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Fruzaqla
fruquintinib
Adult Dosing .
Dosage forms: CAP: 1 mg, 5 mg
Special Note
- [uses, dosing may vary]
- Info: refer to institution protocols and pkg insert prior to prescribing for uses and dosing including toxicity-related dose adjustments; D/C >2wk before major surgery, restart >2wk after major surgery when wound fully healed
colorectal CA, metastatic
- [5 mg PO qd on days 1-21 of 28-day cycle]
- Info: for patients with disease progression after fluoropyrimidine-, oxaliplatin- and irinotecan-containing chemo, anti-VEGF tx, and anti-EGFR tx if RAS wild-type; do not open cap
renal dosing
- [see below]
- CrCl >30: no adjustment; CrCl <30: not defined
hepatic dosing
- [see below]
- bilirubin 1.1-1.5x ULN: no adjustment; bilirubin 1.6-3x ULN: not defined; bilirubin >3x ULN: avoid use
Peds Dosing .
Peds dosing is currently unavailable or not applicable for this drug.
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- bilirubin >3x ULN
- HTN, uncontrolled
- GI perforation
- GI fistula
- surgical wound, unhealed
- major surgery within prior 2wk
- avoid: tx for at least 2wk before major surgery
- avoid: breastfeeding during tx and x2wk after D/C
- caution: hypersensitivity to tartrazine
- caution: patients of childbearing potential
- caution: male patients of reproductive potential
- caution: thromboembolism history, recent
Drug Interactions .
Overview
fruquintinib
kinase inhibitor
- CYP3A4 substrate
- antiplatelet/anticoagulant effects
- GI mucosal injury/bleeding risk
- hypertensive effects
- immunomodulatory effects
- thrombogenic effects
Contraindicated
Avoid/Use Alternative
Monitor/Modify Tx
Caution Advised
Adverse Reactions .
Serious Reactions
- HTN
- hypertensive crisis
- hemorrhage, severe
- infection
- GI perforation
- hepatotoxicity
- proteinuria
- hand-foot syndrome
- posterior reversible encephalopathy syndrome
- impaired wound healing
- arterial thromboembolism
- hypothyroidism
- pneumonia
Common Reactions
- HTN
- fatigue
- proteinuria
- stomatitis
- hand-foot syndrome
- abdominal pain
- dysphonia
- diarrhea
- hypothyroidism
- musculoskeletal pain
- arthralgia
- hemorrhage
- anorexia
- UTI
- pharyngitis
- rectal pain
- rash
- pneumonia
- epistaxis
- ALT or AST incr.
- sodium decr.
- bilirubin incr.
- Cr incr.
- triglycerides incr.
- Plt decr.
- alk phos incr.
- cholesterol incr.
- albumin decr.
Safety/Monitoring .
Monitoring Parameters
pregnancy test at baseline; BP at baseline, then qwk x1mo, then at least qmo during tx or as clinically indicated; LFTs, urine protein at baseline, then periodically
Pregnancy/Lactation .
Pregnancy
Clinical Summary
weigh risk/benefit during pregnancy; no human data available; risk of fetal harm, including teratogenicity and embryo-fetal death, based on animal data at 0.2-0.5x recommended human dose and drug's mechanism of action
Individuals of Reproductive Potential
obtain pregnancy test before tx start; avoid pregnancy by using effective contraception during tx and x2wk after D/C in patients of childbearing potential and male patients
Lactation
Clinical Summary
avoid breastfeeding during tx and x2wk after D/C; no human data available to assess risk of infant harm or effects on milk production
Pharmacology .
Metabolism: for fruquintinib: unknown; CYP450: 2C8, 2C9, 2C19, 3A (primary) substrate
Excretion: for fruquintinib: urine 60% (0.5% unchanged), feces 30% (5% unchanged); Half-life: 42h
Subclass: Kinase Inhibitors, VEGF Inhibitors ; VEGF Antagonists
Mechanism of Action
for fruquintinib: binds and inhibits vascular endothelial growth factor receptors 1, 2, and 3 (VEGFR-1, VEGFR-2, and VEGFR-3), resulting in decr. angiogenesis, tumor growth, and cancer progression
Formulary .
No Formulary Selected
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