A Double-blind, Placebo-controlled, Phase I Study of the Pharmacokinetic and Pharmacodynamic Interaction of Oral AFA-281 With Alcohol in Healthy Volunteers

The goal of this clinical trial is to evaluate if alcohol interacts with the drug candidate AFA-281 in adults (healthy volunteers). This trial will evaluate blood concentration levels of AFA-281 and ethanol. The main questions it aims to answer are: Does alcohol interact with AFA-281? What are the side effects (if any)? Researchers will compare AFA-281 to a placebo (a look-alike substance that contains no drug) to see if AFA-281 interacts with alcohol.
Participants will take a total of 4 treatment sessions separated by at least 2 days between treatments. The treatments will incorporate AFA-281 or placebo with ethanol or ethanol placebo. After each treatment vital signs will be monitored and blood collected to measure AFA-281 and ethanol levels. Participants will provide an assessment survey of symptoms. The total treatment time will be 9 inpatient days (8 nights), and a final follow-up visit 3 to 5 days after clinic discharge.

开始日期2025-07-01

申办/合作机构

AfaSci, Inc.

NCT06819189

/ Recruiting临床1期IIT

Role of Metal Ion Transporter ZIP8 in Alcohol Related Behaviors

Background:
Alcohol use disorder (AUD) can damage people s health, work, and family. Researchers want to know more about why some people are more vulnerable to AUD than others. The ZIP8 gene may be linked to an increased risk of AUD. Researchers want to find out how different forms of the ZIP8 gene affect how healthy people drink alcohol and how alcohol affects their brain.
Objective:
To study how genes may affect how people drink alcohol and how it affects their brain.
Eligibility:
Healthy people aged 21 to 60 years. They must not smoke, and they must have no history of AUD. They must have European ancestry and be enrolled in Natural History Protocol (14-AA-0181).
Design:
Participants will have 2 study visits.
At the first visit, participants will be given alcohol; it will be infused through a tube attached to a needle inserted into a vein. They may self-administer each dose by pressing a button. Over time, they will have to press the button an increasing number of times to receive more alcohol. The infusion period will last 2.5 hours.
Participants will have blood samples taken and breath measurments, and they will do computer tasks and complete questionnaires during and after the infusion. After the infusion, they will remain in the clinic until their breath alcohol levels drop to a safe level.
At the second visit, participants will have an imaging scan of their brain. They will do tasks and play games on a computer screen during the scan.
Some participants may have an extra visit for screening. A mid-study visit may also be needed if more than 6 months pass between the 2 study visits....

开始日期2025-05-20

申办/合作机构

National Institute on Alcohol Abuse & Alcoholism

NCT06865872

/ RecruitingN/AIIT

Alcohol and Sexual Communication Among Couples in the Laboratory

Intimate Partner Sexual Violence (IPSV) is a significant and understudied public health problem among sexual minority (SM) and heterosexual couples, yet little is known about factors that contribute to IPSV perpetration. This proposal aims to determine the acute effect of alcohol and sexual communication on IPSV. In this study, 240 couples (50% SM) who drink alcohol will be recruited from the Metro-Denver area. Upon arrival to the laboratory, a trained research assistant will check the participant's ID, verify that they adhered to the pre-session guidelines, administer a breath test to ensure a breath alcohol content (BrAC) of 0.00 and conduct a field sobriety test. They will also obtain informed consent for each member of the couple separately. Female participants will take a pregnancy test to ensure a negative result. All participants will complete measures to reverify eligibility criteria and be weighed to determine their correct alcohol dose. Partners will separately complete a baseline survey measuring demographic factors, alcohol use, sexual communication, and daily experiences. After completing the survey, participants will be assigned a beverage condition (alcohol or no-alcohol control) and couples will be randomly assigned to a sexual communication condition (direct verbal or indirect verbal). Participants will be seated in a room separate from their partner, where they will drink an alcoholic or no-alcohol control beverage. Upon reaching a breath alcohol content (BrAC) of .08, or immediately after drinking in the No-Alcohol control condition, participants will complete a laboratory assessment of sexual violence. The main hypotheses are: (1) one's alcohol use will increase IPSV toward partners who are also drinking, (2) one's alcohol use will increase IPSV among partners who use indirect, relative to direct, sexual communication, and (3) actor alcohol use will increase IPSV toward partners who are also drinking and use indirect, relative to direct, sexual communication.

开始日期2025-04-18

申办/合作机构

University of Colorado Denver

[+1]

100 项与乙醇相关的临床结果

登录后查看更多信息

100 项与乙醇相关的转化医学

登录后查看更多信息

100 项与乙醇相关的专利（医药）

登录后查看更多信息

464,609

项与乙醇相关的文献（医药）

2025-12-31·Energy Sources Part A-Recovery Utilization and Environmental Effects

Investigation of fumigation of ethanol and exhaust gas recirculation on combustion and emission characteristics of partially premixed charge compression-ignition engine

作者: Pandey, Shyam ; Kunwer, Ram ; Bhurat, Swapnil Sureshchandra

This paper presents the exptl. investigation of partially-pre-mixed-charge-compression ignition (PCCI) engine.In PCCI, engine ethanol was fumigated in an air intake manifold and diesel injected into the engine cylinder.A fixed 15% of the ethanol was fumigated through an electronically operated multipoint fuel injector with exhaust gas recirculation (EGR-10% to 20%).The effect of fumigation of ethanol was analyzed with six different air-fuel-EGR mixtures, namely, pure diesel (ER0EGR0), 15% ethanol without EGR (ER15EGR0), pure diesel with 10% EGR (ER0EGR10), 15% ethanol with 10% EGR (ER15EGR10), pure diesel with 20% EGR (ER0EGR20), 15% ethanol with 20% EGR (ER15EGR20) at three different loads, i.e., 2, 3, and 4 bar BMEP.The exptl. observations show that the fumigation technique can effectively be implemented in a diesel engine to minimize fossil fuel dependency.At high and moderate load, the results prove that the fumigation of ethanol and EGR decreases NO_x and smoke emissions and marginal gain in brake thermal efficiency (BTE).ER15EGR0 shows a moderate reduction in unburned hydrocarbon (UHC) and carbon monoxide (CO) emission compared to pure diesel combustion.BSFC and ignition-delay (ID) increase with EGR and ethanol fumigation at all engine loads, whereas, it does not affect maximum cylinder pressure at full load.However, at the part and moderate engine load, combustion pressure decreases with fumigation of ethanol and EGR.

2025-12-31·Green Chemistry Letters and Reviews

Optimizing batch distillation parameters for enhanced bioethanol purification from fermentation

作者: Sari, Komang Nickita ; Tauviqirrahman, Mohammad ; Nugraha, Reva Edra ; Ammarullah, Muhammad Imam ; Sari, Ni Ketut ; Ernawati, Dira ; Lestari, Wahyu Dwi

This study aims to improve the purity of bioethanol produced from Bioethanol Recycle of Enzyme Fermentation (BR-EF) by employing batch distillation and absorption techniques.A distillation column with raschig rings and mol. sieve was used, with an initial BR-EF volume of 1 L and concentrations ranging from 15% to 35% (volume/volume).The distillation process, conducted at 78°C using microwave heating, lasted between 2-6 h.The optimal bioethanol concentration of 97.72% (volume/volume) was achieved with a 30% (volume/volume) BR-EF concentration and a 4-h distillation time.Optimal response with a bioethanol concentration of 99.824% (volume/volume).The ideal conditions for Multiple Response Prediction were determined to be flow rate of adsorption and weight of silica gel are 0.116 and 58.295.Further optimization was performed using MATLAB (Matrix Laboratory) and Differential Expert (DE) to assess the impact of BR-EF concentration and distillation time on bioethanol yield, with results visualized in a 3D response surface graph.This study offers valuable insights into optimizing bioethanol production, enhancing its purity and market potential.

2025-12-31·Green Chemistry Letters and Reviews

Insight into the inhibition ability of Eupatorium adenoprum leaves extract as an efficiency corrosion inhibitor for copper in acid solution

作者: Zhang, Ai ; Ma, Xiumin ; Hou, Baorong ; Li, Weihua ; Tian, Huiwen ; Zhu, Haoyuan ; Sun, Xin ; Guo, Lei

Developing corrosion inhibitors with low toxicity, eco-friendly, favorable water solubility, long-term, and efficiency is essential to inhibit metal corrosion.Herein, Eupatorium adenoprum leaves (EAL) extract is prepared via a pure water extraction method, and its inhibition for copper in 0.5 M H2SO4 is explored for the first time.The EIS and polarization curve results show that EAL extract can enhance the film and charge transfer resistance and reduce the c.d. of copper.After 48 h immersion, the inhibition efficiency value of 1000 mg/L EAL extract still reaches 97.7%, demonstrating that EAL extract presents long-term and dependable protection for copper in harsh acidic solutionThe weight loss, SEM/EDS, and AFM results are consistent with the above conclusion.According to Langmuir adsorption and theor. calculations, the interaction in EAL extract mols./copper substrate is discussed in detail.Thanks to the physicochem. adsorption effect, a monolayer EAL extract protective film is formed on copper surface.Furthermore, the crucial active adsorption sites are unsaturated double-bond, aromatic rings, carbonyl groups, and heteroatom in EAL extract mols.Ultimately, we expect this study to offer theor. support for developing new eco-friendly inhibitors and facilitate their application in industrial pickling environments.

项与乙醇相关的新闻（医药）

2025-04-18

·药智网

GLP-1药物制备的关键溶剂介绍

1,3-二甲基-2-咪唑烷酮（1,3-Dimethyl-2-Imidazolidinone，DMI），又名二甲基乙烯脲（Dimethylethyleneurea，DMEU），是一种强极性非质子溶剂。由于它具有出色的溶解能力、稳定性和高品质，因此它在医药化工领域中的应用日渐得到广泛的重视。尤其是近年来，它在GLP-1受体激动剂和Akt激酶抑制剂等新药合成方面的应用屡见报道。1用于原料药的合成由于DMI具有很高介电常数和很强的溶剂化作用，可加速阴离子亲核反应以及伴随发生阳离子溶剂化的反应。同时DMI还具有热稳定性和化学稳定性，对许多有机和无机化合物都具有出色的溶解能力。因此，它在药物合成涉及的许多的反应类型中，作为优良的反应溶剂，发挥很重要的作用。1.羟醛缩合反应在抗炎剂亚苄基衍生物的合成中用作反应溶剂，使产物收率提高到84%。[1]图片来源：参考文献12.硝酸酯化反应在合成抗骨关节炎药萘普西诺的最后一步反应时，采用DMI作反应溶剂，可以使产物收率得到明显提高。[2]图片来源：参考文献2下表列出与采用其他溶剂时不同效果的比较：数据来源：参考文献3.烷基化反应（1）作为γ-丁内酯烷基化合物合成中的反应助剂，使产物收率达90%以上。[3]图片来源：参考文献3（2）在合成药物中间体取代乙炔类化合物的反应中，用作反应助剂，与其他有机溶剂相比，也有明显的促进作用。[4]图片来源：参考文献4上式中，A：一个1至20个碳原子的饱和或不饱和脂肪烃残基。X：一个卤素原子或芳基磺酰氧基。M：一个碱金属原子。B：H、一个烃残基或－C≡C－M。下表列出与采用其他溶剂时不同效果的比较：数据来源：参考文献4.甲硅烷基醚化反应在合成医药中间体甲硅烷基醚类化合物时，用作反应溶剂。[5]图片来源：参考文献5与采用其他溶剂时不同效果的比较见下表：数据来源：参考文献5.酰胺水解反应在合成如下所示的一种GLP-1受体激动剂类的药物时，其中间体由A到B的酰胺键酸性水解反应，在DMI的促进下进行，效果较好。[6]图片来源：参考文献66.肼置换反应文献[7]则报道了在一项Akt激酶抑制剂的合成试验中，以DMI为溶剂，成功地实现了公斤级的肼置换反应，在DMI的作用下，6-氯-3-苯基-1,5-萘啶-2(1H)-酮与浓度为35%的水合肼反应，得到2.585公斤纯度为98.4 wt%的产品6-肼基-3-苯基-1,5-萘啶-2(1H)-酮，反应收率为84%。[7]图片来源：参考文献77.多肽的环合反应多有文献报道DMI用于有生物活性、可作为潜在药物开发的多肽或环肽的人工合成。有研究表明，DMI在如下潜在药物的合成中，作为溶剂，取得了较好的效果。[8]如，(S)-2-(2-羟基-N-甲基乙酰胺基)-3-苯基-N-((3R,6S,9S,123.15S,2iS,24S,27S)-6,15,21-三苄基-24-异丁基-3-(巯基甲基)-9,10,12,16,19,25-六甲基-2,5,8,11,14,17,20,23,26-九氧代-1,4,7,10,13,16,19,22,25-九氮杂三十烷-27-基)丙酰胺（化合物P-151）1-((6R,12S,15S,18R)-15-[1H-吲哚-3-基)甲基)-6-氨基-18-(叔丁基二硫烷基)甲基)-12-(4-(二甲氨基)丁基)-2,2-二甲基-7,10,13,16-四氧代-3,4-二硫杂-8,11,14,17-四氮杂十九烷)吡咯烷-2-甲酸(S)-2-((S)-6-氨基-1-(S)-4-(苄基硫)-1-((S)-2-氨基甲酰基吡咯烷-1-基)-1,4-二氧代丁-2-烷基氨基)-1-氧代己-2-烷基氨基)-2-氧代乙酯（化合物SP605）(S)-N-((3R,6S,9S,12R,16S,19S)-6-((1H-吲哚-3-yl)甲基)-16-((S)-2-氨基甲酰基吡咯烷-1-羰基)-9-(4-(二甲基氨基)丁基)-3,12-双(巯甲基)-2,5,8,11,14,18-六氧代-1,4,7,10,13,17-六氮杂二十三烷-19-基)-1-(2-羟乙酰基)吡咯-2-甲酰胺（化合物SP617）(S)-N-((3S,6S,9S,12S,155,18S,2IS,24S,27S)-3,12-苄基-1,24-二异丁基-6,9,10,13,15,19,21,22-八甲基-2,5,8,11,14,17,20,23,26-九氧代-1,4,7,10,13,16,19,22,25-九氮杂环三十一烷-27-基)-2-(2-羟基乙酰胺)-3-苯基丙酰胺(化合物SP664)(2R)-2-氨基-3-(叔丁基二硫基)-N-(4-((5S,8S,11S,14S,17S,20S,23S,26S,29S,32S)-5,23,32-三苄基]-2-((叔丁基二硫基)甲基)-11,17-二异丁基-13,14,16,20,22,25,26,29-八甲基-3.6,9,12,15,18,21,24,27,30,33-十一氧代-1-氧杂-4,7,10,13,16,19,22,25,28,31-十氮杂环三十三烷-8-基丁基)丙酰胺（化合物SP665）等。图片来源：参考文献82用于透皮吸收制剂（1）安定是一种镇静剂用于治疗焦虑症和一般性失眠。以DMI 72g、已烷25g和安定3g配成药剂，以小老鼠腹部皮肤作透皮测试，在8h内的透皮吸收量是391μg／cm2，大于仅以安定3g和甲基乳酸酯97g配得溶剂的透皮量。可见由DMI和极性物质的组合能够促进药物在皮肤中的传输吸收。由安定1％、乙醇74％和DMI 25％能配制成一种肌肉松弛剂。[9]（2）尼索地平是一种钙离子拮抗剂，用于治疗脑血管疾病。以苯乙烯-异戊二烯聚合物28％、石蜡油17.5％、聚丁烯5％、石油树脂32％和钛白17.5％（按重量比）调配成涂敷剂底料。再在底料中加入尼索地平（活性药物）10％、辅料1-癸基氮杂环壬-2-酮（1-decylazaclononan-2-one）5％以及DMI 10％，所得涂敷剂均匀涂在聚乙烯薄膜的表面，测试透皮性能，有较好的效果。[10]（3）没药醇是一种钙离子拮抗剂。以没药醇（纯度87％）3％、DMI 7％以及镍5％配入底料85％中，制得药剂（按重量比）（底料是以丙烯酸和丙烯酸丁酯的共聚物溶入20％的丙酮而得）。该药剂涂于聚乙烯薄膜上测试得较好的透皮效果。[11]（4）盐酸普萘洛尔主要用于治疗心律不齐。以盐酸普萘洛尔（活性药物）1％、DMI74％、十二烷基烟碱25％（按重量比）配成药剂，在玻璃试管中测试它的透皮吸收性能。与以盐酸普萘洛尔1％和DMSO 99％配得药剂相比，透皮量要高出12.9倍，与以盐酸普萘洛尔1％和N-吡咯烷酮99％配得的药剂相比，透皮量要高出2.3倍。[12]（5）灭吐灵又名甲氧普胺、胃复安，是一种镇吐药。以灭吐灵1％、DMI 89％和十二烷基烟碱10％配得药剂，测试药物皮肤渗透量。与以药品1％和DMSO 99％配得的药剂相比，透皮量要高出15.8倍，与以药品1％和N-吡咯烷酮99％配得的药剂相比，透皮量要高出30倍。[13]（6）DMI具备配制软膏的溶剂所必须具备的多项条件，因此能用于配制各种药物软膏。如：立体异构或非立体异构各类治疗眼病的消炎药剂，心脏病药物、抗菌剂、抗病毒剂、激素、镇痛剂等等。在甾体激素软膏调制中，以DMI 3g、乙二醇3g、异丙基肉豆蔻2g、白凡士林92g，混合，再加入甾体激素B，配制成治疗软膏。图片来源：参考文献9用甾体激素A和甾体激素B分别与几种不同的有机物相容混，得到如下数据:数据来源：参考文献由此可知，与调制膏剂常用的其他有机溶剂相比，1,3-二甲基-2-咪唑烷酮对于甾体药物表现出极为出色的溶解能力。该项研究还通过对健康成年男子进行皮肤贴片测试，结果显示，加入了1,3-二甲基-2-咪唑烷酮的软膏基剂具有良好的皮肤亲和性，无过敏反应，且在保湿性和稳定性方面表现出色。[14]（7）DMI能够显著地增强视黄醇和视黄酸酯对角化细胞的增殖和变异的作用效果。单独的DMI对皮肤细胞并没有产生作用，但当它与视黄醇或视黄酸酯相混合后，DMI分子与视黄醇或视黄酸酯分子之间产生协同相互作用，从而显著地增强了对角化细胞的增殖和变异的作用效果。这种皮肤调节剂成分包括（a）一种视黄醇或视黄酸酯含量0.001％～10％，（b）DMI含量0.001％～10％，（c）a与b的含量比例可以从60∶1～1∶160均有较好效果。如以下药剂的配制：（按重量比）视黄醇0.5％，完全氢化的椰子油3.9％、DMI 0.2％、聚氧乙烯油脂5％、皂土油38％、七水合硫酸镁0.3％、丁基化羟基甲苯0.01％，香料适量，加水至100％，即可配制成一种促进角化细胞增殖的药剂。[15]（8）环孢菌素是一种免疫抑制药，它在生物体内的生物利用率很低，如果加入乳酸甘油脂AXOL、DMI等辅料后，能控制药物的释放，促进它在生物体内的传输吸收，提高它的生物利用率。DMI可以用于配制软胶囊、口服制剂、栓剂、乳剂等。其配比如下表。[16]数据来源：参考文献由以上这些例子可以说明，以DMI溶解药物和以DMSO或N-吡咯烷酮作溶剂相比，药物的透皮吸收量有较大的提高，如果在DMI中再加入少量极性物质（如十二烷基烟碱、乙醇等）则透皮性能更好。可以预计DMI在药物透皮吸收剂中的应用将会不断地得到扩展。3用于中间体的合成DMI在各类有机中间体（尤其是医药、农药中间体）的合成中有非常广泛的应用。1.作为溶剂用在苯醚的合成中，见于文献报道的四种苯醚产物的合成收率都在90%以上。[17,18,19,20]（1）图片来源：参考文献17（2）图片来源：参考文献18（3）图片来源：参考文献19（4）图片来源：参考文献202.胺类化合物的合成。[21,22,23]（1）图片来源：参考文献21（2）图片来源：参考文献22（3）图片来源：参考文献233.氟苯类化合物的合成。[24,25]（1）图片来源：参考文献24，25应用效果比较：数据来源：参考文献（2）图片来源：参考文献应用效果比较：数据来源：参考文献4.还原反应DMI有极强的溶解能力，不仅能溶解有机化合物及树脂材料，还能溶解金属氢化物，因此以NaBH4还原剂时，DMI是一种优良的溶剂。溶解在DMI中的NaBH4可用来还原睛、酰胺、羧酸和酯。[26]图片来源：参考文献265.氧化反应由于DMI在酸碱性条件下有很强生物稳定性，且对碱有活化作用，因此在碱性条件下用空气中的氧可以氧化含有活泼氢的芳香族化合物，而在碱性条件下和DMF和DMSO等都是不稳定的。[27]图片来源：参考文献276.柯尔贝-施密特反应在含有DMI的混合溶剂中，酚类的碱金属盐在加压下与CO2反应，可生成羟基苯甲酸，所得产物的收率比不用DMI时高很多。[28]图片来源：参考文献287.自缩合反应。[29]图片来源：参考文献298.二聚化反应。[30]图片来源：参考文献309.加成反应。[31]图片来源：参考文献3110.乌尔曼反应用DMI作反应溶剂，铜粉作催化剂，芳卤与芳胺乌尔曼发生反应，生成联苯胺，反应收率高达90%。[32]图片来源：参考文献32参考文献（上下滑动阅览）[1] Oda Katsuo. (SHIONOGI & CO) . Novel method for producing benzylidene derivative. WO2004089921A[2] Belli, A., Cannata, V., Villa, M., Hedberg, M., Westermark, A., Fonduca, T. (NicOx S.A.). Process for the Preparation of the (S)-naproxen 4-nitrooxybutyl ester. US2011034719A1[3] Bryan Li, Richard A. Buzon, and Michael J. Castaldi. Case Study of a γ-Butyrolactone Alkylation with 1,3-Dimethyl-2-imidazolidinone as a Promoter, Organic Process Research & Development , 5(6), 609-611(2001)[4] Saito Yuzuru, Yoshida Kokichi,. (TAKEDA CHEMICAL INDUSTRIES LTD). Production of substituted acetylenic compounds. EP0284237A1[5] Thomas C. Britton. (Eli Lilly and Company). Process for preparing 2,2-difluoroketene silyl acetals and α,α-difluoro-β- silyloxy-1,3-dioxolane-4-propanoic acid esters. US5618951A[6] Ayman D. et al., (Eli Lilly and Company). Process to make GLP1 RA and intermediates therefor. US20250042899[7] Pintipa Grongsaard, et al., Convergent, Kilogram Scale Synthesis of an Akt Kinase Inhibitor. Organic Process Research & Development , 16, 1069−1081(2012)[8] Peptide-compoud cyclization method（肽类化合物环合的方法）US20240166689A1[9] Base composition and Drug composition for external use.（基础成分与外用药成分）JPS58164520A[10] Drug composition. （药物组分）JPS6133128A[11] Pharmaceutical composition. （药物组分）JPS61129140[12] Composition for percutaneous administration.（经皮给药成分）EP0182635[13] Composition for exodermis administration.（外皮层给药组合物）JPS6287527A[14] Ointment bases and ointments.（软膏基质和软膏）EP0137212[15] Skin care compositions containing dimethyl imidazolidinone and retinol or retinyl ester.（含有二甲基咪唑烷酮和视黄醇或视黄醇酯的护肤组合物）US5536740[16] Medical preparations containing N-methylated cyclic undecapeptides. （含有N-甲基化环状十肽的药物制剂）US5670478A[17] Process for production of m-phenoxybenzyl alcohol（生产间苯氧苄基醇的工艺）US4694110[18] Method for Producing Nitrophenoxybenzene Amines（生产硝基苯氧基苯胺类化合物的方法）JPH0651662B2[19] Production of 4-biphenyl p-tolyl ether.（4-联苯对甲苯醚的生产方法）JP01160935A[20] Production of 4-nitrophenetole.（4-硝基苯醇的生产方法）JP03232841A[21] Production of anthraquinone compound（蒽醌类化合物的生产）JPH06247912A[22] Production of anthraquinone compound（蒽醌类化合物的生产）JPH05170713A[23] Production of N,N-diphentlacylamides.（N,N-二苯基酰胺的生产）JPS63165350A[24] Production of 3,4-difluorobenzonitrile.（二氟苯甲腈的生产）JPH03145449A[25] Production of polyfluorohalogenobenzenes. （多氟卤代苯的生产）JPH05117181A[26] Reducation of organic compounds.（有机化合物的还原反应）JPS54144301A[27] Preparation of ketone derivative.（酮衍生物的制备）JPS54144348A[28] Production of 3,5-dialkylsalicylic acid. （3,5-二烷基水杨酸的生产）JPH0390047A[29] Production of 3,3'-dinitro-5.5'-bis(trifluoromethyl)diphenyl ether.（3,3'-二硝基-5.5'-双（三氟甲基）二苯醚的生产）JPH05178796A[30] Production of 4,4'-dinitrostilbene-2,2'-disulfonic acid or its salt.（4,4'-二硝基二苯乙烯-2,2'-二磺酸或其盐的生产）JPH05230012A[31] Production of 3-cyano-3,5,5-trimethylcyclohexanone.（3-氰基-3,5,5-三甲基环己酮的生产）JPH04164057A[32] 胡爱国，华东理工大学硕士论文，1993,6声明：本内容仅用作医药行业信息传播，不代表药智网立场。对本文有异议或投诉，请联系maxuelian@yaozh.com。责任编辑 | 史迪威合作、投稿 | 马老师 18323856316（同微信）阅读原文，是受欢迎的文章哦

临床结果

2025-04-17

·GlobeNewswire-Health Care

VIVUS Announces Enrollment of First Patient in Phase 2 Clinical Trial Assessing Ethanol-Free Carmustine as a Component of High-Dose Chemotherapy Prior to Transplant in Patients with Hodgkin or Non-Hodgkin Lymphoma

— Innovative ethanol-free formulation intended to provide improved safety and advance care for patients undergoing high-dose conditioning therapy prior to autologous hematopoietic cell transplantation (AHCT) — First patient dosed at City of Hope National Medical Center April 14, 2025 -- VIVUS LLC, a biopharmaceutical company committed to the development and commercialization of innovative therapies that focus on advancing treatments for patients with serious unmet medical needs, today announced the first patient has been enrolled in a Phase 2 clinical trial evaluating VI-0609, an innovative ethanol-free formulation of carmustine, as a component of high-dose conditioning chemotherapy in patients with refractory or relapsed Hodgkin or non-Hodgkin lymphoma undergoing autologous hematopoietic cell transplant (AHCT). While the most commonly used conditioning regimen (BEAM) includes carmustine formulated with ethanol, VI-0609 is expected to improve safety of this important chemotherapy agent. “The initiation of this trial further demonstrates VIVUS’ commitment and ability to advance innovative drug formulations that can improve patient outcomes,” said John Amos, Chief Executive Officer at VIVUS LLC. “Conditioning regimens prior to AHCT are arduous, and VI-0609 may help to reduce patient burden by improving the safety profile and enabling shorter infusion times compared with high-dose BiCNU. Consequently, we believe that VI-0609 will provide benefit to treatment centers, health systems and patients.” The Phase 2 study (NCT06915246) is a randomized multicenter trial designed to evaluate the effects of VI-0609 versus BiCNU in the BEAM high-intensity conditioning regimen for AHCT in subjects with lymphomas. The primary objectives are to evaluate infusion-related toxicities for VI-0609/BiCNU within 24 hours post infusion and unacceptable toxicities for VI-0609/BiCNU from start of BEAM through Day 30 post-AHCT. “While BEAM is an effective conditioning regimen for AHCT, it is associated with toxicities harmful to patients, such as facial pain, vomiting and swelling of the tongue, some of which likely result from the high levels of ethanol that patients receive during BiCNU infusion,” said Geoffrey Shouse, D.O., Ph.D., Principal Investigator and Assistant Professor, Division of Lymphoma, Department of Hematology & Hematopoietic Cell Transplantation, City of Hope. “As an ethanol-free carmustine formulation, VI-0609 holds promise as an alternative component of BEAM that can effectively prepare patients for AHCT with fewer toxicities. City of Hope is a world leader in setting high standards for stem cell transplantation and improving patient outcomes and this would be an important advancement in the treatment of relapsed and refractory lymphomas.” “We’re incredibly excited to embark on the launch of our carmustine pipeline. This program, fueled by our strong development engine, represents a significant leap forward in our commitment to patients,” said Santosh T. Varghese, MD, President VIVUS Global Pharmaceutical Development and Chief Medical Officer at VIVUS LLC. “At VIVUS, we believe that by leveraging our robust scientific expertise and pushing the boundaries of innovation, we aim to deliver hope and improved outcomes to patients facing refractory or relapsed Hodgkin or non-Hodgkin lymphoma.” City of Hope National Medical Center is one of the largest and most advanced cancer research and treatment organizations in the United States, with its National Medical Center in Los Angeles ranked among the nation’s top 5 cancer centers by U.S. News & World Report. VIVUS is a biopharmaceutical company committed to the development and commercialization of innovative therapies that focus on advancing treatments for patients with serious unmet medical needs. For more information about the Company, please visit http://www.vivus.com. VIVUS has developed VI-0609, an innovative ethanol-free formulation of carmustine for injection. This formulation is expected to decrease infusion related reactions versus the current BiCNU ethanol based formulation utilized in high-dose carmustine treatment for myeloablative conditioning. The content above comes from the network. if any infringement, please contact us to modify.

细胞疗法

2025-03-11

·FiercePharma

A once-yearly PrEP? Gilead's lenacapavir shows promise as company plots phase 3

Gilead Sciences plans to start a phase 3 program for once-yearly lenacapavir in the second half of this year, with the potential for regulatory filings in 2027, Jared Baeten, M.D., Ph.D., the company’s vice president of HIV clinical development, said. After Gilead Sciences' lenacapavir made waves with stellar clinical results as a twice-yearly HIV prevention candidate, the drug has shown promise being dosed even further apart at only once a year.Two different once-yearly formulations of lenacapavir achieved blood concentrations that exceeded those associated with the strong HIV prevention efficacy that twice-yearly lenacapavir showed in phase 3 preexposure prophylaxis (PrEP) studies.The pharmacokinetic results came from a small phase 1 trial presented at the Conference on Retroviruses and Opportunistic Infections and simultaneously published in The Lancet.Based on the early-stage data, Gilead plans to start a phase 3 program for once-yearly lenacapavir in the second half of this year, with the potential for regulatory filings in 2027, Jared Baeten, M.D., Ph.D., Gilead’s vice president of HIV clinical development, told Fierce Pharma.Gilead’s application for twice-yearly lenacapavir as a PrEP option is currently under FDA priority review with a decision expected by June 19. The drug is already approved under the brand name Sunlenca for use alongside other antivirals to treat multidrug-resistant HIV infection.Twice-yearly lenacapavir comes as subcutaneous injections of 927 mg of the drug administered every half a year. For the once-yearly study, researchers at Gilead examined two intramuscular presentations of lenacapavir given in a 5-g dose, formulated with either 5% or 10% of ethanol, which lowers the thickness of the injection.“We’ve talked with the scientific community and with people affected by HIV about where the unmet need is, and people said ‘longer’ [dosing intervals],” Baeten said in an interview with Fierce.Gilead picked the intramuscular route because of the amount of drug needed to be delivered and a better pharmacology profile compared with a subcutaneous injection, according to Baeten. In the phase 1 study, the two once-yearly formulations were given to 20 individuals each. At the end of the one-year mark, median concentration of lenacapavir in the blood was 57 ng/mL and 65.5 ng/mL, respectively. Both exceeded the 23.4 ng/mL recorded by twice-yearly subcutaneous lenacapavir at the end of 26 weeks, according to analyses of samples collected from the phase 3 Purpose 1 and Purpose 2 studies. Peak concentrations for lenacapavir were reached after a median of about 12 weeks or 10 weeks for the two formulations, respectively. Their levels then dropped slowly—generally in a stable way—and remained above that of subcutaneous lenacapavir for the rest of the study.It wasn’t just the median number. For all participants, intramuscular lenacapavir’s blood concentration at the end of 12 months was “similar to or higher than” that for twice-yearly subcutaneous drug at the half-year mark, Gilead’s researchers pointed out in the Lancet article.In terms of safety, both formulations were well tolerated, with no grade 4 treatment-emergent adverse events recorded. There were some grade 3 lab abnormalities, but they were deemed unlikely to be related to lenacapavir.The most common grade 3 adverse event was elevated low-density lipoprotein (LDL) cholesterol level, which happened in four individuals across the two formulations. However, all four participants had abnormal LDL at baseline and their grade 3 elevation didn’t match lenacapavir exposure.Injection-site pain was common but generally mild and was substantially reduced by pretreatment with ice at the sites of injection, according to the researchers. The positive phase 1 trial leaves Gilead with a couple of key considerations as the company finalizes a phase 3 design.First, because the intramuscular formulation’s Ctrough—the measurement of a drug’s blood concentration before the next dose—is notably higher than expected, the optimal clinical dose for future development is likely to be lower than 5g, the Gilead researchers noted in the study. Gilead won’t launch another study but will instead rely on the “extensive pharmacology data” to choose what lenacapavir dose to bring into phase 3 testing, Baeten said.Second, for the subcutaneous formulation, the two Purpose trials used a loading dose of oral lenacapavir at the time of the first injection to get the drug’s blood concentration to the desirable level faster. For the intramuscular formulation, the increase in initial lenacapavir plasma concentration was faster but still not at a desirable speed, suggesting that oral loading may also be needed here, study researchers pointed out.Finally, like many other trials of a new formulation of an existing drug, the upcoming phase 3 program may be able to adopt a pharmacological endpoint rather than a hard efficacy endpoint like infection rates used in the Purpose trials.Baeten wouldn’t confirm what the primary endpoint would be. But he said that, “this is the same drug, so the safety and target blood concentration targets needed for efficacy are well-established by the Purpose program.”

临床结果临床3期优先审批临床1期

100 项与乙醇相关的药物交易

登录后查看更多信息

研发状态

批准上市

10 条最早获批的记录,

后查看更多信息

适应症	国家/地区	公司	日期
梗阻性肥厚型心肌病	美国	Bpi Labs LLC	2018-06-21
消毒剂	日本	Maruishi Pharmaceutical Co., Ltd.	2003-10-06

未上市

10 条进展最快的记录,

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
甲醇中毒	申请上市	美国	Eton Pharmaceuticals, Inc.	2023-01-11
缺血性卒中	临床前	美国	Wayne State University School of Medicine	2014-04-08
血栓形成	临床前	日本	Nara Medical University	2004-11-16

登录后查看更多信息

临床结果

适应症

分期

评价

查看全部结果

研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


ENDO2024	N/A	原发性甲状旁腺功能亢进症	-	Cinacalcet 30 mg daily	簾艱鬱繭遞獵願範壓蓋(鑰壓襯鬱簾顧鬱鬱淵鹹) = 繭蓋淵願鏇願壓獵壓製鹹餘觸簾鏇獵淵觸淵壓 (網衊顧簾淵憲遞憲積糧 ) 更多	积极	2024-06-01
ENDO2024	N/A	原发性甲状旁腺功能亢进症	-	Cinacalcet 90 mg twice daily	窪遞襯淵製簾醖憲艱襯(願網鹹築夢糧夢構範鏇) = 獵廠獵艱艱構鹹糧製窪夢網壓積選選鏇選鏇艱 (鏇鏇積餘築選糧窪觸窪 )	积极	2024-06-01
ESC2024	N/A	-	-	ethanol (Radiofrequency Ablation (RF))	鹽顧壓鏇醖淵簾築齋構(鹽選願窪網觸鏇鏇鹹築) = 範選顧艱艱鹹鏇襯網窪齋觸製顧觸襯夢獵鹽襯 (廠鬱觸願願網積遞簾鏇 ) 更多	积极	2024-04-09
ESC2023	N/A	心房颤动	21	vein of marshall ethanol infusion	範膚獵夢餘鏇製廠夢築(蓋窪築鏇繭構蓋鹹壓夢) = One patient had mild pericardial effusion due to VoM perforation with a spontaneous resolution 餘憲鏇選鑰壓鬱觸淵淵 (繭襯築廠窪選艱簾醖壓 )	-	2023-08-27
ESC2023	N/A	心房颤动	21	vein of marshall ethanol infusion		-	2023-08-27
ESC2023	N/A	心房颤动一线	133	ethanol	壓顧選膚壓壓餘顧鹹觸(夢選簾蓋網壓憲襯窪齋) = 憲襯鹹憲膚遞鹹淵鹹淵鏇廠選遞遞醖齋簾鑰範 (壓衊艱壓觸網鏇獵蓋鑰 ) 更多	-	2023-08-27
ESC2023	N/A	心房颤动一线	133	ethanol	壓顧選膚壓壓餘顧鹹觸(夢選簾蓋網壓憲襯窪齋) = 夢壓糧窪鹹憲觸鑰願鬱鏇廠選遞遞醖齋簾鑰範 (壓衊艱壓觸網鏇獵蓋鑰 ) 更多	-	2023-08-27
ESC2023	N/A	-	-	Ethanol infusion of Vein of Marshall (EI-VOM)	鏇壓壓鹹衊餘願艱餘觸(膚構壓鏇構願構繭膚廠) = 網構願選鑰膚顧鹹願膚衊鹽窪窪衊廠齋憲構鏇 (獵網製淵鏇鹽窪獵夢壓 ) 更多	-	2023-04-16
EASL2022	N/A	肝损伤 ethanol positive \| Lactic Acid Bacteria (LAB)	146	ethanol (Individuals with NAFLD)	餘衊鹽糧鑰醖製廠醖製(構鹽繭製壓鬱願鏇醖製) = 遞鬱窪衊壓鹽淵範鑰齋築廠憲選淵選膚壓鹹窪 (構製鑰構夢膚蓋積糧壓 )	积极	2022-06-24
DDW2022	N/A	胰腺癌	-	ethanol (PNET)	膚鑰憲醖築憲顧製顧糧(夢網醖築淵繭願網艱醖) = A total of 27 (37.0%) patients experienced adverse events after the procedure, and there were two severe cases 網齋醖簾蓋淵網艱廠選 (鹹鬱餘壓積簾鹽鏇鑰鹹 )	-	2022-05-23
DDW2022	N/A	胰腺癌	-	ethanol (SPT)		-	2022-05-23
Pubmed \| Pacing Clin Electrophysiol	N/A	心房颤动	1,322	ethanol (EI-VOM combined with RFCA)	鏇夢鹹艱艱構遞窪廠積(範鏇夢製齋醖鬱襯憲壓) = 鬱鹽鹽網網構範製艱築鏇醖醖願網壓齋選齋遞 (膚糧選艱觸鑰築觸網鹹, 81.9 ~ 91.4) 更多	积极	2021-07-01
AAI2021	N/A	-	-	Ethanol	醖膚鬱餘鑰觸憲醖憲憲(鏇觸積窪衊遞鬱糧範選) = 60% less A20 淵鹽壓簾觸鬱範鹽蓋簾 (鹽鏇繭鹽餘網壓糧簾選 ) 更多	-	2021-05-01
ESC2021	N/A	心房颤动	121	Ethanol Infusion in the Vein of Marshall	網鬱觸獵簾艱餘獵構網(鹹醖憲鹽衊積網選憲憲) = 憲衊範衊願繭鑰鏇蓋遞選遞醖廠夢壓遞鏇築衊 (糧鏇窪鑰衊淵構簾獵醖 )	-	2021-04-24