Application of Lenvatinib to preparation of medicine for preventing and curing macular degeneration

A technology of macular degeneration and lenvatinib, applied in the field of medicine, can solve problems such as poor curative effect and poor patient compliance

Inactive Publication Date: 2018-05-15
GUANGDONG ZHONGSHENG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to provide the use of lenvatinib in the preparation of drugs for preventing a...

Method used

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  • Application of Lenvatinib to preparation of medicine for preventing and curing macular degeneration
  • Application of Lenvatinib to preparation of medicine for preventing and curing macular degeneration
  • Application of Lenvatinib to preparation of medicine for preventing and curing macular degeneration

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1 In Vitro Cytological Experiment of Lenvatinib's Anti-Angiogenesis Ability in Fundus

[0030] Human choroidal microvascular endothelial cell HCMEC is the primary cell model for research and evaluation of fundus neovascularization. The proliferation, tube formation and migration ability of HCMEC are the pathological process of fundus neovascularization. The following three aspects prove that lenvatinib has The ability to resist neovascularization in fundus.

[0031] 1. Culture of human choroidal microvascular endothelial cells HCMEC

[0032] Human choroidal microvascular endothelial cells HCMEC are cultured in ECM medium containing 5% FBS and 1% growth factor additive ECGS. In order to ensure that the cells are in the best period of morphology and physiological characteristics, only cells within 1-7 passages are used for experiments; The above cell lines need to be added with 100 U / mL penicillin and streptomycin during the culture and experiment process, and cu...

Embodiment 2

[0045] Embodiment 2 Lenvatinib treats macular degeneration in vivo animal experiment

[0046] Based on the high-energy laser photocoagulation of the retina, the destruction of Bruch's membrane, followed by secondary damage repair reaction, inflammation, choroidal epithelial cells, pericytes, fibroblasts, inflammatory cells, etc. enter the subretinal space, forming choroidal neovascularization, that is, subretinal Based on the principle of neovascularization, a C57 mouse choroidal neovascularization model (CNV) was established to evaluate the new use of lenvatinib in the treatment of wet AMD in vivo.

[0047] Instruments and parameters: Maida 532nm argon laser treatment instrument setting parameters: laser spot diameter 50μm; exposure time: 100ms; excitation energy: 150mw.

[0048] (1) Anesthesia: 1% sodium pentobarbital (containing 20% ​​ethanol), intraperitoneal injection of 1% sodium pentobarbital according to the weight of mice at 50 mg / kg.

[0049] (2) Experiment preparat...

Embodiment 3

[0065] Embodiment 3 Lenvatinib pharmacokinetic characteristics in retina

[0066] 1. Animal and Instrument Preparation:

[0067] 25 female SD rats, weighing about 210 grams, aged 7-8 weeks, Huabukang, Beijing; UPLC / MS / MS: Shimadzu UPLC-MS8050 system; TL2010S medium-throughput tissue grinder (Beijing Dinghaoyuan Technology Co., Ltd. company)

[0068] 2. Preparation of reagent consumables:

[0069] Gastric injection needle, ether cotton ball, foam box, timer, sampling registration form (printing), experimental protocol (printing), 1.5mL EP tube (exygen), anticoagulant tube, cotton swab, dry cotton ball, disposable tablecloth, sterile Normal saline, anatomical surgical instruments, ophthalmic microscopic instruments, 75% alcohol and cotton balls, protective masks, gloves, hats, ice boxes, EP tube racks, BD tube racks, marker pens, plates, filter paper, stereoscopes, plug-in boards, Grinding steel ball 3mm specification 24X5 pieces

[0070] 3. Analysis method:

[0071] LC / MS / ...

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Abstract

The invention relates to application of Lenvatinib to preparation of medicine for preventing and curing macular degeneration, and belongs to the field of medicine. The problem that the conventional therapeutic medicine for macular degeneration is low in curative effect and low in patient compliance is solved, and the technical scheme is to provide application of Lenvatinib to preparation of medicine for preventing and curing macular degeneration. Lenvatinib is a multiple target point micromolecularly targeted inhibitor resist to VEGFR, PDGFR and bFGFR, and has been approved by FDA in the market for the treatment of tumors. The invention shows that Lenvatinib has potential for curing macular degeneration, and the application of Lenvatinib is verified by establishing an in vitro and vivo evaluation model, and the application has preferable clinic and social meanings.

Description

technical field [0001] The invention relates to the use of lenvatinib in the preparation of medicines for preventing and treating macular degeneration, which belongs to the field of medicine. Background technique [0002] Age-related macular degeneration (AMD), the onset age is over 45 years old, the older the age, the higher the incidence rate, and the disease occurs successively in both eyes. It is one of the main eye diseases of visual impairment in the elderly; it is divided into two types: atrophic type and exudative type . Atrophic (also known as "dry" or "non-exudative") AMD is mainly atrophic degeneration of the macula caused by choroidal capillary atrophy, glass membrane thickening, and RPE atrophy. Clinically divided into two stages: 1. Early stage (preatrophic stage of atrophy); 2. Late stage (atrophic stage of atrophy stage). Exudative type (also known as "wet" or "discoid") AMD, mainly new blood vessels formed by glass membrane destruction, choroidal blood ves...

Claims

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Application Information

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IPC IPC(8): A61K31/47A61P27/02
CPCA61K31/47
Inventor 杨金亮姚于勤魏仙张婷陈小新龙超峰
Owner GUANGDONG ZHONGSHENG PHARMA
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