Prospective Evaluation of the Effects of Topical Therapy With Sulfamylon® For 5% Topical Solution on Autograft Healing in Subjects With Thermal Injuries Requiring Meshed Autografts: A Comparison to a Historical Control Group

The primary objective is to compare the effectiveness of treatment with Sulfamylon® solution as the initial topical moist dressing over meshed autografts following the initial graft procedure on preventing graft loss in a prospective cohort of subjects versus a historical control group in a non-inferiority trial.

开始日期2007-09-01

申办/合作机构

Mylan, Inc.

[+1]

NCT00675922 / Terminated临床2/3期IIT

Comparing the Use of Sulfamylon 5%, Dakins 0.025%, Cerium, Silver Nitrate 5% and/or Other Topical Antimicrobial Products for the Treatment of Excised and/or Grafted Burn Wounds

Determine effectiveness of various antimicrobial solutions on burn wounds (infections, wound healing, length of hospital stay).

开始日期1995-07-01

申办/合作机构

University of Texas Medical Branch

100 项与醋酸磺胺米隆相关的临床结果

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100 项与醋酸磺胺米隆相关的转化医学

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100 项与醋酸磺胺米隆相关的专利（医药）

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335

项与醋酸磺胺米隆相关的文献（医药）

2024-09-19·MOLECULES

Privileged Scaffold Hybridization in the Design of Carbonic Anhydrase Inhibitors.

Article

作者: Onali, Alessia ; Sanna, Erica ; Distinto, Simona ; Meleddu, Rita ; Maccioni, Elias ; Angeli, Andrea ; Lupia, Antonio ; Atzeni, Giulia ; Cottiglia, Filippo ; Supuran, Claudiu T ; Demuru, Laura ; Secci, Daniela

Human Carbonic Anhydrases (hCA) are enzymes that contribute to cancer's development and progression. Isoforms IX and XII have been identified as potential anticancer targets, and, more specifically, hCA IX is overexpressed in hypoxic tumor cells, where it plays an important role in reprogramming the metabolism. With the aim to find new inhibitors towards IX and XII isoforms, the hybridization of the privileged scaffolds isatin, dihydrothiazole, and benzenesulfonamide was investigated in order to explore how it may affect the activity and selectivity of the hCA isoforms. In this respect, a series of isatin thiazolidinone hybrids have been designed and synthesized and their biological activity and selectivity on hCA I, hCA II, hCA IX, and hCA XII explored. The new compounds exhibited promising inhibitory activity results on isoforms IX and XII in the nanomolar range, which has highlighted the importance of substituents in the isatin ring and in position 3 and 5 of thiazolidinone. In particular, compound 5g was the most active toward hCA IX, while 5f was the most potent inhibitor of hCA XII within the series. When both potency and selectivity were considered, compound 5f appeared as one of the most promising. Additionally, our investigations were supported by molecular docking experiments, which have highlighted the putative binding poses of the most promising compound.

2024-06-01·BIOORGANIC CHEMISTRY

Exploration and structure–activity relationship research of benzenesulfonamide derivatives as potent TRPV4 inhibitors for treating acute lung injury

Article

作者: Zheng, Zhibing ; Cai, Xu ; Ren, Kexin ; Lv, Weizhen ; Ma, Chao ; Du, Na ; Zhang, Yuehao ; Sun, Shiyang ; Yang, Shangze ; Lv, Kai ; Li, Yan ; Li, Pengyun ; Tang, Bowen ; Zhou, Sheng ; Chen, Xingjuan ; Liu, Mingliang ; Wang, Mengyuan ; Wang, Apeng

RN-9893, a TRPV4 antagonist identified by Renovis Inc., showcased notable inhibition of TRPV4 channels. This research involved synthesizing and evaluating three series of RN-9893 analogues for their TRPV4 inhibitory efficacy. Notably, compounds 1b and 1f displayed a 2.9 to 4.5-fold increase in inhibitory potency against TRPV4 (IC₅₀ = 0.71 ± 0.21 μM and 0.46 ± 0.08 μM, respectively) in vitro, in comparison to RN-9893 (IC₅₀ = 2.07 ± 0.90 μM). Both compounds also significantly outperformed RN-9893 in TRPV4 current inhibition rates (87.6 % and 83.2 % at 10 μM, against RN-9893's 49.4 %). For the first time, these RN-9893 analogues were profiled in an in vivo mouse model, where intraperitoneal injections of 1b or 1f at 10 mg/kg notably mitigated symptoms of acute lung injury induced by lipopolysaccharide (LPS). These outcomes indicate that compounds 1b and 1f are promising candidates for acute lung injury treatment.

2024-04-01·Central nervous system agents in medicinal chemistry

Sulfonamide Derivatives: Recent Compounds with Potent Anti-alzheimer’s Disease Activity

Review

作者: Egbujor, Melford Chuka

Abstract::

Facile synthetic procedures and broad spectrum of biological activities are special attributes of sulfonamides. Sulfonamide derivatives have demonstrated potential as a class of compounds for the treatment of Alzheimer's disease (AD). Recent sulfonamide derivatives have been reported as prospective anti-AD agents, with a focus on analogues that significantly inhibit the function of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes and exhibit remarkable antioxidant and anti-inflammatory properties, all of which are critical for the treatment of AD. Sulfonamide- mediated activation of nuclear factor erythroid 2-related factor 2 (NRF2), a key regulator of the endogenous antioxidant response, has also been suggested as a potential therapeutic approach in AD. Additionally, it has been discovered that a number of sulfonamide derivatives show selectivity for the β- and γ-secretase enzymes and a significant reduction of amyloid B (Aβ) aggregation, which have been implicated in AD. The comparative molecular docking of benzenesulfonamide and donepezil, an AD reference drug showed comparable anti-AD activities. These suggest that sulfonamide derivatives may represent a new class of drugs for the treatment of AD. Thus, the current review will focus on recent studies on the chemical synthesis and evaluation of the anti-AD properties, molecular docking, pharmacological profile, and structure-activity relationship (SAR) of sulfonamide derivatives, as well as their potential anti-AD mechanisms of action. This paper offers a thorough assessment of the state of the art in this field of study and emphasizes the potential of sulfonamide derivatives synthesized during the 2012–2023 period as a new class of compounds for the treatment of AD.

项与醋酸磺胺米隆相关的新闻（医药）

2023-07-05

·FiercePharma

Roche pulls a Gavreto approval before Blueprint severance, citing unfeasible trial

Roche is in the process of terminating the Blueprint Medicines partnership and is planning to return the drug to Blueprint by February. Another FDA accelerated approval has run its course, with Roche giving up on a niche indication for cancer drug Gavreto. After speaking with the FDA, Roche’s Genentech unit has decided to withdraw Gavreto for the treatment of advanced RET-mutant medullary thyroid cancer. Blueprint Medicines, the drug’s original developer, revealed the news in a securities filing Friday. Gavreto earned this approval back in 2020 under the FDA’s accelerated approval pathway based on tumor shrinkage data from the phase 1/2 ARROW trial. Now, Roche figures the phase 3 trial AcceleRET-MTC, which is designed to convert the nod into a full approval, is no longer feasible, according to the Blueprint filing. Despite the retreat from RET-mutant disease, Gavreto maintains an approval in RET fusion-positive thyroid cancer. For that indication, the FDA's postmarketing requirements call for additional data from patients in the ARROW trial and the basket TAPISTRY trial, a Blueprint spokesperson told Fierce Pharma. The company remains on track to deliver on that commitment, the spokesperson added. Medullary thyroid cancer only makes up a small fraction of Gavreto’s meager sales. The RET inhibitor only generated altogether CHF 26 million last year. Meanwhile, Roche in February decided to terminate the Blueprint partnership and will return Gavreto to the Massachusetts biotech. The two companies are in a transition period and will officially untie the knot in February. Blueprint is currently searching for a new partner for Gavreto and the biotech doesn’t expect the withdrawal to affect that process, the company spokesperson said. In fact, the termination of the AcceleRET-MTC trial reduces future development costs for any potential partner, the spokesperson added. Besides thyroid cancer, Gavreto’s initial indication is in RET fusion-positive non-small cell lung cancer. In that use, which is also an accelerated approval, Roche is investigating Gavreto in a phase 3 trial. The AcceleRET-Lung trial is pitting Gavreto against chemo with or without Merck’s Keytruda in newly diagnosed RET-positive metastatic NSCLC. The drug was once part of an umbrella phase 3 trial comparing RET-, ALK- and ROS-targeted therapies against AstraZeneca’s Imfinzi in stage 3 NSCLC, but a Genentech spokesperson said the Gavreto arm has been closed. For the NSCLC indication, the FDA wants to see more data from patients in the original ARROW trial as confirmatory evidence for a full nod, the Blueprint spokesperson said. In the past, drugmakers have pulled accelerated approvals because confirmatory trials became difficult to run. In one recent example, Viatris withdrew the antimicrobial powder Sulfamylon because new clinical practice has made it impossible for the company to enroll patients in a controlled phase 4 trial for its product. A Genentech spokesperson said Gavreto’s AcceleRET-MTC trial was not activated “due to changes to the evolving treatment landscape over time." The study was set to study Gavreto against either Exelixis’ Cabometyx or Sanofi’s Caprelsa in previously treated RET-mutant thyroid cancer. It’s possible that given the availability of RET inhibitors, doctors no longer want to treat patients with traditional, less precise multikinase inhibitors. But Eli Lilly is running a similar phase 3 trial for its rival RET inhibitor Retevmo. Coded LIBRETTO-531, that phase 3 is also using Cabometyx or Caprelsa in the control arm. In response to Fierce Pharma’s inquiry, a Lilly spokesperson said its trial “remains on track.” Gavreto’s withdrawal comes against a backdrop of increased scrutiny by the FDA’s oncology department on accelerated approvals that don’t meet confirmatory trial requirements. The agency has pushed for market withdrawals of certain PD-1/L1 inhibitors, PI3K inhibitors, PARP inhibitors, and other meds.

临床3期加速审批

2022-09-29

·Endpts

CMS spent more than $18B in four years on accelerated approvals with incomplete confirmatory trials, inspector general finds

The battle over whether and how to reform the FDA’s accelerated approval pathway is heating up again, just as the Senate punted any talks until the lame duck session just before the end of the year. On Thursday, HHS’ inspector general released a new report reiterating concerns, also noted recently by the FDA’s Oncology Center of Excellence, about delayed or slowed confirmatory trials that are necessary to prove that the accelerated approvals were worth their salt in the first place. The OIG estimates that Medicare and Medicaid spent more than $18 billion from 2018 to 2021 for 18 drugs (or 35 drug applications granted accelerated approval) with incomplete confirmatory trials that are past their original planned completion dates as of May 5. Of the total 278 drug applications granted accelerated approval, OIG finds that 104 (37%) have incomplete confirmatory trials currently, and 34% of AAs with incomplete confirmatory trials (35 of 104) have at least one trial past its original planned completion date. “Four drug applications granted accelerated approval each have confirmatory trials significantly past their original planned completion dates, overdue by at least 64 months or about 5 years. One trial for mafenide acetate ([Viatris’] Sulfamylon) is overdue by 140 months, or nearly 12 years. Trials for two other drug applications, midodrine hydrochloride ([Takeda’s] Proamatine) and pralatrexate ([Acrotech Biopharma’s] Folotyn), are 85 months and 72 months late, respectively,” the report notes. In the case of Sulfamylon, FDA staff acknowledged to OIG that there’s a lack of trial milestones, which undermined their ability to hold the sponsor accountable. For Proamatine, which Medicare Part D spent about $142 million over four years, OIG noted that generic versions are already marketed, and in the time since its approval, the drug’s owner shifted between three different sponsors, slowing the pace of confirmatory trials. And in Folotyn’s case, OIG says that changes in the standard of care for T cell lymphoma rendered the original confirmatory trial plan infeasible, but the FDA and Acrotech agreed to two new trials, the first of which finished in 2021 after a delay, and it submitted to the FDA its protocol for the second trial. The report’s release comes as the FDA’s oncology adcomm recently evaluated one dangling accelerated approval, Oncopeptides’ Pepaxto , and one full approval, Secura Bio’s PI3K inhibitor Copiktra (duvelisib), which won approval in September 2018 as a third-line treatment for relapsed or refractory CLL or SLL, but updated pivotal trial results raised safety questions. The outside experts voted against keeping either drug on the market, although both sponsors have since made clear that they won’t pull their drugs without a fight. The FDA is also engaged in an ongoing fight that will culminate in another adcomm next month over Covis Pharma’s accelerated approval for the preterm birth drug Makena, which failed a confirmatory trial. Medicaid spent almost $700 million on Makena from 2018-2021, OIG said. Makena's accelerated approval withdrawal hearing set for October as Covis wants to do more research In the spring of 2021, the FDA also openly challenged six dangling accelerated approvals, three of which were later pulled by the companies. But perhaps the biggest moment for the accelerated pathway in recent memory came when the FDA pulled it out, seemingly out of nowhere and without mention of it at the adcomm, to sign off on Biogen’s controversial Alzheimer’s drug Aduhelm. And after all the wrangling over Aduhelm, given the positive late-stage results for Eisai and Biogen’s other anti-amyloid drug lecanemab released this week, it remains unknown if Biogen will complete its confirmatory trial for Aduhelm.

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100 项与醋酸磺胺米隆相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D01166	醋酸磺胺米隆	D06BA03	DB06795

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
感染	中国	-	1995-01-01
烧伤	美国	Rising Pharmaceuticals, Inc.初创企业	1969-01-24

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT00634166 (CTgov)	临床4期	烧伤	220	Topical Antimicrobial/Antifungal Medications (Historical Control)	襯膚餘憲醖淵膚積衊憲(鹹醖窪遞繭壓窪顧築網) = 簾衊遞淵夢觸築鏇積簾憲簾餘構構艱憲鏇壓壓 (蓋淵網簾艱蓋壓廠築顧, 範選壓簾鹹膚鹽醖獵獵 ~ 蓋網鏇鹹鬱襯窪膚淵鬱) 更多	-	2014-09-29
				Sulfamylon® For 5 % Topical Solution (Prospective Patients/Active Drug)	襯膚餘憲醖淵膚積衊憲(鹹醖窪遞繭壓窪顧築網) = 醖構鬱壓範範鹹製夢選憲簾餘構構艱憲鏇壓壓 (蓋淵網簾艱蓋壓廠築顧, 餘範膚鹹網遞壓衊蓋鏇 ~ 窪觸簾願顧鏇廠築顧蓋) 更多
NCT00675922 (Soaks, CTgov)	临床2/3期	烧伤	98	Sulfamylon (Percent Infections:Sulfamylon Site)	範膚蓋積壓願願鹽築齋(鹽醖構積膚夢遞廠獵壓) = 積衊廠獵鏇鑰憲製鬱壓鹹積製鹹鑰遞獵製鬱壓 (夢網構憲選築觸範構積, 齋壓艱蓋選膚鏇遞繭繭 ~ 膚繭範醖遞淵鬱艱艱鏇)	-	2013-01-18
				Silver Nitrate (Percent Infections: Silver Nitrate Site)	範膚蓋積壓願願鹽築齋(鹽醖構積膚夢遞廠獵壓) = 積膚衊餘鹽艱選繭憲壓鹹積製鹹鑰遞獵製鬱壓 (夢網構憲選築觸範構積, 繭蓋構積窪餘廠襯艱壓 ~ 衊遞醖憲憲築襯鹹膚廠)