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更新于：2026-04-02
Amphotericin B
两性霉素B
更新于：2026-04-02
概要
基本信息
药物类型 小分子化药 |
别名 AmB、SinuNase、CM001 + [15] |
作用方式 调节剂 |
作用机制 Ergosterol 调节剂(麦角固醇 调节剂) |
非在研适应症 |
最高研发阶段批准上市 |
首次获批日期 (1958-01-01), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、合格传染病产品 (美国)、孤儿药 (欧盟)、快速通道 (美国) |
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结构/序列
分子式C47H73NO17 |
InChIKeyAPKFDSVGJQXUKY-INPOYWNPSA-N |
CAS号1397-89-3 |
关联
139
项与 两性霉素B 相关的临床试验NCT06525389
Liposomal Amphotericin B and Flucytosine Antifungal Strategy for Talaromycosis (LAmB-FAST)
CTIS2025-523501-15-00
A Phase 2, monocentric, prospective, nonrandomized, open-label, experimental study to evaluate efficacy and safety of intrabronchial instillation of liposomal Amphotericin B in patients with simple pulmonary aspergilloma.
NCT07300553
Impact Of The Gut Microbiota On Host Cells Energy Metabolism in Health And In Inflammatory Bowel Disease
100 项与 两性霉素B 相关的临床结果
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100 项与 两性霉素B 相关的转化医学
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100 项与 两性霉素B 相关的专利（医药）
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20,571
项与 两性霉素B 相关的文献（医药）2026-12-31Virulence
The cyclin dependent kinase (CDK)7 inhibitor BS-181 inhibits pathogenic Cryptococcus species, causing G
2
/M arrest and a splicing defect
Article
作者: Bowring, Bethany ; Hewitt, Kim ; Chen, Sharon C-A ; Halliday, Catriona L ; Sethiya, Pooja ; Dinh, Hue ; Djordjevic, Julianne Teresa ; Parsania, Chirag ; Cain, Amy K ; Desmarini, Desmarini
The fungal priority pathogen and basidiomycete, Cryptococcus neoformans (Cn), causes lung and brain infection in predominantly immuno-compromised individuals and there is an urgent need for new treatment options. The pyrazolopyrimidine-based cyclin dependent kinase (CDK)7 inhibitor, BS-181, has anticancer properties, but its antifungal activity has not been investigated. We show that cryptococcal CDK7 more closely resembles the human enzyme than that of ascomycetes, and that BS-181 inhibits its activity. BS-181 inhibited growth of both Cn and Cryptococcus gattii (Cg), but not ascomycete fungi and delayed progression through the G2/M phase of the cell cycle. Transcriptomic analysis revealed that BS-181 induces splicing defects leading to elevated intron retention within the transcriptome and also suppresses translational processes. BS-181 displayed additive or synergistic activity with licensed antifungals against laboratory and clinical Cn and Cg strains, most notably with amphotericin B where synergy (2-4-fold reduction in the amphotericin B MIC) was achieved using low-sub micromolar concentrations of BS-181. Compared with either drug alone, BS-181-AmB combination therapy provided greater protection against Cn infection in a wax moth model (p ≤ 0.032) and extended survival of Cn-infected mice. These findings demonstrate that CDK7 inhibitors, already of interest as anticancer agents, could be repurposed to prevent or treat opportunistic fungal infections in cancer patients when combined with licensed antifungals limited by either toxicity or resistance.
2026-10-01PARASITOLOGY INTERNATIONAL
Therapeutic efficacy of a novel immunotherapeutic formulation, combining a multi-epitope chimeric protein and Amphotericin B, in murine L. infantum infection
Article
作者: Moreira, Gabriel José Lucas ; Campos, Júlia Kelly ; Coelho, Eduardo Antonio Ferraz ; de Souza Dutra, Gabrielle Caroline ; Lage, Daniela Pagliara ; Roatt, Bruno Mendes ; Costa, Scarleth Silva ; Moura E Souza, Ana Clara ; Carvalho, Ana Maria Ravena Severino ; de Ávila, Ricardo Andrez Machado ; Eleutério, Níbia Mariana ; Souza, Thiago Miranda ; Dos Reis Cruz, Luiza ; Duarte, Mariana Costa ; Fernandes, Ana Paula Salles Moura ; Ribeiro, Naianda Rezende ; Menezes-Souza, Daniel
Leishmaniasis is a vector-borne parasitic disease caused by Leishmania protozoa. First-line treatment with pentavalent antimonials faces increasing resistance and significant toxicity. Amphotericin B is an effective second-line alternative but is also toxic and complex to administer, with a safer but expensive liposomal formulation. This study evaluated an immunotherapeutic approach using a chimeric protein composed of multiple T-cell epitopes from Leishmania (L.) infantum, combined with the adjuvant Monophosphoryl Lipid A (MPLA), in a murine model of VL. Our findings demonstrate that the combined rChi+MPLA/Amp-B therapy significantly outperformed monotherapies, inducing a robust TH1-polarized immune response. Splenocytes from this group exhibited markedly higher levels of TNF in both CD4+ (SC/CC = 1.64) and CD8+ T cells (SC/CC = 1.93) compared to Saline, MPLA, and rChi controls (p < 0.05). Furthermore, the combination therapy achieved a significantly higher IFN-γ/IL-10 ratio in CD4+ cells (Ratio = 2.03) compared to Saline, MPLA, and rChi groups (p < 0.05), indicating a shift away from the immunosuppressive environment characterized by high IL-10 levels in untreated Saline controls (SC/CC = 1.58). This protective environment was further corroborated by a marked elevation in nitric oxide (NO) levels in the rChi+MPLA/Amp-B group compared to all other experimental groups (p < 0.05). This potent immune activation correlated with a drastic reduction in parasite load. The rChi+MPLA/Amp-B group achieved statistically significant reductions (p < 0.05) of 98.4% in the lymph nodes, 99.1% in the spleen, and 97.8% in the liver compared to the Saline group. These reductions were also significantly superior (p < 0.05) to those observed in animals treated with Amp-B alone (82.1%, 89.3%, and 79.4%) or rChi+MPLA alone (75.2%, 68.5%, and 72.1%) in the lymph nodes, spleen, and liver, respectively. These results highlight the potential of the rChi+MPLA/Amp-B formulation as a highly effective immunotherapeutic strategy to enhance conventional chemotherapy and improve the clinical management of VL.
2026-05-01PATHOLOGY RESEARCH AND PRACTICE
Modulation of AKT/GSK-3β signaling by ambrisentan alleviates chronic kidney disease
Article
作者: Gaikwad, Anil Bhanudas ; Bhadange, Rohan
Chronic kidney disease (CKD) is a progressive disease leading to severe health complications. Repurposing of existing drugs offers an attractive avenue for advancing drug development in CKD. Ambrisentan (AMB), a selective ET-1A receptor antagonist used in pulmonary arterial hypertension, holds promise in CKD management. Hence, we aimed to investigate the potential of AMB in unilateral ureteral obstruction (UUO)-induced kidney fibrosis in Sprague-Dawley rats and in recombinant human-transforming growth factor-β1 (rh-TGF-β1)-induced fibrosis in NRK-52E cells. Animals were randomly assigned to the sham, UUO, and UUO + AMB (0.5 mg/kg, p.o., o.d.) groups for 21 days. Animals were sacrificed post-treatment, and plasma, urine, and kidney specimens were collected for biochemistry, histology, immunohistochemistry and qRT-PCR. Moreover, NRK-52E cells were exposed to AMB (100 µM) for 48 h and cell samples were collected for cell viability, morphology, immunocytochemistry, immunoblotting, and flow cytometry assays. AMB treatment significantly improves the left kidney weight, kidney mass ratio, kidney function parameters, and plasma protein levels of TGF-β1 and collagen I. Histopathology revealed that AMB treatment significantly preserved kidney histoarchitecture and interstitial fibrosis in UUO kidneys. Mechanistically, AMB suppressed phosphorylation of AKT and GSK-3β, downregulated α-SMA, vimentin and restored E-cadherin expression as shown by immunocytochemistry, immunohistochemistry and immunoblotting assay. Furthermore, AMB mitigated rh-TGF-β1-induced apoptosis, as assessed by flow cytometry, and modulated Bax, Bcl-2, and cleaved caspase-3 expression, as revealed by qRT-PCR and immunohistochemistry. Collectively, the findings indicate that the AMB modulates the AKT/GSK-3β axis, halting fibrotic progression in CKD, suggesting its clinical potential.
100 项与 两性霉素B 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 |
|---|---|---|---|
| 利什曼病 | 日本 | 2009-06-17 | |
| 粒细胞减少性发热 | 日本 | 2006-04-20 | |
| 念珠菌病 | 日本 | 1997-01-31 | |
| 侵袭性真菌感染 | 日本 | 1963-04-18 | |
| 真菌病 | - | 1958-01-01 | |
| 复杂的尿路感染 | 中国 | - | - |
| 细菌性心内膜炎 | 中国 | - | - |
| 脑膜炎 | 中国 | - | - |
| 脓毒症 | 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 |
|---|---|---|---|---|
| 隐球菌脑膜炎 | 临床3期 | - | 2023-01-01 | |
| 肺部疾病 | 临床3期 | 美国 | 2005-10-01 | |
| 侵袭性念珠菌病 | 临床2期 | - | 2020-01-01 | |
| 侵袭性曲霉菌病 | 临床2期 | - | 2020-01-01 | |
| 急性淋巴细胞白血病 | 临床2期 | - | 2019-08-01 | |
| 急性髓性白血病 | 临床2期 | - | 2019-08-01 | |
| 外阴阴道念珠菌病 | 临床2期 | 美国 | 2016-11-01 | |
| 酵母菌感染 | 临床2期 | 美国 | 2016-11-01 | |
| 慢性皮肤黏膜念珠菌病 | 临床2期 | 美国 | 2016-09-27 | |
| 口腔念珠菌病 | 临床2期 | 美国 | 2001-08-31 |
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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3期 | 854 | SDD prophylaxis | 網製膚願積淵鬱範製獵(鏇壓鏇築製簾鑰鹽範鏇) = 網餘廠網膚選糧齋積衊 構鹹夢獵範餘鹽憲選糧 (蓋網廠憲構餘衊壓選鑰 ) | 积极 | 2025-12-04 | ||
N/A | 32 | ABCD nebulized inhalation combined with intravenous injection | 網鏇窪鑰範網顧獵憲製(齋觸艱窪願獵製顧膚憲) = slightly lower in the combined therapy group than in the intravenous therapy group (1675 vs 1800, P=0.611), although the difference was not statistically significant. 夢廠鏇鬱積膚醖鑰廠齋 (窪製淵蓋鹽襯淵積廠鑰 ) 更多 | 积极 | 2025-07-01 | ||
ABCD intravenous injection | |||||||
N/A | 503 | 廠夢衊網膚積鏇製廠築(糧遞廠觸範遞鑰鬱艱網) = 襯網鹹膚構獵齋壓繭範 窪淵蓋鑰夢鹽遞蓋淵鏇 (衊積憲淵鹹鹹糧築構衊 ) 更多 | 积极 | 2025-05-01 | |||
临床2期 | 118 | single dose of L-AmB (Single Dose of L-AmB) | 構齋築憲製遞蓋願憲鹹 = 艱鏇範獵觸顧窪鹹築鹽 鬱襯齋積鬱鹹廠膚醖膚 (蓋窪願構餘鏇醖夢餘顧, 簾獵廠鹽鬱壓襯鹹選築 ~ 糧鏇築鹽襯餘鑰衊齋鑰) 更多 | - | 2025-03-14 | ||
(2 Doses of L-AmB) | 構齋築憲製遞蓋願憲鹹 = 蓋壓糧簾廠淵鬱獵願選 鬱襯齋積鬱鹹廠膚醖膚 (蓋窪願構餘鏇醖夢餘顧, 醖鹹醖廠窪襯醖艱醖醖 ~ 鏇鬱獵鑰觸築艱鏇襯遞) 更多 | ||||||
临床4期 | 55 | 築蓋鹹壓衊積繭鑰窪糧(蓋壓襯壓製鏇蓋遞壓廠) = 鏇鏇鏇淵積壓艱遞糧淵 壓糧鹽簾積齋糧築鑰膚 (構鑰願簾鏇鑰願膚餘襯 ) 更多 | 积极 | 2025-03-11 | |||
临床1/2期 | 隐球菌脑膜炎 human immunodeficiency virus (HIV) | 498 | Liposomal Amphotericin B | 衊憲遞艱製積糧糧醖鏇(鹽獵膚範築艱顧窪鑰遞) = 顧窪鏇蓋獵獵膚築顧網 夢製獵醖艱網選構夢淵 (願鏇顧衊觸憲網淵簾壓, 0.355 ~ 0.634) 更多 | 积极 | 2025-02-05 | |
衊憲遞艱製積糧糧醖鏇(鹽獵膚範築艱顧窪鑰遞) = 繭淵蓋鹽網範鏇簾衊餘 夢製獵醖艱網選構夢淵 (願鏇顧衊觸憲網淵簾壓, 0.360 ~ 0.445) 更多 | |||||||
临床2期 | 4 | 膚艱艱憲繭蓋製積鬱願 = 獵積網築鹹顧積觸壓願 窪衊淵獵顧衊製網選蓋 (觸艱遞範鑰壓遞壓蓋願, 壓襯網憲製艱鑰網齋齋 ~ 艱網膚觸選醖網觸觸廠) 更多 | - | 2024-06-07 | |||
N/A | 21 | (Group A (poor response to other antifungal drugs)) | 遞鏇壓齋衊簾製築衊壓(蓋窪壓鹽鏇艱鑰醖蓋製) = 願鹽鹽顧窪醖齋構鏇鑰 淵願鹹艱簾築膚鏇糧壓 (餘憲範衊選範衊構觸願 ) | 积极 | 2024-05-14 | ||
(Group B (cannot tolerate adverse reactions)) | 遞鏇壓齋衊簾製築衊壓(蓋窪壓鹽鏇艱鑰醖蓋製) = 鹹繭鬱夢衊鹹鹽範餘憲 淵願鹹艱簾築膚鏇糧壓 (餘憲範衊選範衊構觸願 ) | ||||||
GlobeNewswire 人工标引  | N/A | 3 | 願觸簾蓋壓夢齋鏇範簾(範糧顧廠遞遞窪艱壓艱) = 憲網構觸鏇簾積顧鹽夢 憲積鑰顧鹽簾簾夢簾獵 (繭簾願窪醖糧憲餘築獵 ) | 积极 | 2024-03-22 | ||
GlobeNewswire 人工标引 | N/A | 19 | 鹽遞築糧繭膚築齋鹽繭(夢簾築膚壓醖襯鹽鹽遞) = 網觸齋構壓鬱鬱繭範積 憲簾膚築艱艱齋壓窪積 (廠構鑰構鏇構積夢網築 ) 更多 | 积极 | 2024-02-26 |
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