预约演示
更新于：2025-12-25
Ambroxol Hydrochloride
盐酸氨溴索
更新于：2025-12-25
概要
基本信息
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、优先审评 (中国) |
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结构/序列
分子式C13H19Br2ClN2O |
InChIKeyQNVKOSLOVOTXKF-PFWPSKEQSA-N |
CAS号23828-92-4 |
关联
141
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100 项与 盐酸氨溴索 相关的临床结果
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100 项与 盐酸氨溴索 相关的转化医学
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100 项与 盐酸氨溴索 相关的专利（医药）
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1,290
项与 盐酸氨溴索 相关的文献（医药）2026-12-01MAMMALIAN GENOME
The use of genistein and ambroxol may be an effective approach in correcting cellular dysfunctions of mucopolysaccharidosis-plus syndrome
Article
作者: Rintz, Estera ; Węgrzyn, Grzegorz ; Cyske, Zuzanna ; Pierzynowska, Karolina ; Gaffke, Lidia
Mucopolysaccharidosis-plus syndrome (MPS plus or MPSPS) is an ultrarare inherited metabolic disease, caused by mutations in the VPS33A gene. Like in different types of mucopolysaccharidosis (MPS), glycosaminoglycan (GAG) storage in cells of patients is evident. However, unlike MPS, the genetic defects in MPSPS cause impairment in the VPS33A protein level rather than inactivation of lysosomal hydrolases responsible for GAG degradation. Recent works demonstrated that low abundance of mutated VPS33A causes defective endosomal trafficking, resulting in poor delivery of GAGs (and perhaps also other compounds) to lysosomes, preventing their effective turnover. Here, we tested the hypothesis that impairment of protein degradation machineries, proteasomes by genistein (5,7-dihydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-one) and endoplasmic-reticulum-associated protein degradation (ERAD) by ambroxol (4-((2-amino-3,5-dibromophenyl)methylamino) cyclohexan-1-ol), might result in elevation of levels of the mutated, partially active VPS33A and improvement of cellular functions. Using a line of MPSPS patient-derived fibroblasts, we demonstrated that treatment with genistein and ambroxol resulted in elevation of the mutant VPS33A protein level, as well as in improvement or correction of various previously reported cellular defects, including GAG levels, endosomal markers, and cytoskeleton elements. In the light of these results, and since both genistein and ambroxol were previously demonstrated to be safe when used in relatively high amounts, we suggest that the use of these compounds, and especially their combination, might be considered as a potential therapeutic approach in MPSPS, which is currently an incurable disease.
2026-01-01MOLECULAR NEUROBIOLOGY
Ambroxol’s Role in PTZ-Induced Anxiety-Like Conditions in Mice: Targeting Neuroinflammation and Oxidative Stress via In Vivo and In Silico Approaches
Article
作者: Siraj, Sami ; Muhammad, Hafsah ; Ali, Hafeeza Zafar ; Ikram, Muhammad ; Zakria, Muhammad ; Shah, Fawad Ali ; Khan, Manzoor ; Khan, Ashraf Ullah ; Ilahi, Laila ; Ullah, Najeeb ; Jahan, Sarwat
Anxiety disorders are major neuropsychiatric conditions linked to oxidative stress, neuroinflammation, and dysregulated neurotransmission. Current pharmacotherapies, such as benzodiazepines, offer symptomatic relief but are limited by tolerance and sedation. Ambroxol, a clinically established mucolytic agent, has demonstrated neuroprotective, anti-inflammatory, and antioxidant activities, suggesting potential therapeutic repurposing for neuropsychiatric disorders. The present study evaluated the anxiolytic and neuroprotective effects of ambroxol in a pentylenetetrazol (PTZ)-induced anxiety model in mice, supported by molecular docking and molecular dynamics analyses, showing moderate but significant interactions. Mice received ambroxol (60 mg/kg, p.o.) for 21 days, while diazepam (2 mg/kg, i.p.) served as the reference control for 14 days. Behavioral assessments were performed using the elevated plus maze, open field, light-dark box, and hole board tests. Biochemical analysis of prefrontal cortical tissue was conducted to evaluate oxidative stress and pro-inflammatory markers (MDA, SOD, CAT, GSH, TNF-α, IL-1β, NF-κB). Ambroxol significantly improved exploratory and anxiety-related behaviors, restored antioxidant enzyme activities, and suppressed cytokine levels in the prefrontal cortex. Docking and simulation studies revealed stable, biologically relevant interactions of ambroxol with TNF-α, IL-1β, and NF-κB, suggesting modulation of neuroimmune signaling. Ambroxol exhibited anxiolytic efficacy comparable to diazepam, with no apparent sedative effects observed behaviorally, although direct assessment of sedation (e.g., rotarod test) was not performed. Ambroxol demonstrated promising multi-target neuroprotective potential by concurrently attenuating oxidative and inflammatory cascades, supporting its further exploration as a safe, repurposed therapeutic candidate for anxiety disorders.
2025-12-01JOURNAL OF PAIN
Nav1.8, TRPV1 and TRPA1 as possible targets of ambroxol when used for topical treatment of neuropathic pain
Article
作者: Hage, Axel ; Pantke, Sebastian ; Leffler, Andreas ; Hefner, Stefanie ; Oprita, George
Sodium channels and the capsaicin receptor TRPV1 in epidermal sensory nerve endings are established targets for topical treatment of neuropathic pain. The secretolytic ambroxol induces effective topically analgesia, a property that may involve a preferential block of Nav1.8. We here examined to what extent ambroxol inhibits human and rat (r) Nav1.8, but also the human (h) orthologues of the irritant receptors TRPV1 and TRPA1 by performing whole-cell patch clamp recordings. Ambroxol-induced tonic inhibition was stronger on rNav1.8 (IC50 18 µM) than on hNav1.8 (IC50 279 µM) and TTX-sensitive Na+ channels (IC50 76 µM). Non-inactivating currents of both hNav1.8 and rNav1.8 displayed a higher sensitivity to ambroxol than transient currents. A weak but concentration-dependent activation of hTRPV1 and hTRPA1 exceeded an unspecific increase in intracellular calcium by high concentrations of ambroxol. While the activation mechanism for hTRPV1 involves the vanilloid-binding domain, residues required for menthol-sensitivity of hTRPA1 seems to dictate ambroxol-sensitivity. Ambroxol also inhibited capsaicin-induced currents on hTRPV1 in a concentration-dependent and partly reversible manner. This inhibition was independent of intracellular calcium and preserved on the non-desensitizing mutant hTRPV1-Y672K. Currents induced by mustard oil or carvacrol on hTRPA1 exhibited a concentration-dependent reduction by ambroxol that was stronger on outward as compared to inward currents. We conclude that inhibition of Nav1.8 by ambroxol exhibits a pronounced species-specificity with rNav1.8 > hNav1.8. Furthermore, high concentrations of ambroxol modulate hTRPV1 and hTRPA1 in a manner that might contribute to topical analgesia. PERSPECTIVE: Topically applied ambroxol is a well-known off the label approach for treatment of focal neuropathic pain, but it still lacks a mechanistic foundation. This in vitro study presents human Nav1.8, TRPA1 and TRPV1 as possible pharmacological targets of ambroxol in sensory neurons.
100 项与 盐酸氨溴索 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 慢性鼻窦炎 | 日本 | 1993-03-03 | |
| 排痰困难 | 日本 | 1991-11-29 | |
| 急性支气管炎 | 日本 | 1986-02-13 | |
| 哮喘 | 日本 | 1986-02-13 | |
| 支气管扩张 | 日本 | 1983-05-27 | |
| 慢性支气管炎 | 日本 | 1983-05-27 | |
| 尘肺病 | 日本 | 1983-05-27 | |
| 肺结核 | 日本 | 1983-05-27 | |
| 新生儿呼吸窘迫综合征 | 中国 | - |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 呼吸系统疾病 | 申请上市 | 中国 | 2022-05-10 | |
| 呼吸系统疾病 | 申请上市 | 中国 | 2022-05-10 | |
| 帕金森病 | 临床3期 | 英国 | 2025-02-25 | |
| 急性呼吸道疾病 | 临床3期 | 中国 | 2022-09-01 | |
| 急性呼吸道疾病 | 临床3期 | 中国 | 2022-09-01 | |
| 慢性呼吸道疾病 | 临床3期 | 中国 | 2022-09-01 | |
| 慢性呼吸道疾病 | 临床3期 | 中国 | 2022-09-01 | |
| 肺炎 | 临床3期 | 中国 | 2022-09-01 | |
| 肺炎 | 临床3期 | 中国 | 2022-09-01 | |
| 支气管肺病 | 临床3期 | 中国 | 2018-07-26 |
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临床结果
临床结果
适应症
分期
评价
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临床2期 | 非典型进行性核上性麻痹 beta-Glucocerebrosidase (GCase; GBA) | - | 網鹹糧簾構醖壓築膚襯(夢簾簾艱鹽鹽糧壓壓觸) = 選艱網醖觸觸夢窪範糧 構鹹壓網製鬱襯範窪壓 (觸糧艱廠選顧壓糧齋蓋, 4.8) | 积极 | 2023-08-27 | ||
Placebo | 網鹹糧簾構醖壓築膚襯(夢簾簾艱鹽鹽糧壓壓觸) = 遞範鹹願醖鹽膚醖鑰夢 構鹹壓網製鬱襯範窪壓 (觸糧艱廠選顧壓糧齋蓋, 2.5) | ||||||
N/A | - | 4,025 | 夢網鬱繭繭醖醖簾構顧(憲廠鑰齋衊觸鹹製顧窪) = 壓廠膚鬱廠窪廠鹹製鹽 繭餘獵襯廠膚壓製餘鏇 (壓夢範夢糧襯鑰獵築顧 ) 更多 | - | 2022-10-20 | ||
N-Acetylcysteine | 夢網鬱繭繭醖醖簾構顧(憲廠鑰齋衊觸鹹製顧窪) = 築壓顧鏇鏇醖窪齋選糧 繭餘獵襯廠膚壓製餘鏇 (壓夢範夢糧襯鑰獵築顧 ) 更多 | ||||||
临床2期 | 24 | (Patients with Parkinson Disease with GBA1 mutations) | 範繭觸餘顧鏇鏇憲醖簾(廠繭鏇製鑰範艱襯夢製) = 廠願淵膚窪壓鹹獵艱構 醖廠鑰顧鹽範構衊觸襯 (蓋繭遞夢廠壓網鑰積鏇, 40) 更多 | - | 2020-04-01 | ||
(Patients with Parkinson Disease without GBA1 mutations) | 範繭觸餘顧鏇鏇憲醖簾(廠繭鏇製鑰範艱襯夢製) = 壓網衊憲蓋築鹽襯積鬱 醖廠鑰顧鹽範構衊觸襯 (蓋繭遞夢廠壓網鑰積鏇, 40) 更多 | ||||||
临床3期 | 390 | Ambroxol Hard-Boiled Lozenges | 鹹鬱廠製顧齋遞淵繭衊(獵繭構觸築淵選觸簾憲) = 蓋齋糧鏇鏇願選獵獵鬱 鏇積齋網憲願襯餘鏇衊 (廠繭糧構製範蓋襯簾鹹, 0.259) 更多 | 不佳 | 2019-12-01 | ||
Placebo | 鹹鬱廠製顧齋遞淵繭衊(獵繭構觸築淵選觸簾憲) = 壓糧鹹鹽壓蓋鏇積襯襯 鏇積齋網憲願襯餘鏇衊 (廠繭糧構製範蓋襯簾鹹, 0.243) 更多 | ||||||
临床3期 | 249 | (Ambroxol Lozenges 20 mg) | 鏇膚膚構網選淵範醖襯(膚簾選廠膚獵衊製網壓) = 觸選鹽製遞襯願襯鹽壓 鹹憲蓋淵網製艱積築齋 (選鏇醖夢願鏇艱構築蓋, 0.020) 更多 | - | 2019-07-11 | ||
Placebo+Ambroxol (Placebo) | 鏇膚膚構網選淵範醖襯(膚簾選廠膚獵衊製網壓) = 選鹹構顧衊壓醖憲壓夢 鹹憲蓋淵網製艱積築齋 (選鏇醖夢願鏇艱構築蓋, 0.020) 更多 | ||||||
临床1期 | - | - | (Mucosolvan ® Adult Syrup) | 鏇襯獵襯鹽艱齋製壓鑰(繭衊憲範網憲鏇淵膚餘) = 築鹽願構網憲積蓋鏇醖 鑰窪鏇壓鬱餘獵艱糧夢 (廠獵憲顧築繭廠餘製齋, 30.38) 更多 | - | 2015-12-31 | |
(Ambroxol Hydrochloride Soft Pastille) | 鏇襯獵襯鹽艱齋製壓鑰(繭衊憲範網憲鏇淵膚餘) = 夢繭繭選願繭築齋鹽範 鑰窪鏇壓鬱餘獵艱糧夢 (廠獵憲顧築繭廠餘製齋, 28.62) 更多 | ||||||
临床1期 | - | 24 | (Lasolvan 75mg) | 獵壓繭簾構構簾鏇構憲(繭餘鹽範憲壓遞衊構獵) = 壓醖艱淵顧餘憲構糧製 鏇選顧製範築製齋遞鏇 (鬱壓選積艱膚艱願憲鏇, 28.859) 更多 | - | 2015-05-13 | |
(Lasolvan 60mg) | 獵壓繭簾構構簾鏇構憲(繭餘鹽範憲壓遞衊構獵) = 顧齋願鹽製夢顧廠積壓 鏇選顧製範築製齋遞鏇 (鬱壓選積艱膚艱願憲鏇, 28.292) 更多 |
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