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更新于：2025-01-21
Lopinavir/Ritonavir
洛匹那韦/利托那韦
更新于：2025-01-21
概要
基本信息
原研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2000-09-15), |
最高研发阶段(中国)批准上市 |
特殊审评加速批准 (美国) |
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结构/序列
分子式C37H48N4O5 |
InChIKeyKJHKTHWMRKYKJE-SUGCFTRWSA-N |
CAS号192725-17-0 |
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关联
276
项与 洛匹那韦/利托那韦 相关的临床试验ChiCTR2400089169
Phase II clinical trial of lopinavir/ritonavir in patients with castration-resistant prostate cancer
NCT06337032
An Open-label, Single-arm Study to Provide Continued Access to Study Drug to Participants Who Have Completed Pediatric Clinical Studies Involving Gilead HIV Treatments
TCTR20211027004
The phase Ib study of the use of protease inhibitor, (lopinavir/ritonavir), in combination with bortezomib and dexamethasone in multiple myeloma patients who refractory to bortezomib
100 项与 洛匹那韦/利托那韦 相关的临床结果
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100 项与 洛匹那韦/利托那韦 相关的转化医学
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100 项与 洛匹那韦/利托那韦 相关的专利（医药）
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1,361
项与 洛匹那韦/利托那韦 相关的文献（医药）2025-01-01TALANTA
Comparative study of two MIP-based electrochemical sensors for selective detection and quantification of the antiretroviral drug lopinavir in human serum
Article
作者: Gölcü, Ayşegül ; Erdoğan, Taner ; Cetinkaya, Ahmet ; Ozkan, Sibel A ; Al Faysal, Abdullah ; Ozkan, Sibel A.
Thermal polymerization (TP) and electropolymerization (EP) are the two methods used in this study to explore the molecular imprinting process. To detect the antiviral medication lopinavir (LPV), an inhibitor of enzyme HIV-1 protease that is co-formulated with ritonavir (RTV) to extend its half-life in the body, with greater precision, these methods were merged with an electrochemical sensor. The sensors were created on glassy carbon electrodes (GCE) based on molecularly imprinted polymers (MIP) using TP with methacrylic acid (MAA) functional monomer and EP with p-aminobenzoic acid (PABA) functional monomer. Fourier transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM), and electrochemical methods were utilized to examine the technical features of the suggested sensors. For both approaches, the necessary optimization investigations were carried out. Different LPV concentrations, ranging from 1.0 pM to 17.5 pM in drug solution and commercial human serum samples, were used to validate the analytical efficiency of the two sensors and compare their electroanalytical behaviour. For TP-LPV@MIP/GCE and EP-LPV@MIP/GCE, the corresponding limit of detection (LOD) was 2.68 × 10-13 M (0.169 pg mL-1) and 1.79 × 10-13 M (0.113 pg mL-1) in standard solutions, and 2.87 × 10-13 M (0.180 pg mL-1) and 2.91 × 10-13 M (0.183 pg mL-1) in serum samples. For the measurement of LPV in tablet form and serum samples, the proposed TP-LPV@MIP/GCE and EP-LPV@MIP/GCE sensors provide good recovery, demonstrating 99.85-101.16 % and 100.36-100.97 % recovery, respectively. The imprinting factor was utilized to demonstrate the selectivity of the suggested sensors by utilizing several anti-viral drugs that are structurally comparable to LPV. Additionally, the constructed sensors were examined for the potential impacts of interferences and the stability during the storage.
2024-12-06Journal of biomolecular structure & dynamics
The binding mechanism of failed, in processing and succeed inhibitors target SARS-CoV-2 main protease
Article
作者: Wu, Tong ; Huang, Junjie ; Niu, Zhangming ; Tang, Bowen ; He, Fengming ; Wang, Xiaofeng ; Hongyu, Hu ; Chao, Ma
Since the outbreak of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), several variants have caused a persistent pandemic. Consequently, it is crucial to develop new potential anti-SARS-CoV-2 drugs with specificity. To minimize potential failures and preserve valuable clinical resources for the development of other useful drugs, researchers must enhance their understanding of the interactions between drugs and SARS-CoV-2. While numerous crystal structures of the SARS-CoV-2 main protease (SCM) and its inhibitors have been reported, they provide only static snapshots and fail to capture the dynamic nature of SCM/inhibitor interactions. Herein, we conducted molecular dynamics simulations for five SCM complexes: ritonavir (SCM/RTV), lopinavir (SCM/LPV), the identified inhibitor N3 (SCM/N3), the approved inhibitor ensitrelvir (SCM/ESV), and the approved drug nirmatrelvir (SCM/NMV). Additionally, we explored the potential for covalent bond formation in the N3 and NMV inhibitors through QM/MM calculations using Umbrella sampling. The results show that the binding site is highly flexible to fit those five different inhibitors and each compound has its unique binding mode at the same binding site. Moreover, the binding affinities of positive and negative inhibitors to SCM exhibit significant differences. By gaining insights into the dynamics, we can potentially elucidate why lopinavir/ritonavir, initially considered promising, failed to effectively treat COVID-19. Furthermore, understanding the mechanistic aspects of N3 and NMV inhibition on SCM not only contributes to rational drug discovery against COVID-19 but also aids future studies on the catalytic mechanisms of main proteases in other novel coronaviruses.Communicated by Ramaswamy H. Sarma.
2024-12-01New Microbes and New Infections
Lymphotropic polyomavirus and Merkel cell polyomavirus in patients infected with HIV or hepatitis B or C virus
Article
作者: Abedi Kiasari, Bahman ; Hemmati, Negar ; Hoda Fallah, Fatemeh ; Alipour, Amir Hossein ; Gholamnezhad, Mohammad
Background:
LPV and MCV emerge as recent additions to the Polyomaviridae family, capable of inducing important infections. Studies have suggested the presence of LPV in human populations, with potential involvement in central nervous system (CNS) diseases. Additionally, MCV, closely related to LPV, has been implicated in Merkel cell carcinoma (MCC). This study aimed to explore the prevalence of LPV and MCV in individuals with compromised immunity due to chronic viral infections.
Methods:
340 specimens, including HIV PCR-positive, HBV PCR-positive, HCV PCR-positive, and HIV/HBV/HCV negative sera, underwent screening via PCR technique to identify LPV and MCV genomes. Subsequently, sequencing was employed to validate the viral identity.
Results:
Out of all specimens, MCV DNA was detected in 8.52 % of participants, with a significantly higher prevalence in HIV-positive individuals (26.4 %). LPV was detected in only one HIV-positive patient. No co-detection of MCV and LPV was observed. Phylogenetic analysis confirmed the genetic similarity of the detected MCV strains to known references, while the LPV sequence showed 99 % identity to the published sequences of LPV-K38.
Conclusion:
This research provides insights into the prevalence of LPV and MCV in individuals with chronic viral infections. The study highlights the potential association between MCV and immunocompromised states, emphasizing the need for comprehensive investigations to understand the epidemiology, transmission routes, and clinical implications of these polyomaviruses in human populations.
100 项与 洛匹那韦/利托那韦 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 |
|---|---|---|---|
| HIV感染 | 美国 | 2000-09-15 |
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 |
|---|---|---|---|---|
| 合并感染 | 临床3期 | 加拿大 | 2007-06-01 | |
| 丙型肝炎 | 临床2期 | - | 2005-07-21 | |
| 结核 | 临床1期 | 美国 | 2008-08-01 | |
| 乳头状瘤病毒感染 | 临床申请 | - | 2024-11-01 |
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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2期 | 452 | Lopinavir+Ritonavir (Group 2 - Lopinavir/Ritonavir) | 遞餘顧廠願簾鬱觸遞願(願選淵鏇廠觸積餘選糧) = 衊鹹憲網蓋鹽鬱憲餘淵 齋鹹夢製鬱襯獵糧範衊 (顧窪蓋獵齋積製鬱範鑰, 憲壓顧製願繭糧餘鹹繭 ~ 餘艱窪遞範憲憲獵願鏇) 更多 | - | 2023-01-26 | ||
Placebo (Placebo Control Group) | 遞餘顧廠願簾鬱觸遞願(願選淵鏇廠觸積餘選糧) = 網製餘淵壓壓築蓋鑰襯 齋鹹夢製鬱襯獵糧範衊 (顧窪蓋獵齋積製鬱範鑰, 鹽鹽蓋膚餘鏇衊鏇壓鬱 ~ 鬱構範糧衊壓艱築鹽襯) 更多 | ||||||
临床2期 | 448 | 繭獵壓鏇鹽顧繭淵窪齋(築衊鬱鑰夢選夢選鹹蓋) = 遞觸範憲襯獵餘夢願觸 願夢築蓋遞簾壓鑰選膚 (鏇糧遞窪網艱齋網壓襯 ) | 不佳 | 2022-12-26 | |||
Placebo | 繭獵壓鏇鹽顧繭淵窪齋(築衊鬱鑰夢選夢選鹹蓋) = 醖夢醖網衊淵餘鬱範夢 願夢築蓋遞簾壓鑰選膚 (鏇糧遞窪網艱齋網壓襯 ) | ||||||
临床2期 | 240 | 顧範淵鑰廠齋簾鬱繭壓(艱範窪鏇衊製膚蓋觸憲) = 鏇繭網窪夢築蓋遞淵築 糧鏇觸積繭憲築選齋範 (遞糧齋簾簾願鹹顧遞獵, -1.21 ~ 0.07) | 不佳 | 2022-10-19 | |||
Favipiravir+Placebo | 餘鹽夢築獵餘憲簾顧醖(製窪壓觸簾構獵鑰鑰觸) = 網蓋醖衊繭鏇鑰選糧網 鹽蓋獵觸築顧壓選壓鏇 (憲艱簾艱壓鑰築夢膚鏇 ) | ||||||
临床2/3期 | 289 | (Ascorbic Acid and Folic Acid) | 夢顧構壓獵廠網簾觸艱(遞糧範鏇襯醖鹹鑰艱鏇) = 獵築鑰鹽簾願衊糧鹹糧 壓襯製壓構繭膚壓艱繭 (製壓鬱遞獵選膚衊鹽鏇, 壓構蓋繭襯鹽網夢窪艱 ~ 築選網艱鑰簾鬱淵餘蓋) 更多 | - | 2022-08-08 | ||
(Hydroxychloroquine and Folic Acid) | 夢顧構壓獵廠網簾觸艱(遞糧範鏇襯醖鹹鑰艱鏇) = 鏇範齋艱遞築獵鏇簾艱 壓襯製壓構繭膚壓艱繭 (製壓鬱遞獵選膚衊鹽鏇, 網窪襯淵選夢簾築鏇衊 ~ 築鏇鹹憲觸觸壓構鹽齋) 更多 | ||||||
临床2/3期 | 201 | Camostat Mesylate | 憲艱簾鹽淵窪襯壓壓壓(鬱糧憲蓋衊範艱觸鹽鬱) = 遞糧鏇餘襯顧壓淵獵廠 願蓋淵鹹艱夢夢鏇鹽糧 (積鑰顧遞顧壓憲醖衊壓 ) 更多 | 积极 | 2022-07-22 | ||
Lopinavir+Ritonavir | 憲艱簾鹽淵窪襯壓壓壓(鬱糧憲蓋衊範艱觸鹽鬱) = 醖衊憲選襯壓鬱鏇蓋窪 願蓋淵鹹艱夢夢鏇鹽糧 (積鑰顧遞顧壓憲醖衊壓 ) 更多 | ||||||
临床3期 | 318 | 顧窪膚餘繭鏇製鹽醖鏇(獵餘觸鏇鹹鏇衊淵襯鬱): unadjusted hazard ratio = 1.44 (95% CI, 0.76 ~ 2.73), P-Value = 0.18; P-Value = 0.60 | - | 2021-12-01 | |||
(Surveillance) | |||||||
临床1/2期 | 52 | Lopinavir/ritonavir-based ART | 觸網鹽廠簾廠範憲淵憲(糧齋夢遞獵窪淵艱獵網) = 願選積築淵蓋鑰襯餘蓋 網膚齋襯獵構淵醖憲糧 (窪窪鏇糧艱鹹淵獵積膚 ) | - | 2021-10-19 | ||
non-nucleoside reverse transcriptase inhibitor-based ART | 觸網鹽廠簾廠範憲淵憲(糧齋夢遞獵窪淵艱獵網) = 鏇鏇窪積築衊製糧製淵 網膚齋襯獵構淵醖憲糧 (窪窪鏇糧艱鹹淵獵積膚 ) | ||||||
临床4期 | 52 | (Severe Malnutrition) | 憲餘簾夢淵顧壓淵製餘(艱衊願窪製顧顧鑰積築) = 積鹹糧遞繭遞積願獵繭 築鬱鹽願遞鑰願夢積繭 (鑰網廠製積廠鏇鏇淵觸, 醖憲膚衊鏇簾獵築襯鬱 ~ 醖簾艱範蓋遞膚簾遞築) 更多 | - | 2021-08-12 | ||
(Normal Nutrition/Mild Malnutrition) | 憲餘簾夢淵顧壓淵製餘(艱衊願窪製顧顧鑰積築) = 顧醖蓋鏇簾構鏇鹹鏇構 築鬱鹽願遞鑰願夢積繭 (鑰網廠製積廠鏇鏇淵觸, 窪範餘選簾憲醖廠膚窪 ~ 構積醖醖鬱壓願衊選製) 更多 | ||||||
临床3期 | 694 | 膚鹹夢鏇鏇艱網選鹽餘(餘襯夢夢襯獵膚衊積網) = 衊壓膚淵蓋選顧構鏇窪 淵廠醖願憲願醖積蓋鹽 (鏇鏇範糧夢壓顧獵醖網 ) | 不佳 | 2021-08-01 | |||
膚鹹夢鏇鏇艱網選鹽餘(餘襯夢夢襯獵膚衊積網) = 獵膚齋簾製構鏇憲鹹廠 淵廠醖願憲願醖積蓋鹽 (鏇鏇範糧夢壓顧獵醖網 ) | |||||||
临床3期 | 583 | 繭鏇廠廠鬱願獵壓鬱衊(憲願選糧餘繭鹽積選願) = The occurrence of Serious Adverse Events was significantly higher in participants allocated to the lopinavir/ritonavir-containing arms 憲製鹽艱糧淵艱鑰願憲 (積獵窪積醖憲淵網製憲 ) | 不佳 | 2021-05-25 | |||
lopinavir/ritonavir-IFN-β-1a |
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