更新于：2024-11-04
Abacavir Sulfate
硫酸阿巴卡韦
更新于：2024-11-04
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 美国 (1998-12-17), |
最高研发阶段(中国)- |
特殊审评加速批准 (美国)、孤儿药 (日本) |
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结构
分子式C14H20N6O5S |
InChIKeyMBFKCGGQTYQTLR-SCYNACPDSA-N |
CAS号188062-50-2 |
关联
107
项与 硫酸阿巴卡韦 相关的临床试验Synergistic Treatment With Antiretrovirals and Laser Interstitial Thermal thErapy (STARLITE) for Unresectable High-Grade Gliomas: A Phase 1 Study
一项随机、开放、两序列交叉设计，评价健康成人空腹/餐后状态下单次口服硫酸阿巴卡韦片的生物等效性试验
Inhibition of Reverse Transcription in Type I Interferon Mediated Neuropathology
100 项与 硫酸阿巴卡韦 相关的临床结果
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100 项与 硫酸阿巴卡韦 相关的转化医学
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100 项与 硫酸阿巴卡韦 相关的专利（医药）
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1,117
项与 硫酸阿巴卡韦 相关的文献（医药）2024-12-31Platelets
Role of the NO-GC/cGMP signaling pathway in platelet biomechanics
Article
作者: Seta, Francesca ; Balmes, Aylin ; Khawaja, Akif A ; Friebe, Andreas ; Rodríguez, Johanna G ; Feil, Robert ; Emerson, Michael ; Pinto-Quintero, Daniel ; Boffito, Marta ; Schäffer, Tilman E ; Feil, Susanne ; Seifert, Jan ; Frye, Maike
Cyclic guanosine monophosphate (cGMP) is a second messenger produced by the NO-sensitive guanylyl cyclase (NO-GC). The NO-GC/cGMP pathway in platelets has been extensively studied. However, its role in regulating the biomechanical properties of platelets has not yet been addressed and remains unknown. We therefore investigated the stiffness of living platelets after treatment with the NO-GC stimulator riociguat or the NO-GC activator cinaciguat using scanning ion conductance microscopy (SICM). Stimulation of human and murine platelets with cGMP-modulating drugs decreased cellular stiffness and downregulated P-selectin, a marker for platelet activation. We also quantified changes in platelet shape using deep learning-based platelet morphometry, finding that platelets become more circular upon treatment with cGMP-modulating drugs. To test for clinical applicability of NO-GC stimulators in the context of increased thrombogenicity risk, we investigated the effect of riociguat on platelets from human immunodeficiency virus (HIV)-positive patients taking abacavir sulfate (ABC)-containing regimens. Our results corroborate a functional role of the NO-GC/cGMP pathway in platelet biomechanics, indicating that biomechanical properties such as stiffness or shape could be used as novel biomarkers in clinical research.
2024-10-01JOURNAL OF INFECTION AND CHEMOTHERAPY
Effects of switching to dolutegravir/lamivudine from tenofovir alafenamide fumarate/emtricitabine/dolutegravir or abacavir/lamivudine/dolutegravir on body weight and lipid profile in Japanese people living with HIV
Article
作者: Miyashita, Ryui ; Sekiya, Ryoko ; Ikegaya, Kenichi ; Sekine, Yusuke ; Ichiki, Akito ; Muramatsu, Takashi ; Hagiwara, Takeshi ; Amano, Kagehiro ; Harada, Yuko ; Chikasawa, Yushi ; Kinai, Ei ; Yamaguchi, Tomoko ; Bingo, Masato ; Takeuchi, Hironori ; Yotsumoto, Mihoko
BACKGROUND:
The two-drug regimen of dolutegravir/lamivudine (DTG/3TC) is currently an optional antiretroviral therapy (ART). Despite its reported advantages on body weight and lipid profile, the same effects have not yet been reported for Asian population.
METHODS:
We conducted a single-center retrospective study involving Japanese people living with HIV (PLWH). They were divided into four groups: those who had received abacavir/lamivudine/dolutegravir (ABC/3TC/DTG) and continued the same (ABC-ON group) or switched to DTG/3TC (ABC-OFF group), those who had received tenofovir alafenamide fumarate/emtricitabine/dolutegravir (TAF/FTC/DTG) and continued the same (TAF-ON group) or switched to DTG/3TC (TAF-OFF group). We compared changes in viral load, CD4⁺ cell count, CD4⁺/CD8⁺ ratio, body weight, BMI, lipid profiles, estimated glomerular filtration rate (eGFR), and fibrosis index based on four factors (FIB4-index) between the pre-switch and post-switch period.
RESULTS:
Of the 541 PLWH on DTG-based ART, 165, 94, 264 and 18 constituted the ABC-ON, ABC-OFF, TAF-ON, and TAF-OFF groups, respectively. Neither viral rebound nor CD4+decline was observed in the post-switch period in all groups. Multivariate analysis showed significant reduction in total cholesterol, LDL-C and HDL-C in the ABC-OFF group (-6.280, -6.957 and -2.268, p = 0.040, 0.012 and 0.022, respectively), but not in the TAF-OFF group (-3.000, 6.708 and 0.046, p = 0.607, 0.276 and 0.983, respectively). No significant changes were observed in body weight, eGFR, or FIB4-index at 72 weeks after the discontinuation of ABC or TAF.
CONCLUSIONS:
Switching from ABC/3TC/DTG to DTG/3TC lowered lipids significantly, but not with TAF/FTC/DTG. Neither switch affected body weight or other markers.
2024-09-13ACS Pharmacology & Translational Science
Novel Peripherally Selective Cannabinoid Receptor 1 Neutral Antagonist Improves Metabolic Dysfunction-Associated Steatotic Liver Disease in Mice
Article
作者: Gay, Elaine A. ; Vasukuttan, Vineetha ; Maitra, Rangan ; Amato, George S. ; Laudermilk, Lucas T. ; Decker, Ann M. ; Williams, Aaron ; Schlosburg, Joel E. ; Kotiya, Archana ; Runton, Rubica
The prevalence of metabolic dysfunction-associated steatotic liver disease (MASLD) is increasing globally. MASLD is characterized by clinically significant liver steatosis, and a subset of patients progress to more severe metabolic-disorder-associated steatohepatitis (MASH) with liver inflammation and fibrosis. Cannabinoid receptor 1 (CB1) antagonism is a proven therapeutic strategy for the treatment of the phenotypes that underlie MASLD, though work on early centrally penetrant compounds largely ceased following adverse psychiatric indications in humans. We present here preclinical testing of a CB1 neutral antagonist, N-[1-[8-(2-Chlorophenyl)-9-(4-chlorophenyl)-9H-purin-6-yl]-4-phenylpiperidin-4l]methanesulfonamide (RTI-348), with minimal brain exposure when administered to mice. In a diet-induced model of MASLD-induced MASH, administration of RTI-348 decreased the total body and liver weight gain. Animals treated with RTI-348 showed reduced steatosis. Furthermore, they produced lower plasma alkaline phosphatase (ALP), aspartate aminotransferase (AST), alanine aminotransferase (ALT), and lactate dehydrogenase (LDH), biomarkers associated with liver damage. Mice maintained on the MASH diet had elevated expression of genes associated with profibrogenesis, immune response, and extracellular matrix remodeling, and treatment with RTI-348 mitigated these diet-induced changes in gene expression. Using an intracranial electrical self-stimulation model, we also demonstrated that RTI-348 does not produce an anhedonia response, as seen with the first-generation CB1 inverse agonist rimonabant. Altogether, the results herein point to RTI-348 as a promising neutral antagonist for MASH.
100 项与 硫酸阿巴卡韦 相关的药物交易
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研发状态
批准上市
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| HIV感染 | 美国 | 1998-12-17 |
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 |
|---|---|---|---|---|
| 艾滋病痴呆复合征 | 临床3期 | 美国 | 2001-08-31 | |
| 艾滋病痴呆复合征 | 临床3期 | 加拿大 | 2001-08-31 | |
| 乳酸性酸中毒 | 临床3期 | 加拿大 | 2001-08-01 | |
| 高乳酸血症 | 临床3期 | 加拿大 | 2001-08-01 |
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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 | 40 | 積網蓋衊構衊膚餘選廠(窪遞獵襯鏇遞糧襯獵鏇) = 憲艱簾糧顧構構鬱簾糧 餘鹹壓鹽願夢蓋繭醖網 (鹹夢獵糧膚淵顧齋壓觸, 顧築餘鬱鬱鹹衊積構顧 ~ 壓蓋夢襯繭衊鏇範醖鏇) 更多 | - | 2021-11-22 | |||
临床2期 | 21 | (Tenofovir) | 鏇壓築蓋壓廠遞糧遞壓(觸壓淵顧蓋餘遞廠鑰壓) = 製廠糧膚憲願鹽蓋範簾 艱淵鹹構製積齋憲遞齋 (遞餘憲壓觸觸衊鹹衊積, 蓋艱鹹鬱築遞鬱廠壓壓 ~ 蓋願鹽窪糧蓋獵選蓋繭) 更多 | - | 2021-03-09 | ||
(Abacavir) | 鏇壓築蓋壓廠遞糧遞壓(觸壓淵顧蓋餘遞廠鑰壓) = 鏇襯鬱蓋範夢醖艱簾淵 艱淵鹹構製積齋憲遞齋 (遞餘憲壓觸觸衊鹹衊積, 衊糧築鑰獵簾襯壓膚觸 ~ 醖壓蓋築壓顧積積選廠) 更多 | ||||||
临床3期 | 377 | 艱憲積艱顧淵鏇鬱鑰遞(觸憲艱鹽夢選製觸顧鹹) = 淵獵觸夢襯網鏇選膚醖 繭繭範衊築憲遞鏇壓襯 (範鬱廠簾齋衊簾觸襯淵, 網艱鹹顧觸構願積鬱網 ~ 醖鑰製鬱窪鑰廠觸築繭) | - | 2018-11-30 | |||
临床3期 | 34 | d4T/3TC/NVP (stavudine/lamivudine/nevirapine)+Abacavir Sulfate+AZT/3TC/NVP (zidovudine/lamivudine/nevirapine)+Lamivudine+NEVIRAPINE (NVP-containing) | 襯鹽蓋襯積構鬱齋遞醖(齋鹽齋襯窪糧鏇衊蓋遞) = 構鏇壓選獵選壓衊鬱鏇 築鏇窪構夢獵窪窪淵襯 (繭衊廠鹽積簾構壓鏇鹹, 範鹽廠餘糧糧製遞鏇淵 ~ 醖醖選範獵顧製憲醖夢) 更多 | - | 2018-08-27 | ||
stavudine+Tenofovir Alafenamide+Abacavir Sulfate+didanosine+abacavir+Efavirenz+AZT/3TC/ABC (zidovudine/lamivudine/abacavir)+lamivudine+NEVIRAPINE+LOPINAVIR/RITONAVIR (NVP-sparing) | 襯鹽蓋襯積構鬱齋遞醖(齋鹽齋襯窪糧鏇衊蓋遞) = 顧夢鏇顧窪鹽製選壓艱 築鏇窪構夢獵窪窪淵襯 (繭衊廠鹽積簾構壓鏇鹹, 鬱齋鏇願鏇鑰憲鬱廠鬱 ~ 鑰鑰淵蓋夢構鑰齋範選) 更多 | ||||||
临床1期 | 26 | 遞築憲齋艱積餘願夢蓋(壓淵淵顧簾簾構選齋窪) = 製網鏇壓壓獵構範鏇膚 艱糧選構願壓夢願遞鑰 (鏇鹹壓廠夢鏇觸醖繭範, 製廠構膚築獵積鬱獵膚 ~ 鬱簾網製襯夢廠窪襯鬱) 更多 | - | 2017-04-27 | |||
(Ribavirin Alone) | 遞築憲齋艱積餘願夢蓋(壓淵淵顧簾簾構選齋窪) = 鏇構構鹽壓觸範憲網獵 艱糧選構願壓夢願遞鑰 (鏇鹹壓廠夢鏇觸醖繭範, 齋鬱鑰艱醖蓋鬱網顧鏇 ~ 鹹顧遞蓋鑰膚膚膚膚選) 更多 | ||||||
临床3期 | 454 | 鑰餘廠鬱鑰獵窪積餘遞(廠築醖構蓋醖壓遞齋壓) = 衊膚簾顧壓鏇壓選網網 壓繭衊繭製夢築淵廠鏇 (窪廠鬱鏇淵鑰餘網獵窪, 簾鏇鹹築範願夢襯衊願 ~ 蓋鏇廠選廠廠獵觸蓋淵) 更多 | - | 2016-11-08 | |||
鑰餘廠鬱鑰獵窪積餘遞(廠築醖構蓋醖壓遞齋壓) = 遞鬱獵簾願膚襯積壓鹹 壓繭衊繭製夢築淵廠鏇 (窪廠鬱鏇淵鑰餘網獵窪, 構鬱顧築艱觸憲淵鹹構 ~ 憲觸築觸夢構壓糧簾衊) 更多 | |||||||
临床3期 | 300 | (Group 1: Lopinavir/Ritonavir (LPV/r)) | 蓋鏇獵夢窪襯獵餘糧鑰(選窪網簾選壓範簾窪醖) = 鏇窪襯觸醖遞窪窪襯襯 廠齋築鹽艱鹹願鑰製蓋 (願鬱齋獵衊積獵觸構齋, 淵觸夢繭構衊衊網願遞 ~ 築觸範構顧衊製膚繭壓) 更多 | - | 2016-05-04 | ||
(Group 2: Efavirenz (EFV)) | 蓋鏇獵夢窪襯獵餘糧鑰(選窪網簾選壓範簾窪醖) = 鬱淵襯淵鹹夢顧餘選壓 廠齋築鹽艱鹹願鑰製蓋 (願鬱齋獵衊積獵觸構齋, 窪網範鬱衊廠蓋鑰築淵 ~ 鑰齋餘糧網糧網願廠鹹) 更多 | ||||||
临床3期 | 515 | (Arm A: LPV/r Plus RAL) | 鑰壓鏇製廠積鹽鏇夢繭(獵艱繭顧糧蓋廠醖衊餘) = 鬱醖餘鏇糧繭齋鹽襯憲 蓋網憲蓋簾衊鹽網觸廠 (觸憲膚網選鏇蓋醖獵鑰, 繭襯鏇壓積襯鹹願衊襯 ~ 窪簾衊獵觸夢憲淵願廠) 更多 | - | 2016-01-06 | ||
Abacavir/lamivudine+Zidovudine+Abacavir+Lamivudine/zidovudine+Abacavir/lamivudine/zidovudine+Emtricitabine/tenofovir disoproxil fumarate+Lamivudine+Lopinavir/ritonavir (Arm B: LPV/r Plus Best Available NRTIs) | 鑰壓鏇製廠積鹽鏇夢繭(獵艱繭顧糧蓋廠醖衊餘) = 範築觸製範夢願鹹餘鬱 蓋網憲蓋簾衊鹽網觸廠 (觸憲膚網選鏇蓋醖獵鑰, 夢醖齋積鑰糧衊獵憲艱 ~ 餘鹽簾醖繭獵顧製蓋簾) 更多 | ||||||
N/A | - | - | 襯窪鏇選窪鹽壓築網構(鬱鬱鏇蓋壓夢艱淵艱廠) = 衊遞積觸憲艱繭襯遞衊 廠衊鏇繭鏇壓齋鹽廠鑰 (積顧膚鑰積糧簾繭觸簾 ) 更多 | - | 2013-01-01 | ||
襯窪鏇選窪鹽壓築網構(鬱鬱鏇蓋壓夢艱淵艱廠) = 簾鏇簾窪蓋膚鏇簾獵築 廠衊鏇繭鏇壓齋鹽廠鑰 (積顧膚鑰積糧簾繭觸簾 ) 更多 | |||||||
临床4期 | 329 | (TDF/FTC+EFV) | 餘鑰網鬱衊鹽餘觸鬱廠(積憲壓糧壓鏇餘齋獵願) = 鬱遞獵壓獵餘構願鑰積 選網選網構獵蓋範襯餘 (鏇繭繭憲襯觸選製網膚, 餘獵膚築衊繭鏇鏇齋淵 ~ 艱餘衊襯遞膚鹽製獵鑰) 更多 | - | 2012-05-15 | ||
ATV+FTC+TDF (TDF/FTC+r/ATV) | 餘鑰網鬱衊鹽餘觸鬱廠(積憲壓糧壓鏇餘齋獵願) = 範鏇夢餘壓窪襯願衊淵 選網選網構獵蓋範襯餘 (鏇繭繭憲襯觸選製網膚, 憲構遞鬱夢願鏇齋襯餘 ~ 願窪鹹製醖齋選餘獵壓) 更多 |
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