Sofpironium bromide
(Synonyms: BBI 4000) 目录号 : GC63196
Sofpironium bromide (BBI 4000) 是一种抗胆碱能剂，用于研究原发性腋窝多汗症 (PAH)。Sofpironium bromide 通过抑制应用部位外分泌腺中的 M3 毒蕈碱受体来减少出汗。Sofpironium bromide 对 M1、M2、M4 和 M5 亚型也有很高的亲和力。
Cas No.:1628106-94-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Sofpironium bromide (BBI 4000) is an anticholinergic agent used in the study of primary axillary hyperhidrosis (PAH). Sofpironium bromide reduces sweating by inhibiting M3 muscarinic receptors in eccrine glands at the application site. Sofpironium bromide also has a high afnity for the M1, M2, M4 and M5 subtypes[1].
Sofpironium bromide is metabolized mainly through non-enzymatic hydrolysis, and also through oxidative metabolism via CYP2D6 and CYP3A4[1].
Sofpironium bromide exhibits anticholinergic activity by inhibiting the contractile activity of guinea pig ileal tissue in a concentration-dependent manner. In a rat model, Sofpironium bromide reduces footpad sweating induced by Pilocarpine (a muscarinic receptor agonist)[1].
[1]. Julia Paik, et al. Sofpironium Bromide: First Approval. Drugs. 2020 Dec;80(18):1981-1986.
| Cas No. | 1628106-94-4 | SDF | |
| 别名 | BBI 4000 | ||
| 分子式 | C22H32BrNO5 | 分子量 | 470.4 |
| 溶解度 | DMSO : 100 mg/mL (212.59 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1259 mL | 10.6293 mL | 21.2585 mL |
| 5 mM | 0.4252 mL | 2.1259 mL | 4.2517 mL |
| 10 mM | 0.2126 mL | 1.0629 mL | 2.1259 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Sofpironium bromide: First Approval
Drugs 2020 Dec;80(18):1981-1986.PMID:33236266DOI:10.1007/s40265-020-01438-1.
Sofpironium bromide (ECCLOCK® in Japan) gel is a topical anticholinergic agent developed by Bodor Laboratories and licenced to Brickell Biotech for the treatment of hyperhidrosis. The drug is designed to reduce sweating by inhibiting M3 muscarinic receptors in eccrine glands at the application site. In September 2020, Sofpironium bromide gel 5% received its first approval in Japan for the treatment of primary axillary hyperhidrosis (PAH). Clinical studies are currently ongoing in the USA to assess the safety and efficacy of Sofpironium bromide gel 15% in PAH. This article summarizes the milestones in the development of Sofpironium bromide gel leading to this first approval for the treatment of PAH.
Sofpironium bromide: an investigational agent for the treatment of axillary hyperhidrosis
Expert Opin Investig Drugs 2022 Jan;31(1):15-21.PMID:34890517DOI:10.1080/13543784.2022.2017880.
Introduction: In recent years, increased knowledge about pathophysiology of primary hyperhidrosis has led to novel therapeutic advances. Topical and systemic anticholinergic agents have been proven beneficial in reducing sweat production in primary axillary hyperhidrosis (PAH), although their use is limited by the increased likelihood of systemic anticholinergic drug reactions, particularly regarding systemic agents. Areas covered: This paper provides an overview of pharmaceutical characteristics, efficacy and safety data from phase II and III clinical trials on Sofpironium bromide (SB), a topical anticholinergic agent that has been employed for the treatment of PAH and has already received its first approval in Japan for the treatment of PAH in the form of 5% gel formulation. Expert opinion: The retrometabolic drug design of topical SB presents distinct advantages, by limiting systemic absorption and therefore development of anticholinergic adverse events. This along with the popularity of the non-greasy gel formulation is expected to increase compliance. However, this therapy still offers a temporary control of PAH, compared to sympathectomy or device-based treatments, such as microwave thermolysis. Hence, physicians should balance the effectiveness against adverse events of each therapeutic modality and use a personalized approach based on patient's needs.
Two-week prospective observational study of 5% Sofpironium bromide gel in Japanese patients with primary axillary hyperhidrosis
J Dermatol 2022 Jun;49(6):594-599.PMID:35394087DOI:10.1111/1346-8138.16384.
In 2020, 5% Sofpironium bromide (ECCLOCK® ) gel (hereinafter referred to as sofpironium) was approved in Japan for the topical treatment of primary axillary hyperhidrosis. A phase III study of sofpironium demonstrated the efficacy and safety of sofpironium; however, no study has assessed its early efficacy at <6 weeks after starting treatment. Therefore, to assess the earlier effectiveness of sofpironium, we conducted a 2-week, single-center, exploratory, prospective, observational study in Japanese patients with primary axillary hyperhidrosis. Patients aged ≥20 years and satisfying with a Hyperhidrosis Disease Severity Scale (HDSS) score of 3 or 4 at baseline were eligible for the study. The primary endpoint for the effectiveness was change in the proportion of patients with a HDSS score of 1, 2, 3, or 4 during the 2-week study period. In 80 patients included in the full analysis set (FAS), there were more women than men (93.8% vs. 6.3%), and the mean age (±standard deviation [SD]) was 33.3 ± 9.4 years. In the FAS, the proportion of patients with a HDSS score of 1 or 2 was 55.0% on day 7, and statistically significant changes were observed after day 3 compared to baseline (p < 0.05). Mean HDSS scores (±SD) were significantly decreased from baseline value of 3.5 ± 0.5 to 2.4 ± 0.9 on day 7 (p < 0.001). The median period for sofpironium treatment to achieve a HDSS score of 1 or 2 for a continuous 2 days was 6 days (95% confidence interval, 4-8). Safety was evaluated in 92 patients in the safety analysis set, and no adverse events were reported during the study period of 2 weeks. These results suggest that after 1-week treatment with sofpironium for patients with a HDSS score of 3 or 4, approximately 50% of the patients can achieve a HDSS score of 1 or 2, which is a clinically significant improvement for the patients.
Efficacy of Sofpironium bromide gel on clozapine-induced hypersalivation in patients with treatment-resistant schizophrenia: double-blind, controlled crossover study
BJPsych Open 2023 Jan 13;9(1):e14.PMID:36636808DOI:10.1192/bjo.2022.630.
Background: Hypersalivation is a major side-effect of clozapine in patients with treatment-resistant schizophrenia. Aims: We investigated the efficacy of topical anticholinergic formulation Sofpironium bromide gel for improving hypersalivation in patients with treatment-resistant schizophrenia receiving clozapine. Method: A double-blind, controlled crossover study was conducted with Sofpironium bromide gel and a placebo gel to treat clozapine-induced hypersalivation in 16 patients with treatment-resistant schizophrenia. Patients were randomly divided between groups A and B (each n = 8). Group A was treated with Sofpironium bromide gel for 6 weeks, followed by a 2-week washout period and 6 weeks of placebo gel, after which they were observed for another 2 weeks. In contrast, group B was treated with placebo gel for 6 weeks, followed by a 2-week washout period, 6 weeks of Sofpironium bromide gel and a 2-week observation period. One-minute saliva volume, objective salivation ratings (Drooling Severity and Frequency Scale and Nocturnal Hypersalivation Rating Scale) and subjective salivation ratings (Visual Analogue Scale) were assessed every 2 weeks. Results: All patients completed the trials. Three patients reported mild, spontaneously resolved skin itching. Compared with baseline values, the 1-min saliva volumes of both groups were significantly decreased by approximately 30% at the second week of Sofpironium bromide gel treatment (P < 0.001), and significantly decreased by >40% at the fourth and sixth weeks of treatment (P < 0.001). The effects were maintained for over 2 weeks even after the treatment was discontinued. Conclusions: We suggest that Sofpironium bromide gel is effective in treating clozapine-induced hypersalivation in patients with treatment-resistant schizophrenia.
A phase 3, multicenter, randomized, double-blind, vehicle-controlled, parallel-group study of 5% Sofpironium bromide (BBI-4000) gel in Japanese patients with primary axillary hyperhidrosis
J Dermatol 2021 Mar;48(3):279-288.PMID:33410265DOI:10.1111/1346-8138.15668.
A phase 3 study was conducted to verify the efficacy and safety of 5% Sofpironium bromide (BBI-4000) gel (hereinafter referred to as sofpironium) administrated for 6 weeks in Japanese patients with primary axillary hyperhidrosis. The primary efficacy end-point was the proportion of patients who satisfied both criteria of a Hyperhidrosis Disease Severity Score (HDSS) of 1 or 2 at the end of 6-week treatment and a 50% or more reduction in total gravimetric weight of sweat at the end of treatment relative to baseline. A total of 281 patients were randomized to receive 5% sofpironium (141 patients) or vehicle (140 patients), and all patients were included in the full analysis set (FAS). In the FAS, 70.1% of patients were female, and the median age was 35.0 years. The proportion of patients who achieved the primary efficacy end-point was 53.9% in the sofpironium group and 36.4% in the vehicle group, with a statistically significant difference of 17.5% (95% confidence interval, 6.02-28.93) between these two groups (P = 0.003). The incidence of adverse events was 44.0% in the sofpironium group and 30.7% in the vehicle group, and the incidence of adverse drug reactions was 16.3% in the sofpironium group and 5.0% in the vehicle group. Reported adverse events were generally mild or moderate in severity. In the sofpironium group, common events (incidence, ≥5%) were nasopharyngitis (14.2%) and dermatitis/erythema at the application site (8.5%/5.7%), with no serious adverse events reported. This study demonstrated the efficacy and safety of 5% sofpironium.