Tarlige (mirogabalin) / Daiichi Sankyo, Menarini - LARVOL DELTA

Directed evolution of amine dehydrogenase for the catalytic resolution of (1R,5S)-3-ethylbicyclo [3.2.0] hept-3-en-6-one, a chiral intermediate of mirogabalin (PubMed, Sheng Wu Gong Cheng Xue Bao) - "After the reaction was completed, the product was subjected to extraction and acid washing, affording the chiral ketone with an ee value of 97.1% and a yield of 45.4%. This study successfully developed a novel amine dehydrogenase-catalyzed resolution approach for (1R,5S)-1a, which simplifies the post-processing workflow of the product and reduces the consumption of organic reagents, thereby providing robust technical support for the efficient industrial-scale biomanufacturing of (1R,5S)-1a."

Journal

The Role of the Antidepressants in Managing Chemotherapy-Induced Neuropathic Pain: A Systematic Review. (PubMed, Pharmacol Res Perspect) - "Combination therapies involving duloxetine and agents such as tapentadol, pregabalin, mirogabalin, or amitriptyline were associated with additional reductions in pain intensity; however, current evidence remains insufficient to establish additive or synergistic effects. Current evidence supports antidepressants, particularly duloxetine, associated with reductions in pain intensity in heterogeneous studies, whereas evidence for CIPN prevention remains inconclusive. These findings support their continued use in clinical practice and highlight the need for larger, well-designed randomized controlled trials to optimize treatment strategies and further define the role of combination therapies in CIPN management."

Journal • Review • Neuralgia • Oncology • Pain • Peripheral Neuropathic Pain

Mirogabalin, C12H19NO2, and mirogabalin besylate, C12H20NO2+·C6H5O3S. (PubMed, Acta Crystallogr C Struct Chem) - "In the besylate, discrete N-H...O and O-H...O hydrogen bonds link the cations and anions into layers parallel to the bc plane. The powder patterns have been submitted to the ICDD for inclusion in the Powder Diffraction File (PDF)."

Journal • CDKN1A

M-EBMP-IC/BPS: Mirogabalin Plus EBMP for IC/BPS (clinicaltrials.gov) - P1 | N=200 | Not yet recruiting | Sponsor: Beijing Tiantan Hospital

New P1 trial • Interstitial Cystitis • Musculoskeletal Pain • Pain

First-In-Human Study of Mirogabalin (BM2216) Sustained-Release Tablets: Safety, Tolerability, Pharmacokinetics, Food Effect and Dose Proportionality With Comparison to Mirogabalin Besylate in Healthy Participants. (PubMed, Diabetes Obes Metab) - "BM2216 SR was safe and shows linear PK (5.5-3 mg single dose). Due to significant food effect and comparable QD exposure to the reference drug, postprandial QD administration is recommended. These data support further efficacy trials in neuropathic pain patients."

Journal • Diabetic Neuropathy • Neuralgia • Otorhinolaryngology • Pain • Vertigo

Comparison of the Efficacy and Safety of Mirogabalin and Duloxetine in Chemotherapy-induced Peripheral Neuropathy in a Randomized Controlled Trial: a Quality of Life Study in Cancer Survivors (clinicaltrials.gov) - P=N/A | N=66 | Completed | Sponsor: Pusan National University Yangsan Hospital | Not yet recruiting ➔ Completed | Trial completion date: Jun 2025 ➔ Apr 2026 | Trial primary completion date: May 2025 ➔ Apr 2026

HEOR • Trial completion • Trial completion date • Trial primary completion date • Breast Cancer • Oncology • Solid Tumor

Efficacy and safety of mirogabalin in patients with fibromyalgia: protocol for a multicentre, Prospective, Randomised, Open-label, Blinded Endpoint (PROBE) study. (PubMed, BMJ Open) - P=N/A | "Pregabalin, a standard pharmacological treatment, provides relief for some patients but is associated with dose-dependent adverse events (AEs) and incomplete efficacy, highlighting a significant unmet clinical need. Findings from this study will be disseminated through peer-reviewed journals and at scientific conferences. NCT07157852."

Clinical protocol • Journal • CNS Disorders • Depression • Fibromyalgia • Musculoskeletal Pain • Neuralgia • Pain • Psychiatry • Rheumatology

Early-Stage Complex Regional Pain Syndrome of the Foot and Ankle Showing Spontaneous Remission During Treatment With Loxoprofen and Mirogabalin: A Case Report (ASA 2026) - "The patient maintained daily walking for functional rehabilitation and declined interventional procedures. Over seven months, her symptoms progressively resolved and she no longer met the Budapest clinical diagnostic criteria for CRPS, although radiographic bone radiolucency persisted (Figure 2A and B), suggesting that clinical recovery may precede radiographic improvement in early-stage CRPS."

Case report • Clinical • Mood Disorders • Musculoskeletal Pain • Pain

Comparing Efficiency of Mirogabalin and Pregabalin in Primary TKA (clinicaltrials.gov) - P=N/A | N=80 | Recruiting | Sponsor: Thammasat University Hospital | Trial completion date: May 2025 ➔ Aug 2026 | Trial primary completion date: May 2025 ➔ Aug 2026

Trial completion date • Trial primary completion date • Immunology • Orthopedics • Osteoarthritis • Pain • Rheumatology

Efficacy and tolerability of mirogabalin, pregabalin, duloxetine, and placebo in patients with type 2 diabetes mellitus and painful diabetic peripheral neuropathy: A network meta-analysis. (PubMed, Diabetes Res Clin Pract) - "Within the available short-term evidence network, duloxetine demonstrated the most consistent analgesic efficacy and a more favorable metabolic safety profile than the α2δ ligands evaluated. Pregabalin's modest efficacy and disproportionate burden argue against routine first-line use in T2DM-associated PDNP."

Journal • Retrospective data • Review • Diabetes • Diabetic Neuropathy • Metabolic Disorders • Pain • Peripheral Neuropathic Pain • Type 2 Diabetes Mellitus

Comparison of the Efficacy and Safety of Mirogabalin versus Gabapentin in the Treatment of Refractory Chronic Cough: A Single-Center, Open-Label, Randomized Controlled Trial (ChiCTR) - P=N/A | N=122 | Not yet recruiting | Sponsor: Tongji Hospital of Tongji University; Tongji Hospital of Tongji University

New trial • Chronic Cough • Cough • Pulmonary Disease • Respiratory Diseases

The effect of pregabalin on pain and function in knee osteoarthritis: a systematic review and meta-analysis of randomized controlled trials. (PubMed, Inflammopharmacology) - "Pregabalin may enhance functional outcomes and contribute to pain relief when used as adjunctive therapy with NSAIDs in knee OA patients. Its benefit as monotherapy remains limited. While pregabalin was generally well-tolerated, larger, high-quality trials with longer follow-up are needed to confirm its role and long-term safety."

Journal • Retrospective data • Immunology • Musculoskeletal Diseases • Musculoskeletal Pain • Neuralgia • Orthopedics • Osteoarthritis • Pain • Rheumatology

Clinical Outcomes after Onset of Mirogabalin-Related Adverse Drug Reactions in Patients with Lumbar Spinal Stenosis: Post Hoc Analysis of the MiroTAS Study. (PubMed, Pain Ther) - "Our data suggest that dizziness and somnolence are generally manageable under careful monitoring, with most events recovered or improved after onset. The analgesic effect of mirogabalin was weakly associated with LSS duration and not associated with leg pain duration. However, this was a post hoc analysis; given the limited sample size and statistical power, further research is needed."

Adverse drug reaction • Clinical data • Journal • Retrospective data • Musculoskeletal Diseases • Neuralgia • Orthopedics • Pain • Peripheral Neuropathic Pain

Efficacy and Safety of Ion Channel Modulators in Painful Diabetic Neuropathy. (PubMed, Diabetes Obes Metab) - "Ion channel modulators, especially calcium channel blockers and sodium channel antagonists, have favourable safety profiles and beneficial effects on reducing pain and improving the quality of life of patients with PDN."

Journal • Diabetic Neuropathy • Pain

Association Between the Use of Gabapentinoids and Exacerbations of Chronic Obstructive Pulmonary Disease: A Systematic Review and Meta-analysis. (PubMed, Curr Ther Res Clin Exp) - "Subgroup analyses showed increased exacerbation risk with gabapentin (HR = 1.27, 95% CI: 1.02-1.58) and pregabalin (HR=1.37, 95% CI: 1.12-1.67), whereas mirogabalin showed no significant association. Therefore, future long-term studies are required to establish this association with underlying biological mechanisms. [PROSPERO ID: CRD420251248968]."

Journal • Retrospective data • Review • Asthma • Chronic Obstructive Pulmonary Disease • Immunology • Pulmonary Disease • Respiratory Diseases

Gabapentinoids for Neuropathic Pain Management: A Systematic Umbrella Review. (PubMed, Curr Neuropharmacol) - "Gabapentinoids showed efficacy in diabetic peripheral neuropathic pain, cancerrelated neuropathic pain, and spinal cord injury. Gabapentinoids also showed efficacy in patients with the following types of refractory neuropathic pain, including refractory diabetic peripheral neuropathic pain, trigeminal neuralgia, complex regional pain syndrome, and lower back pain. However, in the case of post-herpetic neuralgia, the results were controversial. Most of the included studies were of critically low quality, which reduces confidence in the efficacy of gabapentinoids. Their use was highly associated with drowsiness, somnolence, peripheral edema, and weight gain."

Journal • Back Pain • CNS Disorders • Diabetic Neuropathy • Musculoskeletal Pain • Neuralgia • Oncology • Pain • Peripheral Neuropathic Pain

A case in which a patient repeatedly developed post-mastectomy pain syndrome after three metachronous breast cancer surgeries over approximately 20 years, and was cured with drug therapy. (JBCS 2026) - "The pain improved with a gradual increase in mirogabalin, but sufficient analgesia was not achieved...This is a rare report in the literature and may contribute to prevention and treatment. Further accumulation of cases is necessary."

Clinical • Surgery • Breast Cancer • CNS Disorders • Depression • Musculoskeletal Pain • Neuralgia • Oncology • Pain • Solid Tumor

Pain reduction and tolerability of mirogabalin in trigeminal neuralgia: A prospective observational study. (PubMed, Headache) - "In this prospective, single-arm pilot study, mirogabalin was associated with short-term reductions in pain intensity and appeared to be generally well tolerated in patients with trigeminal neuralgia. These findings are hypothesis-generating and require confirmation in larger, controlled, and longer-term randomized trials to test the efficacy and safety of mirogabalin."

Journal • Observational data • Neuralgia • Pain • Peripheral Neuropathic Pain

Pregabalin enhances the proliferative potential of pancreatic cancer in vitro but not in mice with pancreatic cancer. (PubMed, BMC Pharmacol Toxicol) - "These findings suggest that pregabalin increases the proliferative ability of pancreatic cancer cells in vitro without promoting tumor growth in vivo. Additionally, it induces an alteration with an increase in tumor-infiltrating lymphocytes and dendritic cells, along with a decrease in M2-like tumor-associated macrophages and cancer-associated fibroblasts in vivo."

Journal • Preclinical • Oncology • Pain • Pancreatic Cancer • Pancreatic Ductal Adenocarcinoma • Solid Tumor • CCL19 • CCL2 • CCL21 • CCL3 • CD4 • CD8 • CXCL10 • CXCL16 • IL10 • IL13 • IL15 • IL2 • IL6 • KRAS • PDX1 • TNFA

Post-marketing safety evaluation of mirogabalin using the JADER database. (PubMed, Front Pharmacol) - "This study aimed to identify and characterize adverse event (AE) signals associated with mirogabalin, evaluate demographic differences, and compare signal strength with pregabalin and gabapentin. This study extends the understanding of mirogabalin's post-marketing safety profile by identifying six novel signals and revealing distinct safety signal profiles compared with established α2-δ ligands. Demographic-stratified monitoring strategies are warranted to optimize patient safety."

Journal • P4 data • Cardiovascular • CNS Disorders • Congestive Heart Failure • Dermatology • Diabetic Neuropathy • Geriatric Disorders • Heart Failure • Movement Disorders • Neuralgia • Otorhinolaryngology • Pain • Peripheral Neuropathic Pain • Renal Disease • Respiratory Diseases

Prediction of Analgesic Use After Neurotoxic Chemotherapy: A Machine Learning Study Using Japanese Claims and Health Checkup Data (MASCC-ISOO 2026) - "The primary outcome was analgesic use within 12 months after the end of chemotherapy with gabapentin, duloxetine, pregabalin, tramadol, mirogabalin, mecobalamin, or goshajinkigan, defined as three or more prescriptions of any of the medications. Conclusions Claims-based prescribing trajectories with chemotherapy intensity can moderately predict post-chemotherapy analgesic use after oxaliplatin or paclitaxel. Further research with assessments of neuropathic symptoms or functional measures is needed to develop proactive supportive care and mitigate polypharmacy."

Machine learning • Neuralgia • Pain • Peripheral Neuropathic Pain

Cancer Patients with Neuropathic Pain: Pharmacist-Led Recommendation and Management and Mirogabalin Outcomes in a Single-Center Retrospective Observational Cohort. (PubMed, J Pain Palliat Care Pharmacother) - "Pharmacist-led recommendation and management was associated with higher recorded subjective effectiveness of mirogabalin in the per-protocol analysis. These findings are hypothesis-generating and support prospective evaluation of pharmacist-supported mirogabalin initiation in cancer-related neuropathic pain."

Journal • Observational data • Retrospective data • Neuralgia • Oncology • Pain

Phase II study of mirogabalin for oxaliplatin-associated chemotherapy-induced peripheral neuropathy in gastrointestinal cancer: The SmiliNg trial. (ASCO 2026) - P | "This study suggests that mirogabalin is effective and well-tolerated for the management of moderate-to-severe painful CIPN during oxaliplatin-based chemotherapy. These findings warrant further evaluation in a confirmatory trial."

P2 data • Esophageal Cancer • Gastrointestinal Cancer • Infectious Disease • Neuralgia • Oncology • Pain • Peripheral Neuropathic Pain • Respiratory Diseases • Solid Tumor

Current pharmacological and non-pharmacological approaches to chemotherapy-induced peripheral neuropathy and association with awareness of clinical guidelines. (PubMed, Jpn J Clin Oncol) - "Awareness of CIPN-GL2023 was associated with increased evidence-based practice, particularly through the use of duloxetine for pain and exercise for prevention. Multidisciplinary engagement and targeted efforts to reduce non-recommended practices remain important for improving CIPN management."

Clinical guideline • Journal • Oncology • Pain • Peripheral Neuropathic Pain

Therapeutic potential of combining mirogabalin with antidepressants in relieving hypersensitivity: evidence from a mouse model of neuropathic pain. (PubMed, Pharmacol Rep) - "These results may serve as a basis for further evaluation of the potential use of mirogabalin in the clinical treatment of neuropathic pain. Furthermore, they suggest that using mirogabalin together with amitriptyline or duloxetine may provide significant therapeutic benefits, enabling the use of lower doses of these medications, which may reduce the risk of adverse events."

Journal • Preclinical • Immunology • Neuralgia • Pain