Regorafenib Monohydrate

Introduction

Regorafenib Monohydrate is an oral multi-kinase inhibitor used in the treatment of various types of cancers. It is designed to inhibit tumor cell proliferation and angiogenesis by targeting multiple signaling pathways involved in cancer growth.

Uses

Regorafenib Monohydrate is used for:

Treatment of metastatic colorectal cancer (CRC) in patients who have previously received standard therapies
Management of unresectable hepatocellular carcinoma (HCC) in patients who have previously been treated
Treatment of advanced gastrointestinal stromal tumors (GIST) after disease progression on imatinib and sunitinib
Treatment of advanced renal cell carcinoma (RCC) following prior therapy

Brand Name	Regorafenib Monohydrate
Type
Weight
Generic	Regorafenib Monohydrate
Manufacturer
Available in	English বাংলা

Mechanism of Action

Regorafenib Monohydrate works by inhibiting multiple tyrosine kinases that are involved in tumor cell signaling, angiogenesis, and cancer progression. It blocks the activity of kinases such as VEGFR, PDGFR, and KIT, which are crucial for tumor growth and blood vessel formation.

How Long Does It Take to Work?

Patients may begin to see initial responses to Regorafenib Monohydrate within a few weeks of starting treatment. However, it may take several months to observe the full extent of its therapeutic effects, depending on the type of cancer and individual response.

Absorption

Regorafenib Monohydrate is well-absorbed after oral administration. It reaches peak plasma concentrations approximately 2 to 4 hours post-dose. Food intake can influence the absorption, but it does not significantly affect the overall efficacy of the drug.

Route of Elimination

The drug is primarily metabolized in the liver via cytochrome P450 enzymes, especially CYP3A4. It is excreted mainly in the feces, with a smaller amount eliminated in the urine. Regorafenib and its metabolites are responsible for the drug's therapeutic effects.

Dosage

The recommended dose is 160 mg Regorafenib (four 40 mg tablets) taken orally once daily for the first 21 days of each 28-day cycle. Treatment should be continued until disease progression or unacceptable toxicity. Regorafenib should be taken at the same time each day and swallowed tablet whole with water after a low-fat meal that contains less than 600 calories and less than 30% fat. Two doses of Regorafenib should not be taken on the same day to make up for a missed dose from the previous day.

Dose Modifications: If dose modifications are required, the dose should be reduced in 40 mg (one tablet) increments; the lowest recommended daily dose of Regorafenib is 80 mg daily. Or, as directed by the registered physicians.

Pediatric Use: The safety and efficacy of Regorafenib in pediatric patients less than 18 years of age have not been established.

The recommended dosage of Regorafenib Monohydrate is 160 mg administered orally once daily for 21 days, followed by 7 days off treatment in a 28-day cycle. The exact dosage may vary based on the patient's condition and tolerance.

Administration

Regorafenib Monohydrate should be taken orally, with or without food, at the same time each day. It is typically taken as a single daily dose. Swallow the tablets whole; do not chew or crush them. Adherence to the dosing schedule is important for optimal efficacy.

Side Effects

Common side effects include:

Fatigue
Diarrhea
Hypertension
Hand-foot skin reaction
Nausea

Serious side effects may include liver toxicity, bleeding, and gastrointestinal perforation. Regular monitoring and supportive care may be necessary.

Toxicity

Toxicity symptoms may include severe diarrhea, significant hypertension, or liver enzyme abnormalities. In cases of severe adverse reactions, dosage adjustment or discontinuation of therapy may be required. Immediate medical consultation is advised for managing toxicity.

Precautions

Precautions include:

Monitoring for signs of liver dysfunction and adjusting dosage as needed
Regular blood pressure monitoring due to the risk of hypertension
Assessing for gastrointestinal symptoms such as bleeding or perforation

Ensure that patients are informed of potential side effects and advised to seek medical help if severe symptoms occur.

Interaction

Regorafenib Monohydrate may interact with other medications that affect liver enzymes, particularly CYP3A4 inhibitors or inducers. Inform healthcare providers of all concurrent medications to avoid potential interactions and adjust dosages accordingly.

Disease Interaction

Use Regorafenib Monohydrate with caution in patients with pre-existing liver conditions, gastrointestinal disorders, or uncontrolled hypertension. Dose adjustments and regular monitoring may be necessary for these individuals.

Drug Interaction

Interactions with drugs that impact hepatic metabolism (such as strong CYP3A4 inducers or inhibitors) may affect the efficacy and safety of Regorafenib Monohydrate . Consult with healthcare providers to manage and monitor drug interactions effectively.

Food Interactions

Food intake can affect the absorption of Regorafenib Monohydrate , but the impact is minimal. It is generally recommended to take the medication consistently with or without food as advised by the prescribing physician.

Pregnancy Use

Regorafenib Monohydrate is classified as Category D during pregnancy. It should be used only if the potential benefits outweigh the risks to the fetus. Pregnant women should avoid using this drug unless absolutely necessary and under strict medical supervision.

Lactation Use

The safety of Regorafenib Monohydrate during lactation is not well-established. It is generally advised to avoid breastfeeding during treatment due to potential risks to the infant. Consult with a healthcare provider for appropriate alternatives if breastfeeding is a concern.

Acute Overdose

Acute overdose may result in severe side effects such as pronounced gastrointestinal symptoms, significant blood pressure changes, or liver dysfunction. In case of overdose, seek immediate medical attention to manage and mitigate the effects.

Contraindication

Regorafenib Monohydrate is contraindicated in patients with known hypersensitivity to the drug or its components. It should also be avoided in individuals with severe hepatic impairment due to increased risk of adverse effects.

Use Direction

Administer Regorafenib Monohydrate exactly as prescribed by the healthcare provider. Follow the dosing schedule of once daily for 21 days, followed by a 7-day break, and do not alter the dose without medical guidance.

Storage Conditions

Store Regorafenib Monohydrate at room temperature, away from moisture and heat. Keep the medication in its original container to protect it from light and humidity. Ensure it is kept out of reach of children.

Volume of Distribution

The volume of distribution for Regorafenib Monohydrate is approximately 1200 liters, indicating extensive tissue distribution beyond the plasma compartment.

Half Life

The terminal half-life of Regorafenib Monohydrate is approximately 30 hours, allowing for once-daily dosing. This prolonged half-life supports sustained therapeutic levels throughout the dosing cycle.

Clearance

Regorafenib Monohydrate is primarily cleared through hepatic metabolism and biliary excretion. The clearance rate may be affected by liver function and concurrent use of other medications that influence hepatic metabolism.

See in details version Regorafenib Monohydrate also Regorafenib Monohydrate in bangla