Pazopanib API Manufacturers & Suppliers
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Pazopanib | CAS No: 444731-52-6 | GMP-certified suppliers
A medication that treats advanced renal cell cancer and previously treated advanced soft tissue sarcoma, supporting reliable oncology portfolio needs for global API sourcing teams.
Therapeutic categories
Primary indications
- Treatment of advanced renal cell cancer and advanced soft tissue sarcoma (in patients previously treated with chemotherapy)
Product Snapshot
- Oral small‑molecule API supplied as film‑coated tablet formulations
- Used in products targeting advanced renal cell carcinoma and advanced soft tissue sarcoma
- Approved in major regulated markets including the US, Canada, and the EU
Clinical Overview
Pazopanib exerts its pharmacological activity through potent inhibition of multiple receptor tyrosine kinases central to tumour angiogenesis. Its primary targets include VEGFR‑1, VEGFR‑2, VEGFR‑3, PDGFR‑alpha, PDGFR‑beta, and c‑kit. These pathways regulate endothelial cell proliferation, tumour vascularization, and survival. Steady‑state plasma concentrations exceeding 15 micrograms per millilitre are associated with maximal suppression of VEGFR2 phosphorylation. In clinical settings, these exposures correlate with reduced tumour perfusion, increased tumour apoptosis, decreased interstitial fluid pressure, and the development of intratumoural hypoxia.
Absorption and disposition characteristics are influenced by transporter and enzyme pathways. Pazopanib is a substrate for P‑glycoprotein, BCRP/ABCG2, and multiple cytochrome P450 enzymes, including CYP1A2, CYP2C8, and CYP3A isoforms. It also exhibits inhibitory activity toward several of these pathways. These properties introduce a potential for clinically relevant drug–drug interactions, particularly with compounds sharing narrow therapeutic indices. Hepatic involvement in its clearance aligns with observed risks of hepatotoxicity.
Safety considerations include liver function abnormalities, hypertension, gastrointestinal disturbances, and the potential for QTc prolongation. As a vascular endothelial growth factor pathway inhibitor, pazopanib may also contribute to impaired wound healing or bleeding events in susceptible patients. Use in immunocompromised settings should consider its classification among immunosuppressive and kinase‑inhibiting agents.
Pazopanib is marketed in several regions, with Votrient being a widely recognized brand.
For API procurement, sourcing should prioritize manufacturers with demonstrated control of polymorphic form, impurity profile, and particle characteristics, as these attributes can influence bioavailability, stability, and regulatory acceptability in global markets.
Identification & chemistry
| Generic name | Pazopanib |
|---|---|
| Molecule type | Small molecule |
| CAS | 444731-52-6 |
| UNII | 7RN5DR86CK |
| DrugBank ID | DB06589 |
Pharmacology
| Summary | Pazopanib is a multitargeted tyrosine kinase inhibitor that blocks VEGFR‑1/2/3, PDGFR‑α/β, and c‑Kit, disrupting key signaling pathways that drive tumor angiogenesis and stromal support. By inhibiting these receptors at clinically relevant concentrations, it reduces tumor blood flow, increases apoptotic activity, and suppresses tumor growth. Its pharmacologic profile reflects broad anti‑angiogenic and antiproliferative effects relevant to advanced renal cell carcinoma and soft tissue sarcoma. |
|---|---|
| Mechanism of action | Pazopanib is a second-generation multitargeted tyrosine kinase inhibitor against vascular endothelial growth factor receptor-1, -2, and -3, platelet-derived growth factor receptor-alpha, platelet-derived growth factor receptor-beta, and c-kit. These receptor targets are part of the angiogenesis pathway that facilitates the formation of tumour blood vessel for tumour survival and growth. |
| Pharmacodynamics | Pazopanib is a synthetic indazolylpyrimidine and reaches steady state concentrations of >15 μg/ml. This concentration is high enough to observe maximal inhibition of VEGFR2 phosphorylation and some anti-tumour activity (concentration required to inhibit receptors is 0.01 - 0.084 μmol/L). A reduction in tumour blood flow, increased tumour apoptosis, inhibition of tumour growth, reduction in tumour interstitial fluid pressure, and hypoxia in cancer cells can be observed in patients receiving treatment. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Vascular endothelial growth factor receptor 1 | Humans | inhibitor |
| Vascular endothelial growth factor receptor 2 | Humans | inhibitor |
| Vascular endothelial growth factor receptor 3 | Humans |
ADME / PK
| Absorption | Absorption of pazopanib in cancer patients is slow and incomplete. In patients with solid tumour, over a dose range of 50-2000 mg, absorption is nonlinear. Significant accumulation of pazopanib can also be observed in patients receiving 800 mg once daily for 22 days. Crushing tablets may increase exposure (increase in Cmax and AUC, while Tmax decreases by 2 hours). Bioavailability, oral tablet 800 mg, cancer patient = 21%; Bioavailability may be low due to incomplete absorption from the gastrointestinal tract. The major circulating component of the drug in the systemic is pazopanib, and not its metabolites. Mean maximum plasma concentration= 58.1 µg/mL; Mean AUC= 1037 µg · h/mL; |
|---|---|
| Half-life | 35 hours. Oral absorption is not the rate limiting step of elimination from the plasma. |
| Protein binding | >99% protein bound, independent of concentrations over a range of 10-100 μg/mL. |
| Metabolism | Metabolized by CYP3A4 and to a lesser extent by CYP1A2 and CYP2C8. Metabolites are less active than pazopanib (10 to 20-fold less active). Three of its metabolites can be observed in the systemic and account for <10% of plasma radioactivity. |
| Route of elimination | Primarily excreted via feces (82.2%) and to a negligible extent via urine (<4%) in cancer patients. Most of the administered dose is excreted unchanged. Approximately 10% of dose are oxidative metabolites and are mostly eliminated via the feces. |
| Volume of distribution | Vd steady state, IV administration 5 mg, cancer patient = 11.1 L (range of 9.15 - 13.4) |
| Clearance | CL, cancer patient, IV administration 5 mg = 4mL/min Half of the absorbed dose is cleared via oxidative metabolism. |
Formulation & handling
- Oral small‑molecule with very low aqueous solubility, typically formulated as film‑coated tablets to aid handling and control release.
- Bioavailability is food‑dependent, so formulations should minimize variability related to gastric conditions and pH; coadministration with antacids can impact absorption.
- Solid-state stability is generally good, but manufacturing should account for its lipophilic nature (LogP ~3.6) to ensure consistent dissolution performance.
Regulatory status
| Lifecycle | Patent protection for the API has lapsed in the United States, with expiries occurring between 2021 and 2023, indicating that the product is now in a mature phase. With availability in the US, Canada, and the EU, the market is expected to reflect established competition consistent with post‑patent markets. |
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| Markets | US, Canada, EU |
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Supply Chain
| Supply chain summary | Pazopanib was introduced by a single originator company, which established the reference product across major regulated markets, including the United States, Canada, and the European Union. Branded formulations remain globally available, with some additional regional brand variants outside the core markets. Key US patents expired between 2021 and 2023, indicating that generic manufacturing is already possible and suggesting an expanding competitive landscape. |
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Pazopanib is a type of Protein kinase inhibitors
Protein kinase inhibitors are a vital subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that play a crucial role in targeted cancer therapies. These inhibitors specifically target and block the activity of protein kinases, enzymes that regulate various cellular processes, including cell growth, division, and signal transduction.
Protein kinase inhibitors function by binding to the active site of protein kinases, preventing them from phosphorylating specific proteins and disrupting intracellular signaling pathways. This targeted approach inhibits the uncontrolled growth and proliferation of cancer cells, ultimately leading to their death.
The development of protein kinase inhibitors has revolutionized cancer treatment by providing more effective and less toxic alternatives to traditional chemotherapy. These drugs have demonstrated impressive results in the treatment of various cancers, including lung, breast, and leukemia.
The pharmaceutical industry invests heavily in research and development to discover novel protein kinase inhibitors with improved potency, selectivity, and pharmacokinetic properties. High-throughput screening, computational modeling, and structure-activity relationship studies are employed to identify potential lead compounds.
The success of protein kinase inhibitors in treating cancer has spurred significant interest in this subcategory of APIs. Ongoing research aims to expand their applications to other diseases, such as autoimmune disorders and neurological conditions.
In conclusion, protein kinase inhibitors are a valuable class of pharmaceutical APIs with immense potential for targeted cancer therapies. Continued advancements in this field hold promise for improved treatment outcomes and enhanced patient care.
Pazopanib (Protein kinase inhibitors), classified under Anticancer drugs
Anticancer drugs belong to the pharmaceutical API (Active Pharmaceutical Ingredient) category designed specifically to combat cancer cells. These powerful medications play a crucial role in cancer treatment and are developed to target and destroy cancerous cells, preventing their growth and spread.
Anticancer drugs are classified based on their mode of action and can include various types such as chemotherapy drugs, targeted therapy drugs, immunotherapy drugs, and hormonal therapy drugs. Chemotherapy drugs work by interfering with the cell division process, thereby inhibiting the growth of cancer cells. Targeted therapy drugs, on the other hand, are designed to attack specific molecules or genes involved in cancer growth, minimizing damage to healthy cells. Immunotherapy drugs stimulate the body's immune system to recognize and destroy cancer cells. Hormonal therapy drugs are used in cancers that are hormone-dependent, such as breast or prostate cancer, to block the hormones that fuel cancer cell growth.
These APIs are typically synthesized through complex chemical processes in state-of-the-art manufacturing facilities. Stringent quality control measures ensure the purity, potency, and safety of these drugs. Anticancer APIs undergo rigorous testing and adhere to stringent regulatory guidelines before being approved for clinical use.
Due to their critical role in cancer treatment, anticancer drugs are in high demand worldwide. Researchers and pharmaceutical companies continually strive to develop new and more effective APIs in this category to enhance treatment outcomes and minimize side effects. The ongoing advancements in the field of anticancer drug development offer hope for improved cancer therapies and better patient outcomes.
Pazopanib API manufacturers & distributors
Compare qualified Pazopanib API suppliers worldwide. We currently have 9 companies offering Pazopanib 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 |
|---|---|---|---|---|---|
| Acebright Pharma | Producer | India | India | CoA, USDMF | 9 products |
| Cipla | Producer | India | India | CoA, USDMF | 164 products |
| Dr. Reddy's | Producer | India | India | BSE/TSE, CoA, FDA, GMP, MSDS, USDMF, WC | 170 products |
| Formosa Labs | Producer | Taiwan | Taiwan | CoA, USDMF | 36 products |
| Gonane Pharma | Producer | India | India | BSE/TSE, CoA, GMP, MSDS | 166 products |
| Hetero Labs | Producer | India | India | CoA, GMP, USDMF, WC | 90 products |
| Laurus Labs | Producer | India | India | CoA, GMP, WC | 50 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Shilpa Medicare Ltd | Producer | India | India | BSE/TSE, CoA, GMP, ISO9001, MSDS, WC | 54 products |
When sending a request, specify which Pazopanib 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 Pazopanib 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.
