Regorafenib Dosage

Usual Adult Dose for Colorectal Cancer

Initial dose: 160 mg (four 40 mg tablets) orally once daily for the first 21 days of each 28-day cycle.
Duration of therapy: Continue treatment until disease progression or unacceptable toxicity.

Usual Adult Dose for Gastrointestinal Stromal Tumor

Initial dose: 160 mg (four 40 mg tablets) orally once daily for the first 21 days of each 28-day cycle.
Duration of therapy: Continue treatment until disease progression or unacceptable toxicity.

Renal Dose Adjustments

No adjustment recommended for mild renal impairment.
Data not available for moderate and severe renal impairment.

Liver Dose Adjustments

No adjustment recommended for mild and moderate hepatic impairment.
Use is not recommended for severe hepatic impairment (Child-Pugh Class C).

Dose Adjustments

Hold therapy for:
-NCI CTCAE Version 3.0 (v3.0) Grade 2 hand-foot skin reaction (HFSR) [palmar-plantar erythrodysesthesia (PPE)] that is recurrent or does not improve within 7 days despite dose reduction.
-Grade 3 HFSR. Interrupt therapy for a minimum of 7 days.
-Symptomatic Grade 2 hypertension.
-Any NCI CTCAE v3.0 Grade 3 or 4 adverse reaction.

Reduce dose to 120 mg for:
-The first occurrence of Grade 2 HFSR of any duration.
-After recovery of any Grade 3 or 4 adverse reaction.
-Grade 3 aspartate aminotransferase (AST)/alanine aminotransferase (ALT) elevation; only resume if the potential benefit outweighs the risk of hepatotoxicity.

Reduce dose to 80 mg for:
-Reoccurrence 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).

Discontinue permanently for:
-Failure to tolerate 80 mg dose.
-Any occurrence of AST or ALT more than 20 times the upper limit of normal (ULN).
-Any occurrence of AST or ALT more than 3 times ULN with concurrent bilirubin more than 2 times ULN.
-Reoccurrence of AST or ALT more than 5 times ULN despite dose reduction to 120 mg.
-Any Grade 4 adverse reaction; only resume if the potential benefit outweighs the risks.

Precautions

Safety and effectiveness have not been established in pediatric patients (less than 18 years of age).

Dialysis

-Data not available

Other Comments

Administration advice: Swallow the tablets whole with a low-fat breakfast at the same time each day. Do not double dosage on one day to make up for a missed dose.

Storage requirements: Keep medication in original container, do not put in a daily or weekly pill box. The original bottle contains a desiccant to keep the medication dry, do not remove.