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Valrubicin | CAS No: 56124-62-0 | GMP-certified suppliers
A medication that treats bladder cancer by providing localized antineoplastic activity with reduced systemic toxicity through targeted intravesical administration.
Therapeutic categories
Primary indications
- For the treatment of cancer of the bladder
Product Snapshot
- Valrubicin is an injectable cytotoxic solution formulated for intravesical administration
- It is primarily indicated for the treatment of bladder cancer
- Valrubicin holds regulatory approval in the United States and Canada
Clinical Overview
Pharmacodynamically, valrubicin acts as an anticancer agent primarily through interference with nucleic acid metabolism. After penetrating tumor cells, the drug intercalates DNA, inhibiting incorporation of nucleosides into nucleic acids and inducing chromosomal damage. Valrubicin causes cell cycle arrest at the G2 phase, ultimately leading to cytotoxic effects in rapidly dividing cancer cells. Notably, valrubicin and its metabolites impair the normal DNA breaking-resealing function of topoisomerase II, an enzyme essential for DNA replication and repair. While valrubicin does not exhibit strong DNA binding affinity itself, the topoisomerase II inhibition represents a key mechanism underlying its antineoplastic activity.
Absorption of valrubicin beyond the bladder is limited due to its mode of administration. Metabolism occurs mainly within target tissues, generating active metabolites responsible for topoisomerase II inhibition. Excretion predominantly follows local pathways; systemic exposure is minimal, thus the typical systemic adverse effect profile of anthracyclines, such as cardiotoxicity, is reduced.
Safety considerations include potential local bladder toxicity, with irritative symptoms and potential hemorrhagic cystitis. Systemic toxicity is limited due to localized delivery. As an anthracycline, valrubicin requires careful handling to minimize exposure risk during preparation and administration.
From a procurement perspective, quality assurance for valrubicin APIs mandates stringent control of impurity profiles, stereochemistry, and adherence to good manufacturing practices. Consistency in the chemical synthesis and purity verification is critical due to the compound’s complex semisynthetic nature and potency.
Identification & chemistry
| Generic name | Valrubicin |
|---|---|
| Molecule type | Small molecule |
| CAS | 56124-62-0 |
| UNII | 2C6NUM6878 |
| DrugBank ID | DB00385 |
Pharmacology
| Summary | Valrubicin is an anthracycline anticancer agent that targets DNA and DNA topoisomerase II-alpha, disrupting nucleic acid metabolism. It penetrates cells to intercalate DNA, inhibit nucleoside incorporation, induce chromosomal damage, and cause cell cycle arrest in the G2 phase. Its metabolites interfere with the DNA topoisomerase II-mediated breaking and resealing process, contributing to its cytotoxic effects. |
|---|---|
| Mechanism of action | Valrubicin is an anthracycline that affects a variety of inter-related biological functions, most of which involve nucleic acid metabolism. It readily penetrates into cells, where after DNA intercalation, it inhibits the incorporation of nucleosides into nucleic acids, causes extensive chromosomal damage, and arrests cell cycle in G2. Although valrubicin does not bind strongly to DNA, a principal mechanism of its action, mediated by valrubicin metabolites, is interference with the normal DNA breaking-resealing action of DNA topoisomerase II. |
| Pharmacodynamics | Valrubicin is an anticancer agent. |
Targets
| Target | Organism | Actions |
|---|---|---|
| DNA | Humans | intercalation |
| DNA topoisomerase 2-alpha | Humans | inhibitor |
ADME / PK
| Protein binding | >99% |
|---|---|
| Metabolism | Valrubicin is metabolized to two primary metabolites: N-trifluoroacetyladriamycin and N-trifluoroacetyladriamycinol. |
Formulation & handling
- Valrubicin is a small molecule anthracycline designed for intravesical administration, not for systemic injectable or oral use. Due to low water solubility, formulations are prepared as concentrated aqueous solutions for direct bladder instillation. The compound’s polyketide structure requires protection from light and careful handling to maintain stability during storage and administration.
Regulatory status
| Lifecycle | The API is approaching patent expiry in key markets, including the US and Canada, leading to increased availability of generic formulations. This transition reflects a move towards greater market maturity and competitive pricing. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Valrubicin is manufactured and packaged primarily by Endo Pharmaceutical Solutions Inc. and Primapharm Inc., serving the US and Canadian markets. The branded products, including Valstar and Valtaxin, have a regional presence focused on North America. Patent expiry indicates potential for existing or forthcoming generic competition in these markets. |
|---|
Safety
| Toxicity | The primary anticipated complications of overdosage associated with intravesical administration would be consistent with irritable bladder symptoms. Myelosuppression is possible if valrubicin is inadvertently administered systemically or if significant systemic exposure occurs following intravesical administration (e.g., in patients with bladder/rupture perforation). The maximum tolerated dose in humans by either intraperitoneal or intravenous administration is 600 mg/m<sup>2</sup>. |
|---|
- Avoid systemic exposure to minimize risk of myelosuppression
- Handle with care to prevent intravesical leakage or bladder perforation
- Adhere to maximum tolerated dose limits established for intraperitoneal and intravenous routes
Valrubicin is a type of Antineoplastics
Antineoplastics are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) primarily used in the treatment of cancer. These powerful substances inhibit or destroy the growth of cancer cells, thus impeding the progression of malignancies.
Antineoplastics exert their therapeutic effects through various mechanisms. Some APIs interfere with DNA replication, inhibiting the division and proliferation of cancer cells. Others target specific proteins or enzymes involved in tumor growth, effectively blocking their function. Additionally, certain antineoplastic agents induce programmed cell death, known as apoptosis, in cancer cells.
These APIs find application in a wide range of cancer treatments, including chemotherapy, targeted therapy, immunotherapy, and hormone therapy. They are often administered in combination with other drugs to optimize therapeutic outcomes and minimize drug resistance.
Antineoplastics are typically synthesized through complex chemical processes, ensuring high purity and potency. Stringent quality control measures are implemented throughout manufacturing to meet regulatory standards and ensure patient safety.
Although antineoplastics offer significant benefits in treating cancer, they can also cause adverse effects due to their cytotoxic nature. Common side effects include bone marrow suppression, gastrointestinal disturbances, hair loss, and immune system suppression. Close monitoring and supportive care are essential to manage these side effects effectively.
In conclusion, antineoplastics are a vital category of pharmaceutical APIs used in the treatment of cancer. Through their diverse mechanisms of action, these compounds play a critical role in combating malignancies and improving patient outcomes.
Valrubicin API manufacturers & distributors
Compare qualified Valrubicin API suppliers worldwide. We currently have 2 companies offering Valrubicin API, with manufacturing taking place in 2 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 |
|---|---|---|---|---|---|
| Sicor | Producer | Italy | Italy | CoA, GMP | 47 products |
| Synbias Pharma | Producer | Switzerland | Switzerland | CoA, USDMF | 7 products |
When sending a request, specify which Valrubicin 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.).
Use the list above to find high-quality Valrubicin API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
