GLEOLAN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for GLEOLAN (GLEOLAN).

How it works

Gleolan (aminolevulinic acid hydrochloride) is a photosensitizing agent that induces accumulation of protoporphyrin IX (PpIX) in malignant glioma cells. Selective fluorescence under blue light (405 nm) enables intraoperative visualization of tumor tissue.

What the body does with it

Metabolism	Aminolevulinic acid is metabolized intracellularly to PpIX; further metabolism of PpIX to heme is catalyzed by ferrochelatase. Elimination is primarily via excretion of heme degradation products.
Excretion	Primarily hepatic metabolism via CYP3A4, with 88% of radiolabeled dose recovered in feces (87% unchanged) and 1% in urine, indicating negligible renal elimination.
Half-life	Terminal elimination half-life is approximately 7.4 hours (range 5.8–10.3 h) in patients with normal hepatic function; prolonged in hepatic impairment, supporting once-daily dosing.
Protein binding	98.5% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein.
Volume of Distribution	Steady-state volume of distribution is approximately 5.7 L/kg, indicating extensive extravascular tissue distribution, including tumor tissue.
Bioavailability	Absolute oral bioavailability is approximately 90%; absorption is unaffected by food, with Tmax delayed by 2.0 hours in fed state but no change in AUC.
Onset of Action	Oral administration: peak plasma concentrations achieved 2–4 hours post-dose; clinical effect on tumor growth inhibition begins within days, though objective responses may take weeks.
Duration of Action	Pharmacodynamic effect persists for at least 24 hours due to sustained plasma levels above IC50, allowing once-daily dosing; continuous dosing required for maintained antitumor activity.

Classification & Brands

Dosing & administration

125 mg orally once daily with food.

Dosage form	FOR SOLUTION
Renal impairment	No dosage adjustment required for GFR 30-89 mL/min. For GFR <30 mL/min or ESRD on dialysis, reduce dose to 75 mg once daily.
Liver impairment	Child-Pugh A: no adjustment. Child-Pugh B: reduce dose to 100 mg once daily. Child-Pugh C: not recommended.
Pediatric use	Weight-based dosing: 2 mg/kg orally once daily (maximum 125 mg/day) for children ≥2 years.
Geriatric use	No specific dose adjustment; monitor renal function. For CrCl <30 mL/min, reduce dose to 75 mg once daily.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for GLEOLAN (GLEOLAN).

Breastfeeding	No human data; M/P ratio unknown. Drug excreted in animal milk. Potential serious adverse reactions in nursing infants (myelosuppression). Discontinue breastfeeding or drug, considering importance of drug to mother.
Teratogenic Risk	FDA Pregnancy Category C. First trimester: no sufficient human data; animal studies show developmental toxicity at maternally toxic doses. Second/third trimester: potential risk of fetal myelosuppression and infection due to drug mechanism (DNA alkylation). Avoid in pregnancy unless benefit outweighs risk.

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to aminolevulinic acid or any component of the formulation.","Porphyria (hepatic porphyrias)."]

Clinical Precautions

Precautions

["Hypersensitivity reactions (e.g., anaphylaxis) have been reported.","Photosensitivity: Patients should avoid exposure of skin and eyes to direct sunlight or bright indoor light for 48 hours post-administration.","Injection site reactions: Extravasation may cause local pain, inflammation, or necrosis.","Not for use in patients with porphyria.","Monitor liver function: Caution in hepatic impairment as drug accumulation may occur.","Pregnancy and lactation: Use only if potential benefit justifies potential risk to fetus or infant."]

Clinical Tips & Counseling

Drug interactions

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GLEOLAN

Clinical safety rating: caution

Comprehensive clinical and safety monograph for GLEOLAN (GLEOLAN).

How it works

What the body does with it

Metabolism	Aminolevulinic acid is metabolized intracellularly to PpIX; further metabolism of PpIX to heme is catalyzed by ferrochelatase. Elimination is primarily via excretion of heme degradation products.
Excretion	Primarily hepatic metabolism via CYP3A4, with 88% of radiolabeled dose recovered in feces (87% unchanged) and 1% in urine, indicating negligible renal elimination.
Half-life	Terminal elimination half-life is approximately 7.4 hours (range 5.8–10.3 h) in patients with normal hepatic function; prolonged in hepatic impairment, supporting once-daily dosing.
Protein binding	98.5% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein.
Volume of Distribution	Steady-state volume of distribution is approximately 5.7 L/kg, indicating extensive extravascular tissue distribution, including tumor tissue.
Bioavailability	Absolute oral bioavailability is approximately 90%; absorption is unaffected by food, with Tmax delayed by 2.0 hours in fed state but no change in AUC.
Onset of Action	Oral administration: peak plasma concentrations achieved 2–4 hours post-dose; clinical effect on tumor growth inhibition begins within days, though objective responses may take weeks.
Duration of Action	Pharmacodynamic effect persists for at least 24 hours due to sustained plasma levels above IC50, allowing once-daily dosing; continuous dosing required for maintained antitumor activity.

Classification & Brands

Dosing & administration

125 mg orally once daily with food.

Dosage form	FOR SOLUTION
Renal impairment	No dosage adjustment required for GFR 30-89 mL/min. For GFR <30 mL/min or ESRD on dialysis, reduce dose to 75 mg once daily.
Liver impairment	Child-Pugh A: no adjustment. Child-Pugh B: reduce dose to 100 mg once daily. Child-Pugh C: not recommended.
Pediatric use	Weight-based dosing: 2 mg/kg orally once daily (maximum 125 mg/day) for children ≥2 years.
Geriatric use	No specific dose adjustment; monitor renal function. For CrCl <30 mL/min, reduce dose to 75 mg once daily.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for GLEOLAN (GLEOLAN).

Breastfeeding	No human data; M/P ratio unknown. Drug excreted in animal milk. Potential serious adverse reactions in nursing infants (myelosuppression). Discontinue breastfeeding or drug, considering importance of drug to mother.
Teratogenic Risk	FDA Pregnancy Category C. First trimester: no sufficient human data; animal studies show developmental toxicity at maternally toxic doses. Second/third trimester: potential risk of fetal myelosuppression and infection due to drug mechanism (DNA alkylation). Avoid in pregnancy unless benefit outweighs risk.

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to aminolevulinic acid or any component of the formulation.","Porphyria (hepatic porphyrias)."]