Lee Hyun Joon, Jiang Xu, Abd El-Aty A M, Jeong Ji Hoon, Chung Jae-Yong
Department of Clinical Pharmacology and Therapeutics, Seoul National University College of Medicine and Bundang Hospital, Seongnam, 13620, Republic of Korea.
Department of Health Science and Technology, Seoul National University College of Convergence Science and Technology, Seongnam, 13620, Republic of Korea.
Lipids Health Dis. 2024 Dec 28;23(1):426. doi: 10.1186/s12944-024-02387-4.
Excessive submental fat under the chin is a known aesthetic concern because of its negative impact on facial appearance and psychological well-being. AYP-101 is a newly developed injectable agent containing 93% soybean phosphatidylcholine (SPC) designed to reduce submental fat. We conducted a phase 1 study to evaluate the safety, pharmacokinetic (PK), and lipid profile effects of AYP-101.
This study was a randomized, double-blind, placebo-controlled, single-dose, two-cohort trial. Participants were randomized into groups receiving 250 mg of AYP-101, 500 mg of AYP-101, or placebo at a 9:9:8 ratio across both cohorts. Safety was assessed through standard clinical evaluations. Blood samples were collected up to 144 h postdose in cohort 1 and up to 48 h postdose in cohort 2. The PK parameters were calculated via noncompartmental analysis.
All 26 randomized subjects completed the study. A total of 72 solicited adverse drug reactions (ADRs) were reported by 24 subjects, all of which were mild. The most common ADRs were injection site pain and bruising. There were 29 ADR cases in the 250 mg group; 26 cases in the 500 mg group; and 18 cases in the placebo group, indicating that there were no clinically significant differences in the safety profiles between the groups. All the dose groups presented similar PK profiles, with C values of 12.86, 13.44, and 13.61 µg/L and AUC values of 278.06, 274.79, and 267.63 µg*h/L, respectively. No clinically significant differences in PK or lipid profiles were observed between the postdose group and the baseline group for any of the dose groups.
AYP-101 appears to be a safe candidate for treating submental fat, with localized reactions and no systemic exposure at single subcutaneous doses of up to 500 mg.
ClinicalTrials.gov NCT05476094.
下巴下过多的颏下脂肪因其对面部外观和心理健康的负面影响，是一个公认的美学问题。AYP - 101是一种新开发的注射剂，含有93%的大豆磷脂酰胆碱（SPC），旨在减少颏下脂肪。我们进行了一项1期研究，以评估AYP - 101的安全性、药代动力学（PK）和脂质谱效应。
本研究是一项随机、双盲、安慰剂对照、单剂量、双队列试验。参与者以9:9:8的比例随机分为接受250mg AYP - 101、500mg AYP - 101或安慰剂的组，两个队列均如此。通过标准临床评估评估安全性。在队列1中，给药后最多144小时采集血样；在队列2中，给药后最多48小时采集血样。通过非房室分析计算PK参数。
所有26名随机分组的受试者均完成了研究。24名受试者共报告了72例主动报告的药物不良反应（ADR），均为轻度。最常见的ADR是注射部位疼痛和瘀伤。250mg组有29例ADR病例；500mg组有26例；安慰剂组有18例，表明各组之间的安全性概况无临床显著差异。所有剂量组的PK概况相似，C值分别为12.86、13.44和13.61μg/L，AUC值分别为278.06、274.79和267.63μg*h/L。对于任何剂量组，给药后组与基线组之间在PK或脂质谱方面均未观察到临床显著差异。
AYP - 101似乎是治疗颏下脂肪的安全候选药物，在单次皮下注射剂量高达500mg时，有局部反应且无全身暴露。
ClinicalTrials.gov NCT05476094。
