CI -0.73 to 0.71
  • Placebo vs LX9211 200 mg/20 mg · MMRM model · p = 0.877 · Ls mean difference: 0.06 · 95% CI -0.65 to 0.76
  • Placebo vs LX9211 100 mg/10 mg · MMRM model · p = 0.079 · Ls mean difference: -0.62 · 95% CI -1.32 to 0.07
  • Placebo vs LX9211 200 mg/20 mg · MMRM model · p = 0.163 · Ls mean difference: -0.48 · 95% CI -1.16 to 0.20
  • Placebo vs LX9211 100 mg/10 mg · MMRM model · p = 0.875 · Ls mean difference: -0.05 · 95% CI -0.73 to 0.62
  • Placebo vs LX9211 200 mg/20 mg · MMRM model · p = 0.914 · Ls mean difference: -0.04 · 95% CI -0.69 to 0.62
  • Placebo vs LX9211 100 mg/10 mg · MMRM model · p = 0.219 · Ls mean difference: 0.43 · 95% CI -0.26 to 1.12
  • Placebo vs LX9211 200 mg/20 mg · MMRM model · p = 0.551 · Ls mean difference: 0.20 · 95% CI -0.47 to 0.87
  • Placebo vs LX9211 100 mg/10 mg · MMRM model · p = 0.005 · Ls mean difference: -0.96 · 95% CI -1.63 to -0.30
  • Placebo vs LX9211 200 mg/20 mg · MMRM model · p = 0.002 · Ls mean difference: -1.04 · 95% CI -1.68 to -0.39
  • Placebo vs LX9211 100 mg/10 mg · MMRM model · p = 0.955 · Ls mean difference: -0.02 · 95% CI -0.73 to 0.69
  • Placebo vs LX9211 200 mg/20 mg · MMRM model · p = 0.777 · Ls mean difference: -0.10 · 95% CI -0.79 to 0.59
SecondaryPercentage of Participants Discontinuing Treatment Due to Lack of Efficacy

Lack of efficacy was defined as an increase of 30% from baseline in ADPS based on question 5 of the BPI-DPN. Baseline was defined as the average of the Week 2 Run-in period data collected by participants in the daily pain diary of BPI-DPN. ADPS is based on question 5 of BPI-DPN and assessed on an 11-point numerical rating scale where 0 = No Pain to 10 = pain as bad as you can imagine, higher score indicates higher pain intensity.

Time frame:
Baseline (Week 2 of the Run-in period) to Week 6
Reported as:
Number · percentage of participants
Percentage of Participants Discontinuing Treatment Due to Lack of Efficacy
percentage of participantsPlaceboLX9211 100 mg/10 mgLX9211 200 mg/20 mg
Percentage of Participants Discontinuing Treatment Due to Lack of Efficacy000
SecondaryPatient Global Impression of Change (PGIC) Scale Score at Week 6

PGIC is a 7-point rating scale that assesses participant's belief about the overall improvement experienced after the end of treatment, where 1= very much improved to 7 = very much worse. Higher score indicates worsening.

Time frame:
Baseline (Week 2 of the Run-in period) to Week 6
Reported as:
Least squares mean · score on a scale
Patient Global Impression of Change (PGIC) Scale Score at Week 6
score on a scalePlaceboLX9211 100 mg/10 mgLX9211 200 mg/20 mg
Patient Global Impression of Change (PGIC) Scale Score at Week 63.28 (3.04 to 3.52)2.93 (2.69 to 3.17)3.13 (2.88 to 3.38)
Statistical analysis
  • Placebo vs LX9211 100 mg/10 mg · ANOVA · p = 0.031 · Ls mean difference: -0.35 · 95% CI -0.67 to -0.03
  • Placebo vs LX9211 200 mg/20 mg · ANOVA · p = 0.351 · Ls mean difference: -0.15 · 95% CI -0.48 to 0.17
SecondaryTime to Loss of Efficacy From Week 6 to Week 11 Among Participants Achieving a ≥30% Reduction in Pain Intensity at Week 6

For participants who achieved ≥30% reduction in ADPS based on Question 5 of the BPI-DPN at Week 6, the time to loss of efficacy was defined as the time from the date of Week 6 visit to the date of termination of safety follow-up due to lack of efficacy. ADPS is based on question 5 of BPI-DPN and assessed on an 11-point numerical rating scale where, 0 = No Pain to 10 = pain as bad as you can imagine.

Time frame:
Weeks 6 to 11
Reported as:
Median · weeks
Time to Loss of Efficacy From Week 6 to Week 11 Among Participants Achieving a ≥30% Reduction in Pain Intensity at Week 6
weeksPlaceboLX9211 100 mg/10 mgLX9211 200 mg/20 mg
Time to Loss of Efficacy From Week 6 to Week 11 Among Participants Achieving a ≥30% Reduction in Pain Intensity at Week 6NA (NA to NA)NA (NA to NA)NA (NA to NA)
SecondaryNumber of Participants With Treatment-emergent Adverse Events (TEAEs)

Adverse Events (AE) is defined as any sign, symptom, or diagnosis/disease that is unfavorable or unintended, that is new, or if pre-existing, worsens in participants administered a pharmaceutical product and that does not necessarily have a causal relationship with this treatment. Treatment-emergent AEs are defined as any AEs that occur or worsen after the first dose of study medication.

Time frame:
First dose of study drug after randomization up to the end of study (up to Week 11)
Reported as:
Count of participants · Participants
Number of Participants With Treatment-emergent Adverse Events (TEAEs)
ParticipantsPlacebo (Double-blind Treatment Period)LX9211 100 mg/10 mg (Double-blind Treatment Period)LX9211 200 mg/20 mg (Double-blind Treatment Period)Placebo (Single-blind Follow-up Period)LX9211 100 mg/10 mg (Single-blind Follow-up Period)LX9211 200 mg/20 mg Single-blind Follow-up Period)
Number of Participants With Treatment-emergent Adverse Events (TEAEs)325754152118

Adverse events

Collected over First dose of study drug after randomization up to the end of study (up to Week 11). Non-serious events are listed at a 5% frequency threshold.

Adverse event summary by group
GroupDeathsSeriousOther
Placebo (Double-blind Treatment Period)1/107 (0.9%)1/107 (0.9%)9/107 (8.4%)
LX9211 100 mg/10 mg (Double-blind Treatment Period)0/106 (0%)0/106 (0%)39/106 (36.8%)
LX9211 200 mg/20 mg (Double-blind Treatment Period)1/106 (0.9%)2/106 (1.9%)44/106 (41.5%)
Placebo (Single-blind Follow-up Period)0/104 (0%)1/104 (1%)4/104 (3.8%)
LX9211 100 mg/10 mg (Single-blind Follow-up Period)0/99 (0%)1/99 (1%)2/99 (2%)
LX9211 200 mg/20 mg Single-blind Follow-up Period)0/92 (0%)1/92 (1.1%)6/92 (6.5%)
Most frequent serious events
Most frequent serious events
EventPlacebo (Double-blind Treatment Period)LX9211 100 mg/10 mg (Double-blind Treatment Period)LX9211 200 mg/20 mg (Double-blind Treatment Period)Placebo (Single-blind Follow-up Period)LX9211 100 mg/10 mg (Single-blind Follow-up Period)LX9211 200 mg/20 mg Single-blind Follow-up Period)
Atrial fibrillationCardiac disorders0/1070/1060/1060/1040/991/92
Supraventricular tachycardiaCardiac disorders0/1070/1060/1060/1040/991/92
Coronavirus infectionInfections and infestations0/1070/1060/1060/1041/990/92
Abdominal pain lowerGastrointestinal disorders0/1070/1060/1061/1040/990/92
Oedema peripheralGeneral disorders0/1070/1061/1060/1040/990/92
Type 1 diabetes mellitusMetabolism and nutrition disorders0/1070/1061/1060/1040/990/92
OrthopnoeaRespiratory, thoracic and mediastinal disorders0/1070/1061/1060/1040/990/92
COVID-19Infections and infestations1/1070/1060/1060/1040/990/92
Most frequent other events
Most frequent other events
EventPlacebo (Double-blind Treatment Period)LX9211 100 mg/10 mg (Double-blind Treatment Period)LX9211 200 mg/20 mg (Double-blind Treatment Period)Placebo (Single-blind Follow-up Period)LX9211 100 mg/10 mg (Single-blind Follow-up Period)LX9211 200 mg/20 mg Single-blind Follow-up Period)
DizzinessNervous system disorders2/10716/10629/1062/1041/991/92
NauseaGastrointestinal disorders3/1079/10612/1061/1040/993/92
HeadacheNervous system disorders4/1079/10610/1062/1041/990/92
ConstipationGastrointestinal disorders3/1074/1068/1060/1040/990/92
SomnolenceNervous system disorders0/1077/1062/1060/1040/991/92
VomitingGastrointestinal disorders2/1072/1067/1060/1040/992/92
Balance disorderNervous system disorders0/1076/1065/1060/1040/990/92

Baseline characteristics

The mITT population included all randomized participants who took at least 1 dose of study drug; participants were analyzed according to their randomized treatment.

Age, Continuous
Age, Continuous(years)PlaceboLX9211 100 mg/10 mgLX9211 200 mg/20 mgTotal
Mean62.0 ± 9.5962.8 ± 9.2661.8 ± 10.9662.2 ± 9.94
Sex: Female, Male
Sex: Female, Male(Participants)PlaceboLX9211 100 mg/10 mgLX9211 200 mg/20 mgTotal
Female414843132
Male665863187
Ethnicity (NIH/OMB)
Ethnicity (NIH/OMB)(Participants)PlaceboLX9211 100 mg/10 mgLX9211 200 mg/20 mgTotal
Hispanic or Latino23131854
Not Hispanic or Latino849388265
Unknown or Not Reported0000
Race/Ethnicity, Customized
Race/Ethnicity, Customized(Participants)PlaceboLX9211 100 mg/10 mgLX9211 200 mg/20 mgTotal
American Indian or Alaska Native2002
Asian1315
Native Hawaiian or Other Pacific Islander0202
Black or African American19221859
White827983244
Other3047
Unknown or Not Reported0000
Average Daily Pain Score (ADPS)
Average Daily Pain Score (ADPS)(score on a scale)PlaceboLX9211 100 mg/10 mgLX9211 200 mg/20 mgTotal
Mean6.54 ± 1.1546.59 ± 1.0916.53 ± 1.0286.55 ± 1.089
07

Study locations

44 sites
  • Lexicon Investigational Site
    Mobile, Alabama 36608, United States
  • Lexicon Investigational Site
    Chandler, Arizona 85286, United States
  • Lexicon Investigational Site
    Glendale, Arizona 85308, United States
  • Lexicon Investigational Site
    Kingman, Arizona 86409, United States
  • Lexicon Investigational Site
    Tucson, Arizona 85741, United States
  • Lexicon Investigational Site
    Anaheim, California 92801, United States
  • Lexicon Investigational Site
    Greenbrae, California 94904, United States
  • Lexicon Investigational Site
    Los Angeles, California 90026, United States
  • Lexicon Investigational Site
    North Hollywood, California 91606, United States
  • Lexicon Investigational Site
    Sacramento, California 95821, United States
  • Lexicon Investigational Site
    Tustin, California 92780, United States
  • Lexicon Investigational Site
    Brandon, Florida 33511, United States
  • Lexicon Investigational Site
    Fort Myers, Florida 33912, United States
  • Lexicon Investigational Site
    Jacksonville, Florida 32204, United States
  • Lexicon Investigational Site
    Lake City, Florida 32055, United States
  • Lexicon Investigational Site
    New Port Richey, Florida 34652, United States
  • Lexicon Investigational Site
    Ormond Beach, Florida 32174, United States
  • Lexicon Investigational Site
    Winter Park, Florida 32789, United States
  • Lexicon Investigational Site
    Macon, Georgia 31210, United States
  • Lexicon Investigational Site
    Evansville, Indiana 47714, United States
  • Lexicon Investigational Site
    Boston, Massachusetts 02115, United States
  • Lexicon Investigational Site
    South Dartmouth, Massachusetts 02747, United States
  • Lexicon Investigational Site
    Ann Arbor, Michigan 48109, United States
  • Lexicon Investigational Site
    Dearborn, Michigan 48124, United States
  • Lexicon Investigational Site
    Farmington Hills, Michigan 48334, United States
  • Lexicon Investigational Site
    Sterling Heights, Michigan 48312, United States
  • Lexicon Investigational Site
    Hazelwood, Missouri 63042, United States
  • Lexicon Investigational Site
    Omaha, Nebraska 68130, United States
  • Lexicon Investigational Site
    Berlin, New Jersey 08009, United States
  • Lexicon Investigational Site
    Westfield, New York 14787, United States
  • Lexicon Investigational Site
    Williamsville, New York 14221, United States
  • Lexicon Investigational Site
    Asheville, North Carolina 28803, United States
  • Lexicon Investigational Site
    Cary, North Carolina 27518, United States
  • Lexicon Investigational Site
    Morehead City, North Carolina 28557, United States
  • Lexicon Investigational Site
    Greenville, South Carolina 29607, United States
  • Lexicon Investigational Site
    Austin, Texas 78731, United States
  • Lexicon Investigational Site
    Austin, Texas 78749, United States
  • Lexicon Investigational Site
    Dallas, Texas 75231, United States
  • Lexicon Investigational Site
    Flower Mound, Texas 75028, United States
  • Lexicon Investigational Site
    Houston, Texas 77030, United States
  • Lexicon Investigational Site
    Houston, Texas 77074, United States
  • Lexicon Investigational Site
    Pearland, Texas 77584, United States
  • Lexicon Investigational Site
    Salt Lake City, Utah 84107, United States
  • Lexicon Investigational Site
    Renton, Washington 98057, United States
08

References and documents

Publications

  • Luo G, Chen L, Kostich WA, Hamman B, Allen J, Easton A, Bourin C, Gulianello M, Lippy J, Nara S, Maishal TK, Thiyagarajan K, Jalagam P, Pattipati SN, Dandapani K, Dokania M, Vattikundala P, Sharma V, Elavazhagan S, Verma MK, Das ML, Wagh S, Balakrishnan A, Johnson BM, Santone KS, Thalody G, Denton R, Saminathan H, Holenarsipur VK, Kumar A, Rao A, Putlur SP, Sarvasiddhi SK, Shankar G, Louis JV, Ramarao M, Conway CM, Li YW, Pieschl R, Tian Y, Hong Y, Ditta J, Mathur A, Li J, Smith D, Pawluczyk J, Sun D, Yip S, Wu DR, Vetrichelvan M, Gupta A, Wilson A, Gopinathan S, Wason S, Bristow L, Albright CF, Bronson JJ, Macor JE, Dzierba CD. Discovery of (S)-1-((2',6-Bis(difluoromethyl)-[2,4'-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine (BMS-986176/LX-9211): A Highly Selective, CNS Penetrable, and Orally Active Adaptor Protein-2 Associated Kinase 1 Inhibitor in Clinical Trials for the Treatment of Neuropathic Pain. J Med Chem. 2022 Mar 24;65(6):4457-4480. doi: 10.1021/acs.jmedchem.1c02131. Epub 2022 Mar 8. PubMed 35257579 ↗

Study documents

  • Study protocol · Sep 9, 2021
  • Statistical analysis plan · Jun 7, 2022

Documents are hosted by the registry — open the source record to download them.

09

Registry details

Key details

Study ID
NCT04455633
Lead sponsor
Lexicon Pharmaceuticals
Responsible party
Sponsor
First posted
Jul 2, 2020
Start date
Sep 3, 2020
Primary completion
May 23, 2022
Completion
Jun 28, 2022
Results posted
Jun 25, 2025
Last update
Jun 25, 2025

Study contacts

Suma Gopinathan, PhD
study director · Lexicon Pharmaceuticals

Oversight

Data monitoring committee
Yes
FDA-regulated drug
Yes
FDA-regulated device
No
View the source record on ClinicalTrials.gov ↗

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