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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

PubMedAntimicrobial agents and chemotherapy2026-07-17

Population pharmacokinetics of ritonavir-boosted atazanavir in subsequent-line treatment in African children with HIV.

van Dyk Jennie J, Waitt Catriona C, Mugerwa Henry H, Wiesner Lubbe L et al.

Ritonavir-boosted atazanavir (atazanavir/r) is an effective once-daily option for pediatric subsequent-line antiretroviral therapy when used with two nucleoside reverse transcriptase inhibitors (NRTIs). Tuberculosis co-treatment complicates its use because rifampicin markedly induces atazanavir/r clearance. Although twice-daily atazanavir/r can overcome this interaction in adults, data in children are lacking. We aimed to characterize atazanavir population pharmacokinetics in children with HIV and simulate the effect of rifampicin co-treatment. Atazanavir concentration-time data in African children with HIV from CHAPAS-4 (ISRCTN22964075) and VirTUAL (NCT03923231) were analyzed by nonlinear mixed-effect modeling. We investigated the effect of weight, age, atazanavir formulation, ritonavir dose, and NRTI backbone (tenofovir alafenamide [TAF]-emtricitabine, abacavir-lamivudine, or zidovudine-lamivudine). Simulations were performed across weight bands to evaluate atazanavir/r exposures under standard conditions and, using adult-derived induction effects, predict exposures and possible dosing regimens during rifampicin co-treatment. Seventy children were included, with a median (range) age of 10.9 (3.2-17.7) years and weight of 29 (15-85) kg. A two-compartment model with sequential zero- and first-order absorption best described atazanavir disposition. The estimated typical value of atazanavir clearance was 4.8 L/h for a 27-kg individual. Atazanavir pharmacokinetics in children were unaffected by the NRTI backbone. Once-daily atazanavir/r with current dosing guidelines achieved adequate exposures across weight bands. When simulating pharmacokinetics during rifampicin co-treatment, twice-daily atazanavir/r is expected to restore exposures to levels comparable to once-daily dosing without rifampicin. These findings provide a framework for future clinical evaluation in children with HIV and tuberculosis.

PMID 42467063
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PubMedAmerican journal of cardiovascular drugs : drugs, devices, and other interventions2026-07-17

Food Effects on the Pharmacokinetics of Single Dose and Steady-State Ralinepag, a Novel Oral Prostacyclin Agonist, in Healthy Volunteers.

Lachant Daniel D, Botta Cristian E CE, Giannakoulas George G, Patzlaff Natalie N et al.

Pulmonary arterial hypertension (PAH) is a rare, progressive disorder characterized by pathological pulmonary vascular remodeling leading to right heart failure. Ralinepag extended-release (XR), is a once-daily oral prostacyclin (IP) receptor to treat PAH. This study evaluated the safety, tolerability, and pharmacokinetics (PK) of multiple ascending doses of ralinepag XR tablets in fed and fasted healthy adult volunteers. A single-center, open-label, nonrandomized, multiple-dose titration study of two cohorts (fed (n = 13) or fasted (n = 15)) with once-daily dosing of ralinepag XR for 5 days, with up to four sequential dose escalations. Dosing began at 60 µg and escalated every 5 days as tolerated (120, 180, 240, and 300 µg). Doses were administered after a 10-h overnight fast or a moderate-fat breakfast. PK parameters assessed were maximum observed concentration (Cmax), area under the concentration-time curve from time 0 to 24 h postdose (AUC(0-24)), and time of maximum observed concentration (Tmax) on day 1 (single 60 μg dose); and Cmax, AUC(0-24), and Tmax at steady state. Ralinepag XR exhibited minimal differences in PK parameters between fed and fasted states in the first 24 h. Multiple-dose administration showed a dose-dependent increase in exposure and a median 4-10 h Tmax at steady state, independent of fed status. Ralinepag accumulation was approximately 2.1-fold after 5 days of dosing at 60 μg in both fed and fasted states, consistent with a mean half-life of 20-36 h. There were no serious adverse events attributable to ralinepag. The most commonly reported adverse events were headache, jaw pain, and nausea with no differences between groups. Food status did not significantly affect the PK or safety of ralinepag XR.

PMID 42463617
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PubMedJournal of medicinal chemistry2026-07-17

Rapid Identification of a Potent, Selective, and Orally Active p300/CBP Bromodomain Inhibitor Bearing an Imidazo[1,2-a]pyridine Scaffold via a Highly Efficient Four-Step Synthesis.

Chen Zonglong Z, Zhang Ying Y, Li Zihan Z, Shen Hui H et al.

E1A-binding protein (p300)/CREB-binding protein (CBP) bromodomains represent attractive therapeutic targets for anticancer drug development. Herein, we describe a structure-guided optimization of the lead compound UMB298 through a conformationally constrained cyclization strategy. A concise four-step synthesis (overall yield >30%), centered on a three-component reaction, was developed, enabling efficient construction of a lactam-containing imidazo[1,2-a]pyridine library for rapid screening. Among these compounds, CZL-105 emerges as a promising p300/CBP bromodomain inhibitor. It exhibits potent activity against p300 and CBP while sparing BET and demonstrates strong antiproliferative potency in OPM-2 multiple myeloma cells. Acceptable metabolic stability and pharmacokinetics support once-daily oral dosing, leading to significant tumor growth inhibition (TGI = 61%) in an OPM-2 xenograft model. These results position CZL-105 as a promising lead compound for further development. This work combines a rational design strategy and efficient chemical synthesis, accelerating the discovery of novel p300/CBP bromodomain inhibitors.

PMID 42467465
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PubMedActa ophthalmologica2026-07-17

Efficacy and safety of topical macrolides versus systemic tetracyclines for meibomian gland dysfunction-a systematic review and meta-analysis.

Safir Margarita M, Chan Clara C CC, Teichman Joshua C JC, Arbel Itamar I et al.

To review the efficacy and safety of oral doxycycline antibiotics versus topical macrolides in the treatment of meibomian gland dysfunction (MGD). Systematic review and meta-analysis. A comprehensive search of PubMed, Scopus, Embase, and ClinicalTrials.gov through December 2024 identified randomised controlled trials (RCTs) comparing oral tetracyclines with topical macrolides for MGD. Eligible studies reported outcomes related to tear film stability, meibomian gland function, ocular surface health, or symptom severity. Data extraction followed PRISMA guidelines and risk of bias was assessed using Cochrane methods. Among 3699 publications (1964-2024), six RCTs from distinct locations (374 patients) met inclusion criteria, describing only topical azithromycin and oral doxycycline. Treatment regimens were comparable: one month of topical azithromycin (1-1.5%, once to four times daily) versus three to 8 weeks of oral doxycycline (100-200 mg daily). Both treatments significantly improved MGD signs and symptoms. In pooled analyses, topical azithromycin showed superiority in reducing tear debris (odds ratio [OR], 0.33; 95% confidence interval [CI], 0.15-0.74); however, while the total symptoms score favoured azithromycin, the result was borderline (OR, 0.62; 95% CI, 0.38-1.00) and sensitivity-dependent. Subgroup analysis showed doxycycline was superior for corneal fluorescein staining (standardised mean difference [SMD], 0.64; 95% CI, 0.22-1.05), whereas 1% azithromycin was superior for tear breakup time (mean difference [MD], -1.40; 95% CI, -2.20 to -0.60) and dropout-causing adverse events (risk ratio [RR], 0.07; 95% CI, 0.01-0.49). Both topical azithromycin and oral doxycycline are effective for MGD management. Topical azithromycin demonstrated a more favourable safety profile and may represent a useful therapeutic option, particularly for patients with low tolerance to systemic medications. However, further high-quality studies are needed to strengthen the evidence base.

PMID 42464955
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PubMedCurrent medical research and opinion2026-07-17

A quarter-century of montelukast: clinical lessons for adult and pediatric asthma and allergic rhinitis care.

Redfern Jan S JS, Smith Megan A MA

Montelukast entered routine respiratory practice in the late 1990s and remains widely used for asthma, allergic rhinitis (AR), and exercise-induced bronchoconstriction (EIBC). Its continued use has been driven largely by once-daily oral administration, ease of implementation, broad indications, and perceived advantages in patients with poor adherence to or difficulty using inhaled therapies. However, over time, the role of montelukast has evolved as comparative efficacy data, long-term safety findings, and treatment guidelines have modified expectations regarding its clinical value. This review re-examines the contemporary role of montelukast via integrating evidence on its mechanism of action, comparative clinical efficacy, prescribing patterns, safety outcomes, and future directions for individualized therapy. Clinical evidence demonstrates measurable benefit across asthma, AR, and EIBC; however, treatment effects are generally modest and variable and typically inferior to inhaled corticosteroid (ICS)-based regimens or intranasal corticosteroids (INCS). Nevertheless, patients, with poor inhaler adherence, exercise-related symptoms, aspirin-exacerbated respiratory disease, concomitant AR, or preference for oral therapy, may derive clinically meaningful benefit. Post-marketing surveillance has altered the therapeutic positioning of montelukast. Recognition of infrequent, but potentially serious, neuropsychiatric adverse events culminated in strengthened regulatory warnings and more cautious prescribing practices. Current management, therefore, emphasizes patient selection, pre-treatment counseling, shared decision-making, monitoring for behavioral changes, and timely review of treatment response. Current guidelines generally position montelukast as an alternative or add-on controller rather than a preferred first-line therapy. In the future, advances in pharmacogenomics, biomarker development, and phenotype-guided treatment strategies may improve the identification of patients most likely to benefit from montelukast.

PMID 42466635
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PubMedJournal of orthopaedic trauma2026-07-17

Comparison of Early Bracing Versus Splinting for the Initial Treatment of Acute Humeral Shaft Fractures (The COBRAS Trial).

Kingery Matthew T MT, Ganta Abhishek A, Egol Kenneth A KA

To compare 2 methods of initial immobilization of closed humeral shaft fractures-coaptation splinting followed by delayed functional bracing and immediate functional bracing-with respect to pain, satisfaction, and skin-related complications during the initial 10-day post-injury period. Multicenter, randomized, two-arm, parallel clinical trial. One academic medical center with 2 Level 1 academic trauma centers and 1 tertiary care orthopaedic center. Patients with acute, closed humeral shaft fractures (AO/OTA 12A, 12B, 12C) were randomized to either initial coaptation splinting followed by delayed transition to Sarmiento bracing or immediate Sarmiento bracing. Pain intensity over time measured by a patient-reported Likert scale (numerical rating scale, 0-10) once daily at the same time during the first 10 days post-injury, skin-related complications (skin damage ranging from abrasion or blistering to full-thickness skin loss secondary to pressure from the splint or brace), analgesic consumption in morphine milligram equivalent (MME), Patient-Reported Outcomes Measurement Information System (PROMIS) Physical Function scores, and patient satisfaction. Fifty-eight patients were included in the analysis with a mean age of 48.8 ± 23.9 years (mean 50.5 years [range 18.4-92.2 years] in the coaptation splint group vs. mean 47.3 years [range 19.7-85.9 years] in the immediate Sarmiento brace group). Patients in the immediate Sarmiento bracing group reported significantly higher pain scores compared with coaptation splinting during the first 10 days postinjury (mean treatment effect = 0.97 points, 95% CI [0.26-1.69], P = 0.010; Figure 3). Cumulative opioid consumption over the 10-day period was similar between groups (median 20.0 MME for the coaptation splint group vs. 32.5 MME for the Sarmiento brace group, P = 0.308). PROMIS Physical Function scores were not significantly different between groups on postinjury day 7 (median 53.0 [IQR 44.5-68.5] for the splint group vs. 51.1 [IQR 45.0-60.5] for the brace group, P = 0.756). The rate of skin-related complications was higher in the Sarmiento brace group (33.3% vs. 7.1%, P = 0.022). Patient satisfaction scores at day 7 were not significantly different between groups (6.3 ± 2.7 for the coaptation splint group vs. 5.8 ± 3.1 for the Sarmiento brace group, P = 0.520). Immediate Sarmiento bracing was associated with increased patient-reported pain (roughly 1 point on the 0-10 numeric rating scale) and higher skin complication rates during the initial 10-day period after injury compared with initial coaptation splinting for acute humeral shaft fractures, without demonstrable benefits in function, analgesic requirements, or patient satisfaction. These findings support the traditional approach of initial coaptation splinting followed by delayed transition to functional bracing once acute swelling subsides. Therapeutic Level I. See Instructions for Authors for a complete description of levels of evidence.

PMID 42466769
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