Regonat Regorafenib Tablets 40mg

[Product Name] Regorafenib Tablets

[Other Names] Stivarga / Regorafenib

[English Name] Regorafenib Tablets

[Specification] 40 mg × 28 tablets/box

[Manufacturer] Natco Pharma Ltd

Regorafenib is a novel small-molecule multi-kinase inhibitor capable of blocking various kinases that promote tumor growth—such as vascular endothelial growth factor receptors (VEGFR1-3), tyrosine protein kinase receptors (TIE and Ret), platelet-derived growth factor receptor (PDGFR-β), basic fibroblast growth factor receptor (FGFR-1), serine/threonine protein kinase (Raf), and mitogen-activated protein kinase (p38)—thereby exerting an anti-tumor effect.

Regorafenib has been approved in 60 countries worldwide—including the United States, Europe, and Japan—for the treatment of metastatic colorectal cancer (mCRC). It is also approved for the treatment of adult patients with unresectable or metastatic gastrointestinal stromal tumors (GIST) whose disease has progressed, or who are intolerant to, prior treatment with imatinib and sunitinib.

In April 2017, the U.S. FDA approved Regorafenib for the treatment of unresectable hepatocellular carcinoma. Regorafenib demonstrates significant efficacy in patients with advanced liver cancer who have developed resistance to (or failed) prior treatment with Sorafenib (Nexavar).

[Indications]

Regorafenib is indicated for:

1. Patients with locally advanced, unresectable, or metastatic gastrointestinal stromal tumors (GIST) who have previously been treated with imatinib and sunitinib. Regorafenib is a multi-targeted anti-tumor agent utilized in the treatment of various malignancies; its indications primarily include the following:

Colorectal Cancer

Indicated for patients with metastatic colorectal cancer (mCRC) who have previously been treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy regimens (including anti-VEGF therapy), and—if KRAS wild-type—anti-EGFR therapy. For patients with metastatic colorectal cancer (mCRC) whose disease has progressed following standard first-line and second-line therapies, Regorafenib serves as a third-line treatment option; it significantly extends both progression-free survival and overall survival, thereby providing patients with an additional therapeutic avenue.

Gastrointestinal Stromal Tumors (GIST)

Indicated for the treatment of patients with locally advanced, unresectable, or metastatic gastrointestinal stromal tumors (GIST) who have previously received treatment with Imatinib and Sunitinib. When GIST patients develop resistance to—or intolerance of—first-line therapies such as Imatinib, Regorafenib continues to exert anti-tumor effects by inhibiting specific targets (such as KIT), thereby controlling tumor growth and metastasis and improving patient prognosis.

Hepatocellular Carcinoma (HCC)

Indicated for patients with hepatocellular carcinoma (HCC) who have previously received treatment with Sorafenib. For patients with unresectable HCC, or those experiencing recurrence or metastasis following surgery, Regorafenib serves as a second-line therapy following disease progression on Sorafenib treatment; it inhibits tumor angiogenesis and tumor cell proliferation, thereby extending patient survival and improving quality of life.

Other Potential Applications

Regorafenib has also demonstrated therapeutic potential in the treatment of various other malignancies. For instance, clinical trials involving thyroid cancer, non-small cell lung cancer (NSCLC), and breast cancer have observed that Regorafenib exerts a certain inhibitory effect on these tumors; however, it is not currently approved for the routine treatment of these specific cancers, and relevant research remains ongoing.

The specific use of Regorafenib requires a comprehensive assessment by a physician, taking into account the patient's disease status, physical condition, prior treatment history, and other factors to determine the most appropriate treatment regimen.

3. Indicated for patients with advanced liver cancer who have developed resistance to (or failed) treatment with Nexavar (Sorafenib).

[Dosage and Administration]

Recommended Dosage for Regorafenib: Administer in 28-day cycles. For the first 21 days of each cycle, take orally once daily at a dose of 160 mg (4 tablets). Continue treatment until disease progression occurs or until intolerable toxicity develops. The dosage and administration of Regorafenib may vary depending on factors such as the patient's specific medical condition and physical status. The following outlines the general guidelines:

Recommended Dosage

The usual recommended dose is 160 mg (4 tablets, 40 mg each), taken once daily. The tablets should be swallowed whole at the same time each day, accompanied by a low-fat meal (containing fewer than 600 calories and less than 30% fat).

Treatment Cycle

The medication is taken continuously for 3 weeks, followed by a 1-week break. Each 4-week period constitutes one treatment cycle, which is continued until disease progression occurs or intolerable toxicity develops.

Dosage Adjustments

Adjustments for Adverse Reactions: During the course of treatment, if adverse reactions occur, the dosage may need to be adjusted based on the severity of the reaction. Common adverse reactions include hand-foot skin reactions, hypertension, and diarrhea. Generally, for Grade 1 adverse reactions, no dosage adjustment is required. If a Grade 2 adverse reaction occurs for the first time, temporary discontinuation of the medication may be considered; once symptoms resolve to Grade 0 or 1, treatment may be resumed at the original dose or at a reduced dose level (e.g., decreasing from 160 mg to 120 mg, or subsequently to 80 mg). If a Grade 2 adverse reaction recurs, or if a Grade 3 adverse reaction occurs, the medication typically must be temporarily discontinued; once symptoms resolve, treatment may be resumed at a reduced dose level. In the event of a Grade 4 adverse reaction, the medication must be permanently discontinued.

Adjustments for Special Populations: For patients with mild hepatic impairment (Child-Pugh Class A), no dosage adjustment is required. For patients with moderate hepatic impairment (Child-Pugh Class B), the recommended starting dose is 120 mg once daily. Currently, use in patients with severe hepatic impairment (Child-Pugh Class C) is not recommended. For patients with renal impairment, no dosage adjustment is required for those with mild to moderate impairment; however, experience with the use of this medication in patients with severe renal impairment is limited, and it should be used with caution in this population.

Patients should strictly adhere to their physician's instructions, taking the medication on time and at the prescribed dosage. Patients should not independently increase, decrease, or discontinue the dosage in order to ensure the safety and efficacy of the treatment.

For oral administration: take at the same time each day, accompanied by a low-fat breakfast containing no more than 30% fat. If a dose is missed, do not take a double dose to make up for it.

Product Specifications

Product Name: Regorafenib Hydrochloride Tablets (Regorafenib) 40mg × 28 Tablets — Regonat

Common Name: Regorafenib

Active Ingredient: Regorafenib

Dosage Form: Tablets

Specification: 40mg × 28 tablets/bottle

Manufacturer: Natco Pharma Ltd

Indications: Indicated for the treatment of patients with metastatic colorectal cancer (CRC) who have been previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, an anti-VEGF therapy, and—if KRAS wild-type—an anti-EGFR therapy.

Dosage and Administration: Recommended dosage of Regorafenib: Administer in 28-day cycles, taking 160 mg (4 tablets) orally once daily for the first 21 days of each cycle. Continue treatment until disease progression or unacceptable toxicity occurs.

Administer orally at the same time each day, taken with a low-fat breakfast (containing no more than 30% fat). If a dose is missed, do not take a double dose to make up for it.