Introduction
Pazorest 200 mg, formulated with Pazopanib Hydrochloride, is a potent oral anticancer agent specifically designed for the treatment of various advanced cancers. Manufactured by Everest Pharmaceuticals Ltd and made available globally by Orio Pharma, Pazorest belongs to the class of vascular endothelial growth factor receptor (VEGFR) inhibitors, primarily indicated for renal cell carcinoma (RCC) and soft tissue sarcoma (STS). This medication is an integral part of targeted cancer therapy, delivering enhanced tumor suppression by inhibiting key angiogenesis pathways involved in cancer growth and proliferation.
Key Indications
- Advanced Renal Cell Carcinoma (RCC)
- Advanced Soft Tissue Sarcoma (STS) in patients who have received prior chemotherapy
- Investigational use in other malignancies such as ovarian, thyroid, and cervical cancer
Mechanism of Action
Pazopanib Hydrochloride, the active component of Pazorest 200 mg, functions as a selective multi-targeted tyrosine kinase inhibitor (TKI). It exerts its antitumor effects by inhibiting the activity of several receptor tyrosine kinases (RTKs), including:
- Vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, VEGFR-3)
- Platelet-derived growth factor receptors (PDGFR-α and PDGFR-β)
- Fibroblast growth factor receptor (FGFR)
- c-Kit (stem cell factor receptor)
By targeting these kinases, Pazorest effectively impairs angiogenesis (blood vessel formation), reduces tumor blood supply, and limits cancer cell proliferation.
Dosage and Administration
Recommended Dose:
- The usual dose of Pazorest is 800 mg taken orally once daily without food (at least one hour before or two hours after a meal).
- In clinical practice, dosage adjustments are often made by using 200 mg tablets, such as Pazorest 200 mg, to accommodate tolerability or patient-specific requirements.
Administration Guidelines:
- Swallow whole with water, do not crush or chew
- Take at the same time each day
- Avoid taking with high-fat meals
Dose Adjustments:
- Dose modifications may be required in case of hepatic impairment, hypertension, or intolerable adverse events
Contraindications
- Hypersensitivity to Pazopanib or any component of the formulation
- Severe hepatic impairment
- Concurrent use with strong CYP3A4 inhibitors or inducers without appropriate dose adjustment
Drug Interactions
- CYP3A4 Modulators: Co-administration with CYP3A4 inducers (e.g., rifampin) or inhibitors (e.g., ketoconazole) can affect Pazorest plasma concentrations
- Gastric pH Modifiers: Proton pump inhibitors, H2-receptor antagonists, and antacids may reduce Pazopanib absorption
- QT-Prolonging Agents: Use with caution; monitor ECG if necessary
- Substrates of CYP Enzymes: Pazopanib may alter plasma concentrations of CYP substrates such as simvastatin and warfarin
Side Effects
Common adverse effects include:
- Hypertension
- Diarrhea
- Hair color changes
- Fatigue
- Nausea and vomiting
- Weight loss
- Anorexia
- Elevated liver enzymes (ALT/AST)
- Hand-foot syndrome
Serious but less common adverse events:
- Hepatotoxicity
- Cardiac dysfunction, including QT prolongation
- Gastrointestinal perforation
- Thromboembolic events
- Hemorrhagic events
- Proteinuria and nephrotic syndrome
Regular monitoring of liver function, blood pressure, and cardiac status is strongly recommended during therapy.
Use in Special Populations
Hepatic Impairment:
- Dose adjustments may be necessary in patients with mild-to-moderate hepatic dysfunction.
- Pazorest is not recommended in severe hepatic impairment.
Renal Impairment:
- No dose adjustment required for mild to moderate renal impairment.
Pregnancy and Lactation:
- Classified as Pregnancy Category D: Use only if potential benefit justifies the risk
- Not recommended during breastfeeding; discontinue nursing or the drug
Pediatric Use:
- Safety and efficacy have not been established in pediatric patients
Geriatric Use:
- No overall differences in safety observed, but caution advised in patients aged 65 and above
Storage and Handling
- Store below 30°C in a dry place
- Protect from light and moisture
- Keep out of reach of children
Overdose Management
In cases of overdose, symptomatic treatment and supportive care are recommended. No specific antidote exists. Monitor for signs of toxicity such as hypertension, hepatotoxicity, and QT prolongation.
Therapeutic Class
- Tyrosine Kinase Inhibitor (TKI)
- Anti-angiogenic Agent
Clinical Efficacy
Clinical trials such as the VEG105192 and PALETTE trial have demonstrated the efficacy of Pazopanib in prolonging progression-free survival in patients with advanced RCC and soft tissue sarcoma, respectively. Its oral administration and manageable toxicity profile make it a preferred choice in long-term oncology regimens.
Conclusion
Pazorest 200 mg (Pazopanib Hydrochloride) Tablet offers a clinically proven, targeted treatment option for patients suffering from advanced renal cell carcinoma and soft tissue sarcoma. By blocking multiple angiogenic and proliferative pathways, Pazorest provides oncologists with a versatile and effective tool for managing challenging malignancies. With strict adherence to dosing, monitoring, and supportive care protocols, Pazorest contributes significantly to improving patient outcomes in oncology.
Available through Orio Pharma, a trusted global oncology medicine supplier, and manufactured under stringent standards by Everest Pharmaceuticals Ltd, Pazorest is designed to meet the highest expectations in cancer therapy.