Oxantel pamoate (Oxantel embonate)
(Synonyms: 酚嘧啶扑蛲灵,Oxantel embonate) 目录号 : GC32176
Oxantel Pamoate is the pamoate salt form of oxantel, a tetrahydropyrimidine anthelmintic used against intesitnal worms, particularly in a veterinary setting.
Cas No.:68813-55-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Oxantel Pamoate is the pamoate salt form of oxantel, a tetrahydropyrimidine anthelmintic used against intesitnal worms, particularly in a veterinary setting.
| Cas No. | 68813-55-8 | SDF | |
| 别名 | 酚嘧啶扑蛲灵,Oxantel embonate | ||
| Canonical SMILES | O=C(C1=C(O)C(CC2=C3C=CC=CC3=CC(C(O)=O)=C2O)=C4C=CC=CC4=C1)O.OC5=CC=CC(/C=C/C6=NCCCN6C)=C5 | ||
| 分子式 | C36H32N2O7 | 分子量 | 604.65 |
| 溶解度 | DMSO : ≥ 50 mg/mL (82.69 mM);Water : < 0.1 mg/mL (insoluble) | 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 | 1.6538 mL | 8.2692 mL | 16.5385 mL |
| 5 mM | 0.3308 mL | 1.6538 mL | 3.3077 mL |
| 10 mM | 0.1654 mL | 0.8269 mL | 1.6538 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。
Oxantel pamoate-albendazole for Trichuris trichiura infection
N Engl J Med 2014 Feb 13;370(7):610-20.PMID:24521107DOI:10.1056/NEJMoa1301956.
Background: Infections with soil-transmitted helminths (Ascaris lumbricoides, hookworm, and Trichuris trichiura) are widespread and often occur concomitantly. These parasitic-worm infections are typically treated with albendazole or mebendazole, but both drugs show low efficacy against T. trichiura. Albendazole is the drug of choice against hookworm. Methods: In this double-blind trial conducted on Pemba Island, Tanzania, we randomly assigned children, 6 to 14 years of age, to receive one of four treatments: Oxantel pamoate at a dose of 20 mg per kilogram of body weight, plus 400 mg of albendazole, administered on consecutive days; Oxantel pamoate at a single dose of 20 mg per kilogram; albendazole at a single dose of 400 mg; or mebendazole at a single dose of 500 mg. We assessed the efficacy and safety profile of oxantel pamoate-albendazole when used in the treatment of T. trichiura infection (primary outcome) and concomitant soil-transmitted helminth infection (secondary outcome). Efficacy was determined by means of assessment of the cure rate and egg-reduction rate. Adverse events were assessed four times after treatment. Results: Complete data were available for 458 children, of whom 450 were infected with T. trichiura, 443 with hookworm, and 293 with A. lumbricoides. The cure rate of T. trichiura infection was significantly higher with oxantel pamoate-albendazole than with mebendazole (31.2% vs. 11.8%, P=0.001), as was the egg-reduction rate (96.0% [95% confidence interval {CI}, 93.5 to 97.6] vs. 75.0% [95% CI, 64.2 to 82.0]). The cure rate with albendazole (2.6%) and the egg-reduction rate with albendazole (45.0%; 95% CI, 32.0 to 56.4) were significantly lower than the rates with mebendazole (P=0.02 for the comparison of cure rates). Oxantel pamoate had low efficacy against hookworm and A. lumbricoides. Adverse events (mainly mild) were reported by 30.9% of all children. Conclusions: Treatment with oxantel pamoate-albendazole resulted in higher cure and egg-reduction rates for T. trichiura infection than the rates with standard therapy. (Funded by the Medicor Foundation and the Swiss National Science Foundation; Current Controlled Trials number, ISRCTN54577342.).
Preclinical and Clinical Characteristics of the Trichuricidal Drug Oxantel pamoate and Clinical Development Plans: A Review
Drugs 2021 Jun;81(8):907-921.PMID:33929716DOI:10.1007/s40265-021-01505-1.
Soil-transmitted helminths (Ascaris lumbricoides, hookworm and Trichuris trichiura) infect about one-fifth of the world's population. The currently available drugs are all highly efficacious against A. lumbricoides. However, they are only moderately efficacious against hookworm and poorly efficacious against T. trichiura. Oxantel, a tetrahydropyrimidine derivative discovered in the 1970s, has recently been brought back to our attention given its high efficacy against T. trichiura infections (estimated 76% cure rate and 85% egg reduction rate at a 20 mg/kg dose). This review summarizes the current knowledge on Oxantel pamoate and its use against T. trichiura infections in humans. Oxantel pamoate acts locally in the human gastrointestinal tract and binds to the parasite's nicotinic acetylcholine receptor (nAChR), leading to a spastic paralysis of the worm and subsequent expulsion. The drug is metabolically stable, shows low permeability and low systemic bioavailability after oral use. Oxantel pamoate was found to be safe in humans, with only a few mild adverse events reported. Several clinical trials have investigated the efficacy of this drug against T. trichiura and suggest that Oxantel pamoate is more efficacious against T. trichiura than the currently recommended drugs, which makes it a strong asset to the depleted drug armamentarium and could help delay or even prevent the development of resistance to existing drugs. We highlight existing data to support the use of Oxantel pamoate against T. trichiura infections.
Efficacy and tolerability of triple drug therapy with albendazole, pyrantel pamoate, and Oxantel pamoate compared with albendazole plus Oxantel pamoate, pyrantel pamoate plus Oxantel pamoate, and mebendazole plus pyrantel pamoate and Oxantel pamoate against hookworm infections in school-aged children in Laos: a randomised, single-blind trial
Lancet Infect Dis 2018 Jul;18(7):729-737.PMID:29673735DOI:10.1016/S1473-3099(18)30220-2.
Background: Albendazole and mebendazole are commonly used to control hookworm, but have shortcomings in their efficacy profiles. We assessed whether triple drug therapy (TDT) with albendazole, pyrantel pamoate, and Oxantel pamoate was more effective than the co-administration of two drugs for the treatment of hookworm infections. Methods: A randomised, single-blind trial was done from Sept 27 until Nov 17, 2017, in Laos. Children (6-15 years) from six schools were invited to participate. Hookworm-positive children were randomly assigned (2:2:1:1) by a computer stratified list (block sizes of six and 12) to TDT with albendazole (400 mg), pyrantel pamoate (20 mg/kg), and Oxantel pamoate (20 mg/kg); albendazole plus Oxantel pamoate; pyrantel pamoate plus Oxantel pamoate; or mebendazole (500 mg) combined with both pyrantel pamoate and Oxantel pamoate (used as proof of concept to compare the two TDTs). Two stool samples were collected at baseline and follow-up (17-30 days after treatment) and analysed with the Kato-Katz method. The primary outcome was the proportion of hookworm egg-negative children at follow-up in all Kato-Katz slides (cure rate [CR]) in the TDT with albendazole, pyrantel pamoate, and Oxantel pamoate group compared with the albendazole plus Oxantel pamoate and pyrantel pamoate plus Oxantel pamoate groups. Secondary outcomes were tolerability 3 h and 24 h after treatment, egg reduction rates (ERRs) against hookworm, and efficacy against concomitant soil-transmitted helminth infections. Participating children and field and laboratory technicians were masked to treatment allocation. All children with follow-up data were included in the primary analysis. This trial is registered with ClinicalTrials.gov, number NCT03278431. Findings: 1529 children were assessed for eligibility, of whom 533 provided complete baseline data and 414 provided complete outcome data. The CR was higher for the TDT albendazole, pyrantel pamoate, and Oxantel pamoate (116 [84%] of 138) than with albendazole plus Oxantel pamoate (73 [53%] of 138; odds ratio 4路7, 95% CI 2路7-8路3; p<0路0001) and pyrantel pamoate plus Oxantel pamoate (36 [52%] of 69; 4路8, 2路5-9路3; p<0路0001). The geometric ERR of the TDT albendazole, pyrantel pamoate, and Oxantel pamoate (99路9%) was higher than that for albendazole plus Oxantel pamoate (99路0%; difference in ERR 0路9 percentage points, 95% CI 0路5-1路4), and pyrantel pamoate plus Oxantel pamoate (99路2%; 0路7 percentage points, 0路3-1路3). Adverse events were reported by six (1%) children 3 h and none 24 h after treatment, without any difference across treatment groups. Interpretation: TDT with albendazole, pyrantel pamoate, and Oxantel pamoate could make a difference, in particular in the context of soil-transmitted helminth elimination. Pyrantel pamoate might be a useful alternative to prevent benzimidazole resistance; however, larger trials are needed to confirm this finding. Funding: Swiss National Science Foundation.
Activity of Oxantel pamoate monotherapy and combination chemotherapy against Trichuris muris and hookworms: revival of an old drug
PLoS Negl Trop Dis 2013;7(3):e2119.PMID:23556013DOI:10.1371/journal.pntd.0002119.
Background: It is widely recognized that only a handful of drugs are available against soil-transmitted helminthiasis, all of which are characterized by a low efficacy against Trichuris trichiura, when administered as single doses. The re-evaluation of old, forgotten drugs is a promising strategy to identify alternative anthelminthic drug candidates or drug combinations. Methodology: We studied the activity of the veterinary drug Oxantel pamoate against Trichuris muris, Ancylostoma ceylanicum and Necator americanus in vitro and in vivo. In addition, the dose-effect of Oxantel pamoate combined with albendazole, mebendazole, levamisole, pyrantel pamoate and ivermectin was studied against T. muris in vitro and additive or synergistic combinations were followed up in vivo. Principal findings: We calculated an ED50 of 4.7 mg/kg for Oxantel pamoate against T. muris in mice. Combinations of Oxantel pamoate with pyrantel pamoate behaved antagonistically in vitro (combination index (CI) = 2.53). Oxantel pamoate combined with levamisole, albendazole or ivermectin using ratios based on their ED50s revealed antagonistic effects in vivo (CI = 1.27, 1.90 and 1.27, respectively). A highly synergistic effect (CI = 0.15) was observed when oxantel pamoate-mebendazole was administered to T. muris-infected mice. Oxantel pamoate (10 mg/kg) lacked activity against Ancylostoma ceylanicum and Necator americanus in vivo. Conclusion/significance: Our study confirms the excellent trichuricidal properties of Oxantel pamoate. Since the drug lacks activity against hookworms it is necessary to combine Oxantel pamoate with a partner drug with anti-hookworm properties. Synergistic effects were observed for oxantel pamoate-mebendazole, hence this combination should be studied in more detail. Since, of the standard drugs, albendazole has the highest efficacy against hookworms, additional investigations on the combination effect of oxantel pamoate-albendazole should be launched.
Efficacy and safety of Oxantel pamoate in school-aged children infected with Trichuris trichiura on Pemba Island, Tanzania: a parallel, randomised, controlled, dose-ranging study
Lancet Infect Dis 2016 Jan;16(1):53-60.PMID:26388169DOI:10.1016/S1473-3099(15)00271-6.
Background: Commonly used drugs for preventive chemotherapy against soil-transmitted helminths (ie, albendazole and mebendazole) show low efficacy against Trichuris trichiura. Recent studies with Oxantel pamoate revealed good cure rates and high egg-reduction rates against T trichiura. We aimed to assess the nature of the dose-response relation to determine the optimum dose. Methods: We did a parallel, randomised, placebo-controlled, single-blind trial with Oxantel pamoate in school-aged children (aged 6-14 years) infected with T trichiura on Pemba Island, Tanzania. Children were asked to provide two stool samples and children positive for T trichiura were eligible to participate in the trial. Children were excluded if they suffered from any systematic illness. Children were randomly assigned to six different Oxantel pamoate doses (5-30 mg/kg) or a placebo. Randomisation was stratified by baseline infection intensity using random block sizes of seven and 14. The primary endpoints were cure rates and egg-reduction rates against T trichiura, both analysed by available case. Drug safety was assessed 2 h and 24 h after treatment. The trial is registered at www.isrctn.com, number ISRCTN86603231. Findings: Between Oct 14, and Nov 28, 2014, we enrolled 480 participants and randomly assigned 350 children to the different Oxantel pamoate doses or the placebo. 5 mg/kg Oxantel pamoate was the minimum effective dose (10 of 46 children cured [cure rate 22%, 95% CI 11-36]; egg-reduction rate 85路0%, 64路5-92路9). An increased probability of being cured and reduced egg counts with escalating doses was recorded. At 25 mg/kg Oxantel pamoate 27 of 45 children were cured (cure rate 60%, 95% CI 44-65) with an egg-reduction rate of 97路5% (94路4-98路9), and at 30 mg/kg 27 of 46 children were cured (59%, 43-73) with an egg-reduction rate of 98路8% (96路8-99路6). Oxantel pamoate was well tolerated across all treatment groups; only mild adverse events were reported by the participants 2 h (27 [10%]) and 24 h (12 [4%]) after treatment. Interpretation: Our dose-finding study revealed an excellent tolerability profile of Oxantel pamoate in children infected with T trichiura. An optimum therapeutic dose range of 15-30 mg/kg Oxantel pamoate was defined. With a weight independent dose of 500 mg Oxantel pamoate 95% of children aged 7-14 years in sub-Saharan Africa would receive doses of 11路7-32路0 mg/kg. Future research should include studies with Oxantel pamoate in younger children and on different continents with the ultimate goal to be able to add Oxantel pamoate to soil-transmitted helminth control programmes. Funding: Swiss National Science Foundation.