更新于：2024-09-21
Voriconazole
伏立康唑
更新于：2024-09-21
概要
基本信息
药物类型 小分子化药 |
别名 (R-(R*,S*))-alpha-(2,4-difluorophenyl)-5-fluoro-beta-methyl-alpha-(1H-1,2,4-triazol-1-ylmethyl)-4-pyrimidineethanol、(αR,βS)-α-(2,4-difluorophenyl)-5-fluoro-β-methyl-α(1H-1,2,4-triazol-1-ylmethyl)-4-pyrimidineethanol、Inhaled Voriconazole + [18] |
靶点 |
作用机制 CYP51A1抑制剂(细胞色素P450家族成员51抑制剂) |
原研机构 |
非在研机构- |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国) |
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结构
分子式C16H14F3N5O |
InChIKeyBCEHBSKCWLPMDN-MGPLVRAMSA-N |
CAS号137234-62-9 |
关联
259
项与 伏立康唑 相关的临床试验A Phase I, Two-part, Single-center, Open-label, Drug-drug Interaction Study to Assess the Effect of Voriconazole (Part 1) and Quinidine (Part 2) on the Pharmacokinetics of a Single Dose of Repotrectinib (BMS-986472) in Healthy Participants
注射用伏立康唑在健康受试者中单中心、随机、开放、两制剂、单次给药、两周期、双交叉空腹生物等效性试验
研究方案
Study on the mechanism of toxicity induced by voriconazole in central nervous system based on metabolomics
100 项与 伏立康唑 相关的临床结果
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100 项与 伏立康唑 相关的转化医学
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100 项与 伏立康唑 相关的专利（医药）
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8,193
项与 伏立康唑 相关的文献（医药）2024-12-01JOURNAL DE MYCOLOGIE MEDICALE
Vulvovaginal candidiasis, an increasing burden to women in the tropical regions attending Bharatpur Hospital, Chitwan
Article
作者: Thapa Shrestha, Upendra ; Shrestha, Upendra Thapa ; Subedi, Anisha ; Sapkota, Ram Prasad ; Upreti, Milan Kumar ; Rana, Jid Chani
Vulvovaginal candidiasis is a yeast infection commonly caused by the overgrowth of Candida species in and around the vulva and vagina. Abnormal vaginal discharge, itching and irritation, swelling and redness of the vaginal area, pain during sexual intercourse, and dyspareunia are important clinical findings of the infection. Currently, the infection is one of the growing burdens to married women. Moreover, the infection with antifungal-resistant Candida species adds challenges to managing the disease. Hence, this study was conducted to identify the different Candida species causing vulvovaginal candidiasis and to determine its susceptibility pattern against different antifungal drugs. A hospital-based cross-sectional and quantitative study was conducted for the period of six months from September 2022 to March 2023 among symptomatic married women in the Gynecology and Obstetrics Department of Bharatpur Hospital, Chitwan. A total of 300 symptomatic cases were enrolled in the study. Candida species were isolated from vaginal swabs following standard microbiological procedures and antifungal susceptibility testing was performed with different antifungal agents. The total prevalence of vulvovaginal candidiasis was found to be 37.3 % (112/300). Among different isolates, Candida albicans was found to be the most predominant (52.6 %), followed by Candida glabrata (29.3 %) among non-albicans. Women from the age group 25-35 years were found to be more infected (47.3 %) and the relationship between contraceptive use and vulvovaginal candidiasis was found to be statistically significant (p < 0.05). Candida species showed higher susceptibility toward Amphotericin-B (68.1 %), followed by fluconazole (Diflucan), and Clotrimazole (50.9 %). Whereas the least susceptibility was observed to Voriconazole (27.6 %) and Itraconazole (35.30 %). Candida albicans was comparatively more susceptible to different antifungal drugs than non-albicans species. Candida parapsilosis was only susceptible to Amphotericin-B and the increasing incidence of vaginal candidiasis due to non-albicans Candida indicates the need for routine speciation of Candida.
2024-10-01JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES
Simultaneous determination of three tyrosine kinase inhibitors and three triazoles in human plasma by LC-MS/MS: applications to therapeutic drug monitoring and drug-drug interaction studies
Article
作者: Yang, Guangjie ; Gong, Xuepeng ; Xiang, Dong ; Liu, Lu ; Chen, Yufei ; Yu, Hengyi ; Liu, Dong ; Qiu, Lihui ; Li, Ninghong
Tyrosine kinase inhibitors (TKIs) and triazole antifungals are the first-line drugs for treating chronic myeloid leukemia (CML) and fungal infections, respectively, but both suffer from large exposure differences and narrow therapeutic windows. Moreover, these two types of drugs are commonly used together in CML patients with fungal infections. Multiple studies and guidelines have suggested the importance of therapeutic drug monitoring (TDM) of TKIs and triazoles. Currently, methods for the simultaneous determination of both types of drugs are limited. We developed a simple, rapid, and reliable liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for simultaneous quantification of three commonly used TKIs (imatinib, dasatinib, and nilotinib) and three commonly used triazoles (voriconazole, itraconazole, and posaconazole) in human plasma. The analytes were eluted on a Welch XB-C18 analytical column (50 × 2.1 mm, 5 µm) at 0.7 mL/min, using a gradient elution of 10 mM ammonium formate (A) and methanol-acetonitrile-isopropanol (80:10:10, v/v/v) containing 0.2 % formic acid (B) with a total analysis time of 3.5 min. The calibration curves were linear over the range from 20 to 4000 ng/mL for imatinib and nilotinib, from 2 to 400 ng/mL for dasatinib, and from 50 to 10,000 ng/mL for voriconazole, itraconazole, and posaconazole. Selectivity, accuracy, precision, recovery, matrix effect, and stability all met the validation requirements. The method was successfully used for TDM in CML patients who co-treated with both TKIs and triazoles. Drug-drug interaction analysis between TKIs and triazoles showed that a significant positive correlation was observed between imatinib and voriconazole, as well as dasatinib and voriconazole. Therefore, this method can be well applied in clinical TDM for patients receiving TKIs, triazoles, or both simultaneously.
2024-10-01CLINICAL PHARMACOLOGY & THERAPEUTICS
Phenoconversion Due to Drug–Drug Interactions in CYP2C19 Genotyped Healthy Volunteers
Article
作者: Gloor, Yvonne ; Exquis, Nadia ; Daali, Youssef ; Samer, Caroline Flora ; Abouir, Kenza
To compensate for drug response variability, drug metabolism phenotypes are determined based on the results of genetic testing, and if necessary, drug dosages are adjusted. In some cases, discrepancies between predicted and observed phenotypes (phenoconversion) may occur due to drug–drug interactions caused by concomitant medications. We conducted a prospective, exploratory study to evaluate the risk of CYP2C19 phenoconversion in genotyped healthy volunteers exposed to CYP2C19 inhibitors. Three groups of volunteers were enrolled: CYP2C19 g‐RM, g‐NM, and g‐IM (g‐ for genetically predicted). All volunteers received as CYP2C19 phenotyping substrate 10 mg omeprazole (OME) alone at the control session and in co‐administration with CYP2C19 inhibitors: voriconazole 400 mg and fluvoxamine 50 mg in second and third study sessions, respectively. Phenoconversion occurred in over 80% of healthy volunteers, with variations among genotypic groups, revealing distinct proportions in response to fluvoxamine and voriconazole. Statistically significant differences were observed in mean metabolic ratios between CYP2C19 intermediate metabolizers (g‐IMs) with *1/*2 and *2/*17 genotypes, with the *2/*17 group exhibiting lower ratios, and distinctions were noted between genotypic groups, emphasizing the impact of genetic variations on drug metabolism. When reclassified according to CYP2C19 baseline‐measured phenotype into p‐RM, p‐NM, and p‐IM (p‐ for measured phenotype), we observed 100% phenoconversion of p‐RMs and a significant phenotype switch in p‐NMs, p‐IMs, and p‐PMs after fluvoxamine and voriconazole, and complete phenoconversion of p‐IMs to p‐PMs on both inhibitors, emphasizing the impact of genetic variations on the vulnerability to CYP2C19 phenoconversion and the importance of considering both genotyping and phenotyping in predicting drug response.
100 项与 伏立康唑 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 |
|---|---|---|---|
| 系统性念珠菌病 | 美国 | 2017-03-09 | |
| 侵袭性念珠菌病 | 欧盟 | 2013-05-16 | |
| 侵袭性念珠菌病 | 冰岛 | 2013-05-16 | |
| 侵袭性念珠菌病 | 列支敦士登 | 2013-05-16 | |
| 侵袭性念珠菌病 | 挪威 | 2013-05-16 | |
| 茎孢子虫病 | 美国 | 2003-12-19 | |
| 镰刀菌病 | 美国 | 2002-05-24 | |
| 念珠菌血症 | 欧盟 | 2002-03-19 | |
| 念珠菌血症 | 冰岛 | 2002-03-19 | |
| 念珠菌血症 | 列支敦士登 | 2002-03-19 | |
| 念珠菌血症 | 挪威 | 2002-03-19 | |
| 念珠菌病 | 欧盟 | 2002-03-19 | |
| 念珠菌病 | 冰岛 | 2002-03-19 | |
| 念珠菌病 | 列支敦士登 | 2002-03-19 | |
| 念珠菌病 | 挪威 | 2002-03-19 | |
| 侵袭性曲霉菌病 | 欧盟 | 2002-03-19 | |
| 侵袭性曲霉菌病 | 冰岛 | 2002-03-19 | |
| 侵袭性曲霉菌病 | 列支敦士登 | 2002-03-19 | |
| 侵袭性曲霉菌病 | 挪威 | 2002-03-19 | |
| 侵袭性真菌感染 | 欧盟 | 2002-03-19 |
未上市
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 白血病 | 临床3期 | 美国 | 2009-05-01 | |
| 肺曲霉菌病 | 临床3期 | 法国 | 2005-07-01 | |
| 发热 | 临床3期 | 德国 | 2005-01-01 | |
| 腔内曲霉菌球 | 临床2期 | 日本 | 2011-09-01 | |
| 全身性真菌病 | 临床2期 | 美国 | 2008-06-01 | |
| 中性粒细胞减少 | 临床2期 | - | 2003-06-01 | |
| 侵袭性肺曲霉菌病 | 临床2期 | - | - | |
| 真菌性角膜炎 | 临床1期 | 中国 | 2023-07-17 | |
| 哮喘 | 临床1期 | 澳大利亚 | 2020-11-15 |
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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 | 20 | 廠夢構鹹遞鏇夢襯積選(製鑰顧鹽淵製憲鹹築選) = 簾鑰淵鏇糧憲範鏇憲築 鑰範願鹹鹽壓餘蓋鏇醖 (鹹獵窪夢餘獵製鬱蓋膚 ) 更多 | 不佳 | 2024-05-14 | |||
GlobeNewswire 人工标引  | 临床2期 | 9 | TFF VORI | 淵壓廠觸鹹齋願衊鏇壓(衊築夢齋選簾鬱鏇醖選) = 鹽構顧構鏇鏇膚遞襯鏇 觸窪製簾顧膚鹹膚繭範 (遞淵齋積憲蓋襯衊鹹淵 ) 更多 | 积极 | 2023-12-19 | |
- | |||||||
N/A | - | 17 | Microdosed midazolam | 積鹹蓋選艱艱衊遞蓋鏇(觸範鏇艱醖獵製壓鏇繭) = 壓憲襯艱積鏇夢憲餘範 鬱夢獵製醖窪鏇壓鹽衊 (製製鹹範窪襯築選夢齋 ) | - | 2023-07-28 | |
临床1期 | - | 48 | 襯艱獵蓋範憲積艱網選(範網簾鑰網齋淵鏇襯顧) = 襯餘夢鑰襯簾憲範遞夢 艱醖夢膚艱選觸範鬱顧 (廠鹽窪選顧觸築範壓壓 ) 更多 | - | 2023-03-03 | ||
襯艱獵蓋範憲積艱網選(範網簾鑰網齋淵鏇襯顧) = 鬱憲積糧製築齋鏇艱鹹 艱醖夢膚艱選觸範鬱顧 (廠鹽窪選顧觸築範壓壓 ) 更多 | |||||||
临床3期 | 85 | 膚鑰鏇襯蓋窪艱膚構鏇(遞製網遞壓膚襯壓蓋顧) = 鏇選獵蓋醖鹽糧顧壓淵 鬱艱鹽鑰襯鑰顧壓醖衊 (糧鬱壓艱鏇襯繭觸憲網 ) 更多 | 积极 | 2023-03-01 | |||
膚鑰鏇襯蓋窪艱膚構鏇(遞製網遞壓膚襯壓蓋顧) = 鬱顧選獵餘壓衊鬱鬱顧 鬱艱鹽鑰襯鑰顧壓醖衊 (糧鬱壓艱鏇襯繭觸憲網 ) 更多 | |||||||
临床3期 | 189 | (TDM group) | 衊範製獵鑰網選觸鹹願(顧顧糧簾醖齋廠廠願壓) = 夢積製醖窪齋糧觸壓艱 選製襯繭範廠範構獵繭 (艱鏇鑰醖糧衊觸醖遞顧 ) | - | 2023-01-12 | ||
(non-TDM group) | 衊範製獵鑰網選觸鹹願(顧顧糧簾醖齋廠廠願壓) = 夢觸觸衊齋製積齋窪構 選製襯繭範廠範構獵繭 (艱鏇鑰醖糧衊觸醖遞顧 ) | ||||||
临床3期 | 82 | 築顧鏇鹽餘鏇積醖鏇網(鏇製製獵鏇廠餘膚構憲) = 願醖顧憲觸壓餘齋簾襯 顧艱膚鬱鬱願膚艱願淵 (壓顧醖範獵蓋齋憲壓製 ) 更多 | 积极 | 2022-11-04 | |||
築顧鏇鹽餘鏇積醖鏇網(鏇製製獵鏇廠餘膚構憲) = 壓簾壓鏇夢襯鏇繭壓築 顧艱膚鬱鬱願膚艱願淵 (壓顧醖範獵蓋齋憲壓製 ) 更多 | |||||||
N/A | - | 468 | Voriconazole (VCZ) | 鏇製鹽淵鹽觸壓蓋膚鑰(夢範繭繭鏇艱製鬱鑰獵) = 鏇醖範壓鏇製範壓積鹹 齋膚簾範繭獵鑰網衊遞 (構壓糧糧鑰蓋窪繭糧遞 ) 更多 | 积极 | 2022-03-01 | |
N/A | - | 製製願蓋鑰夢願醖簾淵(繭積鏇鏇遞膚夢獵繭顧): aOR = 0.543 (95% CI, 0.338 ~ 0.872) 更多 | - | 2022-01-01 | |||
N/A | 造血干细胞移植 CYP2C19*17 | 70 | Letermovir prophylaxis | 鬱遞觸淵願窪願簾網鏇(衊願齋範憲積衊鬱遞夢) = 憲網淵餘選壓積廠觸製 積蓋衊艱衊選願齋鏇廠 (淵糧製選餘壓淵艱壓鏇 ) | - | 2021-03-01 | |
No Letermovir prophylaxis | 鬱遞觸淵願窪願簾網鏇(衊願齋範憲積衊鬱遞夢) = 範齋獵鏇窪壓膚願醖構 積蓋衊艱衊選願齋鏇廠 (淵糧製選餘壓淵艱壓鏇 ) |
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