Regorafenib

STIVARGA

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Pronunciation: re-goe-RAF-e-nib (sti-VAR-ga)

Regorafenib ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Regorafenib ballicule

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.

Regorafenib molecular structure (skeletal formula) — Molecular structure: Regorafenib

FDA-approved for

metastatic colorectal cancer (2012)
GIST, hepatocellular carcinoma

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Hepatotoxicity — severe and sometimes fatal; monitor hepatic function before and during treatment; interrupt/reduce/discontinue for hepatotoxicity

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

Available strengths

tab 40 mg

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

Cost

Regorafenib (STIVARGA)

Strength		#/mo	generic $/mo	CostPlus
40 mg	tab	30 qd		not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Regorafenib is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2025

⚠ BOXED WARNING

Hepatotoxicity

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk3 / 4

Legacy pregnancy categoryD

Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.

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