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OPTIMUM

Efficacy and Safety of Pregabalin and Alpha-Lipoic Acid Combination in Patients With Painful Diabetic Peripheral Neuropathy: A Randomized, Open-Label, Non-Inferiority, Phase IV Clinical Trial and Subgroup Analysis (OPTIMUM Study)

Year of Publication: 2026

Authors: Oh TJ, Kim SS, Lee SH, et al.

Journal: Diabetes, Obesity & Metabolism

Citation: Diabetes Obes Metab 2026;28(7):6172-6183

Link: https://doi.org/10.1111/dom.70795

Bottom Line

Pregabalin monotherapy is non-inferior to pregabalin + ALA combination for pain relief in painful DPN over 12 weeks, with comparable safety; combination therapy may offer added benefit only in patients with shorter DPN duration (exploratory).

Major Points

  • Phase 4 open-label, non-inferiority RCT of 151 patients with painful DPN randomized 1:1:1 to ALA 480 mg/day, pregabalin 150-300 mg/day, or combination for 12 weeks.
  • Primary endpoint (VAS change from baseline to Week 12, PPS): pregabalin -19.73 mm vs combination -23.28 mm; LSM difference 3.46 mm (95% CI -4.94 to 11.87), upper bound below the pre-specified non-inferiority margin of 12.20 mm.
  • In FAS, all three arms showed similar VAS reductions (ALA -18.33, pregabalin -19.81, combination -22.78 mm) with no statistically significant differences.
  • Cluster analysis using DPN duration and DN4 score revealed that in cluster 1 (short DPN duration, ~9 months), combination therapy was significantly better than pregabalin (LSM diff 14.79 mm, p=0.0055) and ALA (LSM diff -10.83 mm, p=0.0405).
  • Safety profile was comparable across the three arms; dizziness was the most common AE in pregabalin-containing arms (~8%).

Design

Study Type: Randomized Controlled Trial (Phase 4, non-inferiority)

Randomization: 1

Blinding: Open-label

Enrollment Period: May 2021 - November 2022

Follow-up Duration: 12 weeks

Centers: 15

Countries: South Korea

Sample Size: 151

Analysis: Per-protocol set for non-inferiority; full analysis set (LOCF) for secondary outcomes; safety set for AEs


Inclusion Criteria

  • Adults aged 19-75 years
  • Type 2 diabetes mellitus
  • HbA1c ≤ 10% at screening
  • VAS pain score ≥ 40 mm at randomization
  • Diagnosis of painful DPN confirmed by DN4 score ≥ 4 at screening, OR objective evidence of neuropathy (abnormal peroneal nerve conduction study at screening or abnormal current perception threshold test within past 5 years)

Exclusion Criteria

  • Brittle diabetes mellitus
  • Elevated liver enzymes (ALT or AST > 3× upper normal limit) or active liver disease
  • Severe renal impairment (eGFR < 30 mL/min/1.73 m²)
  • Use of other antiepileptic drugs within 1 week of randomization
  • Presence of non-DPN pain
  • Pregnancy or lactation
  • Hypersensitivity to pregabalin, R-ALA tromethamine, or ALA components

Baseline Characteristics

CharacteristicALA (n=46)Pregabalin (n=43)Combination (n=46)
Mean Age (years)59.35 ± 10.8361.93 ± 10.4061.41 ± 8.53
Age ≥ 6541.30%48.84%41.30%
Sex - Female60.87%46.51%43.48%
Height (cm)161.70 ± 8.43163.00 ± 8.66163.98 ± 9.76
Weight (kg)68.40 ± 11.7866.68 ± 12.0467.73 ± 10.96
BMI (kg/m²)26.13 ± 3.7125.05 ± 3.8625.14 ± 3.23
Current alcohol use26.09%30.23%32.61%
Current smoker15.22%25.58%21.74%
Duration of DN (months)41.97 ± 46.5440.11 ± 46.8337.73 ± 45.07
DN4 total score5.46 ± 1.405.61 ± 1.365.92 ± 1.52
Baseline VAS (mm)60.61 ± 15.9860.47 ± 15.4761.57 ± 14.19

Arms

FieldAlpha-Lipoic Acid (ALA)PregabalinControl
InterventionALA 480 mg/day (Dexid, Bukwang Pharmaceutical)Pregabalin 150 mg/day, up-titratable to 300 mg/day at Week 6 based on pain relief and tolerabilityPregabalin 150-300 mg/day + ALA 480 mg/day
Duration12 weeks12 weeks12 weeks

Outcomes

OutcomeTypeControlInterventionHR / OR / RRP-value
Change in visual analogue scale (VAS) pain score from baseline to Week 12 (PPS): pregabalin monotherapy vs combination therapyPrimary-23.28 ± 18.15 mm (combination)-19.73 ± 18.94 mm (pregabalin)Non-inferiority established (upper bound of 95% CI below NI margin)
VAS change from baseline to Week 12 (FAS) - ALA vs Pregabalin vs CombinationSecondary-22.78 ± 16.70 mm (combination)-18.33 ± 23.74 (ALA) / -19.81 ± 19.75 (pregabalin)NS across groups
≥ 30% VAS reduction at Week 12Secondary63.0% (combination)50.0% (ALA) / 51.2% (pregabalin)NS
≥ 50% VAS reduction at Week 12SecondaryNR (NS)NR (NS)NS
BPI-K pain severity at Week 6SecondaryCombination better than ALAALA vs Combination< 0.05 (combination vs ALA)
TSS, PD-Q, EQ-5D-3L at Weeks 6 and 12SecondaryNRNRNS across groups
Inflammatory biomarkers (IL-1β, hs IL-6, hs TNF-α, hs CRP, IL-10) change at Week 12SecondaryNo significant changeNo significant changeNS
Lipid profile and urinary 8-OHdG at Week 12SecondaryNo significant changeNo significant changeNS
Cluster 1 (short DPN duration ~9 months) VAS at Week 12 - Pregabalin vs CombinationSecondaryCombinationPregabalinLSM diff 14.79 mm (95% CI 4.59-24.99)0.0055
Cluster 1 VAS at Week 12 - ALA vs CombinationSecondaryCombinationALALSM diff -10.83 mm (95% CI -21.18 to -0.49)0.0405
Treatment-by-DPN duration interaction (pregabalin vs combination) in post hoc ANCOVASecondary---0.0107
Any TEAEAdverseALA 32.65% vs Pregabalin 25.53% vs Combination 33.33% (p=0.67)
Adverse drug reactionsAdversep=0.1732 (NS across groups)
Serious adverse eventsAdversep=0.2439 (NS across groups)
Dizziness (pregabalin arm)Adverse8.51%
Dizziness (combination arm)Adverse8.33%
HeadacheAdverse2.04%
HypoesthesiaAdverse2.04%
NauseaAdverse2.04%
DyspepsiaAdverse2.04%
PainAdverse2.04%
Chest painAdverse2.04%
Clinically significant lab / vital sign abnormalitiesAdverseNone observed in any arm

Subgroup Analysis

Cluster analysis (three clusters by DPN duration + DN4 score): Cluster 1 (short DPN duration ~9 months) - combination therapy significantly better than pregabalin (LSM diff 14.79 mm, p=0.0055) and better than ALA (LSM diff -10.83 mm, p=0.0405) at Week 12. Clusters 2 (~64 months) and 3 (~122 months) showed no significant differences among treatment groups. Post hoc analysis confirmed significant treatment-by-DPN-duration interaction between pregabalin and combination (p=0.0107).


Criticisms

  • Open-label design introduces expectancy bias for subjective outcomes such as VAS pain scores.
  • Only 12-week treatment duration – likely insufficient to detect disease-modifying effects of ALA that may require longer exposure.
  • Conservative dosing regimen (pregabalin max 300 mg/day, ALA 480 mg/day) chosen for Asian population may not reflect Western clinical practice.
  • Cluster analysis was exploratory with small subgroup sample sizes, no multiple-comparison correction, and risk of overfitting – findings are hypothesis-generating only.
  • Site-based outcome assessment with no blinded/centralized adjudication may amplify subjective outcome variability.
  • Study conducted entirely in South Korea, limiting generalizability across populations.
  • No depression/anxiety questionnaires or sleep assessments, though these are highly relevant in chronic pain.
  • Industry-funded by Yuhan Corporation (manufacturer of pregabalin used in the study).

Funding

Yuhan Corporation. The funder had no role in study design, conduct, data analysis, interpretation, or manuscript preparation per authors.

Based on: OPTIMUM (Diabetes, Obesity & Metabolism, 2026)

Authors: Oh TJ, Kim SS, Lee SH, et al.

Citation: Diabetes Obes Metab 2026;28(7):6172-6183

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