Hexaminolevulinate hydrochloride (Hexyl 5-aminolevulinate hydrochloride)
(Synonyms: 5-氨基酮戊酸己酯盐酸盐,Hexyl 5-aminolevulinate hydrochloride; P-1206; 5-Aminolevulinic acid hexyl ester hydrochloride) 目录号 : GC33065
A prodrug form of 5-aminolevulinic acid
Cas No.:140898-91-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Hexaminolevulinate is a lipophilic, hexyl ester prodrug form of 5-aminolevulinic acid .1 It produces equivalent protoporphyrin IX (PpIX) induction in WiDr and NHIK 3025 carcinoma cells at concentrations approximately 100-fold lower than 5-aminolevulinic acid. In vivo, hexaminolevulinate penetrates upper skin layers more effectively in pigs and induces higher levels of PpIX fluorescence in nude mice when compared with 5-aminolevulinic acid following topical administration.2 Formulations containing hexaminolevulinate have been used in imaging and photodynamic therapy for a variety of urogenital cancers.
1.Gaullier, J.-M., Berg, K., Peng, Q., et al.Use of 5-aminolevulinic acid esters to improve photodynamic therapy on cells in cultureCancer Res.57(8)1481-1486(1997) 2.Morrow, D.I.J., McCarron, P.A., Woolfson, A.D., et al.Hexyl aminolaevulinate is a more effective topical photosensitiser precursor than methyl aminolaevulinate and 5-aminolaevulinic acids when applied in equimolar dosesJ. Pharm. Sci.99(8)3486-3498(2010)
| Cas No. | 140898-91-5 | SDF | |
| 别名 | 5-氨基酮戊酸己酯盐酸盐,Hexyl 5-aminolevulinate hydrochloride; P-1206; 5-Aminolevulinic acid hexyl ester hydrochloride | ||
| Canonical SMILES | O=C(OCCCCCC)CCC(CN)=O.[H]Cl | ||
| 分子式 | C11H22ClNO3 | 分子量 | 251.75 |
| 溶解度 | DMSO : ≥ 41 mg/mL (162.86 mM) | 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 | 3.9722 mL | 19.861 mL | 39.7219 mL |
| 5 mM | 0.7944 mL | 3.9722 mL | 7.9444 mL |
| 10 mM | 0.3972 mL | 1.9861 mL | 3.9722 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
The cost-effectiveness of blue light cystoscopy in bladder cancer detection: United States projections based on clinical data showing 4.5 years of follow up after a single Hexaminolevulinate hydrochloride instillation
Can J Urol 2013 Apr;20(2):6682-9.PMID:23587507doi
Introduction: Several studies, including the recently published phase III study by Stenzl and colleagues have demonstrated that Hexaminolevulinate hydrochloride, when used with blue light fluorescence cystoscopy, improves detection of non-muscle invasive bladder tumors compared to white light cystoscopy and transurethral resection of bladder tumors (TURB) alone. Materials and methods: The objective of this study was to conduct a detailed assessment of the cost-effectiveness of using Hexaminolevulinate hydrochloride with blue light cystoscopy as an adjunct to white light versus white light cystoscopy alone at time of initial TURB in the United States. A probabilistic decision tree model, using TreeAge Pro 2011 software, was developed using base case scenario cost and utility estimates. Results: Incorporation of Hexaminolevulinate hydrochloride into diagnostic cystoscopy results in lower costs over 5 years ($25,921) as compared to those patients who initially receive white light cystoscopy ($30,581). Those patients who initially receive Hexaminolevulinate hydrochloride blue light TURB also experience a lower overall cancer burden. Conclusions: Hexaminolevulinate hydrochloride may be cost effective when used at first TURB for patients with suspected new or recurrent non-muscle invasive bladder cancer.
Tolerability of Repeat Use of Blue Light Cystoscopy with Hexaminolevulinate for Patients with Urothelial Cell Carcinoma
J Urol 2017 Mar;197(3 Pt 1):596-601.PMID:27664580DOI:10.1016/j.juro.2016.09.076.
Purpose: Hexaminolevulinate hydrochloride with blue light cystoscopy is approved by the U.S. Food and Drug Administration as an adjunct to white light cystoscopy for the detection of urothelial cell carcinoma. In this study we examined the tolerability of the repeat use of white light cystoscopy with blue light cystoscopy. Materials and methods: We retrospectively reviewed the records of all patients who underwent white light cystoscopy with blue light cystoscopy using Hexaminolevulinate hydrochloride during a 34-month period at 2 institutions. We compared the incidence of adverse events after initial and subsequent procedures. We grouped, graded and assigned the degree of attribution for all adverse events. Results: A total of 180 patients underwent 269 white light cystoscopy with blue light cystoscopy procedures. Of those 180 patients 118 (65%) underwent white light cystoscopy with blue light cystoscopy only 1 time. The other 62 (35%) patients underwent white light cystoscopy with blue light cystoscopy 2 or more times, including 43 (24%) 2 times and 19 (10%) 3 or more times. We noted 89 adverse events out of 269 procedures (33%), of which 66 (74%) occurred after the first white light cystoscopy with blue light cystoscopy; 14 (16%) after the second time and 9 (10%) after the third time or more. We found no statistically significant difference in adverse events between those patients undergoing 1 vs 2 or more white light cystoscopy with blue light cystoscopy procedures (p=0.134). We observed 1 grade 3 adverse event and no grade 4 or 5 adverse events. None of the adverse events were classified as probably or definitely related to Hexaminolevulinate hydrochloride. Conclusions: In this retrospective study we found no statistically significant difference in the frequency or the grade of adverse events between first and repeat use of white light cystoscopy with blue light cystoscopy using Hexaminolevulinate hydrochloride.
Hexaminolevulinate hydrochloride blue-light flexible cystoscopy in the detection and follow-up of nonmuscle-invasive bladder cancer: cost consequences during outpatient surveillance in Sweden
Future Oncol 2016;12(8):1025-38.PMID:26975197DOI:10.2217/fon-2015-0021.
Aim: This study explored the cost consequences of introducing hexaminolevulinate hydrochloride-guided blue-light flexible cystoscopy (HAL BLFC) as an adjunct to white-light flexible cystoscopy compared with white-light flexible cystoscopy alone, for the detection and management of nonmuscle invasive bladder cancer in Sweden. Methods: The model evaluated 231 patients in the outpatient setting after successful initial transurethral resection of the bladder tumor. Results: HAL BLFC introduction across all risk groups resulted in minimal budget impact (+1.6% total cost/5 years, or 189 Swedish Krona [SEK] per patient/year), and translated to cost savings in intermediate- and high-risk groups from year 2. Conclusion: HAL BLFC allowed more outpatient treatment with improved recurrence detection and reduced transurethral resection of the bladder tumors, cystectomies, bed days and operating room time, with minimal cost impact across all risk groups, demonstrating the economic benefits of introducing HAL.
Is there a learning curve for photodynamic diagnosis of bladder cancer with Hexaminolevulinate hydrochloride?
Can J Urol 2012 Jun;19(3):6269-73.PMID:22704312doi
Introduction: To assess the learning curve for fluorescence cystoscopy using Hexaminolevulinate hydrochloride (HAL) in patients with bladder cancer. Material and methods: Fifty patients underwent bladder instillation with HAL. Two senior residents inspected separately the bladder using white light cystoscopy, followed by fluorescence cystoscopy and mapped the lesions. An experienced with photodynamic diagnosis (PDD) urologist also performed both cystoscopies, mapped, resected or cold biopsied suspect lesions under the supervision of another experienced urologist. To evaluate the learning curve, patients were divided into five subgroups, including group 1 (patients 1-10), group 2 (11-20), group 3 (21-30), group 4 (31-40) and group 5 (41-50). The kappa statistics was calculated to assess interobserver agreement between the physicians and the false positive rates of urologists and residents were also compared. Results: Histologically verified tumors were diagnosed in 103 of 142 lesions identified by PDD. The interobserver agreement between urologists and residents was moderate, moderate, good, excellent, and excellent for group 1, 2, 3, 4, and 5, respectively. Both residents had increased false positive rates compared to urologists in all subgroups of patients but this difference did not reach statistical significance. In addition, false positive rate of residents was declining as the number of procedures was increasing. Conclusions: Our data suggest that 20 cases of HAL PDD are required to achieve a good interobserver agreement between inexperienced and experienced operator, and excellent agreement is achieved after 30 cases. The false positive rate of inexperienced operators was comparable to the experts and showed a gradual decrease.
Budget impact of incorporating one instillation of Hexaminolevulinate hydrochloride blue-light cytoscopy in transurethral bladder tumour resection for patients with non-muscle-invasive bladder cancer in Sweden
BJU Int 2016 Jun;117(6B):E102-13.PMID:26305667DOI:10.1111/bju.13261.
Objectives: To explore the cost impact on Swedish healthcare of incorporating one instillation of Hexaminolevulinate hydrochloride (HAL) blue-light cystoscopy into transurethral resection of bladder tumour (TURBT) in patients with suspected new or recurrent non-muscle-invasive bladder cancer (NMIBC). Materials and methods: A decision tree model was built based on European Association of Urology guidelines for the treatment and management of NMIBC. Input data were compiled from two recent studies comparing recurrence rates of bladder cancer in patients undergoing TURBT with either the current standard of care (SOC) of white-light cystoscopy, or with the SOC and HAL blue-light cystoscopy. Using these published data with clinical cost data for surgical and outpatient procedures and pharmaceutical costs, the model reported on the clinical and economic differences associated with the two treatment options. Results: This model demonstrates the significant clinical benefits likely to be observed through the incorporation of HAL blue-light cystoscopy for TURBT in terms of reductions in recurrences of bladder cancer. Analysis of economic outputs of the model found that the use of one instillation of HAL for TURBT in all Swedish patients with NMIBC is likely to be cost-neutral or cost-saving over 5 years relative to the current SOC of white-light cystoscopy. Conclusions: The results of this analysis provide additional health economic rationale for the incorporation of a single instillation of HAL blue-light cystoscopy for TURBT in the treatment of patients with NMIBC in Sweden.