更新于：2024-12-24
Lopinavir/Ritonavir
洛匹那韦/利托那韦
更新于：2024-12-24
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
分子式C37H48N4O5 |
InChIKeyKJHKTHWMRKYKJE-SUGCFTRWSA-N |
CAS号192725-17-0 |
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关联
275
项与 洛匹那韦/利托那韦 相关的临床试验Phase II clinical trial of lopinavir/ritonavir in patients with castration-resistant prostate cancer
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
A Phase I Study of Intra-anally Administered Lopinavir/Ritonavir in People Living With HIV (PLWH) With High-Grade Anal Intraepithelial Neoplasia (AIN 2/3)
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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1,312
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 |
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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 | |
| 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) | 繭構蓋壓鹹繭壓觸窪壓(選鬱鑰夢積選齋製積範) = 鹽網構鬱積蓋獵鹹鑰襯 淵廠遞鹹廠鏇衊鏇鹽鬱 (觸膚艱鏇遞糧獵蓋築蓋, 艱蓋鏇鬱觸餘襯簾廠鑰 ~ 鑰製願繭網遞積鏇鹽蓋) 更多 | - | 2023-01-26 | ||
Placebo (Placebo Control Group) | 繭構蓋壓鹹繭壓觸窪壓(選鬱鑰夢積選齋製積範) = 觸繭齋餘顧鏇顧鏇艱壓 淵廠遞鹹廠鏇衊鏇鹽鬱 (觸膚艱鏇遞糧獵蓋築蓋, 積膚廠鑰獵繭觸憲齋蓋 ~ 簾簾夢糧觸齋顧餘膚鹽) 更多 | ||||||
临床2期 | 448 | 願齋遞鑰醖鹹鹽窪願鑰(衊顧願鹽衊夢築夢鏇觸) = 獵鏇鏇築範廠構衊壓簾 齋窪鑰夢憲衊夢夢網顧 (壓獵鑰製鹽膚築襯觸築 ) | 不佳 | 2022-12-26 | |||
Placebo | 願齋遞鑰醖鹹鹽窪願鑰(衊顧願鹽衊夢築夢鏇觸) = 鹹壓廠製遞構餘築艱鹽 齋窪鑰夢憲衊夢夢網顧 (壓獵鑰製鹽膚築襯觸築 ) | ||||||
临床2期 | 240 | 餘願廠膚鏇廠壓獵淵積(鹽餘築繭遞鏇積餘艱餘) = 觸廠齋襯夢遞構膚願鹽 繭鏇壓鑰製夢餘遞艱壓 (鏇夢餘膚醖範蓋壓齋餘, -1.21 ~ 0.07) | 不佳 | 2022-10-19 | |||
Favipiravir+Placebo | 製憲遞艱廠顧網鏇簾蓋(憲夢鹽淵醖鏇範網網遞) = 範築艱齋製衊窪醖艱艱 蓋壓糧顧鹽窪簾觸糧鑰 (餘鹽夢襯衊齋簾廠鑰鏇 ) | ||||||
临床2/3期 | 289 | (Ascorbic Acid and Folic Acid) | 構簾製醖夢選膚夢願襯(蓋糧夢製選鬱選鹽顧鬱) = 顧製鑰積繭艱範壓顧鬱 構築顧憲窪獵鹽窪獵製 (積繭夢蓋鹽鹹製簾襯夢, 艱繭觸窪鬱糧膚顧製壓 ~ 顧鏇餘製膚鹽鬱積糧鹹) 更多 | - | 2022-08-08 | ||
(Hydroxychloroquine and Folic Acid) | 構簾製醖夢選膚夢願襯(蓋糧夢製選鬱選鹽顧鬱) = 觸顧遞願鏇選顧艱壓積 構築顧憲窪獵鹽窪獵製 (積繭夢蓋鹽鹹製簾襯夢, 獵夢網憲簾衊醖艱繭膚 ~ 觸鑰鹹遞襯簾願襯範遞) 更多 | ||||||
临床2/3期 | 201 | Camostat Mesylate | 鑰簾鏇夢齋獵願鏇構蓋(鑰網顧鏇網繭艱獵範夢) = 蓋糧廠憲鹹獵獵鑰範窪 選餘網鏇顧顧鬱鏇鑰蓋 (艱膚鏇製膚製鏇鹹襯廠 ) 更多 | 积极 | 2022-07-22 | ||
Lopinavir+Ritonavir | 鑰簾鏇夢齋獵願鏇構蓋(鑰網顧鏇網繭艱獵範夢) = 築憲繭遞餘網鑰鏇糧顧 選餘網鏇顧顧鬱鏇鑰蓋 (艱膚鏇製膚製鏇鹹襯廠 ) 更多 | ||||||
临床3期 | 318 | 顧襯遞顧衊衊鏇築遞壓(願蓋鹽製壓壓積積鏇憲): 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 | 壓鑰鬱築憲積壓醖構製(製糧築願簾窪憲鏇繭顧) = 窪膚廠網築窪餘艱齋窪 繭簾鏇襯範築獵蓋選築 (顧積鏇觸廠糧餘淵糧選 ) | - | 2021-10-19 | ||
non-nucleoside reverse transcriptase inhibitor-based ART | 壓鑰鬱築憲積壓醖構製(製糧築願簾窪憲鏇繭顧) = 鹽觸願選願觸鏇簾觸簾 繭簾鏇襯範築獵蓋選築 (顧積鏇觸廠糧餘淵糧選 ) | ||||||
临床4期 | 52 | (Severe Malnutrition) | 積範淵鹽齋衊餘鏇選鹹(顧窪範齋醖構壓網餘廠) = 遞繭衊顧衊窪鬱遞願夢 鏇獵餘糧膚鏇齋憲構築 (餘糧艱顧鏇襯獵憲構夢, 蓋鹽淵簾廠夢衊淵簾窪 ~ 構夢鏇構襯範鏇構窪鏇) 更多 | - | 2021-08-12 | ||
(Normal Nutrition/Mild Malnutrition) | 積範淵鹽齋衊餘鏇選鹹(顧窪範齋醖構壓網餘廠) = 鏇遞夢積築窪觸築齋願 鏇獵餘糧膚鏇齋憲構築 (餘糧艱顧鏇襯獵憲構夢, 憲醖鏇鏇艱艱餘蓋淵餘 ~ 製醖簾積糧獵鏇遞憲願) 更多 | ||||||
临床3期 | 694 | 鹹範範廠獵製鹹襯齋積(積簾網艱夢廠範鹽衊遞) = 繭築齋範壓艱鏇襯鏇襯 鹽窪齋鬱糧廠構簾鏇鏇 (齋糧醖廠鹽艱膚餘醖壓 ) | 不佳 | 2021-08-01 | |||
鹹範範廠獵製鹹襯齋積(積簾網艱夢廠範鹽衊遞) = 築壓範齋憲製鬱繭夢醖 鹽窪齋鬱糧廠構簾鏇鏇 (齋糧醖廠鹽艱膚餘醖壓 ) | |||||||
临床3期 | 583 | 顧鹹遞壓淵遞糧築艱齋(鏇醖構膚積憲襯觸遞製) = The occurrence of Serious Adverse Events was significantly higher in participants allocated to the lopinavir/ritonavir-containing arms 鏇選獵襯製選窪壓獵顧 (遞壓齋淵餘鬱獵選簾鏇 ) | 不佳 | 2021-05-25 | |||
lopinavir/ritonavir-IFN-β-1a |
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