Valganciclovir
(Synonyms: 缬更昔洛韦) 目录号 : GC37882
Valganciclovir HCl is a prodrug for ganciclovir with antiviral activity used to treat cytomegalovirus infections.
Cas No.:175865-60-8
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
Valganciclovir HCl is a prodrug for ganciclovir with antiviral activity used to treat cytomegalovirus infections.
Valganciclovir hydrochloride is a hydrochloride salt of the L-valyl ester of ganciclovir that exists as a mixture of two diastereomers. [1] After administration, these diastereomers are rapidly converted to ganciclovir by hepatic and intestinal esterases. In cytomegalovirus (CMV)-infected cells, ganciclovir is initially phosphorylated to the monophosphate form by viral protein kinase, then it is further phosphorylated via cellular kinases to produce the triphosphate form. This triphosphate form is slowly metabolized intracellularly. The phosphorylation is dependent upon the viral kinase and occurs preferentially in virus-infected cells. The virustatic activity of ganciclovir is due to the inhibition of viral DNA synthesis by ganciclovir triphosphate. Ganciclovir triphosphate is incorporated into the DNA strand replacing many of the adenosine bases. This results in the prevention of DNA synthesis, as phosphodiester bridges can longer to be built, destabilizing the strand. Ganciclovir inhibits viral DNA polymerases more effectively than it does cellular polymerase, and chain elongation resumes when ganciclovir is removed. [2]
After oral administration, intestinal and hepatic esterases hydrolyze both diastereomers to ganciclovir, which inhibits replication of the human cytomegalovirus. Valganciclovir is well absorbed from the gastrointestinal tract and the absolute bioavailability from valganciclovir tablets (following administration with food) is approximately 60%.[2]
[1] Sugawara M, et al. J Pharm Sci, 2000, 89(6), 781-789. [2] Cvetkovi? RS, et al. Drugs, 2005, 65(6), 859-878.
| Cas No. | 175865-60-8 | SDF | |
| 别名 | 缬更昔洛韦 | ||
| Canonical SMILES | N[C@@H](C(C)C)C(OCC(OCN1C=NC2=C1N=C(N)NC2=O)CO)=O | ||
| 分子式 | C14H22N6O5 | 分子量 | 354.36 |
| 溶解度 | Soluble in DMSO | 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 | 2.822 mL | 14.1099 mL | 28.2199 mL |
| 5 mM | 0.5644 mL | 2.822 mL | 5.644 mL |
| 10 mM | 0.2822 mL | 1.411 mL | 2.822 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。
Valganciclovir: recent progress
Am J Transplant 2010 Jun;10(6):1359-64.PMID:20455881DOI:10.1111/j.1600-6143.2010.03112.x.
In 2001 Valganciclovir was approved by the FDA for treatment of HIV associated retinitis and in 2003 for prevention of post transplant CMV. This review provides an update on the status of its use and areas of controversy: How long should prophylaxis be given?; What is the appropriate dose for prophylaxis?; Can it be used in children, and at what dose?; Can it be used to treat CMV disease? The question of optimal dosing will probably not be settled as the sample size for controlled trials would be prohibitive. Other trials clearly show that extended therapy provides added benefit, the drug is safe and an appropriate dose has been identified in children and oral therapy of CMV disease is effective.
Pharmacokinetics, Pharmacodynamics, and Therapeutic Drug Monitoring of Valganciclovir and Ganciclovir in Transplantation
Clin Pharmacol Ther 2022 Aug;112(2):233-276.PMID:34596243DOI:10.1002/cpt.2431.
Ganciclovir and Valganciclovir are first choice drugs for the prevention and treatment of cytomegalovirus infection and disease in solid organ and stem cell transplant recipients. Only a few studies on the pharmacokinetics and exposure/efficacy or exposure/safety relationships of ganciclovir and Valganciclovir in transplant recipients have been published so far, and there are still controversies about the exposure parameter to use for therapeutic drug monitoring (TDM). We performed an extensive literature review of the clinical pharmacokinetics data, the exposure/effect relationships in terms of efficacy and safety, and the available tools for Valganciclovir and ganciclovir TDM in adults and pediatrics transplant recipients. The pharmacokinetics of ganciclovir and Valganciclovir is well described in adults and children, and a high interindividual variability is commonly observed. In contrast, the drug pharmacodynamics has been poorly described in adults and barely in children. The average 24-hour area under the concentration-time curve (AUC0-24h ) seems to be the best predictor of efficacy and toxicity. The benefit of TDM remains controversial in adult patients but should be considered in children due to higher interindividual variability and lower probability of target attainment. Several bayesian estimators based on limited sampling strategies have been developed with this aim and may be used in clinical practice for the AUC-based individual dose adjustment of ganciclovir and Valganciclovir.
Maribavir for Refractory Cytomegalovirus Infections With or Without Resistance Post-Transplant: Results From a Phase 3 Randomized Clinical Trial
Clin Infect Dis 2022 Sep 10;75(4):690-701.PMID:34864943DOI:10.1093/cid/ciab988.
Background: Therapies for refractory cytomegalovirus infections (with or without resistance [R/R]) in transplant recipients are limited by toxicities. Maribavir has multimodal anti-cytomegalovirus activity through the inhibition of UL97 protein kinase. Methods: In this phase 3, open-label study, hematopoietic-cell and solid-organ transplant recipients with R/R cytomegalovirus were randomized 2:1 to maribavir 400 mg twice daily or investigator-assigned therapy (IAT; Valganciclovir/ganciclovir, foscarnet, or cidofovir) for 8 weeks, with 12 weeks of follow-up. The primary endpoint was confirmed cytomegalovirus clearance at end of week 8. The key secondary endpoint was achievement of cytomegalovirus clearance and symptom control at end of week 8, maintained through week 16. Results: 352 patients were randomized (235 maribavir; 117 IAT). Significantly more patients in the maribavir versus IAT group achieved the primary endpoint (55.7% vs 23.9%; adjusted difference [95% confidence interval (CI)]: 32.8% [22.80-42.74]; P < .001) and key secondary endpoint (18.7% vs 10.3%; adjusted difference [95% CI]: 9.5% [2.02-16.88]; P = .01). Rates of treatment-emergent adverse events (TEAEs) were similar between groups (maribavir, 97.4%; IAT, 91.4%). Maribavir was associated with less acute kidney injury versus foscarnet (8.5% vs 21.3%) and neutropenia versus Valganciclovir/ganciclovir (9.4% vs 33.9%). Fewer patients discontinued treatment due to TEAEs with maribavir (13.2%) than IAT (31.9%). One patient per group had fatal treatment-related TEAEs. Conclusions: Maribavir was superior to IAT for cytomegalovirus viremia clearance and viremia clearance plus symptom control maintained post-therapy in transplant recipients with R/R cytomegalovirus. Maribavir had fewer treatment discontinuations due to TEAEs than IAT. Clinical Trials Registration. NCT02931539 (SOLSTICE).
Valganciclovir: therapeutic role in pediatric solid organ transplant recipients
Expert Opin Pharmacother 2013 Apr;14(6):807-15.PMID:23469871DOI:10.1517/14656566.2013.778244.
Introduction: Cytomegalovirus (CMV) infection is a common infectious complication after solid organ transplantation (SOT) and is associated with the increased risk of opportunistic infections and allograft rejection, as well as decreased patient survival. Ganciclovir has been the mainstay antiviral agent for prevention and treatment of CMV; however, its clinical use is hampered by the poor oral bioavailability and the need for intravenous access. Valganciclovir, an oral prodrug of ganciclovir, is up to 10 times more bioavailable than oral ganciclovir and has replaced ganciclovir as a first-line agent in the management of CMV in adult SOT patients. Areas covered: This article examines the safety and efficacy of Valganciclovir in pediatric SOT patients, with a particular focus on prophylaxis of CMV infections. An in-depth review of the literature, including pertinent data from the adult SOT population, and a discussion of unmet needs are provided. The pharmacokinetics and pharmacodynamics of Valganciclovir in the pediatric population are also discussed. Expert opinion: Existing evidence supports the use of Valganciclovir in pediatric SOT patients for CMV prophylaxis. Although comprehensive data are lacking, Valganciclovir is a treatment option for CMV infection in pediatric SOT patients. The role of Valganciclovir in pediatrics is expected to grow given its demonstrated efficacy in a variety of clinical settings and its advantages over ganciclovir.
CMV: Prevention, Diagnosis and Therapy
Am J Transplant 2013 Feb;13 Suppl 3:24-40; quiz 40.PMID:23347212DOI:10.1111/ajt.12006.
Cytomegalovirus (CMV) is the most common infection after organ transplantation and has a major impact on morbidity, mortality and graft survival. Optimal prevention, diagnosis and treatment of active CMV infection enhance transplant outcomes, and are the focus of this section. Methods to prevent CMV include universal prophylaxis and preemptive therapy; each has its merits, and will be compared and contrasted. Diagnostics have improved substantially in recent years, both in type and quality, allowing for more accurate and savvy treatment; advances in diagnostics include the development of an international standard, which should allow comparison of results across different methodologies, and assays for cellular immune function against CMV. Therapy primarily involves ganciclovir, now rendered more versatile by data suggesting oral therapy with Valganciclovir is not inferior to intravenous therapy with ganciclovir. Treatment of resistant virus remains problematic, but is enhanced by the availability of multiple novel therapeutic agents.