Delving into the Latest Updates on Loteprednol Etabonate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Loteprednol etabonate (JAN/USAN), Loteprednol Etabonate Ophthalmic Suspension, CDDD-5604

+ [13]

Target

GR x cPLA2α

Action

agonists

Mechanism

GR agonists(Glucocorticoid receptor agonists), cPLA2α agonists(Cytosolic phospholipase A2 agonists)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesNervous System Diseases+ [3]

Active Indication

Dry Eye SyndromesPainHerpes Zoster Ophthalmicus+ [10]

Inactive Indication

BlepharitisBlepharokeratoconjunctivitisCataract+ [8]

Originator Organization

Bausch & Lomb, Inc.

Active Organization

Bausch & Lomb, Inc.Bausch & Lomb (Australia) Pty Ltd.Alcon Laboratories, Inc.

Inactive Organization

Kala Bio, Inc.Bausch Health Americas, Inc.

W World Corp.

+ [2]

License Organization-

Drug Highest PhaseApproved

First Approval Date

United States (09 Mar 1998),

Conjunctivitis, AllergicConjunctivitisCyclitis+ [7]

Regulation-

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Structure/Sequence

Molecular FormulaC24H31ClO7

InChIKeyDMKSVUSAATWOCU-HROMYWEYSA-N

CAS Registry82034-46-6

Patients are already receiving an intravitreal injection as a standard of care, but they are consenting to receiving a loteprednol drop following the intravitreal injection. This clinical trial is studying the role of loteprednol (corticosteroid) in reducing pain following intravitreal injections for patients with age-related macular degeneration. As of now, there is no definitive pain management technique following intravitreal injections. Loteprednol is a corticosteroid widely used in ophthalmology to treat pain and inflammation, however, it has not been studied as a treatment for pain following intravitreal injections. Our overall goal is to manage pain to improve quality of care after intravitreal injections. Participants will be given either loteprednol, or artificial tears following one visit for an intravitreal injection to test how effective loteprednol is in pain reduction. Pain levels will be assessed by asking participants over the phone about their pain from a scale of 0 to 10 at three different times over a 1-week period. Artificial tear and medication usage will also be tracked over a 1-week period.

Start Date22 Dec 2022

Sponsor / Collaborator

Virginia Polytechnic Institute & State University

[+1]

CTRI/2022/07/044211

/ Not yet recruitingPhase 3

A Multicentric Randomized Double Blind Double Dummy Parallel Group Two Arm Comparative Phase III Clinical Study to Evaluate Efficacy Safety and Tolerability of Loteprednol Etabonate Ophthalmic Suspension 1% w/v of Ajanta Pharma Ltd versus Loteprednol Etabonate Ophthalmic Suspension 0.5% w/v in treatment of Post-Operative Inflammatory conditions of Eye - Phase III

Start Date25 Jul 2022

Sponsor / Collaborator

Ajanta Pharma Ltd.

NCT05136443

/ CompletedPhase 4

Prospective Analysis of Loteprednol Etabonate Ophthalmic Suspension 0.25% for Prevention of Immunologic Rejection After Descemet Membrane Endothelial Keratoplasty

The purpose of this study is to assess off-label use of loteprednol etabonate 0.25% ophthalmic suspension (Eysuvis) for prevention of immunologic rejection in the first year after Descemet membrane endothelial keratoplasty (DMEK). Topical corticosteroids have long been the mainstay for preventing and treating cornea transplant rejection although none are specifically approved for this purpose. The rates of immunologic rejection episodes and steroid-induced ocular hypertension will be compared with the respective rates observed in earlier studies with prednisolone acetate 1% suspension, loteprednol etabonate 0.5% gel, and fluorometholone 0.1% suspension after DMEK.

Start Date23 Nov 2021

Sponsor / Collaborator

Price Vision Group

[+1]

100 Clinical Results associated with Loteprednol Etabonate

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100 Translational Medicine associated with Loteprednol Etabonate

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100 Patents (Medical) associated with Loteprednol Etabonate

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354

Literatures (Medical) associated with Loteprednol Etabonate

01 Aug 2025·FOOD CHEMISTRY

Investigation into the effects of acute heat stress on stress level, meat quality, myofibrillar proteins properties and serum metabolites release of Muscovy ducks (Cairina moschata)

Article

Author: Huang, Tianran ; Xiao, Mengchao ; Huang, Jichao ; Li, Zimu ; Zhu, Zongshuai ; Huang, Ming

This study systematically investigated the effects of acute heat stress (AHS) on Muscovy ducks, focusing on plasma stress indicators, meat quality, myofibrillar proteins (MPs) properties, and serum metabolite profiles. AHS significantly elevated stress level, impairing meat quality, as evidenced by higher L* value, shear force, drip loss, and cooking loss (P < 0.05). It also induced MPs oxidation and aggregation, reflected by elevated carbonyl content, turbidity, zeta potential, and particle size. MPs structural alterations were confirmed by fluorescence quenching and increased exposure of hydrophobic groups. Correlation analysis revealed strong associations between physicochemical changes and MPs oxidation. Metabolomic analysis identified 161 and 105 differential metabolites in the CON vs. LS and CON vs. SS comparisons, respectively, involving 25 metabolic pathways related to energy, amino acids, and fatty acids. These findings provide novel insights into the molecular pathways of AHS-induced meat quality deterioration and reveal potential intervention timing for the poultry industry.

01 Jun 2025·EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Overcoming barriers in formulating practically insoluble loteprednol etabonate in ophthalmic nanoemulsion

Article

Author: Petriček, Igor ; Juretić, Marina ; Bočkor, Luka ; Krtalić, Iva ; Špoljarić, Drago ; Kocbek, Petra ; Pepić, Ivan ; Lovrić, Jasmina ; Hafner, Anita ; Ljubica, Josip ; Dukovski, Bisera Jurišić ; Kučuk, Maša Sufundžić

Loteprednol etabonate (LE) is a soft corticosteroid recently approved for the short-term treatment of signs and symptoms of dry eye disease. LE is available on the market as a suspension, which can release only limited amount of dissolved corticosteroid after application at the ocular surface. This study is focused on the development of an oil-in-water nanoemulsion (NE) to effectively deliver dissolved LE to the ocular surface, in order to promote its absorption. We newly developed an extended-throughput 3D model of the corneal epithelium for biocompatibility study, and an innovative approach to investigate the effect of biorelevant dilution on LE release from the NE oil phase. Castor oil, Capryol® 90, Kolliphor® EL and Soluplus® were selected as NE excipients based on their potential to dissolve LE. Design of experiments was successfully employed to develop biocompatible and physically stable NE with high LE content (0.15 %, w/w) and retention efficiency (87 % after 10 months of storage at room temperature). LE retention within oil droplets (above 90 % of the initial LE content) despite biorelevant dilution simulating tear turnover suggests the potential for direct LE absorption from the NE oil droplets into the lipophilic corneal epithelium. The results obtained encourage the extension of the studies in terms of in vitro permeability and in vivo eye-related bioavailability assessment to prove the potential of the proposed LE formulation.

01 May 2025·INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES

Loteprednol etabonate alleviates NLRP3 inflammasome-associated inflammatory diseases in mice by suppressing the transcription of IL-1β

Article

Author: Li, Weiling ; Fu, Zhengqi ; Huang, Weichen ; Xie, Shoufeng ; Yao, Yulin ; Wan, Pin ; Ye, Lirui ; Peng, Qian ; He, Qi ; Liu, Yuchen ; Sun, Binlian

Excessive activation of the NLRP3 inflammasome leads to cellular inflammation and tissue damage. Finding an inhibitor of its activation is urgent need for NLRP3 inflammasome-associated inflammatory diseases. In this study, we identified Loteprednol etabonate (LE), a well-known anti-inflammatory drug for ocular conditions, as a potent inhibitor of NLRP3 inflammasome activation through screening an FDA-approved drug library. In cellular models, LE significantly reduced IL-1β transcription, suppressed NLRP3 inflammasome activation, and finally inhibited the maturation and secretion of IL-1β and GSDMD-mediated pyroptosis. Mechanistic investigations showed that LE might inhibit IL-1β transcription by blocking both NF-κB and AP-1 signaling pathways. Furthermore, in mouse models of NLRP3 inflammasome-associated inflammatory diseases, including LPS-induced sepsis and DSS-induced colitis, intraperitoneal injection of LE significantly suppressed inflammatory response and improved mice survival rate. Collectively, these findings identify LE as a novel inhibitor of NLRP3 inflammasome activation, offering a promising therapeutic strategy for the treatment of NLRP3 inflammasome-associated inflammatory diseases.

49

News (Medical) associated with Loteprednol Etabonate

29 May 2025

·www.fiercepharma.com

Alcon gains first FDA prescription drug nod since Novartis split, scoring with drops for dry eye disease

Alcon has gained its first FDA nod for a prescription product since its 2019 split with Novartis, securing an approval for dry eye disease treatment Tryptyr. Six years after being spun out from Novartis and becoming a public company, eye care specialist Alcon has gained its first FDA approval for a prescription drug, scoring a nod for dry eye disease (DED) treatment Tryptyr (acoltremon ophthalmic solution).Tryptyr, which is administered as a single drop twice daily, is a first-in-class TRPM8 receptor agonist intended to activate tear production. “Tryptyr is the first eye drop that stimulates corneal nerves to directly address tear deficiency, a known cause of (DED),” Marjan Farid, M.D., professor of ophthalmology at the University of California, Irvine, said in a release.There are roughly 38 million in the U.S. who have DED. Fewer than 10% of those who have been diagnosed are being treated with a prescription product, according to Alcon.“We believe Tryptyr is an exciting new treatment option for a significant number of dry eye patients given its rapid efficacy,” David Endicott, CEO of Alcon, said in a release, adding that the approval was a “tremendous milestone” for the 80-year-old company. The company said it expects to launch Tryptyr in the third quarter.Backing the nod were two phase 3 trials that included more than 930 DED patients. In one study, 43% of patients on Tryptyr had a 10-millimeter increase in natural tear production on the Schirmer test at Day 14, compared to 8% of those on vehicle. In another study, the figures came in at 53% versus 14%, favoring the Tryptyr arm.After operating as a Novartis subsidiary for eight years, Alcon split from the Swiss pharma giant in 2019. Since then, Alcon has been on a growth splurge. In 2022, it paid $770 million to acquire Aerie Pharmaceuticals and its marketed glaucoma and ocular hypertension meds Rhopressa and Rocklatan. The company also ponied up $355 million to gain U.S. rights to Novartis’ Simbrinza, which treats the same ocular conditions. Also in 2022, Alcon gained DED treatment Eysuvis as part of a $60 million transaction with struggling Kala Pharmaceuticals.In addition, two months ago, Alcon secured a majority stake in clinical-stage company Aurion Biotech.In February, Alcon reported 2024 revenue at $9.8 billion, which was up 5% from the prior year.

Clinical ResultAcquisitionPhase 3Drug Approval

29 May 2025

·firstwordpharma.com

Alcon's dry eye treatment Tryptyr secures FDA nod

The FDA approved Alcon's Tryptyr (acoltremon) eye drops for managing dry eye disease (DED), marking the first prescription product approved for the eye care company since its spin-out from Novartis as an independent publicly traded company.“We believe Tryptyr is an exciting new treatment option for a significant number of dry eye patients given its rapid efficacy," said Alcon CEO David Endicott. Tryptyr, earlier codenamed AR-15512, entered Alcon’s portfolio in 2022 through its acquisition of Aerie Pharmaceuticals for nearly $770 million.With this approval — the first-in-class TRPM8 receptor agonist that stimulates corneal sensory nerves to rapidly increase natural tear production — gains a lead in DED therapeutics over Aldeyra’s investigational RASP modulator reproxalap rejected twice by the FDA, initially in 2023 and once again last month.Tryptyr’s approval is supported by robust clinical data from the Phase III COMET-2 and COMET-3 trials. Results showed that participants receiving Tryptyr experienced at least a 10 mm increase in natural tear production at day 14 compared with control vehicle — 42.6% versus 8.2% in COMET-2 and 53.2% versus 14.4% in COMET-3. Notably, Tryptyr demonstrated significant tear production as early as day 1, with consistent results maintained through day 90. Alcon noted that Tryptyr will be available as a 0.003% ophthalmic solution in single-dose vials for twice-daily administration. The company anticipates a US launch in the third quarter, with international market expansion plans on the cards. Earlier this month, Stifel analysts seemed optimistic about the drug’s approval but flagged concerns that may temper its launch, including transient burning or stinging side effects and mixed symptomatic results that could limit labelling, alongside growing competition in the DED space.Besides Tryptyr, other FDA-approved DED therapies include Alcon's Eysuvis (loteprednol etabonate) — bought from Kala Pharmaceuticals in 2022 and Bausch + Lomb's Xiidra (lifitegrast) — gained from Novartis a year later. Alcon also markets a range of over-the-counter dry-eye products such as Systane Dry Eye Drops and GenTeal Tears.

Clinical ResultPhase 3Drug ApprovalAcquisition

04 Apr 2025

·pharma.economictimes.indiatimes.com

US FDA declines to approve Aldeyra's eye disease drug

Bengaluru: The U.S. Food and Drug Administration has once again declined to approve Aldeyra Therapeutics treatment for dry eye disease , the company said on Thursday, sending its shares down 73% premarket. In its complete response letter, the FDA said the application for the drug, reproxalap , failed to demonstrate efficacy and requested the company to conduct at least one additional trial to show a positive effect of the treatment. This marks the second consecutive setback for reproxalap, as the drug once again faces the need for an additional trial from the FDA, following a similar request in 2023 when it failed to secure marketing approval. The health regulator's decision was based on a late-stage trial with 132 patients where the drug was tested to reduce symptoms of ocular discomfort , an unpleasant sensation in the eyes. The company said it has two ongoing trials for the drug, and plans to resubmit its marketing application mid-year, pending positive results and discussions with the FDA. Aldeyra partners with AbbVie on reproxalap with AbbVie having the option to acquire a co-exclusive license to develop, manufacture and commercialize the drug in the U.S. Dry eye disease (DED) is a condition where the eyes don't produce enough tears or poor-quality tears, leading to discomfort and potentially vision problems. Nearly 16.4 million Americans have DED, with higher prevalence in women and increasing with age, according to the National Institutes of Health. Other FDA-approved treatments for DED include Alcon's Eysuvis and Bausch + Lomb's Xiidra. (Reporting by Christy Santhosh and Padmanabhan Ananthan in Bengaluru; Editing by Vijay Kishore)

License out/inDrug ApprovalClinical Study

100 Deals associated with Loteprednol Etabonate

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External Link

KEGG	Wiki	ATC	Drug Bank
D01689	Loteprednol Etabonate	S01BA14	DB14596

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Dry Eye Syndromes	United States	Alcon Laboratories, Inc.	26 Oct 2020
Pain	United States	Bausch & Lomb, Inc.	15 Apr 2011
Herpes Zoster Ophthalmicus	China	Bausch & Lomb, Inc.	10 Jan 2007
Conjunctivitis	United States	Bausch & Lomb, Inc.	09 Mar 1998
Conjunctivitis, Allergic	United States	Bausch & Lomb, Inc.	09 Mar 1998
Cyclitis	United States	Bausch & Lomb, Inc.	09 Mar 1998
Iritis	United States	Bausch & Lomb, Inc.	09 Mar 1998
Keratitis	United States	Bausch & Lomb, Inc.	09 Mar 1998
Keratitis, Herpetic	United States	Bausch & Lomb, Inc.	09 Mar 1998
Ocular inflammation	United States	W World Corp.	09 Mar 1998
Post procedural inflammation	United States	Bausch & Lomb, Inc.	09 Mar 1998
Rosacea	United States	Bausch & Lomb, Inc.	09 Mar 1998
Seasonal allergic conjunctivitis	United States	Bausch & Lomb, Inc.	09 Mar 1998

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Kerato conjunctivitis sicca	Phase 3	United States	Kala Bio, Inc.	01 Jun 2016
Pain, Postoperative	Phase 3	United States	Kala Bio, Inc.	01 Jun 2016
Eye Infections	Phase 3	United States	Kala Bio, Inc.	01 May 2014
Cataract	Phase 3	United States	Bausch & Lomb, Inc.	01 Jun 2013
Blepharitis	Phase 3	Singapore	Bausch & Lomb, Inc.	01 Oct 2009
Blepharokeratoconjunctivitis	Phase 3	Singapore	Bausch & Lomb, Inc.	01 Oct 2009
Meibomian Gland Dysfunction	Phase 2	United States	Kala Bio, Inc.	01 Jul 2014
Postoperative Complications	Phase 1	Canada	Sandoz International GmbH	26 Apr 2018
Eye Pain	Phase 1	United States	Bausch Health Americas, Inc.	01 Feb 2015
Diabetic macular oedema	Clinical	United States	Kala Bio, Inc.	01 Jul 2014

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT05136443 (CTgov)	Phase 4	Graft Rejection \| Corneal Edema \| Iridocorneal Endothelial Syndrome	70	loteprednol etabonate 0.25% ophthalmic suspension	nstefyngdl = acznyrwtis ccexiqgvcn (jrbzhaiahx, kzstmqunlx - ozxqwvkkxl) View more	-	14 Aug 2024
NCT05136443 (Pubmed \| Cornea) Manual	Phase 4	Fuchs' Endothelial Dystrophy	70	Loteprednol Etabonate 0.25% ophthalmic suspension	opyjdfrppa(ukbqcsswsl) = hhqchcsevc aarpiduoex (wvtmifeogi ) View more	Positive	01 Aug 2024
NCT04555694 (CTgov)	Phase 4	Dry Eye Syndromes	30	Cyclosporine+loteprednol etabonate (Restasis and Lotemax)	bocqryptzf(lquynqdptr) = jgyoommyga vwopihgbmg (eunhpggpjl, 1.5) View more	-	11 Oct 2023
				Cyclosporine+Dexamethasone Ophthalmic 0.4 Mg Ophthalmic Insert (Restasis and Dextenza)	bocqryptzf(lquynqdptr) = bcvztsfehz vwopihgbmg (eunhpggpjl, 1.0) View more
NCT02120079 (CTgov)	Phase 4	Xerophthalmia	37	In Vivo Confocal Microscopy (IVCM)+Lotemax (Lotemax)	buzmdaqdhq(gvfuowgevs) = lrvdfdchsx ahbudmcpzi (foyrcmtsry, 5.13) View more	-	23 Mar 2022
				In Vivo Confocal Microscopy (IVCM)+Soothe Tired Eyes Lubricant Eye Drop (Artificial Tears) (Soothe Tired Eyes Lubricant Eye Drop (Artificial Tears))	buzmdaqdhq(gvfuowgevs) = gkmbjginzn ahbudmcpzi (foyrcmtsry, 26.09) View more
AAO2021	Not Applicable	Nummular eczema	100	Tacrolimus 0.1%	jtdochohbs(npqohknaky) = jxyilzpwjz ptmkpgmuga (londmpmopf )	-	13 Nov 2021
				Loteprednol 0.5%	jtdochohbs(npqohknaky) = vwjuwpxaxt ptmkpgmuga (londmpmopf )
ARVO2021	Not Applicable	-	-	Loteprednol Etabonate Eluting Adhesive Ocular Patch	zfjcurvbbe(uxohihpqoy) = irxwqjbxvf xinsimmtey (pfkomoupnw ) View more	-	01 Jun 2021
ARVO2021	Not Applicable	-	-	Loteprednol etabonate (submicron) ophthalmic gel 0.38%	zutxcubfxl(kepgxrdtsn) = vbnmgtzmks fbriqyxcwm (gvemzwrvgo, 1.3)	-	01 Jun 2021
				Prednisolone acetate ophthalmic suspension 1.0%	zutxcubfxl(kepgxrdtsn) = dwrqytpwmz fbriqyxcwm (gvemzwrvgo, 1.39)
NCT03616899 (STRIDE 3, CTgov)	Phase 3	Kerato conjunctivitis sicca	901	KPI-121 Ophthalmic Suspension (KPI-121 0.25% Ophthalmic Suspension)	onqebqkazi(zqzlpcsono) = eniurwoxid bnsajmwosd (ngnslueeml, 19.379) View more	-	02 Apr 2021
				Vehicle (Vehicle of KPI-121 0.25% Ophthalmic Suspension)	onqebqkazi(zqzlpcsono) = njgqilgesr bnsajmwosd (ngnslueeml, 17.579) View more
NCT02218489 (Maui, CTgov)	Phase 2	Blepharitis \| Meibomian Gland Dysfunction	206	Vehicle (Vehicle)	tgbnewmfie(vwbvwjypfd) = hgqpcpvehw disqbcbyqg (wedatlujoh, 13.8) View more	-	11 Jan 2021
				KPI-121 (KPI-121 0.25% Ophthalmic Suspension)	tgbnewmfie(vwbvwjypfd) = owufgqtnhl disqbcbyqg (wedatlujoh, 16.7) View more
NCT02188160 (Kauai, CTgov)	Phase 2	Kerato conjunctivitis sicca	150	KPI-121 (KPI-121 0.25% Ophthalmic Suspension)	mgopgtclyi(cqhsiinazc) = ttnukiqpwd orllnlpbfc (ufabinotgt, 0.633) View more	-	06 Jan 2021
				Placebo (Vehicle)	mgopgtclyi(cqhsiinazc) = jikchokmpc orllnlpbfc (ufabinotgt, 0.626) View more