Regorafenib
STIVARGA
What it isOral RET/VEGFR multikinase inhibitor; refractory colorectal cancer, GIST, and hepatocellular carcinoma.
Why this oneIts clinical niche spans three otherwise distinct gastrointestinal cancers after standard options fail.
What limits itHand-foot skin reaction is often dose-limiting; hepatotoxicity, hypertension, and bleeding require monitoring.
FDA-approved for
- metastatic colorectal cancer (2012)
- GIST, hepatocellular carcinoma
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Metastatic colorectal cancer, GIST, hepatocellular carcinoma | Adults | 160 mg QD, days 1-21 of each 28-day cycle | 160 mg QD (days 1-21) | 160 mg/day |
Renal No adjustment needed
Hepatic No adjustment for mild-moderate impairment; not recommended in severe (bilirubin >3x ULN)
21 days on, 7 days off (28-day cycle)
Instructions
- Take after a low-fat meal (<600 cal, <30% fat)
- Swallow tablets whole with water at the same time each day
- Do not take two doses on the same day for a missed dose
- Reduce dose in 40 mg increments; lowest dose 80 mg/day
- Withhold >=2 wks before elective surgery
Cautions
- Hepatotoxicity — monitor LFTs
- Infections
- Hemorrhage (discontinue if severe)
- GI perforation/fistula (discontinue)
- Dermatologic toxicity / hand-foot skin reaction
- Hypertension
- Cardiac ischemia/infarction
- Reversible posterior leukoencephalopathy syndrome (RPLS)
- Impaired wound healing
- Embryo-fetal toxicity
Adverse reactions
- Pain
- Hand-foot skin reaction
- Asthenia/fatigue
- Diarrhea
- Decreased appetite
- Hypertension
- Infection
- Dysphonia
- Hyperbilirubinemia
- Fever
- Mucositis
- Weight loss
- Rash
- Nausea
Pregnancy Can cause fetal harm — embryolethal and teratogenic in animals below human exposures
Lactation Do not breastfeed during treatment and for 2 wks after final dose
⚠ BOXED WARNING
- Hepatotoxicity
Cost, est. cash$5,000–$30,000+/month or cycle
Generic entry2025
Classes and tags
Clinical profile
Legacy pregnancy categoryD
Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.
Mechanism of action: Regorafenib ballicule
