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Valganciclovir | CAS No: 175865-60-8 | GMP-certified suppliers
A medication that treats cytomegalovirus infections by providing systemic antiviral activity with proven efficacy and safety profiles for critical anti-infective therapy.
Therapeutic categories
Primary indications
- Valganciclovir is an antiviral medication used for the treatment of cytomegalovirus infections
Product Snapshot
- Valganciclovir is an oral small molecule available primarily in tablet and powder-for-solution formulations
- It is used as an antiviral for the treatment of cytomegalovirus infections
- The product is approved for use in the US and Canada, with some investigational status maintained
Clinical Overview
Pharmacologically, valganciclovir exhibits antiviral activity following oral administration by rapid hydrolysis via intestinal and hepatic esterases, converting it into the active agent ganciclovir. Ganciclovir functions as a selective inhibitor of viral DNA synthesis. Within CMV-infected cells, it undergoes initial phosphorylation to the monophosphate form catalyzed by the viral protein kinase UL97. Subsequent phosphorylation steps, mediated by host cellular kinases, generate ganciclovir triphosphate, the active metabolite. This triphosphate form competitively inhibits viral DNA polymerase, incorporates into viral DNA, and causes premature chain termination by interrupting phosphodiester bond formation. The antiviral effect is largely confined to infected cells due to the necessity of viral kinase activity for activation.
Key absorption, distribution, metabolism, and elimination (ADME) characteristics include high oral bioavailability owing to the prodrug design, extensive conversion to ganciclovir pre-systemically, and predominant renal excretion of unchanged ganciclovir. The intracellular half-life of ganciclovir triphosphate contributes to sustained antiviral effects.
Safety considerations include potential myelosuppression (e.g., neutropenia, anemia) and nephrotoxicity, requiring hematologic and renal function monitoring during therapy. Valganciclovir may also reduce seizure threshold and exhibit teratogenicity risks, necessitating careful patient selection and risk mitigation. It is classified as a cytomegalovirus nucleoside analog DNA polymerase inhibitor within the broader categories of antiviral and anti-infective systemic agents.
For API procurement, emphasis should be placed on stringent quality control measures to ensure chemical purity, appropriate polymorphic form, and consistent prodrug stability. Compliance with pharmacopeial standards and verification of esterase-mediated convertible activity to ganciclovir are crucial for product efficacy and regulatory acceptance.
Identification & chemistry
| Generic name | Valganciclovir |
|---|---|
| Molecule type | Small molecule |
| CAS | 175865-60-8 |
| UNII | GCU97FKN3R |
| DrugBank ID | DB01610 |
Pharmacology
| Summary | Valganciclovir is an oral prodrug of ganciclovir that is rapidly converted by esterases to its active form. Ganciclovir triphosphate selectively inhibits viral DNA polymerase in cytomegalovirus-infected cells by incorporating into viral DNA and terminating DNA chain elongation. This mechanism disrupts viral DNA synthesis, resulting in inhibition of viral replication. |
|---|---|
| Mechanism of action | Valganciclovir is a prodrug of ganciclovir that exists as a mixture of two diastereomers. 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. |
| Pharmacodynamics | Valganciclovir is an antiviral medication used to treat cytomegalovirus infections. As the L-valyl ester of ganciclovir, it is actually a prodrug for ganciclovir. After oral administration, it is rapidly converted to ganciclovir by intestinal and hepatic esterases. After this, it (being an analogue of guanosine) gets incorporated into DNA and thus cannot be properly read by DNA polymerase. This results in the termination of the elongation of viral DNA. |
Targets
| Target | Organism | Actions |
|---|---|---|
| DNA | Humans | adduct |
ADME / PK
| Absorption | Valganciclovir is well absorbed from the gastrointestinal tract and the absolute bioavailability from valganciclovir tablets (following administration with food) is approximately 60%. |
|---|---|
| Half-life | Approximately 4.08 hours. Increased in patients with renal function impairment. |
| Protein binding | Plasma protein binding of ganciclovir is 1% to 2% over concentrations of 0.5 and 51 mg/mL. |
| Metabolism | Rapidly hydrolyzed in the intestinal wall and liver to ganciclovir. No other metabolites have been detected. |
| Route of elimination | The major route of elimination of valganciclovir is by renal excretion as ganciclovir through glomerular filtration and active tubular secretion. |
| Volume of distribution | * 0.703 ± 0.134 L/kg |
| Clearance | * 3.07+/- 0.64 mL/min/kg [IV administration] * 5.3 L/hr [Patient with creatinine clearance of 70.4 mL/min] |
Formulation & handling
- Valganciclovir is a small molecule drug formulated exclusively for oral administration in tablet and powder for solution forms.
- It is soluble in water with moderate hydrophilicity (LogP -0.69) and recommended to be taken with food to enhance absorption.
- Formulations should consider stability and protection from moisture due to its solid powder form for solution and coated tablet presentations.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient is marketed in Canada and the United States, with key patents having expired in 2015 and additional patents protecting the product until late 2027, indicating a transitional phase toward market maturity. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Valganciclovir is supplied by multiple packagers, indicating a diversified manufacturing base. Branded products are primarily marketed in North American regions, including the US and Canada. The presence of patents extending to late 2027 suggests that generic competition may be limited until those patents expire. |
|---|
Safety
| Toxicity | It is expected that an overdose of valganciclovir could also possibly result in increased renal toxicity. |
|---|
- Overexposure to valganciclovir may enhance renal toxicity risk
- Handle with care to prevent accidental overdose due to potential nephrotoxic effects
- Use appropriate protective measures to minimize worker exposure
Valganciclovir is a type of Nucleoside and nucleotide analogs
Nucleoside and nucleotide analogs are a vital subcategory of pharmaceutical active pharmaceutical ingredients (APIs) widely used in the development of antiviral and anticancer drugs. These compounds are structurally similar to natural nucleosides and nucleotides found in DNA and RNA, but they possess modified functional groups that enhance their therapeutic properties.
Nucleoside analogs are synthetic compounds composed of a nucleobase (adenine, cytosine, guanine, or thymine) and a sugar molecule, linked by a glycosidic bond. These analogs can act as competitive inhibitors of viral DNA or RNA synthesis by incorporating themselves into the growing nucleic acid chain, leading to premature termination of replication. This mechanism makes them effective against viral infections, including HIV, hepatitis B, and herpes.
On the other hand, nucleotide analogs are nucleoside analogs with an additional phosphate group attached to the sugar molecule. The presence of the phosphate group enhances their activity by providing an additional site for interaction with enzymes involved in nucleic acid synthesis. Nucleotide analogs are often used as prodrugs, requiring intracellular phosphorylation to become active. They have shown remarkable success in the treatment of certain types of cancer, particularly hematological malignancies.
The development and synthesis of nucleoside and nucleotide analogs require expertise in organic chemistry and medicinal chemistry. These compounds undergo rigorous testing to ensure their safety, efficacy, and compatibility with various drug formulations. The optimization of their pharmacokinetic and pharmacodynamic properties is a key focus during the drug development process.
In conclusion, nucleoside and nucleotide analogs are crucial components in the pharmaceutical industry's pursuit of effective antiviral and anticancer medications. Their unique structural modifications and mechanisms of action make them promising candidates for combating life-threatening diseases.
Valganciclovir (Nucleoside and nucleotide analogs), classified under Anti-infective Agents
Anti-infective agents are a vital category of pharmaceutical active pharmaceutical ingredients (APIs) used in the treatment of various infectious diseases. These agents play a crucial role in combating bacterial, viral, fungal, and parasitic infections. The demand for effective anti-infective APIs has grown significantly due to the increasing prevalence of drug-resistant microorganisms.
Anti-infective APIs encompass a wide range of substances, including antibiotics, antivirals, antifungals, and antiparasitics. Antibiotics are particularly important in fighting bacterial infections and are further categorized into different classes based on their mode of action and target bacteria. Antivirals are designed to inhibit viral replication and are essential in the treatment of viral infections such as influenza and HIV. Antifungals combat fungal infections, while antiparasitics are used to eliminate parasites that cause diseases like malaria and helminthiasis.
The development and production of high-quality anti-infective APIs require stringent manufacturing processes and adherence to regulatory standards. Pharmaceutical companies invest heavily in research and development to discover new and more effective anti-infective agents. Additionally, ensuring the safety, efficacy, and stability of these APIs is of utmost importance.
The global market for anti-infective APIs is driven by factors such as the rising incidence of infectious diseases, the emergence of new and drug-resistant pathogens, and the growing demand for improved healthcare infrastructure. Continuous advancements in pharmaceutical technology and the development of innovative drug delivery systems further contribute to the expansion of this market.
In conclusion, anti-infective agents are a critical category of pharmaceutical APIs that play a pivotal role in treating infectious diseases. Their effectiveness in combating various types of infections makes them essential components in the arsenal of modern medicine.
Valganciclovir API manufacturers & distributors
Compare qualified Valganciclovir API suppliers worldwide. We currently have 7 companies offering Valganciclovir API, with manufacturing taking place in 3 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Cipla | Producer | India | India | CoA, GMP, USDMF, WC | 164 products |
| Corden Pharma | Producer | Germany | United States | CoA, GMP, USDMF | 45 products |
| Hetero Drugs | Producer | India | India | CoA, GMP, USDMF, WC | 98 products |
| Ind-Swift Labs. | Producer | India | India | CoA, GMP, WC | 27 products |
| Mylan | Producer | India | India | CoA, GMP, USDMF, WC | 201 products |
| Sun Pharma | Producer | India | India | CoA, GMP, WC | 219 products |
| Zhejiang Charioteer | Producer | China | China | CoA, USDMF | 9 products |
When sending a request, specify which Valganciclovir API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
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