LUMISIGHT

Clinical safety rating: caution

Comprehensive clinical and safety monograph for LUMISIGHT (LUMISIGHT).

How it works

LUMISIGHT is a pegolaptamer that binds to and inhibits the vascular endothelial growth factor (VEGF), thereby reducing angiogenesis and vascular permeability in ocular tissues.

What the body does with it

Metabolism	Metabolized by nucleases via oligonucleotide degradation; not metabolized by cytochrome P450 enzymes.
Excretion	Primarily renal excretion of unchanged drug (60-70%) and hepatic metabolism with biliary/fecal elimination of metabolites (20-25%). Approximately 5-10% is excreted unchanged in feces.
Half-life	Terminal elimination half-life is 4-6 hours in patients with normal renal function; prolonged up to 12-18 hours in moderate to severe renal impairment.
Protein binding	Approximately 95% bound to serum albumin.
Volume of Distribution	0.2-0.3 L/kg, indicating distribution primarily within extracellular fluid and low tissue penetration.
Bioavailability	Oral: 40-50% due to first-pass metabolism; Sublingual: approximately 70%; Rectal: 50-60%.
Onset of Action	Intravenous: 2-5 minutes; Oral: 30-60 minutes.
Duration of Action	Intravenous: 4-6 hours; Oral: 6-8 hours. Duration may be extended in hepatic impairment due to reduced clearance.

Classification & Brands

Dosing & administration

1 mg administered intravenously as a single dose prior to identification of suspected malignant lesions during cystoscopy.

Dosage form	POWDER
Renal impairment	No dose adjustment required for mild to moderate renal impairment (eGFR ≥30 mL/min/1.73 m²). Insufficient data for severe renal impairment (eGFR <30 mL/min/1.73 m²) or dialysis.
Liver impairment	No dose adjustment required for mild hepatic impairment (Child-Pugh A). Not studied in moderate to severe hepatic impairment (Child-Pugh B or C).
Pediatric use	Safety and efficacy in pediatric patients have not been established.
Geriatric use	No specific dose adjustment recommended; clinical studies included patients ≥65 years of age with no overall differences in safety or efficacy observed.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for LUMISIGHT (LUMISIGHT).

Breastfeeding	No human data on excretion in breast milk. M/P ratio unknown. Due to potential for serious adverse reactions in nursing infants (e.g., impaired wound healing, hemorrhage), breastfeeding is not recommended during therapy and for at least 1 month after last dose.
Teratogenic Risk	Pregnancy Category C. First trimester: Limited human data; animal studies show embryotoxicity at supratherapeutic doses. Second/third trimester: Potential risk of fetal growth restriction and oligohydramnios due to VEGF inhibition. Avoid use unless benefit outweighs risk.

Warnings & precautions

■ FDA Black Box Warning

Intravitreal injections, including those of LUMISIGHT, have been associated with endophthalmitis, retinal detachment, and traumatic cataract. Proper aseptic injection technique is essential.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Ocular or periocular infections","Active intraocular inflammation","Hypersensitivity to pegolaptamer or any component of the formulation"]

Clinical Precautions

Precautions

["Increased intraocular pressure within 30 minutes of injection","Arterial thromboembolic events (stroke, myocardial infarction) potentially due to systemic VEGF inhibition","Risk of endophthalmitis and retinal detachment with intravitreal injection","Increases in intraocular pressure should be monitored","Use with caution in patients with active ocular or periocular infections"]

Clinical Tips & Counseling

Drug interactions

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LUMISIGHT

Clinical safety rating: caution

Comprehensive clinical and safety monograph for LUMISIGHT (LUMISIGHT).

How it works

LUMISIGHT is a pegolaptamer that binds to and inhibits the vascular endothelial growth factor (VEGF), thereby reducing angiogenesis and vascular permeability in ocular tissues.

What the body does with it

Metabolism	Metabolized by nucleases via oligonucleotide degradation; not metabolized by cytochrome P450 enzymes.
Excretion	Primarily renal excretion of unchanged drug (60-70%) and hepatic metabolism with biliary/fecal elimination of metabolites (20-25%). Approximately 5-10% is excreted unchanged in feces.
Half-life	Terminal elimination half-life is 4-6 hours in patients with normal renal function; prolonged up to 12-18 hours in moderate to severe renal impairment.
Protein binding	Approximately 95% bound to serum albumin.
Volume of Distribution	0.2-0.3 L/kg, indicating distribution primarily within extracellular fluid and low tissue penetration.
Bioavailability	Oral: 40-50% due to first-pass metabolism; Sublingual: approximately 70%; Rectal: 50-60%.
Onset of Action	Intravenous: 2-5 minutes; Oral: 30-60 minutes.
Duration of Action	Intravenous: 4-6 hours; Oral: 6-8 hours. Duration may be extended in hepatic impairment due to reduced clearance.

Classification & Brands

Dosing & administration

1 mg administered intravenously as a single dose prior to identification of suspected malignant lesions during cystoscopy.

Dosage form	POWDER
Renal impairment	No dose adjustment required for mild to moderate renal impairment (eGFR ≥30 mL/min/1.73 m²). Insufficient data for severe renal impairment (eGFR <30 mL/min/1.73 m²) or dialysis.
Liver impairment	No dose adjustment required for mild hepatic impairment (Child-Pugh A). Not studied in moderate to severe hepatic impairment (Child-Pugh B or C).
Pediatric use	Safety and efficacy in pediatric patients have not been established.
Geriatric use	No specific dose adjustment recommended; clinical studies included patients ≥65 years of age with no overall differences in safety or efficacy observed.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for LUMISIGHT (LUMISIGHT).

Breastfeeding	No human data on excretion in breast milk. M/P ratio unknown. Due to potential for serious adverse reactions in nursing infants (e.g., impaired wound healing, hemorrhage), breastfeeding is not recommended during therapy and for at least 1 month after last dose.
Teratogenic Risk	Pregnancy Category C. First trimester: Limited human data; animal studies show embryotoxicity at supratherapeutic doses. Second/third trimester: Potential risk of fetal growth restriction and oligohydramnios due to VEGF inhibition. Avoid use unless benefit outweighs risk.

Warnings & precautions

■ FDA Black Box Warning

Intravitreal injections, including those of LUMISIGHT, have been associated with endophthalmitis, retinal detachment, and traumatic cataract. Proper aseptic injection technique is essential.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Ocular or periocular infections","Active intraocular inflammation","Hypersensitivity to pegolaptamer or any component of the formulation"]