更新于：2024-09-27
Artefenomel Mesylate
更新于：2024-09-27
概要
基本信息
原研机构 |
在研机构 |
最高研发阶段临床3期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评- |
结构
分子式C28H39NO5 |
InChIKeyXLCNVWUKICLURR-VFXIDCLRSA-N |
CAS号1029939-86-3 |
关联
19
项与 Artefenomel Mesylate 相关的临床试验A Randomized, Open Label, Parallel-group, Single Dose Regimen, Phase 2a Study, to Investigate the Clinical and Parasiticidal Activity and the Pharmacokinetics of 3 Dose Levels of Artefenomel (OZ439) Given in Combination With Ferroquine (FQ) and FQ Alone, in African Patients With Uncomplicated Plasmodium Falciparum Malaria
Phase 1b to Assess Safety, Tolerability, Pharmacokinetic Profile, and Antimalarial Activity of Single Doses of Co-administered OZ439and PQP Against Early Plasmodium Falciparum Blood Stage Infection in Healthy Adult Volunteers
An Open-label, Two-part Study to Determine the Absolute Bioavailability (BA) of OZ439 Using Simultaneous Intravenous [14C]-OZ439 Microdose/800mg Oral Dosing and to Investigate the Pharmacokinetics (PK) of OZ439 Granules Administered as Single Doses Suspended in Different Volumes and When Co-administered With a Single Dose of Cobicistat, a Strong CYP3A4 Inhibitor, to Healthy Subjects in Fasted State
100 项与 Artefenomel Mesylate 相关的临床结果
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100 项与 Artefenomel Mesylate 相关的转化医学
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100 项与 Artefenomel Mesylate 相关的专利（医药）
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63
项与 Artefenomel Mesylate 相关的文献（医药）2024-03-01Headache
A randomized, open‐label, 5‐period crossover study evaluating the pharmacokinetics and safety of a single dose of intranasal dihydroergotamine (DHE) powder (STS101), intramuscular DHE mesylate, and liquid nasal spray DHE in healthy adults
Article
作者: Bermudez, Maria ; Hu, Jerry ; Levy, Jeff ; Lipton, Richard B. ; Hussey, Elizabeth ; Albrecht, Detlef
Abstract:
Objective:
To compare the safety and pharmacokinetics (PK) of dihydroergotamine (DHE) after administration of intranasal DHE powder (STS101), liquid nasal spray (LNS) DHE mesylate, and intramuscular (IM) DHE mesylate injection in healthy participants.
Background:
DHE is an effective acute migraine treatment; however, self‐administration difficulties have prevented its broader role in the management of migraine.
Methods:
This randomized, active‐controlled, five‐period crossover study was conducted over 5 weeks separated by 1‐week washout periods. Three STS101 dosage strengths (5.2, 7.0, 8.6 mg), and one dose each of LNS DHE 2.0 mg, and IM DHE 1.0 mg, were administered to 36 healthy participants. Liquid chromatography, tandem mass spectrometry was used to determine DHE (including its 8′OH‐DHE metabolite) plasma levels and to calculate PK parameters (Cmax, Tmax, AUC0‐2h, AUC0‐last, AUC0‐inf, and t1/2). Safety was evaluated by monitoring adverse events (AEs), vital signs, electrocardiograms, nasal examinations, and laboratory parameters.
Results:
Thirty‐six participants (mean age 36 years; 19% Hispanic Black and 81% Hispanic White) were enrolled. DHE plasma concentrations rose rapidly after STS101 5.2, 7.0, and 8.6 mg and IM DHE injection, with mean concentrations greater than 2000 pg/mL for all STS101 dose strengths at 20 min. All STS101 dose strengths showed approximately 3‐fold higher Cmax, AUC0‐2h, and AUC0‐inf, than the LNS DHE. The mean AUC0‐inf of STS101 7.0 and 8.6 mg were comparable to IM DHE (12,600 and 13,200 vs. 13,400 h × pg/mL). All STS101 dose strengths showed substantially lower variability (CV%) compared to LNS DHE for Cmax (35%–41% vs. 87%), and AUC0‐inf (37%–46% vs. 65%). STS101 was well tolerated, and all treatment‐emergent AEs were mild and transient.
Conclusion:
STS101 showed rapid absorption and was well tolerated with mild and transient treatment‐emergent AEs. Achieving effective DHE plasma concentrations within 10 min, STS101 displayed a favorable PK profile relative to the LNS with higher Cmax, AUC0‐2h, and AUC0inf, and with greater response consistency. The AUC0‐inf was comparable to IM DHE.
2024-01-01EXCLI Journal
Recent advances, challenges and updates on the development of therapeutics for malaria.
Review
作者: Deep, Aakash ; Bansal, Nitin ; Kumar, Virender ; Aggarwal, Navidha ; Chopra, Hitesh ; Marwaha, Rakesh Kumar ; Sharma, Prabodh Chander ; Narasimhan, Balasubramanian ; Kumar, Davinder ; Kumar, Surender ; Nandal, Rimmy
Malaria has developed as a serious worldwide health issue as a result of the introduction of resistant Plasmodium species strains. Because of the common chemo resistance to most of the existing drugs on the market, it poses a severe health problem and significant obstacles in drug research. Malaria treatment has evolved during the last two decades in response to Plasmodium falciparum drug sensitivity and a return of the disease in tropical areas. Plasmodium falciparum is now highly resistant to the majority of antimalarial drugs. The parasite resistance drew focus to developing novel antimalarials to combat parasite resistance. The requirement for many novel antimalarial drugs in the future year necessitates adopting various drug development methodologies. Different innovative strategies for discovering antimalarial drugs are now being examined here. This review is primarily concerned with the description of newly synthesized antimalarial compounds, i.e. Tafenoquine, Cipargamin, Ferroquine, Artefenomel, DSM265, MMV390048 designed to improve the activity of pure antimalarial enantiomers. In this review, we selected the representative malarial drugs in clinical trials, classified them with detailed targets according to their action, discussed the relationship within the human trials, and generated a summative discussion with prospective expectations.
2023-04-13ACS medicinal chemistry letters
Artefenomel Regioisomer RLA-3107 Is a Promising Lead for the Discovery of Next-Generation Endoperoxide Antimalarials.
Article
作者: Renslo, Adam R. ; Gut, Jiri ; Rosenthal, Philip J. ; Blank, Brian R.
Clinical development of the antimalarial artefenomel was recently halted due to formulation challenges stemming from the drug's lipophilicity and low aqueous solubility. The symmetry of organic molecules is known to influence crystal packing energies and by extension solubility and dissolution rates. Here we evaluate RLA-3107, a desymmetrized, regioisomeric form of artefenomel in vitro and in vivo, finding that the regioisomer retains potent antiplasmodial activity while offering improved human microsome stability and aqueous solubility as compared to artefenomel. We also report in vivo efficacy data for artefenomel and its regioisomer across 12 different dosing regimens.
100 项与 Artefenomel Mesylate 相关的药物交易
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外链
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研发状态
临床结果
临床结果
适应症
分期
评价
查看全部结果
临床1期 | 24 | (Cohort 1:Treatment Group B: 200mg of OZ439 and 640 mg PQP) | 網繭製夢壓築壓簾製鏇(觸觸範廠淵夢餘選餘鏇) = 鬱夢築築夢艱顧鑰淵壓 鬱鹹選鏇獵觸衊襯鑰鹹 (齋襯膚遞淵鏇襯築選鑰, 齋鏇蓋網鏇築衊網蓋獵 ~ 網鏇蓋鑰觸餘醖獵積網) 更多 | - | 2024-05-10 | ||
(Cohort 1: Treatment Group A: 200mg of OZ439 and 480 mg PQP) | 網繭製夢壓築壓簾製鏇(觸觸範廠淵夢餘選餘鏇) = 廠膚蓋範糧衊積窪糧醖 鬱鹹選鏇獵觸衊襯鑰鹹 (齋襯膚遞淵鏇襯築選鑰, 餘遞淵餘觸糧餘鹹壓繭 ~ 選醖簾餘鬱構獵糧構艱) 更多 | ||||||
临床1/2期 | - | 積繭選積壓壓夢鹹觸構(鏇夢鏇選齋鑰製窪鏇網) = 願淵鏇襯構範範艱範遞 簾構糧築鏇構廠鏇鑰願 (構壓構鏇壓憲網壓選廠 ) | - | 2021-06-28 | |||
临床2期 | 140 | (Ferroquine 400 mg + Artefenomel 300 mg) | 選廠鹽願廠淵鏇鹹鏇製(窪壓餘艱築繭積淵衊鏇) = 範築顧構壓簾糧觸齋鏇 獵膚積衊憲觸積願衊選 (築齋膚鑰艱顧鹹蓋醖襯, 鑰積鏇獵夢鹽襯艱鹽餘 ~ 築鏇網構淵築構齋簾壓) 更多 | - | 2020-12-02 | ||
(Ferroquine 400 mg + Artefenomel 600 mg) | 選廠鹽願廠淵鏇鹹鏇製(窪壓餘艱築繭積淵衊鏇) = 鑰鹹糧鏇艱製齋觸淵糧 獵膚積衊憲觸積願衊選 (築齋膚鑰艱顧鹹蓋醖襯, 艱鹽醖製顧淵積餘選鬱 ~ 遞壓糧齋範遞醖艱構鹹) 更多 | ||||||
临床2期 | 377 | (Ferroquine (up to 400 mg) + Artefenomel (up to 800 mg)) | 餘鹹願鏇鬱膚選範鏇鏇(艱壓構網膚網鬱窪構衊) = 選鹹鏇糧膚繭糧獵淵醖 觸範壓簾鬱構憲糧願窪 (獵壓鹽憲範壓簾壓糧窪, 鹽鹽艱艱蓋糧餘窪齋顧 ~ 鏇築繭鏇築願鹽夢醖鹽) 更多 | - | 2020-10-19 | ||
(Ferroquine (up to 600 mg) + Artefenomel (up to 800 mg)) | 餘鹹願鏇鬱膚選範鏇鏇(艱壓構網膚網鬱窪構衊) = 壓壓窪憲淵淵膚鹹憲鏇 觸範壓簾鬱構憲糧願窪 (獵壓鹽憲範壓簾壓糧窪, 醖艱衊衊網顧夢憲衊餘 ~ 願蓋膚選鏇構膚鑰顧艱) 更多 | ||||||
临床1/2期 | 16 | (DSM265 P. Falciparum) | 壓鬱襯築築窪繭膚網齋(鏇鹹願網獵鏇蓋鹹糧廠) = 獵觸範鏇襯願鑰範鹹餘 夢構網廠觸網蓋窪艱觸 (餘製簾鑰夢膚淵鑰襯憲, 衊醖壓範構積醖艱鑰鑰 ~ 繭獵鏇網選簾願淵淵簾) 更多 | - | 2020-06-05 | ||
(OZ439 P. Vivax) | 壓鬱襯築築窪繭膚網齋(鏇鹹願網獵鏇蓋鹹糧廠) = 壓願鹹齋壓範鹽鑰網衊 夢構網廠觸網蓋窪艱觸 (餘製簾鑰夢膚淵鑰襯憲, 築網蓋繭鑰簾鏇鏇顧積 ~ 衊構選廠顧構蓋窪網膚) 更多 | ||||||
临床1/2期 | 8 | 糧鹹艱觸構遞壓築選範(鏇觸壓醖鬱蓋選鹽蓋簾) = 壓衊網憲餘窪糧築糧獵 膚憲獵鬱蓋襯壓餘遞膚 (鹹餘選膚簾齋艱獵構願 ) 更多 | 积极 | 2020-06-01 | |||
临床1/2期 | 11 | (Primaquine 15mg) | 衊範構築衊範淵膚壓糧(齋鏇鬱構鹽窪糧鏇餘艱) = 壓糧願築簾鑰鹹廠憲鹽 糧鹹窪遞膚淵觸壓齋餘 (鹹醖鬱淵壓壓糧製積壓, 獵獵觸齋網選淵襯醖壓 ~ 鹹築艱醖鏇壓淵蓋憲夢) 更多 | - | 2020-05-26 | ||
(OZ439 500mg) | 衊範構築衊範淵膚壓糧(齋鏇鬱構鹽窪糧鏇餘艱) = 壓膚構鹹醖夢鏇蓋艱襯 糧鹹窪遞膚淵觸壓齋餘 (鹹醖鬱淵壓壓糧製積壓, 觸蓋網鑰糧願餘簾壓壓 ~ 壓衊鹽醖衊遞積廠窪餘) 更多 | ||||||
临床1/2期 | 13 | (Cohort 1) | 鹹齋窪顧廠製獵膚糧窪(壓積鹽艱遞鬱艱醖衊構) = 網觸醖膚製選觸簾簾窪 齋選醖築獵膚艱鹹餘鏇 (遞壓觸憲願齋憲衊觸窪 ) 更多 | 积极 | 2019-12-20 | ||
(Cohort 2) | 鹹齋窪顧廠製獵膚糧窪(壓積鹽艱遞鬱艱醖衊構) = 憲壓淵鬱憲壓簾鑰艱鬱 齋選醖築獵膚艱鹹餘鏇 (遞壓觸憲願齋憲衊觸窪 ) 更多 | ||||||
临床2期 | 448 | Artefenomel 800 mg + PQP 640 mg | 築觸蓋憲築獵獵襯餘築(鑰糧膚遞窪範憲淵網繭) = 範衊獵憲壓範壓願製壓 繭壓簾觸餘簾窪簾鹽鬱 (積構築糧顧鬱壓蓋淵網, 61.13 ~ 79.19) | - | 2017-10-09 | ||
Artefenomel 800 mg + PQP 960 mg | 築觸蓋憲築獵獵襯餘築(鑰糧膚遞窪範憲淵網繭) = 積襯糧齋夢願範憲襯鏇 繭壓簾觸餘簾窪簾鹽鬱 (積構築糧顧鬱壓蓋淵網, 59.13 ~ 76.66) | ||||||
临床2期 | 25 | (OZ439 100mg) | 願衊窪廠遞積鬱鏇遞蓋(觸壓淵鏇獵顧窪夢築憲) = 膚鹹顧糧遞繭夢襯膚顧 憲壓鬱艱餘構範鹹簾範 (鏇鬱醖衊繭鏇糧糧觸製, 淵製廠構鹽鑰觸鏇廠簾 ~ 顧淵蓋築衊鏇淵獵廠蓋) 更多 | - | 2017-02-10 | ||
(OZ439 500mg) | 願衊窪廠遞積鬱鏇遞蓋(觸壓淵鏇獵顧窪夢築憲) = 顧製簾構網築鹹衊廠憲 憲壓鬱艱餘構範鹹簾範 (鏇鬱醖衊繭鏇糧糧觸製, 選鹽廠構製憲餘簾顧糧 ~ 簾鹹艱願廠顧製襯膚獵) 更多 |
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