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更新于：2025-09-05
Posaconazole
泊沙康唑
更新于：2025-09-05
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C37H42F2N8O4 |
InChIKeyRAGOYPUPXAKGKH-XAKZXMRKSA-N |
CAS号171228-49-2 |
关联
172
项与 泊沙康唑 相关的临床试验NCT07155226
A Modular Phase I/II, Open-label, Multi-Centre Study to Evaluate the Safety, Tolerability, Pharmacokinetics, Pharmacodynamics, and Preliminary Efficacy of AZD3632 Monotherapy or in Combination With Anticancer Agents in Participants With Advanced Haematologic Malignancies With KMT2Ar, NPM1m, or Other Genotypes Associated With HOX Overexpression
NCT06802757
A Phase II, Randomised, Open-label, Multicentre Study of Posaconazole Plus Pembrolizumab and Chemotherapy Versus Pembrolizumab and Chemotherapy as Neoadjuvant Therapy for Triple Negative Breast Cancer
ChiCTR2500098742
A multicenter, randomized controlled phase II clinical study of oral posaconazole combined with chemotherapy and PD-1 inhibitors as neoadjuvant treatment for early or locally advanced triple-negative breast cancer
100 项与 泊沙康唑 相关的临床结果
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100 项与 泊沙康唑 相关的转化医学
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100 项与 泊沙康唑 相关的专利（医药）
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4,937
项与 泊沙康唑 相关的文献（医药）2025-12-31Emerging Microbes & Infections
Emerging antifungal resistance in
Trichophyton mentagrophytes
: insights from susceptibility profiling and genetic mutation analysis
Article
作者: Richardson, Malcolm ; Bai, Lin ; Richardson, Riina ; Shao, Jin ; Shao, Yakun ; Wan, Zhe ; Yu, Jin ; Song, Yinggai ; Verweij, Paul ; Li, Ruoyu ; de Hoog, Sybren
ABSTRACTTrichophyton species, the leading cause of dermatophytosis globally, are increasingly resistant to antifungal treatments, concerns about effective management strategies. In light of the absence of established resistance criteria for terbinafine and azoles, coupled with a dearth of research on resistance mechanisms in Trichophyton, antifungal susceptibility and drug resistance gene diversity were analyzed across 64 T. mentagrophytes, 65 T. interdigitale, and 2 T. indotineae isolates collected in China between 1999 and 2024 and 101 published T. indotineae strains. Analyses of the minimum inhibitory concentrations (MICs) of terbinafine, itraconazole, voriconazole, posaconazole, and isavuconazole revealed a concerning increase in T. indotineae with terbinafine resistance, including two novel isolates from China. Compared with T. interdigitale, T. mentagrophytes presented higher terbinafine MICs but similar azole susceptibility. Notably, 27 T. interdigitale isolates were classified as non-wild-type for terbinafine. Genetic diversity was analyzed for the SQLE, CYP51A and CYP51B gene. Specifically, T. indotineae isolates presented SQLE protein changes linked to terbinafine resistance. SQLE diversity was linked to terbinafine sensitivity, whereas alterations in CYP51A were associated with itraconazole sensitivity, with notable statistical significance evident across various protein isoforms. The relationship between protein diversity and drug sensitivity is presented in detail. Together, these findings highlight a growing prevalence of antibiotic resistance among Trichophyton and identify potential target genes for new therapies, underscoring the need for ongoing monitoring and offering directions for novel therapeutics.
2025-12-01JOURNAL OF CLINICAL IMMUNOLOGY
Pulmonary Aspergillosis and Low HIES Score in a Family with STAT3 N-Terminal Domain Mutation
Article
作者: Lima de Souza, Suiane ; Saarela, Janna ; Martelius, Timi ; Chen, Zhi ; Kuismin, Outi ; Asano, Takaki ; Hautala, Timo ; Kaustio, Meri ; Yannopoulos, Fredrik ; Lappi-Blanco, Elisa ; Casanova, Jean-Laurent ; Tiitto, Leena ; Varjosalo, Markku ; Seppänen, Mikko R J ; Glumoff, Virpi ; Jartti, Airi ; Keskitalo, Salla ; Pikkarainen, Keela ; Boisson, Bertrand
Abstract:
Signal transducer and activator of transcription 3 (STAT3) plays a key role in leukocytic and non-leukocytic cells. Germ line mutations in STAT3, which are mainly found in the SH2, DNA binding and transactivation domains, can be loss- or gain-of-function (LOF and GOF). STAT3 N-terminal domain (NTD) mutations are rare, and their biological effects remain incompletely understood. We explored the significance of STAT3 NTD p.Trp37* variant in a patient with chronic pulmonary aspergillosis and a low Hyper-IgE syndrome (HIES) score. In cell culture models, the expression of full-length p.Trp37* allele showed shorter STAT3 protein expression suggesting a re-initiation (Met99 or Met143). STAT3 activity using luciferase reporter assay showed a twofold-increased activity of the STAT3 p.Trp37* STAT3 protein compared with WT STAT3 at basal level and upon IL-6 stimulation. In contrast, the activity of the short pTrp37* peptide (amino acids 1 to 37) was amorphic but without dominant negative (DN) effect on transcriptional activity or STAT3 Tyr705 phosphorylation. The proteins initiated at Met99 and Met143 were surprisingly hypermorphic. In carriers’ peripheral blood mononuclear cells (PBMCs), both WT and mutated STAT3 mRNA were equally present and the global amount of STAT3 protein was not significantly reduced. In stimulated heterozygous carriers’ PBMCs, however, STAT3 Tyr705 phosphorylation and Th17 were reduced but not completely abolished. This suggests a DN effect of an unknown product of the p.Trp37* allele. Transcriptomics analysis of PBMCs from the index revealed selectively distinct gene expression. We conclude that heterozygosity for the NTD p.Trp37* STAT3 mutation defines a novel allelic form of STAT3 deficiency, associated with a chronic pulmonary aspergillosis and minor signs of HIES.
2025-12-01MOLECULAR BIOLOGY REPORTS
A comprehensive in vitro and in silico assessment of eugenol glycoconjugates against azole and amphotericin B resistant Rhizopus spp.
Article
作者: Sengupta, Abhishek ; Chauhan, Aastha ; Bhattacharya, Asish K ; Vijayaraghavan, Pooja ; Goswami, Lakshmi ; Sen, Pooja ; Gupta, Lovely
BACKGROUND:
Rhizopus spp. is a major cause of mucormycosis, a severe infectious disease with high morbidity and mortality. Treatment is challenging due to rising antifungal resistance. Glycosylation is a crucial technique for enhancing the properties of phenolic compounds like eugenol. The present study aims to examine the antifungal efficacy of eugenol glycoconjugates against azole and amphotericin B-resistant Rhizopus isolates.
METHODS AND RESULTS:
Out of 50 soil samples, 12 isolates belonging to Mucorales were obtained, of which 7 were identified as Rhizopus spp. via 18S ITS sequencing. Antifungal susceptibility testing (AST) revealed that all Rhizopus isolates were resistant to amphotericin B (MIC > 1 µg/mL). Most isolates also showed resistance towards posaconazole (MIC > 1 µg/mL) and itraconazole (MIC > 2 µg/mL). AST of eugenol glycoconjugate (coded 6g) showed efficacy against resistant Rhizopus isolates, with MIC values ranging from 6.25 µg/mL to 25 µg/mL. Flow cytometry confirmed its fungicidal activity, correlating with MIC data. Compound 6g significantly reduced conidial germination within 24 h and exhibited no cytotoxicity on A549 lung cancer cells. In-silico analysis revealed a negative binding affinity of compound 6g for the spore coat protein CotH3, which could be a potential antifungal target.
CONCLUSION:
Compound 6g could be an potential antifungal molecule against resistant Rhizopus spp, which requires further studies.
100 项与 泊沙康唑 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 |
|---|---|---|---|
| 毛霉菌感染 | 日本 | 2020-01-23 | |
| 曲霉菌病 | 中国 | 2013-06-03 | |
| 念珠菌病 | 美国 | 2006-09-15 | |
| 侵袭性真菌感染 | 澳大利亚 | 2006-03-15 | |
| 接合菌病 | 澳大利亚 | 2006-03-15 | |
| 着色霉菌病 | 欧盟 | 2005-10-25 | |
| 着色霉菌病 | 欧盟 | 2005-10-25 | |
| 着色霉菌病 | 冰岛 | 2005-10-25 | |
| 着色霉菌病 | 冰岛 | 2005-10-25 | |
| 着色霉菌病 | 列支敦士登 | 2005-10-25 | |
| 着色霉菌病 | 列支敦士登 | 2005-10-25 | |
| 着色霉菌病 | 挪威 | 2005-10-25 | |
| 着色霉菌病 | 挪威 | 2005-10-25 | |
| 球孢子菌病 | 欧盟 | 2005-10-25 | |
| 球孢子菌病 | 欧盟 | 2005-10-25 | |
| 球孢子菌病 | 冰岛 | 2005-10-25 | |
| 球孢子菌病 | 冰岛 | 2005-10-25 | |
| 球孢子菌病 | 列支敦士登 | 2005-10-25 | |
| 球孢子菌病 | 列支敦士登 | 2005-10-25 | |
| 球孢子菌病 | 挪威 | 2005-10-25 |
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 |
|---|---|---|---|---|
| 深部真菌病 | 临床3期 | - | 2014-07-29 | |
| 肺曲霉菌病 | 临床3期 | - | 2014-07-29 | |
| 侵袭性肺曲霉菌病 | 临床3期 | - | 2013-09-25 | |
| 白细胞减少 | 临床3期 | - | 2008-11-01 | |
| 急性髓性白血病 | 临床3期 | - | 2002-07-01 | |
| 骨髓增生异常综合征 | 临床3期 | - | 2002-07-01 | |
| 中性粒细胞减少 | 临床3期 | - | 2002-07-01 | |
| 口腔念珠菌病 | 临床3期 | 美国 | 1998-08-01 | |
| 口腔念珠菌病 | 临床3期 | 巴巴多斯 | 1998-08-01 | |
| HIV感染 | 临床3期 | 美国 | 1998-08-01 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | 急性髓性白血病 CYP3A enzymes | 31 | 膚憲網鬱遞壓廠獵壓窪(鬱觸壓夢簾構壓齋觸鬱) = 襯網壓積鏇餘夢簾選襯 廠艱簾遞築壓醖遞餘願 (鏇顧糧壓遞壓糧鹹膚構 ) 更多 | 积极 | 2025-05-30 | ||
膚憲網鬱遞壓廠獵壓窪(鬱觸壓夢簾構壓齋觸鬱) = 壓壓觸夢鏇鏇齋襯憲網 廠艱簾遞築壓醖遞餘願 (鏇顧糧壓遞壓糧鹹膚構 ) 更多 | |||||||
临床4期 | 88 | standard of care (SOC)+Posaconazole (SOC + 'Posaconazole 18 MG/ML') | 蓋簾觸顧鹹獵餘窪製築 = 醖淵選積窪壓觸鹹廠範 積顧顧醖蓋觸夢網憲構 (膚簾膚襯鑰淵鏇遞膚網, 餘餘築鏇顧顧網糧蓋鬱 ~ 顧齋網壓淵鑰網醖艱憲) 更多 | - | 2025-04-08 | ||
standard of care (SOC) (Standard of Care) | 蓋簾觸顧鹹獵餘窪製築 = 積襯醖觸鬱製窪顧齋網 積顧顧醖蓋觸夢網憲構 (膚簾膚襯鑰淵鏇遞膚網, 廠顧壓構憲餘簾壓鏇積 ~ 窪觸餘醖簾齋壓壓構構) 更多 | ||||||
临床2期 | 10 | 膚膚製構糧廠繭鹹製選 = 鏇願衊醖遞獵築網齋鏇 淵窪構願簾獵壓鹹餘廠 (窪鹹網壓鹹膚觸選願齋, 願鑰壓範壓網鹽膚願鏇 ~ 醖廠壓鹹夢衊醖夢衊簾) 更多 | - | 2025-01-22 | |||
临床2期 | 31 | (Age Cohort 1 (2 -< 12 Years Old)) | 壓築築糧壓網製蓋觸願 = 繭鬱觸窪積選選鑰膚網 範糧顧鹽製顧醖構壓齋 (蓋觸鏇鹽夢繭獵簾鑰網, 觸鑰築衊範製鹽齋選遞 ~ 壓艱膚選夢憲鑰繭獵範) 更多 | - | 2025-01-14 | ||
(Age Cohort 2 (12 -< 18 Years Old)) | 壓築築糧壓網製蓋觸願 = 顧鑰艱壓鹹鏇憲範衊獵 範糧顧鹽製顧醖構壓齋 (蓋觸鏇鹽夢繭獵簾鑰網, 鹽願繭鹽鏇鹽製顧遞夢 ~ 鹹糧艱網網遞積廠窪齋) 更多 | ||||||
N/A | - | 鹹範觸簾艱襯積蓋鬱糧(顧顧廠選憲廠憲網鏇觸) = 蓋廠醖獵築鑰醖積選醖 淵淵範窪淵製齋鹹構夢 (衊遞選網衊蓋遞膚齋顧 ) | 积极 | 2025-01-01 | |||
No antifungal prophylaxis | 鹹範觸簾艱襯積蓋鬱糧(顧顧廠選憲廠憲網鏇觸) = 餘夢積憲廠鹽憲選蓋餘 淵淵範窪淵製齋鹹構夢 (衊遞選網衊蓋遞膚齋顧 ) | ||||||
临床2期 | 20 | 獵繭衊壓壓鏇繭範鹹糧 = 獵積鹹艱製糧襯窪繭窪 餘艱鑰鏇餘壓積鹽窪淵 (夢糧繭顧襯襯鬱糧簾築, 鑰鏇願鑰衊觸蓋艱遞範 ~ 顧顧膚鹽簾顧範廠齋鬱) 更多 | - | 2024-12-20 | |||
N/A | - | 獵衊襯願襯構積構鏇夢(製鏇衊觸餘獵觸範夢鏇) = There were no significant differences in survival outcomes, in months, including PFS (5.7 vs 4.2, p=0.53) 衊淵衊獵憲顧鏇壓艱衊 (襯觸繭艱醖餘膚鹽衊醖 ) 更多 | - | 2024-12-07 | |||
临床2期 | 20 | Posaconazole 300mg twice daily | 選築衊淵構積憲衊鏇衊(窪襯鏇淵齋醖構鑰鬱夢) = 鬱膚鏇糧製繭餘廠鹹鬱 獵網簾鏇選淵簾鑰憲憲 (觸鹽遞鏇糧淵壓衊觸製 ) 更多 | 积极 | 2024-05-14 | ||
N/A | 94 | 製齋壓顧壓鹽淵膚襯遞(夢鏇廠膚膚醖顧窪鬱壓) = 餘鬱蓋膚糧膚製餘蓋簾 範積範襯獵鬱願獵範壓 (鹽築壓鹹顧構獵簾繭網 ) 更多 | 积极 | 2024-05-14 | |||
No posaconazole prophylaxis | 製齋壓顧壓鹽淵膚襯遞(夢鏇廠膚膚醖顧窪鬱壓) = 鏇艱壓積淵窪選廠遞鏇 範積範襯獵鬱願獵範壓 (鹽築壓鹹顧構獵簾繭網 ) 更多 | ||||||
临床1期 | 70 | 構廠憲簾淵範衊憲艱憲(廠夢顧鬱廠獵襯鹽簾鑰) = 簾齋構艱獵選淵製鑰鬱 鑰顧窪膚顧淵蓋選襯願 (廠廠構願齋壓壓製壓製, 36%) 更多 | - | 2022-02-15 | |||
願簾憲範鑰範網鏇簾網(獵衊築鹽齋襯選齋鹹構) = 願鹽鬱壓鏇膚繭壓蓋願 鬱構夢觸窪願願襯夢鏇 (網鏇夢窪觸憲構鑰襯鑰, 42.4%) |
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