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Regorafenib Dosage

Medically reviewed by Drugs.com. Last updated on March 13, 2020.

Applies to the following strengths: 40 mg

Usual Adult Dose for Colorectal Cancer

160 mg orally once a day for the first 21 days of each 28-day cycle until disease progression or unacceptable toxicity

Uses:
-Metastatic colorectal cancer (CRC) previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, an anti-VEGF therapy, and an anti-EGFR therapy if RAS wild-type
-Locally advanced, unresectable or metastatic GI stromal tumor (GIST) previously treated with imatinib mesylate and sunitinib malate
-Hepatocellular carcinoma (HCC) previously treated with sorafenib

Usual Adult Dose for Gastrointestinal Stromal Tumor

160 mg orally once a day for the first 21 days of each 28-day cycle until disease progression or unacceptable toxicity

Uses:
-Metastatic colorectal cancer (CRC) previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, an anti-VEGF therapy, and an anti-EGFR therapy if RAS wild-type
-Locally advanced, unresectable or metastatic GI stromal tumor (GIST) previously treated with imatinib mesylate and sunitinib malate
-Hepatocellular carcinoma (HCC) previously treated with sorafenib

Usual Adult Dose for Hepatocellular Carcinoma

160 mg orally once a day for the first 21 days of each 28-day cycle until disease progression or unacceptable toxicity

Uses:
-Metastatic colorectal cancer (CRC) previously treated with fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapy, an anti-VEGF therapy, and an anti-EGFR therapy if RAS wild-type
-Locally advanced, unresectable or metastatic GI stromal tumor (GIST) previously treated with imatinib mesylate and sunitinib malate
-Hepatocellular carcinoma (HCC) previously treated with sorafenib

Renal Dose Adjustments

No adjustment recommended.

Liver Dose Adjustments

Mild (Child-Pugh A) hepatic impairment: No adjustment recommended.
Moderate (Child-Pugh B) hepatic impairment: Dose adjustment(s) may be required; however, no specific guidelines have been suggested. Caution recommended.
Severe (Child-Pugh C) hepatic impairment: Not recommended.

DOSE MODIFICATIONS FOR HEPATIC IMPAIRMENT:
ALT AND/OR AST:
GREATER than or equal to 5 times upper limit of normal (ULN) (maximum Grade 2):
-Any occurrence: Continue therapy; monitor liver function weekly until transaminases return to less than 3 x ULN (Grade 1) or baseline
GREATER than 5 x ULN to less than or equal to 20 x ULN (Grade 3):
-First occurrence: Interrupt therapy; monitor transaminases weekly until return to less than 3 times ULN or baseline.
-Restart: If the potential benefit outweighs the risk of hepatotoxicity, restart therapy, reduce dose by 40 mg, and monitor liver function weekly for at least 4 weeks
-Reoccurrence: Permanently discontinue therapy.
GREATER than 20 times ULN (Grade 4):
-Any occurrence: Permanently discontinue therapy.
GREATER than 3 times ULN (Grade 2 or higher) with concurrent bilirubin greater than 2 x ULN:
-Any occurrence: Permanently discontinue therapy; Monitor liver function weekly until resolution or return to baseline.
-Exception: Patients with Gilbert's syndrome who develop elevated transaminases should be managed as per the above outlined recommendations for the respective observed elevation of ALT and/or AST.

Dose Adjustments

If dose modifications are required, reduce the dose in 40 mg increments; the lowest recommended daily dose is 80 mg daily.

INTERRUPT DOSING FOR:
-Grade 2 hand-foot skin reaction (HFSR; palmar-plantar erythrodysesthesia syndrome) that is recurrent or does not improve within 7 days despite dose reduction; interrupt dosing for at least 7 days for Grade 3 HFSR.
-Symptomatic Grade 2 hypertension
-Any Grade 3 or 4 adverse reaction
-Worsening infection of any Grade

REDUCE DOSE to 120 mg for:
-First occurrence of Grade 2 HFSR of any duration
-After recovery of any Grade 3 or 4 adverse reaction (except infection)

REDUCE DOSE to 80 mg for:
-Recurrence of Grade 2 HFSR at the 120 mg dose
-After recovery of any Grade 3 or 4 adverse reaction at the 120 mg dose (except hepatotoxicity or infection)

PERMANENTLY DISCONTINUE THERAPY for:
-Failure to tolerate 80 mg dose
-Any Grade 4 adverse reaction; only resume therapy if the potential benefit outweighs the risks

Precautions

US BOXED WARNINGS:
HEPATOTOXICITY:
-Severe, sometimes fatal, hepatotoxicity has been reported.
Recommendations:
-Monitor hepatic function prior to and during therapy.
-Interrupt and then reduce the dose or discontinue this drug for hepatotoxicity as manifested by elevated liver function tests or hepatocellular necrosis, depending upon severity and persistence.

CONTRAINDICATIONS:
-None

Safety and efficacy have not been established in patients younger than 18 years.

Consult WARNINGS section for additional precautions.

Dialysis

Data not available

Other Comments

Administration advice:
-Take this drug at the same time each day.
-Swallow tablet whole with water after a low-fat meal that contains less than 600 calories and less than 30% fat.
-Do not take 2 doses of this drug on the same day to make up for a missed dose from the previous day.

Storage requirements:
-Store at 25C (77F); excursions are permitted from 15C to 30C (59F to 86).
-To protect from moisture, keep tablets in the original bottle and do not remove the desiccant.
-Keep the bottle tightly closed after opening; discard any unused tablets 7 weeks after opening the bottle.

Reconstitution/preparation techniques:
-The manufacturer product information should be consulted.

General:
-Overdose: There is no known antidote; in the event of suspected overdose: immediately interrupt dosing, institute supportive care, and observe until clinical stabilization.

Monitoring:
-Cardiovascular: Blood pressure (weekly for the first 6 weeks of therapy and then every cycle or more frequently, as clinically indicated)
-Hepatic: ALT, AST, bilirubin (at least every 2 weeks during the first 2 months of therapy; thereafter, monitor monthly or more frequently as clinically indicated)
-Metabolism: Biochemical and metabolic parameters (periodically during treatment)

Patient advice:
-Avoid drinking grapefruit juice and taking St. John's Wort during treatment.
-Take this drug after eating a low-fat meal that contains less than 30% fat and less than 600 calories. An example: 1 cup of cereal (about 30 g), 1 glass (about 250 mL) of skim milk, 1 slice of toast with jam, 1 glass of apple juice, and 1 cup of coffee or tea (2 g fat, 520 calories).

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.