Aesthet Surg J. 2023 Sep 14;43(10):NP797-NP806. doi: 10.1093/asj/sjad195.
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.
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.
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.
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).
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.
Tapencarium（RZL-012）（5-（3.6-二溴-9H-咔唑-9-基）-N，N，N-三甲基戊-1-铵氯化物）是一种具有细胞溶解特性的新型可注射合成分子，能够减少皮下脂肪量。
这项 3 臂、随机、双盲、安慰剂对照的 2b 期研究的目的是确定低剂量和高剂量 RZL-012 与安慰剂相比在减少颏下脂肪（SMF）方面的安全性和疗效。
患有过多 SMF 的患者（n=151，年龄 18-65 岁）在颏下区域接受单次 RZL-012 或安慰剂治疗，之后监测 84 天。在基线和给药后使用新开发的量表（即临床医生颏评估工具（C-CAT）和受试者颏评估工具（S-CAT））评估 SMF。在筛查和治疗后第 84 天还通过磁共振成像（MRI）评估 SMF。
与安慰剂组相比，高剂量 RZL-012 组在第 84 天与基线相比 C-CAT 和/或 S-CAT 改善 1 级或 2 级的患者比例显著更高（P<.002）。高剂量 RZL-012 组与低剂量 RZL-012 或安慰剂组相比，MRI 测量的 SMF 体积（第 84 天与筛查相比）的相对百分比减少显著更大（P<.0001）。局部注射部位反应是最常见的不良事件（AE）。
将 RZL-012 单次注射到 SMF 中，可显著改善颏下外观，由临床医生、患者和 MRI 评估。从安全性角度来看，在研究过程中没有严重的 AE，也没有生命体征或实验室检查的临床意义上的变化。
