Pazopanib
 |
|
| Clinical data | |
|---|---|
| Pronunciation | /pæˈzoʊpənɪb/ paz-OH-pə-nib |
| Trade names | Votrient |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a610013 |
| License data | |
| Pregnancy category |
|
| Routes of administration |
By mouth (tablets) |
| ATC code | |
| Legal status | |
| Legal status | |
| Pharmacokinetic data | |
| Bioavailability | 14–21% |
| Protein binding | >99.5% |
| Metabolism | Liver: CYP3A4 (major), 1A2 and 2C8 (minor) |
| Biological half-life | 30.9–31.9 hours |
| Excretion | Faeces (primary), urine (<4%) |
| Identifiers | |
|
|
| CAS Number | |
| PubChem CID | |
| IUPHAR/BPS | |
| DrugBank | |
| ChemSpider | |
| UNII | |
| KEGG | |
| ChEBI | |
| ChEMBL | |
| Chemical and physical data | |
| Formula | C21H23N7O2S |
| Molar mass | 437.517 g/mol |
| 3D model (Jmol) | |
|
|
|
|
  (what is this?)
|
|
Pazopanib (trade name Votrient) is a potent and selective multi-targeted receptor tyrosine kinase inhibitor that blocks tumour growth and inhibits angiogenesis. It has been approved for renal cell carcinoma and soft tissue sarcoma by numerous regulatory administrations worldwide.
It is approved by numerous regulatory administrations worldwide (including the FDA (19 October 2009), EMA (14 June 2010), MHRA (14 June 2010) and TGA (30 June 2010)) for use as a treatment for advanced/metastatic renal cell carcinoma and advanced soft tissue sarcomas. In Australia and New Zealand, it is subsidised under the PBS and by Pharmac respectively, under a number of conditions, including:
It has also demonstrated initial therapeutic properties in patients with ovarian and non-small cell lung cancer, though plans to apply to the EMA for a variation to include advanced ovarian cancer have been withdrawn and a license will not be sought in any country.
The only contraindication is hypersensitivity to pazopanib or any of its excipients. Cautions include:
It has one black box warning by the US FDA, severe hepatotoxicity, including fatalities.
The most common side effects of pazopanib are nausea, vomiting, diarrhoea (occurs in about half of patients), changes in hair colour, hypertension (which usually occurs during the first few weeks of treatment), appetite loss, hyperglycaemia, hypoglycaemia, electrolyte abnormalities (including hypocalcaemia, hypomagnesemia, hypophosphatemia), lab anomalies (including increased AST, ALT and protein in the urine), oedema, hair loss or discolouration, taste changes, abdominal pain, hypertension, rash, fatigue and myelosuppression (including leucopenia, neutropenia, thrombocytopenia and lymphopenia). It has been associated with a low, but real risk of potentially fatal liver damage.
...
Wikipedia