预约演示
更新于：2026-10-12
RZL-012
更新于：2026-10-12
概要
基本信息
非在研机构 |
最高研发阶段临床3期 |
首次获批日期- |
最高研发阶段(中国)临床3期 |
特殊审评- |
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结构/序列
分子式C20H25Br2ClN2 |
InChIKeyGYDHQSBIPOHCIM-UHFFFAOYSA-M |
CAS号1436920-57-8 |
关联
10
项与 RZL-012 相关的临床试验CTR20251086
一项评价RZL-012在颏下脂肪（SMF）堆积造成的中度至重度轮廓隆起或过度丰满人群中的疗效和安全性的多中心、随机、双盲、安慰剂对照III期临床试验
NCT05763160
An Open Label Phase 2 Study to Evaluate the Safety and Efficacy of a Second Treatment Session of RZL-012 Into Submental Fat in Subjects Seeking Further Improvement
NCT05476679
An Open Label Phase 2 Study to Evaluate the Effects of a Local Anesthetic, Anti-inflammatory Medications and Compression Garments on RZL-012-Induced Adverse Events
100 项与 RZL-012 相关的临床结果
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100 项与 RZL-012 相关的转化医学
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100 项与 RZL-012 相关的专利（医药）
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8
项与 RZL-012 相关的文献（医药）2023-09-14Aesthetic surgery journal
Efficacy and Safety of Tapencarium (RZL-012) in Submental Fat Reduction
Article
作者: Steve Yoelin ; Michael Gold ; Racheli Gueta ; Sabrina Fabi ; Brian Biesman ; Glynis Ablon ; Derek Jones ; Patricia Walker ; Jeanine Downie ; Joel Cohen ; Ava Shamban ; Steven Fagien ; Sachin M Shridharani ; Steven Dayan
Abstract:
Background:
Tapencarium (RZL-012) (5-(3.6-dibromo-9H-carbazol-9-yl)-N, N, N-trimethylpentan-1-aminium chloride) is a novel injectable synthetic molecule with cytolytic properties, capable of reducing subcutaneous fat volume.
Objectives:
The goal of this 3-armed, randomized, double-blind, placebo-controlled phase 2b study was to determine the safety and efficacy of low- and high-dose RZL-012 vs placebo on submental fat (SMF) reduction.
Methods:
Patients (n = 151, age 18-65 years) with excess SMF received a single treatment session of RZL-012 or placebo in the submental area, after which they were monitored for 84 days. SMF was assessed at baseline and after dosing with newly developed scales, namely the Clinician Chin Assessment Tool (C-CAT) and Subject Chin Assessment Tool (S-CAT). SMF was also assessed by magnetic resonance imaging (MRI) at screening and on Day 84 after treatment.
Results:
The proportion of patients who had a 1-grade or 2-grade improvement in C-CAT and/or S-CAT on Day 84 vs baseline was significantly higher in the high-dose RZL-012 group vs the placebo group (P < .002). The relative percentage reduction in MRI-measured SMF volume (Day 84 vs screening) was significantly greater in the high-dose RZL-012 group vs the low-dose RZL-012 or the placebo group (P < .0001). Local injection site reactions were the most common adverse events (AEs).
Conclusions:
A single administration of RZL-012 into SMF resulted in significant improvement in submental appearance as assessed by clinicians, patients, and MRI. From a safety perspective, there were no serious AEs and no clinically significant changes in vital signs or laboratory tests over the course of the study.
Level of Evidence: 1:
2021-12-01Dermatologic surgery : official publication for American Society for Dermatologic Surgery [et al.]3区 · 医学
Mode of Action of RZL-012, a New Fat-Reducing Molecule
3区 · 医学
Article
作者: Blaugrund, Eran ; Zernov, Anton ; Bloomenfeld, Alon ; Gueta, Racheli
BACKGROUND:
RZL-012 (5-[3,6-dibromo-9H-carbazol-9-yl]-N,N,N-trimethylpentan-1-aminium chloride) is a novel investigational drug injected subcutaneously into fat tissues in patients with fat-related disorders (Dercum disease) or subjects seeking aesthetic changes.
OBJECTIVE:
Preclinical studies were undertaken to understand RZL-012's mechanism of action.
MATERIALS AND METHODS:
The effects of RZL-012 were tested in vitro by measuring adipocyte cell killing, membrane integrity, cytosolic calcium, and mitochondrial membrane potential (MMP). In vivo studies in pigs evaluated RZL-012's adipocyte killing effect and measured pig fat thickness in the injected areas.
RESULTS:
RZL-012 triggered adipocyte cell killing with IC50 values ranging from 25 to 106 μM. RZL-012 demonstrated initial effects on membrane integrity and calcium levels with delayed alterations in MMP. Incubation of RZL-012 with nanoghosts increased membrane permeability, culminating in full membrane destruction. Analysis of injected areas in pigs revealed liponecrosis 24 hours after dosing followed by an inflammatory response and formation of fibrotic tissue. Three months after dosing, an 18% reduction in mean fat thickness was observed in RZL-012 treated pigs.
CONCLUSION:
RZL-012 destroys adipocytes by directly disrupting cell membrane integrity. Replacement of dead fat tissue by fibrotic tissue enables healing and causes contraction of the injected area. These effects are translated into significant reduction in fat tissue volume.
2021-08-01Dermatologic surgery : official publication for American Society for Dermatologic Surgery [et al.]3区 · 医学
RZL-012, a New Fat Dissolving Molecule, Tested in Dercum's Disease Patients
3区 · 医学
Article
作者: Racheli Gueta ; Eran Blaugrund ; Alon Bloomenfeld ; Karen L. Herbst
RZL-012 [5-(3,6-dibromo-9H-carbazol-9-yl)-N,N,Ntrimethylpentan-l-aminium chloride] is a novel investigational drug intended for adipose tissue reduction on injection into s.c. fat.Based on in vitro and in vivo preclin. studies, the putative mechanism of action of RZL-012 seems to operate through induction of significant fat cell necrosis after a single injection with transient side effects, mostly at the injected area.An open label Phase 2a rial in 6 Dercum′s disease patients1,2 was undertaken to confirm initial safety and efficacy.Patients were dosed once by injecting the compound into painful lipomas.Lipoma height and pain were assessed at baseline, 28, and 56 days after injection.Lipomas demonstrated an average reduction of 48in height and 71in pain on Day 56 vs. baseine.The adverse event (AE) profile was benign without any serious AEs.
100 项与 RZL-012 相关的药物交易
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研发状态
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 局部肥胖 | 临床3期 | 中国 | 2025-03-03 | |
| 局部肥胖 | 临床3期 | 中国 | 2025-03-03 | |
| 痛性肥胖症 | 临床2期 | 美国 | 2018-06-28 | |
| 脂肪水肿 | 临床2期 | 美国 | 2018-06-28 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 12 | 壓獵選夢醖鏇壓鏇繭鏇 = 簾鑰淵遞膚觸齋齋壓製 憲鹹壓鬱繭簾製鏇淵鹹 (衊餘衊憲觸夢夢遞鹽廠, 顧憲鑰淵積夢鑰積膚膚 ~ 獵遞選願繭遞獵簾鹽遞) 更多 | - | 2024-02-08 | |||
临床2期 | 38 | (RZL-012) | 窪觸獵淵壓選淵網衊製(築鹹醖網簾範獵遞窪觸) = 網鑰鏇鑰築膚遞網蓋繭 糧膚積鹹鏇獵廠襯鬱鏇 (願膚齋獵鹹築淵鹹簾艱, 25.56) 更多 | - | 2024-02-07 | ||
Vehicle (Vehicle of RZL-012) | 窪觸獵淵壓選淵網衊製(築鹹醖網簾範獵遞窪觸) = 願築壓廠醖齋艱簾鏇製 糧膚積鹹鏇獵廠襯鬱鏇 (願膚齋獵鹹築淵鹹簾艱, 23.96) 更多 | ||||||
临床1/2期 | - | 20 | (Chinese) | 憲鑰積鏇獵壓膚齋遞願(淵壓獵衊顧淵齋夢積膚) = 選淵膚獵窪糧鹽網齋廠 糧廠艱觸壓製觸遞簾憲 (繭襯鏇壓築鑰夢選醖夢, 183.6) 更多 | - | 2023-12-19 | |
(Non-Chinese) | 憲鑰積鏇獵壓膚齋遞願(淵壓獵衊顧淵齋夢積膚) = 鏇獵鹽襯範鹹廠膚襯醖 糧廠艱觸壓製觸遞簾憲 (繭襯鏇壓築鑰夢選醖夢, 186.8) 更多 | ||||||
临床2期 | 28 | Placebo (Vehicle) | 窪鑰繭選醖觸選製製夢 = 衊廠築製艱襯糧鑰膚餘 願鹽淵願窪糧築範壓網 (膚鏇構鹹齋衊遞網憲憲, 壓齋積範鑰製糧膚鹽艱 ~ 艱淵衊網觸遞鑰憲獵餘) 更多 | - | 2023-11-18 | ||
(RZL-012) | 廠網選鹹鬱鑰鬱鹽醖鹽(築築遞餘膚鹹鏇獵艱積) = 廠鹽襯鏇遞蓋壓鏇醖鬱 鹽鹽遞蓋蓋構鹽襯構窪 (窪醖蓋顧膚壓簾餘遞選, 8) 更多 | ||||||
临床2期 | - | 12 | (RZL-012 50mg/ml) | 獵齋蓋膚壓膚窪構糧積 = 醖淵窪構簾鏇淵獵餘願 網壓醖簾鹽選鏇憲鹹製 (遞憲觸鏇夢窪鏇繭蓋選, 繭齋糧獵廠選鹹鹽鬱膚 ~ 膚積繭繭餘顧範鏇餘鹹) 更多 | - | 2023-11-18 | |
Placebo (Placebo) | 獵齋蓋膚壓膚窪構糧積 = 餘範簾醖廠淵簾鏇憲遞 網壓醖簾鹽選鏇憲鹹製 (遞憲觸鏇夢窪鏇繭蓋選, 鬱繭窪製艱壓衊醖窪簾 ~ 窪繭襯憲鑰鹹糧鬱蓋築) 更多 | ||||||
临床2期 | - | 151 | (RZL-012 50mg/ml) | 膚範簾艱鏇蓋遞鏇遞積 = 夢範憲築糧鑰廠鏇選鑰 夢糧觸繭遞憲夢選範願 (醖憲淵觸齋衊廠糧糧製, 艱鹹築鹽鑰糧醖顧製壓 ~ 衊艱鬱簾衊簾遞願選膚) 更多 | - | 2023-09-28 | |
(RZL-012 34mg/ml) | 膚範簾艱鏇蓋遞鏇遞積 = 鹽襯齋艱壓齋襯衊夢鹽 夢糧觸繭遞憲夢選範願 (醖憲淵觸齋衊廠糧糧製, 顧構憲鑰鏇糧鏇選鹽醖 ~ 鬱網餘窪網願簾選顧願) 更多 | ||||||
临床2期 | 32 | Placebo | 夢觸壓獵鏇窪製膚製鹽 = 艱鬱淵繭膚積網鹽顧鑰 衊憲餘壓觸蓋餘鬱網餘 (夢鹽憲憲廠遞糧衊廠壓, 淵窪製鹽獵鏇獵鑰顧鑰 ~ 齋艱淵襯齋網糧鑰鏇鑰) 更多 | - | 2019-08-21 |
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