TRUSELTIQ

Clinical safety rating: caution

Comprehensive clinical and safety monograph for TRUSELTIQ (TRUSELTIQ).

How it works

TRUSELTIQ (infigratinib) is a fibroblast growth factor receptor (FGFR) inhibitor that binds to and inhibits FGFR1, FGFR2, and FGFR3, thereby blocking FGFR-mediated signal transduction pathways, including STAT, MAPK, and PI3K/AKT, leading to reduced tumor cell proliferation and angiogenesis.

What the body does with it

Metabolism	Primarily metabolized by CYP3A4.
Excretion	Primarily hepatic metabolism, with <1% excreted unchanged in urine. Fecal excretion accounts for approximately 86% of the administered dose, while renal excretion accounts for about 12%.
Half-life	Terminal elimination half-life is approximately 11 hours (range 6.1–19.8 hours), supporting twice-daily dosing.
Protein binding	High protein binding: 99.8%, primarily to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	Apparent volume of distribution (Vd/F) is approximately 33.8 L (0.45 L/kg for a 75 kg individual), indicating moderate distribution into tissues.
Bioavailability	Absolute oral bioavailability is approximately 76% (fasted state). Food increases absorption; taking with a high-fat meal increases Cmax and AUC by approximately 2-fold and 1.6-fold, respectively.
Onset of Action	Time to reach steady-state is approximately 3 days with twice-daily dosing. Clinical effect (e.g., tumor response) typically observed within weeks of initiation.
Duration of Action	Duration of action is related to pharmacokinetic profile; clinical effect persists as long as therapeutic concentrations are maintained. Steady-state is achieved within 3 days, and drug effect wanes upon discontinuation.

Classification & Brands

Dosing & administration

600 mg orally twice daily with food.

Dosage form	CAPSULE
Renal impairment	No dose adjustment required for mild to moderate renal impairment (GFR ≥30 mL/min). Not studied in severe renal impairment (GFR <30 mL/min) or ESRD.
Liver impairment	Child-Pugh A: No adjustment. Child-Pugh B: Reduce starting dose to 300 mg orally twice daily. Child-Pugh C: Not recommended.
Pediatric use	Safety and efficacy not established in pediatric patients.
Geriatric use	No specific dose adjustment recommended; pharmacokinetics similar to younger adults.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for TRUSELTIQ (TRUSELTIQ).

Breastfeeding	No human data available. Based on molecular weight (low) and structural properties, excretion into breast milk is possible. M/P ratio unknown. Breastfeeding is contraindicated during treatment and for at least 2 weeks after the last dose due to potential adverse effects in the infant.
Teratogenic Risk	FDA Pregnancy Category D. First trimester: high risk of major congenital malformations including craniofacial abnormalities, cardiac defects, and neural tube defects based on animal studies. Second and third trimesters: risk of fetal growth restriction, oligohydramnios, and potential fetal demise due to FGFR inhibition affecting placental development.

Warnings & precautions

■ FDA Black Box Warning

None.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Concomitant use with strong CYP3A4 inducers or inhibitors.","History of hypersensitivity to infigratinib or any of its excipients."]

Clinical Precautions

Precautions

["Ocular toxicity including central serous retinopathy and retinal pigment epithelial detachment; perform ophthalmic examinations prior to treatment, monthly for 6 months, and every 3 months thereafter.","Hyperphosphatemia due to FGFR inhibition; monitor serum phosphate levels and manage with phosphate-lowering therapy or dose modifications.","Embryo-fetal toxicity; can cause fetal harm, advise females of reproductive potential to use effective contraception during treatment and for 1 month after the last dose."]

Clinical Tips & Counseling

Drug interactions

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TRUSELTIQ

Clinical safety rating: caution

Comprehensive clinical and safety monograph for TRUSELTIQ (TRUSELTIQ).

How it works

What the body does with it

Metabolism	Primarily metabolized by CYP3A4.
Excretion	Primarily hepatic metabolism, with <1% excreted unchanged in urine. Fecal excretion accounts for approximately 86% of the administered dose, while renal excretion accounts for about 12%.
Half-life	Terminal elimination half-life is approximately 11 hours (range 6.1–19.8 hours), supporting twice-daily dosing.
Protein binding	High protein binding: 99.8%, primarily to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	Apparent volume of distribution (Vd/F) is approximately 33.8 L (0.45 L/kg for a 75 kg individual), indicating moderate distribution into tissues.
Bioavailability	Absolute oral bioavailability is approximately 76% (fasted state). Food increases absorption; taking with a high-fat meal increases Cmax and AUC by approximately 2-fold and 1.6-fold, respectively.
Onset of Action	Time to reach steady-state is approximately 3 days with twice-daily dosing. Clinical effect (e.g., tumor response) typically observed within weeks of initiation.
Duration of Action	Duration of action is related to pharmacokinetic profile; clinical effect persists as long as therapeutic concentrations are maintained. Steady-state is achieved within 3 days, and drug effect wanes upon discontinuation.

Classification & Brands

Dosing & administration

600 mg orally twice daily with food.

Dosage form	CAPSULE
Renal impairment	No dose adjustment required for mild to moderate renal impairment (GFR ≥30 mL/min). Not studied in severe renal impairment (GFR <30 mL/min) or ESRD.
Liver impairment	Child-Pugh A: No adjustment. Child-Pugh B: Reduce starting dose to 300 mg orally twice daily. Child-Pugh C: Not recommended.
Pediatric use	Safety and efficacy not established in pediatric patients.
Geriatric use	No specific dose adjustment recommended; pharmacokinetics similar to younger adults.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for TRUSELTIQ (TRUSELTIQ).

Breastfeeding	No human data available. Based on molecular weight (low) and structural properties, excretion into breast milk is possible. M/P ratio unknown. Breastfeeding is contraindicated during treatment and for at least 2 weeks after the last dose due to potential adverse effects in the infant.
Teratogenic Risk	FDA Pregnancy Category D. First trimester: high risk of major congenital malformations including craniofacial abnormalities, cardiac defects, and neural tube defects based on animal studies. Second and third trimesters: risk of fetal growth restriction, oligohydramnios, and potential fetal demise due to FGFR inhibition affecting placental development.

Warnings & precautions

■ FDA Black Box Warning

None.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Concomitant use with strong CYP3A4 inducers or inhibitors.","History of hypersensitivity to infigratinib or any of its excipients."]