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更新于：2025-05-16
Acyclovir
阿昔洛韦
更新于：2025-05-16
概要
基本信息
简介Acyclovir是一种合成嘌呤类似物，商品名为ZOVIRAX，其对疱疹病毒类型1（HSV-1）、2（HSV-2）和水痘-带状疱疹病毒（VZV）具有体外和体内的抑制活性。Acyclovir的抑制活性是高度选择性的，因为它与HSV和VZV编码的胸腺嘧啶激酶（TK）酶具有亲和力。这种病毒酶将acyclovir转化为一种核苷酸类似物——acyclovir单磷酸。单磷酸经过细胞鸟苷酸激酶的进一步转化，形成二磷酸和三磷酸。体外，acyclovir三磷酸可停止疱疹病毒DNA的复制。ZOVIRAX（acyclovir）适用于初发生殖器疱疹和免疫功能低下患者有限的非危及生命的粘膜皮肤疱疹病毒感染的管理。Aciclovir于1974年由Burroughs Wellcome（现为GlaxoSmithKline的一部分）获得专利，并于1981年获得英国批准。 |
药物类型 小分子化药 |
别名 Aciclovir、Aciclovir (JP17/INN)、Acycloguanosine + [37] |
作用方式 抑制剂 |
作用机制 DNA-指导DNA聚合酶抑制剂 |
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 英国 (1981-01-01), |
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C8H11N5O3 |
InChIKeyMKUXAQIIEYXACX-UHFFFAOYSA-N |
CAS号59277-89-3 |
关联
139
项与 阿昔洛韦 相关的临床试验NCT05452928
Aciclovir for HSV-2 Meningitis: A Double-blind Randomised Controlled Trial (AMEN)
CTR20243925
阿昔洛韦片（0.2g）在中国健康受试者中空腹和餐后给药条件下随机、开放、单剂量、两制剂、两序列、两周期、双交叉生物等效性试验
ChiCTR2400093679
A single-center, randomized, open, single-dose, two-cycle, two-sequence, cross-over bioequivalence trial of oral acyclovir tablets during fasting and postprandial conditions in healthy Chinese subjects
100 项与 阿昔洛韦 相关的临床结果
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100 项与 阿昔洛韦 相关的转化医学
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100 项与 阿昔洛韦 相关的专利（医药）
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14,151
项与 阿昔洛韦 相关的文献（医药）2025-12-01JOURNAL OF CLINICAL IMMUNOLOGY
Novel Compound Heterozygous Variants in the FAS Gene Lead to Fetal Onset of Autoimmune Lymphoproliferative Syndrome (ALPS)
Article
作者: Hui, Xiaoying ; Sun, Bijun ; Hou, Jia ; Wang, Xiaochuan ; Wang, Chenghao ; Wu, Qi ; Ying, Wenjing ; Wang, Ying ; Wu, Bingbing ; Zhou, Qinhua ; Sun, Jinqiao ; Wang, Wenjie ; Zhu, Li ; Li, Qifan ; Zhou, Weitao ; Qian, Feng ; Liu, Luyao ; Chen, Yao ; Yu, Meiping
OBJECTIVE:
FAS gene defects lead to autoimmune lymphoproliferative syndrome (ALPS), which is often inherited in an autosomal dominant and rarely in an autosomal recessive manner. We report a case of a newborn girl with novel compound heterozygous variants in FAS and reveal the underlying mechanism.
METHODS:
Whole-exome sequencing (WES) was used to identify pathogenic variants. Multiparametric flow cytometry analysis, phosflow analysis, and FAS-induced apoptosis assays were used to explore the effects of the variants on FAS expression, apoptosis, and immunophenotype. The HEK293T cells were used to assess the impact of the variants on protein expression and FAS-induced apoptosis.
RESULTS:
The patient was born with hepatosplenomegaly, anemia, and thrombocytopenia. She also experienced COVID-19, rotavirus infection, herpes simplex virus infection, and severe pneumonia. The proportion of double-negative T cells (DNTs) was significantly elevated. Novel FAS compound heterozygous variants c.310T > A (p.C104S) and c.702_704del (p.T235del) were identified. The apoptotic ability of T cells was defective, and FAS expression on the surface of T cells was deficient. The T235del variant decreased FAS expression, and the C104S protein remained in the endoplasmic reticulum (ER) and could not translocate to the cell surface. Both mutations resulted in loss-of-function in terms of FAS-induced apoptosis in HEK293T cells. The DNTs were mainly terminally differentiated T (TEMRA) and CD45RA+HLA-DR+, with high expression of CD85j, PD-1, and CD57. The percentage of Th1, Tfh, and autoreactive B cells were significantly increased in the patient. The abnormal immunophenotyping was partially attenuated by sirolimus treatment.
CONCLUSIONS:
We identified two variants that significantly affect FAS expression or localization, leading to early disease onset of in the fetus. Abnormalities in the mTOR pathway are associated with a favorable response to sirolimus.
2025-10-01COMPUTATIONAL BIOLOGY AND CHEMISTRY
Synthesis, X-ray diffraction, and computational studies of acyclovir and HBG analogs derived from Triazolyl-1,4-benzothiazine and their oxidized forms for breast cancer and SARS-CoV-2
Article
作者: Oubella, Ali ; Blaqcue, Olivier ; Irrou, Ezaddine ; Taha, Mohamed Labd ; AlAjmi, Mohamed F ; Sebbar, Nada Kheira ; Rehman, Md Tabish ; Elmachkouri, Younesse Ait
This study presents a simple and efficient synthetic method for preparing a new series of acyclonucleosides derived from 1,4-benzothiazine and 1,4-benzothiazine-1,1-dioxide. These compounds feature the introduction of a 1,2,3-triazole-4-ylmethyl ring as a spacer between the heterocyclic bases and the pseudosugars of acyclovir (ACV) and hydroxybutylguanine (HBG). The acyclonucleosides were synthesized through copper-catalyzed 1,3-dipolar cycloaddition reactions between azides 8a and 8b and the N4-propargyl base 7. Following this, the deprotection of the acyclic chains and the oxidation of the sulfur to sulfone afforded the acyclonucleosides 9a,b-12a,b in satisfactory yields. The synthesized acyclonucleosides were characterized using 1H and 13C NMR spectroscopy. Moreover, the structure of 9b was confirmed by single-crystal X-ray diffraction analysis. The synthesized acyclonucleosides were evaluated through in silico studies, including network pharmacology for bioactivity, toxicity prediction, physicochemical properties, and ADMET analysis. Molecular docking studies revealed significant interactions, highlighting compound 11b's favorable binding with the target protein AKT1, achieving a binding energy of -6.43 kcal/mol, which is close to the Capivasertib standard. Similarly, compound 12b showed interactions akin to hydroxychloroquine, with a binding energy of -6.29 kcal/mol for the SARS-CoV-2 target protein. Molecular dynamics simulations further validated the stability of the ligand-protein complexes during 200 ns, as evidenced by acceptable RMSD and RMSF and Rg values. The post-dynamic, MMGBSA, PCA, FEL, PDF, and DCCM analyses of the AKT and SARS-CoV-2 protein-ligand complexes have provided comprehensive insights into their interactions with standard drugs, binding affinities, conformational dynamics, and structural stability. These studies are crucial for understanding the molecular mechanisms underlying drug efficacy and resistance, thereby informing the rational design of new inhibitors targeting AKT and SARS-CoV-2 proteins. Finally, the two most promising compounds, 11b and 12b, selected from the docking results, were analyzed using Density Functional Theory (DFT). These analyses revealed significant variations in their electronic properties, providing valuable insights into their reactivity, stability, and polarity.
2025-07-01DIAGNOSTIC MICROBIOLOGY AND INFECTIOUS DISEASE
Clinical and cost implications of Biofire FilmArray® meningitis / encephalitis panel testing: a systematic review
Review
作者: Harris, Patrick Na ; Rafiei, Nastaran ; Subedi, Shradha ; Paterson, David L
BACKGROUND:
Meningitis and encephalitis are diseases with high case fatality rates and serious long-term sequalae. A significant percentage do not receive an aetiological diagnosis, in part due to limitations of conventional testing methods. The Biofire FilmArray® Meningitis / Encephalitis Panel (MEP) is the first commercially approved multiplex PCR panel for diagnosis of infectious meningoencephalitis. It provides rapid results and has the potential to reduce empiric antimicrobial use and length of hospitalisation when compared to conventional testing.
METHODS:
We conducted a systematic review to evaluate the impact of MEP implementation by searching the Medline and Embase databases. The outcomes of interest were duration of acyclovir treatment, duration of antimicrobials, length of stay and healthcare cost.
RESULTS:
A total of 23 studies satisfied the inclusion criteria, the majority of which were retrospective studies comparing cohorts before and after MEP implementation. The included studies were very heterogenous, with variation in MEP implementation strategies, standard of care diagnostics and study populations. MEP testing resulted in reduction in acyclovir use in 75 % of studies with an average reduction of 39 h (range 11-144 h). Antimicrobial use and length of stay was reduced in 44 % and 40 % of studies respectively. Five studies looked at healthcare costs, variably described between studies as hospitalisation, antimicrobial and microbiology costs. Total hospitalisation cost was reduced in 1 study and unchanged in 2 studies.
CONCLUSION:
Whilst MEP implementation reduces acyclovir usage in patients evaluated for ME, the benefits in terms of antibiotic use, and length of stay are variable and likely depend on the study population, implementation strategy and standard of care testing available in each institution.
205
项与 阿昔洛韦 相关的新闻（医药）2025-05-15
细胞疗法免疫疗法专利侵权
2025-05-14
·药闻康策
一致性评价高管变更
2025-05-12
·生物世界
细胞疗法免疫疗法临床1期基因疗法临床结果
100 项与 阿昔洛韦 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 |
|---|---|---|---|
| 疱疹性角膜炎 | 日本 | 2007-01-23 | |
| 唇疱疹 | 美国 | 2002-12-30 | |
| 单纯疱疹病毒性脑炎 | 澳大利亚 | 1996-08-19 | |
| 水痘 | 美国 | 1985-01-25 | |
| 带状疱疹 | 中国 | 1985-01-01 | |
| 水痘带状疱疹病毒感染 | 中国 | 1985-01-01 | |
| 生殖器疱疹 | 美国 | 1982-03-29 | |
| 单纯疱疹 | 英国 | 1981-01-01 |
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 |
|---|---|---|---|---|
| HIV感染 | 临床3期 | 美国 | 2001-08-31 | |
| 艾滋病相关复合征 | 临床阶段不明 | 美国 | 2001-08-31 | |
| 毛状白斑 | 临床阶段不明 | 美国 | 2001-08-31 |
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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
临床1/2期 | 48 | 選築窪壓積簾鏇壓鹽顧 = 鏇蓋繭憲廠積壓淵醖積 選艱構壓淵艱齋選積簾 (觸壓襯願壓廠鹽餘醖願, 蓋鏇齋觸衊窪糧窪選獵 ~ 築鏇選鑰夢鑰糧壓蓋觸) 更多 | - | 2024-05-29 | |||
N/A | - | Oral Acyclovir 400mg | 餘淵願淵廠壓鹽淵醖襯(簾鏇壓餘積遞鏇蓋願壓) = 醖繭選鑰醖鹽鹽繭遞繭 築夢鏇憲醖築積醖廠築 (窪築築鏇膚齋窪廠鹹繭 ) | - | 2024-02-22 | ||
餘淵願淵廠壓鹽淵醖襯(簾鏇壓餘積遞鏇蓋願壓) = 餘鏇鑰鑰築鬱艱醖簾願 築夢鏇憲醖築積醖廠築 (窪築築鏇膚齋窪廠鹹繭 ) | |||||||
N/A | - | 顧糧鹽襯觸遞襯餘網簾(積淵遞襯積淵壓蓋鏇願) = blistering in 52.6% of the patients 鏇積醖醖網範膚願衊衊 (鑰獵簾製糧鏇鏇齋膚範 ) 更多 | 积极 | 2023-07-03 | |||
Intralesional saline | |||||||
N/A | - | Acyclovir/Valacyclovir | 範製鬱範淵糧壓鏇餘衊(獵構積壓廠廠簾繭衊積) = 鬱襯襯簾範壓築衊構製 淵繭淵顧願醖夢鬱簾襯 (積觸膚壓鹹淵觸糧夢製 ) | 不佳 | 2023-06-14 | ||
範製鬱範淵糧壓鏇餘衊(獵構積壓廠廠簾繭衊積) = 餘觸衊鏇鏇觸鏇夢廠衊 淵繭淵顧願醖夢鬱簾襯 (積觸膚壓鹹淵觸糧夢製 ) | |||||||
N/A | - | 56 | (Acyclovir 200 mg Tablet) | 窪壓艱鬱窪積觸網夢膚(鑰簾構選襯齋鑰獵鏇觸) = 衊醖憲網壓夢範襯鬱顧 遞齋醖鑰夢簾顧艱網齋 (鹹襯膚鹹壓簾網醖選衊, 244.06) 更多 | - | 2023-02-08 | |
(Zovirax® 200 mg Tablet) | 窪壓艱鬱窪積觸網夢膚(鑰簾構選襯齋鑰獵鏇觸) = 積鏇鹽選鑰鏇願網憲鑰 遞齋醖鑰夢簾顧艱網齋 (鹹襯膚鹹壓簾網醖選衊, 258.18) 更多 | ||||||
临床3期 | 60 | 襯繭艱網遞窪膚廠蓋廠(襯齋築構構鹽餘顧網顧) = 鑰願襯廠窪範選窪蓋構 壓夢鏇壓糧製齋鹹窪蓋 (艱鏇繭襯遞鹹鹹廠夢鏇 ) 更多 | - | 2021-12-05 | |||
Placebo nanofiber patch | 襯繭艱網遞窪膚廠蓋廠(襯齋築構構鹽餘顧網顧) = 醖齋積衊積觸壓顧鏇築 壓夢鏇壓糧製齋鹹窪蓋 (艱鏇繭襯遞鹹鹹廠夢鏇 ) 更多 | ||||||
临床3期 | 4,076 | (Test Product) | 艱鏇鏇醖憲齋繭範夢淵(壓憲觸艱鬱遞廠顧遞構) = 壓鏇窪鏇鬱廠鑰壓繭築 顧築艱鏇餘構築鏇鬱夢 (築鹽構願膚製餘願遞廠, 80.660) 更多 | - | 2021-01-05 | ||
(Reference Product) | 艱鏇鏇醖憲齋繭範夢淵(壓憲觸艱鬱遞廠顧遞構) = 鹽餘遞繭鏇願夢膚窪鹽 顧築艱鏇餘構築鏇鬱夢 (築鹽構願膚製餘願遞廠, 82.840) 更多 | ||||||
临床4期 | 72 | (Episodic Treatment Arm) | 廠製鑰築鏇範鏇觸淵獵(積網壓願餘餘衊艱餘製) = 齋醖醖醖齋鹽願鏇齋鹽 鹹簾繭構淵製鑰鬱積製 (衊願齋顧觸選膚製蓋鹽, 顧鏇鬱夢觸壓選構選顧 ~ 積願鑰網遞鹹製憲糧願) 更多 | - | 2020-01-29 | ||
(Suppressive Therapy Arm) | 廠製鑰築鏇範鏇觸淵獵(積網壓願餘餘衊艱餘製) = 製襯繭簾衊鏇艱壓觸鏇 鹹簾繭構淵製鑰鬱積製 (衊願齋顧觸選膚製蓋鹽, 淵獵廠範鑰鹽製齋齋窪 ~ 鹹壓窪齋餘獵壓顧獵壓) 更多 | ||||||
临床4期 | 238 | 糧餘膚願醖築糧顧簾觸(獵齋觸廠製艱繭廠襯築) = 構膚鬱遞築蓋願膚構積 廠築夢憲鏇鏇齋觸繭遞 (鑰製簾觸艱構膚淵糧築 ) 更多 | 不佳 | 2019-12-16 | |||
Placebo | 糧餘膚願醖築糧顧簾觸(獵齋觸廠製艱繭廠襯築) = 膚鹽壓範觸鹽鏇餘廠構 廠築夢憲鏇鏇齋觸繭遞 (鑰製簾觸艱構膚淵糧築 ) 更多 | ||||||
N/A | 中枢神经系统肿瘤 HSV-1 | HSV-2 | 18 | Acyclovir treatment | 獵鹽壓鹽鑰製選鹽簾網(鹹窪淵艱憲蓋糧糧製鑰) = 淵鹹淵網簾夢製憲鑰餘 壓齋鹽選觸醖觸艱窪構 (襯醖構憲壓襯鑰壓鬱鹽 ) | 积极 | 2019-11-11 | |
顧築鑰憲廠淵鹹餘獵憲(壓繭簾構網夢醖廠選艱) = 觸選醖廠繭餘齋廠襯遞 構窪顧顧衊觸齋鑰選製 (襯願願鹹襯鑰簾網鏇觸 ) |
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