Fruquintinib
FRUZAQLA
What it isSelective VEGFR angiokinase inhibitor blocking tumor blood-vessel growth; refractory metastatic colorectal cancer.
Why this oneIts narrow VEGFR focus offers an oral option after chemotherapy and biologic regimens have been exhausted.
What limits itHypertension, hemorrhage, proteinuria, impaired wound healing, and GI perforation require monitoring.
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Metastatic colorectal cancer (previously treated) | Adults | 5 mg QD days 1-21 of each 28-day cycle | Continue until disease progression or unacceptable toxicity | 5 mg QD |
Renal Undefined
Hepatic Mild: no adjustment. Moderate: not sufficiently studied. Severe: not recommended
Dose reductions for toxicity: 4 mg QD, then 3 mg QD; permanently discontinue if 3 mg QD not tolerated
Instructions
- Swallow capsule whole; with or without food, same time each day
- Missed dose: take if <12 h late; never double up; if vomiting after dose, do not re-dose - continue with next scheduled dose
- Withhold >=2 weeks before major surgery; do not give for >=2 weeks after and until adequate wound healing
Cautions
- Hypertension (49%; Grade 3-4 19%) - control BP before starting; monitor weekly first month then monthly
- Hemorrhagic events, may be fatal - monitor at-risk patients and INR on anticoagulants
- Infections incl. fatal - do not start during active infection; withhold for Grade 3-4
- GI perforation/fistula (1.3%) - permanently discontinue
- Hepatotoxicity - monitor LFTs at baseline and periodically
- Proteinuria - monitor urine protein; discontinue for nephrotic syndrome
- Palmar-plantar erythrodysesthesia
- Posterior reversible encephalopathy syndrome (PRES) - discontinue immediately if confirmed
- Impaired wound healing
- Arterial thromboembolic events - discontinue if occur; caution with recent history
- Contains FD&C Yellow No. 5 (tartrazine) and No. 6 - possible allergic reactions incl. bronchial asthma
- Embryo-fetal toxicity - contraception during treatment and 2 weeks after (F and M)
Adverse reactions
- Hypertension, palmar-plantar erythrodysesthesia, proteinuria, dysphonia, abdominal pain, diarrhea, asthenia (>=20%)
Pregnancy Can cause fetal harm (rat teratogenicity/embryolethality below clinical exposure); verify pregnancy status before starting; no human data
Lactation Do not breastfeed during treatment and for 2 weeks after last dose
NO BOXED WARNINGS
Principal riskNo FDA boxed warning.
Cost, est. cash$5,000–$30,000+/month or cycle
Generic entry2035 est.
Classes and tags
Clinical profile
Legacy pregnancy categoryNot assigned — PLLR-era drug
Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.
Mechanism of action: Fruquintinib ballicule
