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pregabalin (pregabalin, YuHan / YHD 1119 / YHD1119)

✓ Approved

YuHan · CACNA2D1 · Small Molecule

What is pregabalin?

pregabalin is a small molecule developed by YuHan. It is approved for therapeutic indications via oral (po).

Drug Profile

Brand Namespregabalin, YuHan, YHD 1119, YHD1119
CompanyYuHan
Drug ClassSmall Molecule
Molecular TargetCACNA2D1
RouteOral (PO)
StatusApproved
Sources: ClinicalTrials.gov, YuHan

Mechanism of Action

Molecular Targets

pregabalin acts on 1 molecular target:

CACNA2D1calcium voltage-gated channel auxiliary subunit alpha2delta 1 (LINC01112, CACNA2)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

pregabalin is developed for 2 unique indications across 1 therapeutic area.

Therapeutic AreaConditionPhase
Nervous system disordersDiabetic neuropathy✓ Approved
Nervous system disordersPost herpetic neuralgia✓ Approved

Related Research Articles

PubMedTurkish journal of anaesthesiology and reanimation2026-08-28

Effect of Multimodal Pre-emptive Analgesia with Pregabalin Versus Naproxen on Post-Thoracotomy Pain and Opioid Consumption: A Randomized Clinical Trial.

Das Prajjal P, Gupta Rajni R

Thoracotomy produces severe postoperative pain that limits deep breathing and coughing and may worsen recovery. Opioid-centred regimens can cause adverse effects; pre-emptive multimodal analgesia may reduce central sensitisation and opioid use. In this randomized, active-controlled, assessor-blinded trial (CTRI/2022/07/043800), adults aged 18-70 years (American Society of Anesthesiologists I-II) undergoing thoracotomy were randomized (39 per group) to receive oral pregabalin 2.5 mg kg-1 or oral naproxen 7 mg kg-1 (maximum 500 mg) 2 hours preoperatively. All patients received standardized general anaesthesia combined with thoracic epidural analgesia. Numerical rating scale (NRS) pain at rest and during deep breathing and coughing were assessed at 2, 6, 12, and 24 hours. A rescue opioid was administered when NRS exceeded 3. Time to first rescue, total 24-hour opioid consumption, number of rescue doses, sleep interference, and adverse events were recorded. Baseline demographics and perioperative haemodynamics were comparable. Resting pain scores and sleep interference were similar between groups. Pregabalin reduced opioid requirement: fewer patients required rescue analgesia (46.2% vs. 69.2%; P=0.042), time to first rescue was longer (7.6±3.1 vs. 5.4±2.8 h; P=0.001), and 24-hour opioid consumption was lower (6.2±3.0 vs. 8.6±3.4 mg morphine equivalents; P=0.001). Dynamic pain during deep breathing and coughing was lower with pregabalin at early time points; sedation was slightly higher at 2 hours, without significant adverse neurocognitive events. Pre-emptive pregabalin improved functional analgesia and produced an opioid-sparing effect compared with naproxen after thoracotomy, with acceptable short-term safety, thereby supporting enhanced recovery pathways.

PMID 42664442
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PubMedJournal of biomaterials science. Polymer edition2026-08-27

Formulation, optimization, and preclinical assessment of a QbD-engineered transethosomal pregabalin patch for neuropathic pain.

Safdar Janita J, Ahmed Naveed N, Fatima Syeda Komal SK, Gul Parsa P et al.

Neuropathic pain is a major clinical challenge since it has complex pathophysiology and multifactorial etiology. Pregabalin is an anticonvulsant drug that binds with the α2δ subunit of voltage-gated calcium channels, decreases their influx, and eventually lowers the release of excitatory neurotransmitters. The conventional oral Pregabalin exhibits lower therapeutic efficacy because of its variable absorption, CNS side effects, and frequent dosing. This present study suggests a new transdermal formulation containing transethosomes loaded with pregabalin to provide sustained drug release, enhanced drug penetration into the skin, and subsequently reduced systemic side effects. Transethosomes were formulated by thin-film hydration method, and their optimization was done through Box Behnken design, which recorded optimal particle size of 124.4 ± 2.54 nm, zeta potential of -20.5 ± 0.35 mV, and entrapment efficiency of 83.4 ± 0.8%. Formulation was then added to a transdermal patch containing eucalyptus oil and checked for in vitro release, which revealed that PGB-TES-P + EO showed more sustained drug release. Enhanced transdermal penetration of PGB-TES-P + EO was proved by ex vivo permeation and through fluorescence microscopy. In vivo assessment in the streptozotocin-induced diabetic neuropathic pain model demonstrated significant improvement in locomotor activity and pain responses, as well as a decline in the proinflammatory markers such as TNF-α and COX-2, which post-treatment values of 120.5 ± 6.57 and 119.1 ± 2.82, respectively. The final formulation showed no irritation to the skin and was found to be stable according to the ICH guidelines. Altogether, this system presents a potential alternative for non-invasive delivery for Pregabalin with improved drug permeation in neuropathic pain management.

PMID 42658921
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PubMedPharmaceuticals (Basel, Switzerland)2026-08-27

Possible Signals of Ocular Disorders Associated with Gabapentinoids: A Three-Arm Study.

Murray Mya M, Guirguis Amira A, Deslandes Paul P, Corkery John Martin JM et al.

Background: Gabapentinoids (gabapentin and pregabalin) are medications used to treat epilepsy and diabetic neuropathy. Reports of gabapentinoid-associated adverse drug reactions (ADRs) are increasing. This study aimed to explore these potential signals, with a focus on ocular adverse effects. Methods: A mixed-methods design was adopted, utilising quantitative and qualitative approaches encompassing: (I) a social listening approach using Reddit; (II) a pharmacovigilance retrospective disproportionality analysis study using serious reports to the FDA Adverse Event Reporting System (FAERS) (2015-2025); and (III) a literature review (2014-2025). Results: Reddit data revealed several user-reported adverse ocular effects, including blurred vision, diplopia and photosensitivity, across 78 and 40 identified reactions for gabapentin and pregabalin, respectively. Pharmacovigilance findings identified positive signals for eye disorders with both gabapentinoids compared to active control diazepam, amitriptyline and carbamazepine). Incidental findings highlighted potential discrepancies between FAERS data and undesired effects listed within the manufacturer's literature, with pregabalin exhibiting higher reporting odds than gabapentin for cataract (ROR: 4.55; 95% CI: 2.51-8.26) and blindness (ROR: 2.63; 95% CI: 1.85-3.73). The literature review reinforced eye disorder concerns, specifically retinal effects with gabapentinoids, noting the absence of robust, high-quality research. Nevertheless, it identified a plausible biological mechanism involving the CACNA2D1 receptor in retinal cells of animal models, with evidence of an effect following oral administration of pregabalin. Conclusions: This study suggests an increase in eye disorder reports associated with gabapentinoid use. Further clinical and epidemiological studies are warranted to validate these real-world signals.

PMID 42653672
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PubMedCase reports in neurological medicine2026-08-26

Probable Postsurgical Parsonage-Turner Syndrome Following Endoscopic Endonasal Pituitary Surgery: A Diagnostic Challenge Case Report: Illustrative Case.

Javidialsaadi Mousa M, Obillo Alexi A, Germanwala Alec A, Ghannad Andrew S AS et al.

Brachial neuritis is a rare inflammatory brachial plexopathy characterized by acute and severe shoulder or upper-extremity pain followed by progressive weakness and sensory disturbances. Commonly associated with viral illness, vaccination, or trauma, it can also occur as a postoperative complication. A 65-year-old gentleman presented with visual loss from a large recurrent pituitary adenoma and underwent an uncomplicated resection. Shortly after surgery, he developed swelling and pain in the right forearm and hand, which later evolved into patchy sensory loss and progressive weakness throughout the arm. Examination demonstrated proximal and distal weakness, muscle wasting, and multifocal sensory deficits without signs of cervical radiculopathy, myelopathy, or carpal tunnel syndrome. Pregabalin and gabapentin provided minimal symptom relief. Electromyography and nerve conduction studies performed 6 weeks later showed a moderate right median mononeuropathy and chronic, inactive C7 radiculopathy, findings that did not fully explain his clinical picture. The clinical presentation was most consistent with probable postsurgical Parsonage-Turner syndrome after exclusion of structural and compressive causes, and the patient improved with physical and occupational therapy, achieving near-complete recovery at 6 months. While early recognition is essential, as electrodiagnostic or radiographic studies may be nondiagnostic, timely therapy can facilitate meaningful functional recovery.

PMID 42643691
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PubMedBMJ open2026-08-25

Efficacy and safety of mirogabalin in patients with fibromyalgia: protocol for a multicentre, Prospective, Randomised, Open-label, Blinded Endpoint (PROBE) study.

Liu Minying M, Li Yanhua Y, Yao Xiugao X, Liang Yingping Y et al.

Fibromyalgia (FM) is a prevalent chronic pain condition that significantly impairs quality of life. The current treatments for FM still have some disadvantages and limitations. 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. Mirogabalin, as a novel α2δ ligand similar to pregabalin but with distinct binding properties, has shown a favourable safety profile and potential analgesic effects in preclinical studies and trials for other neuropathic pain conditions. However, data on its efficacy in FM are limited and no studies have directly compared mirogabalin with pregabalin in an Asian FM population. This is a prospective, multicentre, randomised, open-label, blinded endpoint trial to compare the efficacy and safety of mirogabalin versus pregabalin for the management of pain and other core symptoms in adult patients with FM. This study will be conducted at the Department of Pain Management, Beijing Tiantan Hospital, the First Affiliated Hospital of Nanchang University, Chongqing University Three Gorges Hospital, the First Affiliated Hospital of Army Medical University and the Affiliated Hospital of Yanbian University. Patients aged over 18 years, diagnosed with FM according to the 2016 Revisions to the 2010/2011 FM diagnostic criteria, will be enrolled. 674 qualified patients experiencing moderate-to-severe FM will be randomly assigned to either the pregabalin group or the mirogabalin group in a 1:1 ratio. Treatment will involve individualised dose titration based on treatment response and tolerability. All participants will be followed for a duration of 12 weeks. The primary outcome will be the proportion of patients achieving a pain reduction of at least 50% at 12 weeks. Secondary endpoints will include the average pain intensity, the worst pain intensity, the Revised FM Impact Questionnaire, the Brief Pain Inventory severity and interference subscales, the Short-Form 36 Health Survey, the Medical Outcomes Study Sleep Scale, the Beck Depression Inventory-II, AEs throughout the study. An open-label administration is selected to reflect real-world clinical practice and to allow individualised dose titration according to tolerability and response, while blinded endpoint assessment is implemented to minimise evaluation bias and preserve methodological rigour. This study was approved by the Institutional Review Board of Beijing Tiantan Hospital, Capital Medical University (KY2025-217-03), the First Affiliated Hospital of Nanchang University (IIT (2026) Clinical Ethics Review no. 676), Chongqing University Three Gorges Hospital (2026 Scientific Ethics Review no. 41), the Affiliated Hospital of Yanbian University (Yan Medical Ethics no. 20260275) and the First Affiliated Hospital of Army Medical University (AIIT2026081KX). All participants will provide written informed consent prior to enrolment. This study will be conducted in accordance with the Declaration of Helsinki. Findings from this study will be disseminated through peer-reviewed journals and at scientific conferences. NCT07157852.

PMID 42642082
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PubMedFrontiers in medicine2026-08-25

Comparison of common pharmacological strategies for post-photorefractive keratectomy pain management: a systematic review and network meta-analysis.

Yan Xin X, Lei Shiqi S, Yi Jiasheng J, Hu Lifen L et al.

To systematically evaluate the comparative efficacy and safety of common pharmacological strategies for managing post-photorefractive keratectomy (PRK) eye pain through a network meta-analysis, providing evidence-based guidance for clinical medication. Randomized controlled trials (RCTs) were systematically retrieved from Cochrane Library, Web of Science, PubMed, and EMbase (from inception to November 15, 2025). Using R Studio, we conducted a network meta-analysis to assess differences in Visual Analogue Scale (VAS) scores and adverse events across pharmacological interventions. SUCRA (Surface Under the Cumulative Ranking) values were calculated to determine the relative ranking of interventions, while accounting for heterogeneities in administration timing and dosage. A total of 28 studies were included, involving 2,797 patients. In route-stratified analyses, Ofloxacin (SUCRA = 0.84) and Proparacaine (0.76) were the top-ranked topical agents for analgesia, while Codeine combined with Acetaminophen (0.71) ranked highest among systemic agents. The exploratory combined network yielded identical top-three rankings, though these cross-route comparisons are susceptible to transitivity violations. Notably, effect sizes for most interventions relative to placebo spanned the line of no effect. Regarding safety, Diclofenac (SUCRA = 0.81), Ketorolac (0.70), and Nepafenac (0.53) demonstrated the optimal profiles. The highest numbers of adverse events occurred with Pregabalin (39 cases), Fentanyl (20 cases), and Codeine combined with Acetaminophen (13 cases); however, safety conclusions remain limited as only seven studies reported highly heterogeneous adverse event data. Ofloxacin demonstrates superior relative efficacy for pain control following PRK, while Diclofenac offers the most favorable safety profile. Clinicians should synthesize these comparative findings with individual patient profiles to optimize drug selection, ensuring a balanced approach between effective pain relief and minimized adverse risks. https://www.crd.york.ac.uk/PROSPERO/view/CRD420251238092, CRD420251238092.

PMID 42638662
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