Introduction

Regotab 40 mg (Regorafenib) is an advanced targeted cancer therapy designed to combat metastatic colorectal cancer, gastrointestinal stromal tumors, and hepatocellular carcinoma in patients who have undergone previous treatments. As a small molecule inhibitor, Regotab works by targeting multiple membrane-bound and intracellular kinases involved in critical pathological processes such as oncogenesis, tumor angiogenesis, and metastasis. This pharmaceutical innovation from Eskayef Pharmaceuticals offers renewed hope for patients with advanced cancer conditions who have exhausted standard treatment options.

How Regotab Works

Regorafenib, the active ingredient in Regotab, functions as a multikinase inhibitor that blocks several enzymes responsible for cancer cell growth and blood vessel development in tumors. By inhibiting kinases like VEGFR1-3, KIT, PDGFR-alpha/beta, FGFR1-2, and several others, Regotab effectively cuts off the tumor’s blood supply and prevents cancer cells from multiplying. This targeted approach allows for precision therapy that attacks cancer pathways while minimizing damage to healthy cells.

Key Indications

Regotab 40 mg is specifically indicated for:

• Metastatic Colorectal Cancer: For patients previously treated with fluoropyrimidine, oxaliplatin, irinotecan-based chemotherapy, anti-VEGF therapy, and anti-EGFR therapy (if RAS wild-type)
• Gastrointestinal Stromal Tumors: For advanced, unresectable, or metastatic GIST in patients previously treated with Imatinib Mesylate and Sunitinib Malate
• Hepatocellular Carcinoma: For patients with HCC who have previously received Sorafenib treatment

Dosage & Administration

The recommended dosage regimen for Regotab is 160 mg (four 40 mg tablets) taken once daily for the first 21 days of each 28-day treatment cycle. For optimal absorption, tablets should be swallowed whole with water following a low-fat meal containing less than 600 calories and under 30% fat content. Treatment should continue until disease progression or unacceptable toxicity occurs.

If dose modifications become necessary due to adverse effects, physicians may reduce the dose in 40 mg increments, with a minimum recommended daily dose of 80 mg. Consistency in administration timing is crucial for maintaining therapeutic blood levels of the medication.

Pharmacological Profile

Regotab demonstrates comprehensive pharmacokinetic properties that support its therapeutic efficacy:

• Absorption: After a single 160 mg dose, Regorafenib reaches peak plasma concentration at approximately 4 hours
• Distribution: Highly protein-bound (99.5%) in plasma with enterohepatic circulation resulting in multiple concentration peaks
• Metabolism: Primarily metabolized by CYP3A4 and UGT1A9 enzymes, forming active metabolites M-2 and M-5
• Elimination: Mean elimination half-life of approximately 28 hours, with 71% excreted in feces and 19% in urine

Safety Considerations

Before prescribing Regotab, healthcare providers should carefully evaluate patients for potential risks. Regular monitoring is essential during treatment, particularly for hepatic function during the first two months. Key safety considerations include:

• Hepatotoxicity: Liver function tests should be performed before initiation and monitored bi-weekly during the first two months
• Cardiovascular Effects: Blood pressure monitoring is recommended weekly for the first six weeks, then at each treatment cycle
• Dermatological Reactions: Hand-foot skin reactions may occur, particularly in Asian patients
• Hemorrhage Risk: Patients on anticoagulants require close monitoring of INR levels
• Interaction Potential: Strong CYP3A4 inducers or inhibitors should be avoided during treatment

Drug Interactions

Several important drug interactions should be considered when prescribing Regotab:

• CYP3A4 Inducers: Medications like Rifampin, Phenytoin, and St. John’s Wort may decrease Regotab efficacy
• CYP3A4 Inhibitors: Clarithromycin, Ketoconazole, and similar agents may increase Regotab toxicity
• BCRP Substrates: Medications like Methotrexate and certain statins may show increased plasma concentrations when co-administered

Precautions & Special Populations

Regotab requires specific precautions for special patient populations:

• Pregnancy & Breastfeeding: Contraindicated due to potential fetal harm; effective contraception is necessary during treatment and for 2 months after
• Fertility: Both male and female patients should use contraception during treatment and for 2 months afterward
• Surgical Patients: Treatment should be discontinued at least 2 weeks before scheduled surgery
• Hepatic Impairment: Requires careful monitoring and potential dose adjustments

Quality Assurance

Each Regotab tablet is manufactured under strict quality control protocols by Eskayef Pharmaceuticals Ltd., a leading pharmaceutical company with over three decades of experience in producing premium-quality medications. The manufacturing process adheres to international standards, ensuring consistency, potency, and purity in every tablet.

Storage & Handling

To maintain optimal efficacy, Regotab should be stored below 30°C in a cool, dry place away from direct sunlight. Keep out of reach of children. The original packaging protects the medication from environmental factors that might affect its stability.

Conclusion

Regotab 40 mg represents a significant advancement in targeted cancer therapy for patients with advanced colorectal cancer, gastrointestinal stromal tumors, and hepatocellular carcinoma who have undergone previous treatments. With its multikinase inhibitory action, Regotab offers an important treatment option that may help control disease progression and potentially extend survival in these challenging cancer types. As with any powerful anticancer medication, Regotab should be prescribed by specialists familiar with oncology treatments, with careful consideration of the patient’s overall condition, comorbidities, and potential drug interactions.