Delving into the Latest Updates on Levobetaxolol Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(S)-betaxolol, Levobetaxolol, Levobetaxolol hydrochloride (USAN)

+ [5]

Target

β1-adrenergic receptor

Mechanism

β1-adrenergic receptor antagonists(Beta-1 adrenergic receptor antagonists)

Therapeutic Areas

Eye Diseases

Active Indication-

Inactive Indication

GlaucomaGlaucoma, Open-AngleOcular Hypertension

Originator Organization

Alcon AG

Active Organization-

Inactive Organization

Alcon Research Ltd.Alcon Pharmaceuticals Ltd.

Lee's Pharmaceutical Holdings Ltd.

Drug Highest PhaseWithdrawn

First Approval Date

US (23 Feb 2000),

Glaucoma, Open-AngleOcular Hypertension

Regulation-

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Structure

Molecular FormulaC18H30ClNO3

InChIKeyCHDPSNLJFOQTRK-LMOVPXPDSA-N

CAS Registry116209-55-3

View All Structures (2)

PURPOSETo critically discuss the randomized clinical trials (RCTs) on glaucoma medical therapy for the management of pediatric glaucoma.METHODSRCTs on glaucoma drugs carried out on pediatric subjects with ocular hypertension and glaucoma were identified through systematic searches. The methods of the RCTs and the safety and the efficacy of the glaucoma drugs were reviewed and discussed.RESULTSWe included five RCTs. One study compared dorzolamide with 0.5% timolol gel; one brinzolamide with 0.5% levobetaxolol; one 0.25% betaxolol, 0.25% timolol gel, and 0.5% timolol gel; one latanoprost with 0.5% timolol; and one travoprost with 0.5% timolol. The primary outcome was safety for two studies and efficacy for three studies. None of the RCTs was powered to detect statistically significant differences in intraocular pressure (IOP) between treatments. In total, 658 subjects received at least one dose of study medication. Beta-blockers were administered to 359 patients, carbonic anhydrase inhibitor (CAI) to 154, and prostaglandins to 145 patients. IOP-lowering efficacy ranged from 20 to 23% for CAI, from 9 to 36% for beta-blockers, and from 26 to 27% for prostaglandins. The percentage of responders was 50% for CAI, ranged from 38 to 74% for beta-blockers and from 60 to 83% for prostaglandins. Two patients receiving timolol experienced a systemic, drug-related serious adverse event (one patient bradycardia and one pneumonia). Systemic, nonserious drug-related events occurred in 15 patients randomized to beta-blockers and in 8 patients randomized to CAI. No adverse events occurred in children treated with prostaglandins.CONCLUSIONRCTs that are available on medical therapy for glaucoma are few and underpowered. The proportion of responders is lower in children; however, in subjects who are responders, the efficacy of glaucoma drugs seemed to be comparable to that in adults. As systemic adverse events have been reported, including serious events with timolol, a particular attempt to minimize the absorption of the drug (using the lowest dose and the gel formulation of beta-blockers or considering the lacrimal punctum occlusion) and a follow-up that is more frequent and more focused on safety should be considered in pediatric subjects who are on topical glaucoma medications.

01 Jan 2016·OphthalmologyQ1 · MEDICINE

Comparative Effectiveness of First-Line Medications for Primary Open-Angle Glaucoma

Q1 · MEDICINE

Review

Author: Wormald, Richard ; Lindsley, Kristina ; Hong, Hwanhee ; Shi, Qiyuan ; Dickersin, Kay ; Rouse, Benjamin ; Friedman, David S ; Li, Tianjing

TOPICPrimary open-angle glaucoma (POAG) is a highly prevalent condition worldwide and the most common cause of irreversible sight loss. The objective is to assess the comparative effectiveness of first-line medical treatments in patients with POAG or ocular hypertension through a systematic review and network meta-analysis, and to provide relative rankings of these treatments.CLINICAL RELEVANCETreatment for POAG currently relies completely on lowering the intraocular pressure (IOP). Although topical drops, lasers, and surgeries can be considered in the initial treatment of glaucoma, most patients elect to start treatment with eye drops.METHODSWe included randomized controlled trials (RCTs) that compared a single active topical medication with no treatment/placebo or another single topical medication. We searched CENTRAL, MEDLINE, EMBASE, and the Food and Drug Administration's website. Two individuals independently assessed trial eligibility, abstracted data, and assessed the risk of bias. We performed Bayesian network meta-analyses.RESULTSWe included 114 RCTs with data from 20 275 participants. The overall risk of bias of the included trials is mixed. The mean reductions (95% credible intervals) in IOP in millimeters of mercury at 3 months ordered from the most to least effective drugs were as follows: bimatoprost 5.61 (4.94; 6.29), latanoprost 4.85 (4.24; 5.46), travoprost 4.83 (4.12; 5.54), levobunolol 4.51 (3.85; 5.24), tafluprost 4.37 (2.94; 5.83), timolol 3.70 (3.16; 4.24), brimonidine 3.59 (2.89; 4.29), carteolol 3.44 (2.42; 4.46), levobetaxolol 2.56 (1.52; 3.62), apraclonidine 2.52 (0.94; 4.11), dorzolamide 2.49 (1.85; 3.13), brinzolamide 2.42 (1.62; 3.23), betaxolol 2.24 (1.59; 2.88), and unoprostone 1.91 (1.15; 2.67).CONCLUSIONSAll active first-line drugs are effective compared with placebo in reducing IOP at 3 months. Bimatoprost, latanoprost, and travoprost are among the most efficacious drugs, although the within-class differences were small and may not be clinically meaningful. All factors, including adverse effects, patient preferences, and cost, should be considered in selecting a drug for a given patient.

01 Aug 2009·ChiralityQ4 · CHEMISTRY

Application of kinetic resolution using HCS as chiral auxiliary: Novel synthesis of β‐blockers (S)‐betaxolol and (S)‐metoprolol

Q4 · CHEMISTRY

Article

Author: Xiao-Jun Wang ; Jia-Xin Zheng ; Pei Wang ; Jing-Yu Zhang ; Hong-Min Liu

AbstractOptically pure (S)‐betaxolol and (S)‐metoprolol were prepared with an extremely facile and practical method using kinetic resolution of β‐amino alcohols employing HCS as chiral auxiliary. High enantiomeric purity (ee > 99%) was achieved and the synthetic strategy is amenable to industrial scale‐up. Chirality, 2009. © 2008 Wiley‐Liss, Inc.

100 Deals associated with Levobetaxolol Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
D04710	Levobetaxolol Hydrochloride	S01	DB09351

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Glaucoma	Discovery	-	Alcon Research Ltd.	01 Jan 2003
Glaucoma, Open-Angle	Discovery	US	Alcon Pharmaceuticals Ltd.	23 Feb 2000

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00061516 (Pubmed \| J AAPOS)	Phase 3	Glaucoma	78	Brinzolamide suspension, 1%	(mybqlvhyvk) = hxjbzgjucz mikuaednii (irjqocxsmk )	-	01 Jun 2008
				Levobetaxolol suspension, 0.5%	(mybqlvhyvk) = ocpkawcxbs mikuaednii (irjqocxsmk )