Delving into the Latest Updates on Bimatoprost/Timolol Maleate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Bimatoprost and Timolol Maleate, Bimatoprost/Timolol, Ganfort

+ [6]

Target

Prostanoid receptor x β-adrenoceptors

Action

agonists, antagonists

Mechanism

Prostanoid receptor agonists, β-adrenoceptors antagonists(Beta adrenergic receptors antagonists)

Therapeutic Areas

Eye Diseases

Active Indication

Glaucoma, Open-AngleOcular Hypertension

Inactive Indication-

Originator Organization

Allergan UC

Active Organization

AbbVie Deutschland GmbH & Co. KG

Inactive Organization

Allergan UC

License Organization

Pharmaniaga Bhd.

Inter Pharma PCLZhaoke Ophthalmology Ltd.

+ [1]

Drug Highest PhaseApproved

First Approval Date

European Union (19 May 2006),

Glaucoma, Open-AngleOcular Hypertension

Regulation-

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Structure/Sequence

Molecular FormulaC25H37NO4

InChIKeyAQOKCDNYWBIDND-FTOWTWDKSA-N

CAS Registry155206-00-1

View All Structures (2)

To compare the efficacy and safety of the fixed-dose combination (FDC) of netarsudil 0.02%/latanoprost 0.005% ophthalmic solution (NET/LAT; Roclanda®) with bimatoprost 0.03%/timolol maleate 0.5% (BIM/TIM; Ganfort®) ophthalmic solution in the treatment of open-angle glaucoma (OAG) and ocular hypertension (OHT).

Methods:

MERCURY-3 was a 6-month prospective, double–masked, randomized, multicenter, active-controlled, parallel-group, non-inferiority study. Patients (≥ 18 years) with a diagnosis of OAG or OHT in both eyes that was insufficiently controlled with topical medication (IOP ≥ 17 mmHg in ≥ 1 eye and < 28 mmHg in both eyes) were included. Following washout, patients were randomized to once-daily NET/LAT or BIM/TIM for up to 6 months; efficacy was assessed at Week 2, Week 4, and Month 3; safety was evaluated for 6 months. Comparison of NET/LAT relative to BIM/TIM for mean IOP at 08:00, 10:00, and 16:00 h was assessed at Week 2, Week 6, and Month 3. Non-inferiority of NET/LAT to BIM/TIM was defined as a difference of ≤ 1.5 mmHg at all nine time points through Month 3 and ≤ 1.0 mmHg at five or more of nine time points through Month 3.

Results:

Overall, 430 patients were randomized (NET/LAT, n = 218; BIM/TIM, n = 212), and all received at least one dose of study medication. Efficacy analyses were performed at Month 3 on 388 patients (NET/LAT, n = 184; BIM/TIM, n = 204). NET/LAT demonstrated non-inferiority to BIM/TIM, with a between-treatment difference in IOP of ≤ 1.5 mmHg achieved at all time points and ≤ 1.0 mmHg at the majority of time points (six of nine) through Month 3. Mean diurnal IOP during the study ranged from 15.4 to 15.6 mmHg and 15.2 to 15.6 mmHg in the NET/LAT and BIM/TIM groups respectively, with no between-group statistically significant difference. No significant differences were observed in key secondary endpoints. No serious, treatment-related adverse events (AEs) were observed, and AEs were typically mild/moderate in severity. The most common treatment-related AEs were conjunctival hyperemia (NET/LAT, 30.7%; BIM/TIM, 9.0%) and cornea verticillata (NET/LAT, 11.0%; BIM/TIM, 0%).

Conclusions:

Once-daily NET/LAT was non-inferior to BIM/TIM in IOP reduction in OAG and OHT, with AEs consistent with previous findings. NET/LAT offers a compelling alternative FDC treatment option for OAG and OHT.

04 May 2023·Current medical research and opinion

A randomized clinical trial comparing three fixed combinations of bimatoprost with timolol in patients with open-angle glaucoma or ocular hypertension

Article

Author: Mrukwa-Kominek, Ewa ; Stalmans, Ingeborg ; Garhofer, Gerhard ; Misiuk-Hojlo, Marta ; Csutak, Adrienne

OBJECTIVE:

To compare the efficacy and safety of two fixed combination, preservative-free eye drops (bimatoprost 0.01% in combination with either timolol 0.1% or 0.5%) in a gel formulation, with bimatoprost 0.03%/timolol 0.5% in patients with open-angle glaucoma (OAG) or ocular hypertension (OHT).

METHODS:

Phase II, randomized, investigator-masked, multicenter, 3-arm parallel group (Eudract No. 2017-002823-46). Eighty-six patients aged ≥18 years with OAG or OHT, with intraocular pressure (IOP) initially controlled for at least 6 months by a combination therapy of a dual prostaglandin and timolol or insufficiently controlled by first-line monotherapy were included. Patients were randomized to receive T4030a (bimatoprost 0.01%/timolol 0.1%; N = 29), T4030c (bimatoprost 0.01%/timolol 0.5%; N = 29) or bimatoprost 0.03%/timolol 0.5% (N = 28), administered once daily in the evening for 12 weeks. Primary endpoint was defined as change in IOP from day 1 to week 12 measured at 08:00 (±1 h). Further efficacy, safety and pharmacokinetic endpoints were assessed as secondary outcomes.

RESULTS:

The mean change in IOP from baseline to week 12 was -9.8 ± 2.1 mmHg for T4030a, -10.1 ± 2.5 mmHg for T4030c and -10.0 ± 2.8 mmHg for bimatoprost 0.03%/timolol 0.5%. All treatments were well tolerated with no safety issues identified in any group. In patients treated with T4030a, the systemic concentration of timolol was significantly lower after 12 weeks than in patients treated with T4030c or bimatoprost 0.03%/timolol0.5%.

CONCLUSIONS:

These study results suggest that the preservative-free ophthalmic formulation of T4030a (bimatoprost 0.01%/timolol 0.1%) can be regarded as a useful tool in the therapeutic management of OAG and OHT.

01 Feb 2023·Ophthalmology and therapy

Safety of Fixed-Combination Bimatoprost 0.03%/Timolol 0.5% Ophthalmic Solution at 6 Months in Chinese Patients with Open-Angle Glaucoma or Ocular Hypertension

Article

Author: Yang, Jingyuan ; Duan, Xuanchu ; Goodkin, Margot L ; Xing, Xiaoli ; Liu, Qinghuai ; Chen, Michelle Y ; Yu, Minbin ; Yao, Ke ; Fang, Aiwu ; Sun, Xinghuai ; Zhang, Hong

INTRODUCTION:

Fixed-combination bimatoprost 0.03%/timolol 0.5% ophthalmic solution (FCBT; Ganfort^®, Allergan, an AbbVie company) effectively reduces intraocular pressure (IOP) via complementary mechanisms of action of the agents, but long-term (> 12 weeks) safety evaluations of FCBT remain limited. FCBT safety is evaluated herein, with particular focus on hyperemia and eyelash growth, at 24 weeks in Chinese patients with open-angle glaucoma (OAG) or ocular hypertension (OHT).

METHODS:

In this multicenter, open-label, noncomparative, phase 4 study conducted in China, patients diagnosed with OAG or OHT having insufficient response to β-blocker- or prostaglandin analogue/prostamide (PGA)-based IOP-lowering monotherapy in one or both eyes were switched from their current IOP-lowering treatment to FCBT (one drop per eye every evening) without prior washout. Assessment visits were scheduled at baseline and weeks 4, 12, and 24 (or study exit). The primary outcome measure was adverse event (AE) incidence through 24 weeks.

RESULTS:

Of 725 patients enrolled, 632 (87.2%) completed the study; 93 (12.8%) patients discontinued, including 29 (4.0%) due to AEs. Of 1326 FCBT-treated eyes (total), 594 (44.8%) experienced ≥ 1 ocular treatment-related AE during the study. Conjunctival hyperemia (the most common AE overall) and eyelash growth were reported in 269 (20.3%) and 54 (4.1%) FCBT-treated eyes, respectively. The incidence of other known PGA-related AEs (including blepharal pigmentation and erythema of eyelid) was < 10% each. Most conjunctival hyperemia reports were mild in severity (214/259; 82.6%) and only 1/259 (0.4%) was severe. Similarly, most cases of eyelash growth were mild (46/52; 88.5%); none were severe. One (< 0.1%) FCBT-treated eye had a serious ocular AE (OAG) considered FCBT-related.

CONCLUSIONS:

The frequency and severity of FCBT-related AEs, including conjunctival hyperemia and eyelash growth, are consistent with previously published findings. No new safety concerns were raised. This prospective study reaffirms that once-daily FCBT is a safe and well-tolerated therapy for OAG and OHT.

CLINICALTRIALS:

GOV IDENTIFIER:

NCT02571712.

100 Deals associated with Bimatoprost/Timolol Maleate

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External Link

KEGG	Wiki	ATC	Drug Bank
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R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Glaucoma, Open-Angle	European Union	AbbVie Deutschland GmbH & Co. KG	19 May 2006
Glaucoma, Open-Angle	Iceland	AbbVie Deutschland GmbH & Co. KG	19 May 2006
Glaucoma, Open-Angle	Liechtenstein	AbbVie Deutschland GmbH & Co. KG	19 May 2006
Glaucoma, Open-Angle	Norway	AbbVie Deutschland GmbH & Co. KG	19 May 2006
Ocular Hypertension	European Union	AbbVie Deutschland GmbH & Co. KG	19 May 2006
Ocular Hypertension	Iceland	AbbVie Deutschland GmbH & Co. KG	19 May 2006
Ocular Hypertension	Liechtenstein	AbbVie Deutschland GmbH & Co. KG	19 May 2006
Ocular Hypertension	Norway	AbbVie Deutschland GmbH & Co. KG	19 May 2006

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Glaucoma	Phase 3	United States	Allergan UC	01 Aug 2001
Glaucoma	Phase 3	Canada	Allergan UC	01 Aug 2001

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01737853 (Pubmed)	Not Applicable	Glaucoma, Open-Angle \| Ocular Hypertension	90	Fixed-combination bimatoprost/timolol	jbsabirriv(jathpwodry) = aoqczfhjjr ilqajnrqon (xlmmzjfeue ) View more	-	19 Dec 2014
				Fixed-combination dorzolamide/brimonidine/timolol	jbsabirriv(jathpwodry) = lwkrdsyymv ilqajnrqon (xlmmzjfeue ) View more
NCT01177098 (CTgov)	Phase 3	Glaucoma	561	bimatoprost /timolol formulation A fixed combination ophthalmic solution (Bimatoprost/Timolol Formulation A)	fmxvymzwdm(uuwhpiacmy) = cylcaurbll fdbhfqorup (fwwtfaheqh, 2.232) View more	-	12 Mar 2013
				bimatoprost/timolol fixed combination ophthalmic solution (Bimatoprost/Timolol Fixed Combination Ophthalmic Solution)	fmxvymzwdm(uuwhpiacmy) = mkinvnfvak fdbhfqorup (fwwtfaheqh, 2.209) View more
NCT01243567 (CTgov)	Phase 4	Glaucoma, Open-Angle	81	bimatoprost 0.03%/timolol 0.5% combination ophthalmic solution (Bimatoprost 0.03%/Timolol 0.5% Combination Ophthalmic Solution)	dripllsulf(roxwssxymv) = vdxiuidjog okxgqjbsqw (lnxsjnjllo, 3.35) View more	-	26 Feb 2013
				latanoprost 0.005% ophthalmic solution (Latanoprost 0.005% Ophthalmic Solution)	dripllsulf(roxwssxymv) = ituwharwmy okxgqjbsqw (lnxsjnjllo, 2.57) View more
NCT01068964 (CTgov)	Not Applicable	Glaucoma, Open-Angle	235	0.03% Bimatoprost/0.5% Timolol Ophthalmic Solution (0.03% Bimatoprost/0.5% Timolol in Same Bottle)	ttfmuwrwzi(tmerihsfbm) = hsjghycbuk gpjnocigih (fjqqmfhppw, 3.06) View more	-	20 Jan 2012
				0.03% Bimatoprost Ophthalmic Solution and 0.5% Timolol Ophthalmic Solution (0.03% Bimatoprost and 0.5% Timolol in Separate Bottles)	ttfmuwrwzi(tmerihsfbm) = ppywrsiufi gpjnocigih (fjqqmfhppw, 3.88) View more
NCT00486486 (Pubmed \| Br J Ophthalmol)	Phase 4	Glaucoma	60	Morning administered bimatoprost/timolol fixed combination (BTFC)	aidsjopely(tqnfqhvtwb) = fygssxzrmk ipmvfkoedz (ilwwvtlkyb ) View more	-	01 Feb 2010
				Evening administered bimatoprost/timolol fixed combination (BTFC)	aidsjopely(tqnfqhvtwb) = iewoiszgsn ipmvfkoedz (ilwwvtlkyb ) View more
NCT00486486 (ARVO2009)	Phase 4	Glaucoma	60	Morning administered bimatoprost/timolol fixed combination (BTFC)	cnmwypcbiz(immsynmpob) = qcxiocsvsq zefnqzqsbf (pqreoicwvk )	-	01 Apr 2009
				Evening administered bimatoprost/timolol fixed combination (BTFC)	cnmwypcbiz(immsynmpob) = xxckwvdfay zefnqzqsbf (pqreoicwvk )
NCT00332540 \| NCT00332072 (ARVO2007)	Phase 3	Ocular Hypertension \| Glaucoma	1,061	Bimatoprost/timolol Fixed Combination	bqgsdgdeuh(msigycvssy) = GAN, a single-bottle, fixed combination represents a convenient, therapeutic advantage over separate bottles xqxshgwshb (mrvswtrarx )	Positive	01 May 2007
				Bimatoprost