Latanoprostene Bunod
(Synonyms: 拉坦前列素硝酸酯,NCX116; LBN) 目录号 : GC44039
A nitric oxide-donating FP receptor agonist
Cas No.:860005-21-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Latanoproste bunod is a nitric oxide-donating prostaglandin F2α (FP) receptor agonist that is converted to latanoprost (free acid) and nitric oxide (NO) in vivo. It induces cGMP accumulation in PC12 and HEK293 cells (EC50s = 1.6 and 9.2 μM, respectively). Topical administration of latanoprost bunod (0.036% solution) reduces intraocular pressure (IOP) in canine and rabbit models of glaucoma. It also decreases IOP in a cynomolgus monkey model of laser-induced ocular hypertension.
| Cas No. | 860005-21-6 | SDF | |
| 别名 | 拉坦前列素硝酸酯,NCX116; LBN | ||
| Canonical SMILES | O[C@@H]1[C@H](C/C=C\CCCC(OCCCCO[N+]([O-])=O)=O)[C@@H](CC[C@H](CCC2=CC=CC=C2)O)[C@H](O)C1 | ||
| 分子式 | C27H41NO8 | 分子量 | 507.6 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,Ethanol:PBS (pH 7.2) (1:2): 0.33 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9701 mL | 9.8503 mL | 19.7006 mL |
| 5 mM | 0.394 mL | 1.9701 mL | 3.9401 mL |
| 10 mM | 0.197 mL | 0.985 mL | 1.9701 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
New glaucoma medications: Latanoprostene Bunod, netarsudil, and fixed combination netarsudil-latanoprost
Eye (Lond) 2020 Jan;34(1):72-88.PMID:31695162DOI:10.1038/s41433-019-0671-0.
Reduction of intraocular pressure is the only proven method to treat glaucoma. Initial treatment of glaucoma commonly involves using anti-glaucoma medications either as monotherapy or combination therapy. Studies on aqueous humour dynamics have contributed to our understanding of aqueous outflow mechanisms that have led to the discovery of new drugs. Three new drugs (Latanoprostene Bunod 0.24%, netarsudil 0.02%, and fixed combination netarsudil 0.02% -latanoprost 0.005%) have been introduced recently in the market with novel mechanisms of action. Latanoprostene Bunod 0.024% is a nitric oxide-donating prostaglandin F2α analogue which increases the aqueous outflow both by uveoscleral and trabecular pathways. Netarsudil 0.02% is a potent Rho kinase/norepinephrine transporter inhibitor acting by increasing the trabecular outflow, decreasing the aqueous production, and possibly decreasing the episcleral venous pressure. This review highlights the role of these drugs in the management of glaucoma, with an overview of the major clinical trials on their efficacy, safety, and tolerability.
Latanoprostene Bunod 0.024% in the Treatment of Open-Angle Glaucoma and Ocular Hypertension: A Meta-Analysis
J Clin Med 2022 Jul 26;11(15):4325.PMID:35893417DOI:10.3390/jcm11154325.
Latanoprostene Bunod (LBN) 0.024%, a newly approved glaucoma eye drop, is metabolized into latanoprost acid and a nitric oxide (NO)-donating moiety, thus increasing the outflow of aqueous humor through the uveoscleral and trabecular routes, respectively. This study aimed to evaluate the intraocular pressure (IOP)-lowering effect of LBN among patients with open-angle glaucoma (OAG) and ocular hypertension (OHT). The effectiveness of LBN was also compared with timolol maleate 0.5% and latanoprost 0.005%. We searched PubMed and Embase between 1 January 2010, and 31 March 2022 and adopted only peer-reviewed clinical studies in our meta-analysis. A total of nine studies (2389 patients with OAG or OHT) assessing the IOP-reduction effect of LBN were included. Standardized mean differences (SMDs) of IOP between post-treatment time points (2 weeks, 6 weeks, 3 months, 6 months, 9 months, and 12 months) and baseline were calculated. The pooled analysis according to each time point revealed a significant IOP drop after LBN treatment (all p values for SMD < 0.05). In addition, LBN revealed a significantly stronger efficacy in decreasing IOP than timolol maleate 0.5% and latanoprost 0.005% during the follow-up period of three months. No serious side effects of LBN 0.024% were reported. Our study concluded that LBN could achieve good performance for IOP reduction in patients with OAG and OHT. The safety was favorable with no severe side effects.
Latanoprostene Bunod Ophthalmic Solution 0.024%: A Review in Open-Angle Glaucoma and Ocular Hypertension
Drugs 2018 May;78(7):773-780.PMID:29761382DOI:10.1007/s40265-018-0914-6.
Latanoprostene Bunod ophthalmic solution 0.024% (hereafter referred to as Latanoprostene Bunod 0.024%) [Vyzulta™] is a nitric oxide (NO)-donating prostaglandin F2α analogue approved in the USA for the reduction of intraocular pressure (IOP) in patients with open-angle glaucoma (OAG) or ocular hypertension. It is thought to lower IOP by increasing aqueous humour outflow through the uveoscleral pathway (mediated by latanoprost acid) and increasing the facility of aqueous humour outflow through the trabecular meshwork pathway (mediated by NO). Results from two multinational, phase III studies (APOLLO and LUNAR) and a pooled analysis of these studies demonstrated the noninferiority of Latanoprostene Bunod 0.024% to timolol ophthalmic solution 0.5% (hereafter referred to as timolol 0.5%) in terms of IOP-lowering efficacy over 3 months in patients with OAG or ocular hypertension, with the superiority of Latanoprostene Bunod 0.024% over timolol 0.5% subsequently demonstrated in APOLLO and the pooled analysis. Moreover, there was no apparent loss of IOP-lowering effect in subsequent safety extension periods of up to 9 months. The IOP-lowering efficacy seen in APOLLO and LUNAR was confirmed in a phase III study (JUPITER) in Japanese patients, with IOP reductions observed early (week 4) and maintained over the longer-term (12 months). Latanoprostene Bunod 0.024% was well tolerated over up to 12 months in these studies, with most ocular treatment-emergent adverse events (TEAEs) being mild to moderate in severity. Thus, current evidence indicates once-daily Latanoprostene Bunod 0.024% is an effective and well tolerated treatment option for the reduction of IOP in adults with OAG or ocular hypertension.
Newer advances in medical management of glaucoma
Indian J Ophthalmol 2022 Jun;70(6):1920-1930.PMID:35647957DOI:10.4103/ijo.IJO_2239_21.
The burden of irreversible vision loss from Glaucoma continues to rise. While the disease pathogenesis is not well understood, intraocular pressure (IOP) is the only modifiable risk factor identified to prevent glaucomatous vision loss. Medical management remains the first-line of treatment in most adult glaucomas and the evolution of medical therapy for glaucoma has followed an exponential curve. This review tracks the rapid development of new medications and drug delivery systems in the recent years. Introduction of Rho kinase inhibitors with an entirely new mechanism of action from that of the currently used anti glaucoma medications has been a significant milestone. Latanoprostene Bunod is a novel, single molecule which provides two active metabolites that work through two different pathways for reducing intra ocular pressure. Bimatoprost implants and travoprost punctum plugs attempt to ease chronic medication use in glaucoma patients. Nanotechnology is an evolving route of drug delivery. Role of cannabinoids in medical management of glaucoma remain equivocal. The relatively short term effect on IOP, the risks of developing tolerance and side effects impacting patients' neurocognitive health greatly outweigh the potential benefit. Research on Latrunculin B, Adenosine receptor agonists, Specific gene silencing and Stem cell therapy are poised to make an impact on glaucoma treatment. While there is some evidence to support the role of Brimonidine in neuroprotection, further research is needed to clarify the role of Memantine and Neurotrophins. Evidence for benefit from dietary supplementation with Alpha lipoic acid, Forskolin , and Ginko Biloba is limited.
Latanoprostene Bunod ophthalmic solution 0.024% for IOP lowering in glaucoma and ocular hypertension
Expert Opin Pharmacother 2017 Mar;18(4):433-444.PMID:28234563DOI:10.1080/14656566.2017.1293654.
Intraocular pressure (IOP)-lowering has been demonstrated to slow the progression or onset of visual field loss in open-angle glaucoma (OAG) or ocular hypertension (OHT). Pharmacological lowering of IOP is the most common initial intervention in patients with OAG or OHT, however, many patients will require more than one therapy to achieve target IOP. Latanoprostene Bunod is a novel nitric oxide (NO)-donating prostaglandin F2α analog for the reduction of IOP. Areas covered: Current knowledge concerning the mechanism of action of Latanoprostene Bunod is presented. Additionally, clinical safety and efficacy data from published Phase 1 (KRONUS), Phase 2 (VOYAGER, CONSTELLATION) and Phase 3 (APOLLO, LUNAR, JUPITER) studies are reviewed. Expert opinion: Latanoprostene Bunod is a dual mechanism, dual pathway molecule, consisting of latanoprost acid, which is known to enhance uveoscleral (unconventional) outflow by upregulating matrix metalloproteinase expression and remodeling of the ciliary muscle's extracellular matrix, linked to an NO-donating moiety, which enhances trabecular meshwork/Schlemm's canal (conventional) outflow by inducing cytoskeletal relaxation via the soluble guanylyl cyclase-cyclic guanosine monophosphate (sGC-cGMP) signaling pathway. Latanoprostene Bunod 0.024% solution applied topically once daily appears more effective in reducing IOP in OHT and OAG subjects than either latanoprost or timolol, with a side effect profile similar to that of latanoprost.