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nepafenac (Ilevro)

✓ Approved

Alcon, Inc. · PTGS1 · Small Molecule

What is nepafenac?

nepafenac is a small molecule developed by Alcon, Inc.. It is approved for therapeutic indications via others.

Drug Profile

Brand NamesIlevro
CompanyAlcon, Inc.
Drug ClassSmall Molecule
Molecular TargetPTGS1, PTGS2
RouteOthers
StatusApproved
Sources: ClinicalTrials.gov, Alcon, Inc.

Mechanism of Action

Molecular Targets

nepafenac acts on 2 molecular targets:

PTGS1prostaglandin-endoperoxide synthase 1 (COX3, PCOX1)
PTGS2prostaglandin-endoperoxide synthase 2 (GRIPGHS, hCox-2)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

nepafenac is developed for 3 unique indications across 2 therapeutic areas.

Therapeutic AreaConditionPhase
Eye disordersDiabetic retinal oedema✓ Approved
Eye disordersCataract✓ Approved
Injury, poisoning and procedural complicationsProcedural pain✓ Approved

Related Research Articles

PubMedExpert review of clinical pharmacology2026-05-25

Is dose adjustment of dolutegravir necessary in Chinese adults living with HIV across different body weight levels? A population pharmacokinetics analysis.

Chen Rui R, Zhang Renfang R, Xing Ya-R YR, Wang Jiang-R JR et al.

Dolutegravir (DTG) is an integrase strand transfer inhibitor indicated for human immunodeficiency virus (HIV) infection. Although intrinsic factors show no ethnic-specific impact on DTG pharmacokinetics, extrinsic factors may modulate its pharmacokinetic profile. This study developed a population pharmacokinetic model for DTG in Chinese adults living with HIV and to identify key covariates influencing its pharmacokinetics using a nonlinear mixed-effects modeling. A total of 302 DTG concentrations from 293 Chinese patients receiving once-daily 50 mg DTG were analyzed. A one-compartment model with first-order absorption and elimination characterized the data. The estimated parameters were as follows: an absorption rate constant of 0.222 h-1, an apparent clearance of 0.843 L/h, and a volume of distribution of 9.32 L. Body weight (WT) was identified as a significant (P < 0.01) covariate influencing apparent clearance. Monte Carlo simulations indicated that under the standard 50 mg once-daily regimen, DTG exposure was comparable across the WT range of 40-100 kg. The findings may contribute to more personalized and effective treatment for Chinese adults living with HIV. In this predominantly male cohort, WT-based dose adjustment was generally not warranted among patients weighing 40-100 kg who received DTG 50 mg once daily.

PMID 42178823
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PubMedCureus2026-05-25

Safety and Tolerability of Vildagliptin 100 mg Sustained-Release Formulation in Type 2 Diabetes Mellitus: Results From a Prospective, Multicenter, Single-Arm, Post-marketing Surveillance Study.

Soni Pravin P, Sonawane Ashutosh A, Gaidhani Sandeep S, Baxi Niddhi N et al.

Management of type 2 diabetes mellitus (T2DM) often requires multiple medications and complex dosing schedules, which can compromise adherence, especially in those with multiple comorbidities. Strategies that reduce pill burden and dosing frequency may enhance patient convenience and compliance. Vildagliptin administered as a 100 mg sustained-release (SR) formulation once daily offers an alternative to the conventional 50 mg twice-daily regimen. This prospective post-marketing surveillance study evaluated the safety and tolerability of vildagliptin 100 mg SR over 24 weeks in patients with T2DM. This was a prospective, multicenter, single-arm, open-label study. Adults (≥18 years) with a clinical diagnosis of T2DM were prescribed vildagliptin 100 mg sustained-release once daily. The incidence of adverse drug reactions (ADRs) and mean changes in glycated hemoglobin (HbA1c), fasting plasma glucose (FPG), postprandial glucose (PPG), alanine aminotransferase (ALT), aspartate aminotransferase (AST), serum creatinine, serum amylase, and serum lipase were evaluated at 12 and 24 weeks. A total of 210 patients (129 males and 81 females) with a mean (SD) age of 52.63 (10.77) years were enrolled. A total of nine ADRs were reported in seven patients (3.3%), corresponding to an overall incidence of 4.3%. All events were mild in intensity, non-serious, and assessed as having a probable or likely relationship with the study drug. The mean HbA1c level decreased significantly from 7.89 at baseline to 7.27 at week 12 and 7.06 at week 24 (both p<0.001). Mean FPG levels at baseline, week 12, and week 24 were 145.92, 138.29, and 135.82 mg/dL, respectively, while the corresponding PPG levels were 201.84, 186.62, and 180.99 mg/dL, respectively. The p-values for the declines in both parameters at both time points were <0.001. There were no clinically meaningful changes (p>0.05) in AST and serum creatinine levels. The mean serum alanine aminotransferase (ALT) level decreased from 29.08 U/L to 27.76 U/L (p<0.05) at week 24. Similarly, mean serum amylase and lipase levels decreased from 59.36 U/L and 49.06 U/L to 56.50 U/L (p<0.05) and 45.38 U/L (p<0.01), respectively, at week 24. This study demonstrated that vildagliptin 100 mg SR once daily monotherapy given over 24 weeks was well tolerated and effective in patients with T2DM. It effectively controlled glycemic parameters with no significant adverse events or harmful renal or hepatic effects.

PMID 42181455
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PubMedFrontiers in medicine2026-05-25

Case Report: Successful treatment of dystrophic epidermolysis bullosa pruriginosa with upadacitinib in a patient with COL7A1, CARD14, and G6PD gene mutations.

Li Hao H, Zhang Yu Y, Lin Xuewen X, Yan Tianmeng T et al.

Dystrophic epidermolysis bullosa pruriginosa (DEB-Pr) is a rare subtype of dystrophic epidermolysis bullosa (DEB) characterized by intensely pruritic blisters, prurigo-like nodules, and scarring on the extensor aspects of the extremities. We present a 43-year-old female patient with a 30-year history of recurrent erythematous plaques, nodules, and blisters, which was accompanied by severe pruritus affecting the scalp, back, and extremities. Whole-exome sequencing identified a heterozygous likely pathogenic variant in COL7A1 (c.6760G>A, p.Gly2254Arg), a heterozygous variant of uncertain significance (VUS) in CARD14 (c.2172C>A, p.Tyr724*), and a heterozygous pathogenic variant in G6PD (c.1388G>A, p.Arg463His). Combined with the patient's clinical manifestations, histopathological findings, direct immunofluorescence results, negative results for pemphigus and pemphigoid autoantibodies, genetic testing results, and past medical history, the patient was diagnosed with refractory DEB-Pr and glucose-6-phosphate dehydrogenase (G6PD) deficiency. To the best of our knowledge, the co-occurrence of these three distinct variants in a patient with DEB-Pr has not been previously reported in the literature. Oral upadacitinib (initiated at 15 mg once daily) induced rapid and substantial relief of pruritus as well as improvement of cutaneous lesions. Clinical symptoms continued to improve during subsequent gradual dose tapering, and maintenance therapy with 15 mg once weekly has been administered since month 16 of treatment, with a 7-month follow-up to date. No treatment-related adverse events were observed throughout the entire 22-month follow-up period. This case suggests that Janus kinase (JAK) inhibitors may represent a feasible therapeutic option for patients with similar refractory DEB-Pr.

PMID 42180729
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PubMedJournal of orthopaedic translation2026-05-25

Efficacy of once-weekly teriparatide versus alendronate in Chinese postmenopausal osteoporosis: a randomised, open-label, active-controlled, 48-week, multicentre phase III study.

Gu Jiemei J, Chao Aijun A, Huo Yanan Y, Zhang Yawei Y et al.

This randomised controlled trial assessed the effectiveness and safety of weekly 56.5 μg teriparatide (SAL056) compared to alendronate in postmenopausal women in China with osteoporosis at high risk of fractures over 48 weeks. This phase 3, multicentre, randomised, open-label, active-controlled, parallel-group, non-inferiority trial enrolled postmenopausal women aged 45-80 years with osteoporosis at 37 centres in China. Participants were randomised (1:1) to receive either subcutaneous teriparatide 56.5 μg weekly or 70 mg oral alendronate weekly for 48 weeks, with the primary efficacy assessment at Week 48. Between November 2021 and September 2023, 493 patients were enrolled (243 in the teriparatide group and 250 in the alendronate group). The primary endpoint, lumbar spine bone mineral density (BMD) at L1-L4, showed a significantly greater increase in the teriparatide group compared to the alendronate group at Week 48 (5.01% vs. 4.20%, mean difference 0.80%, P = 0.025). Sensitivity analysis confirmed these results. At Weeks 24 and 48, teriparatide also resulted in higher hip BMD than alendronate (1.50% vs. 1.46%, P > 0.05 and 3.27% vs. 1.67%, P < 0.001). Procollagen type 1 N-terminal propeptide (P1NP) levels in the teriparatide group increased transiently at Week 12, then declined toward baseline by Weeks 24 and 48, and a decrease in serum cross-linked c-terminal telopeptide of type I collagen (S-CTX) levels from baseline to the end of treatment. Meanwhile, in the alendronate (a typical bone resorption inhibitor) group, CTX level remained continuously suppressed from the baseline. Clinical fracture rates were lower in the teriparatide group than in the alendronate group at Weeks 24 (1.2% vs. 2.8%, P > 0.05) and 48 (1.7% vs. 4.0%, P > 0.05). Teriparatide was generally safe and well tolerated. Teriparatide (56.5 μg once weekly) was more effective than alendronate in treating postmenopausal osteoporosis with a high fracture risk, significantly increasing L1-L4 BMD over 48 weeks. It was safe, well tolerated, and had a safety profile similar to that of Teribone®. This study demonstrates that once-weekly teriparatide significantly improves bone mineral density and reduces fracture risk in postmenopausal osteoporosis patients. As a patient-friendly alternative to daily injections, it may enhance adherence and inform clinical guidelines, representing a promising strategy for patients and healthcare systems.

PMID 42182073
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PubMedFrontiers in oncology2026-05-25

Sequential almonertinib therapy following osimertinib-induced interstitial lung disease in early-stage EGFR-mutant lung adenocarcinoma: a case report.

Zhang Jianbin J, Huang Sishi S, Shen Hui H

Osimertinib is the standard adjuvant therapy for resected epidermal growth factor receptor (EGFR)-mutant non-small cell lung cancer (NSCLC). However, its use is limited by osimertinib-induced interstitial lung disease (Osi-ILD). We describe the case of a 62-year-old woman with resected stage IIB (pT1cN1M0) EGFR L858R-mutant lung adenocarcinoma who developed grade 2 Osi-ILD, characterized by new bilateral ground-glass opacities on high-resolution computed tomography (HRCT), after 3 months of adjuvant osimertinib therapy. Osimertinib was immediately discontinued, leading to complete symptomatic and radiographic resolution within 8 weeks without corticosteroid therapy. Given the high risk of ILD recurrence upon rechallenge and the suboptimal efficacy of chemotherapy, a multidisciplinary team consensus recommended switching to almonertinib (110 mg once daily). Remarkably, the patient has maintained disease-free survival without ILD relapse for 36 months. This case provides clinical evidence that switching to almonertinib may represent a viable and safe therapeutic strategy, thereby addressing a critical unmet need in the management of resected early-stage EGFR-mutant NSCLC after Osi-ILD.

PMID 42180063
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PubMedACS omega2026-05-25

Supraphysiological Doses of Vitamin A Promote Changes in Hippocampal Oscillation Bands and Cardiac Activity in Wistar Rats.

Hartcopff Priscille Fidelis Pacheco PFP, Lins Axell A, de Araujo Daniella Bastos DB, Barbosa Gabriela Brito GB et al.

Vitamin A is an essential micronutrient involved in growth, immune regulation, and central nervous system function; however, excessive intake may disrupt systemic homeostasis. This study investigated the electrophysiological effects of experimental hypervitaminosis A on hippocampal activity and cardiac function in male Wistar rats. Animals received a supraphysiological dose of vitamin A (50,000 IU/kg, intraperitoneally) once daily for 3, 7, or 14 days. Serum calcium levels were quantified, and electrophysiological recordings were obtained from the CA1 hippocampal region (EEG) and through electrocardiography (ECG). Vitamin A administration produced a time-dependent increase in total hippocampal spectral power. Power elevations were observed across multiple frequency bands, particularly theta (4-8 Hz), α (8-12 Hz), β (12-28 Hz), and γ (28-40 Hz) oscillations after 7 and 14 days of exposure. Serum calcium levels showed modest increases but remained within physiological reference ranges. Cardiac assessment revealed increased heart rate accompanied by reductions in R-R and QT intervals while maintaining sinus rhythm and preserved ECG morphology. These findings demonstrate that short-term exposure to supraphysiological vitamin A levels alters hippocampal oscillatory dynamics and modulates cardiac electrophysiological parameters in rats. Although the functional and mechanistic implications require further investigation, the results indicate that excessive vitamin A intake can influence neurocardiac electrophysiological homeostasis even in the absence of overt hypercalcemia.

PMID 42179620
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