FRUZAQLA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for FRUZAQLA (FRUZAQLA).
Fruzaqla (fruquintinib) is a selective oral inhibitor of vascular endothelial growth factor receptors (VEGFR-1, -2, -3), blocking VEGF-mediated signaling and thereby inhibiting tumor angiogenesis and tumor growth.
| Metabolism | Primarily metabolized by CYP3A4 and to a lesser extent by CYP3A5; also undergoes hydrolysis and glucuronidation. |
| Excretion | Primarily hepatic metabolism (CYP3A4) followed by fecal excretion (77% of dose as metabolites, 20% as unchanged drug) and renal excretion (<1% unchanged). |
| Half-life | Terminal elimination half-life is approximately 20–30 hours, supporting once-daily dosing. |
| Protein binding | 99.7% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Apparent Vd/F is approximately 1.3 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Absolute bioavailability not determined; relative bioavailability ~30–40% (capsule formulation). |
| Onset of Action | Clinical effect (plasma exposure) observed within 2–4 hours after oral administration; steady-state reached by day 15. |
| Duration of Action | 24-hour dosing interval; sustained VEGF receptor inhibition throughout the dosing period. |
Adult: 5 mg orally once daily, with or without food, until disease progression or unacceptable toxicity.
| Dosage form | CAPSULE |
| Renal impairment | For GFR 30-89 mL/min: no adjustment. For GFR <30 mL/min: not recommended (no data). |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: reduce to 3 mg once daily. Child-Pugh C: not recommended (no data). |
| Pediatric use | Safety and efficacy not established in pediatric patients. |
| Geriatric use | No specific dose adjustment required, but monitor for adverse events due to potential age-related renal or hepatic impairment. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for FRUZAQLA (FRUZAQLA).
| Breastfeeding | No data on presence in human milk or effects on breastfed infant. Due to potential for serious adverse reactions, advise women not to breastfeed during treatment and for at least 2 weeks after last dose. |
| Teratogenic Risk | FRUZAQLA (fruquintinib) is an antiangiogenic agent. Based on its mechanism of action, there is a risk of teratogenicity. Animal studies suggest adverse effects on fetal development, including increased resorptions and malformations. In humans, use is contraindicated during pregnancy. First trimester exposure carries highest risk of major malformations and spontaneous abortion. Second and third trimester exposure may cause fetal growth restriction, oligohydramnios, and potential fetal renal impairment. |
■ FDA Black Box Warning
No boxed warning.
| Serious Effects |
["None known."]
| Precautions | ["Hemorrhage: Severe, sometimes fatal hemorrhagic events including gastrointestinal, pulmonary, and intracranial hemorrhage.","Hypertension: Monitor blood pressure; manage with antihypertensives; withhold or permanently discontinue for severe hypertension.","Arterial thromboembolic events: Discontinue if such events occur.","Proteinuria: Monitor urine protein; discontinue for nephrotic syndrome.","Hepatotoxicity: Monitor liver function; discontinue for severe hepatotoxicity.","Posterior reversible encephalopathy syndrome (PRES): Discontinue if PRES is confirmed.","Wound healing complications: Withhold for at least 2 weeks before elective surgery; do not resume for at least 2 weeks after major surgery and until adequate wound healing.","Fistula formation: Discontinue if gastrointestinal fistula occurs.","Thyroid dysfunction: Monitor thyroid function.","Embryo-fetal toxicity: Can cause fetal harm; advise females of reproductive potential of potential risk and to use effective contraception."] |
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| Fetal Monitoring | Monitor blood pressure every 2 weeks initially, then monthly; assess for proteinuria via urinalysis; monitor for signs of hemorrhage; perform liver function tests regularly; monitor thyroid function; assess fetal growth and amniotic fluid volume by ultrasound if pregnancy occurs. |
| Fertility Effects | May impair fertility in females based on animal studies showing effects on ovarian function. In males, testicular degeneration observed in animals. Reversibility unknown. |