Absorption: IV administration results in complete bioavailability.
Distribution: Unknown.
Protein Binding: Irinotecan 3068%; SN38 (active metabolite) 95%.
Metabolism/Excretion: Converted by the liver to SN38, its active metabolite, which is metabolized by the liver by UDP-glucuronosyl 111 transferase 1A1 (UGT1A1) and CYP3A4. Small amounts excreted by kidneys.
Half-life: 6 hr.
CV: edema, vasodilation.
Derm: alopecia, rash, sweating.
EENT: rhinitis.
F and E: dehydration.
GI: DIARRHEA, ↑LIVER ENZYMES, abdominal pain/cramping, anorexia, constipation, dyspepsia, flatulence, nausea, stomatitis, vomiting, abdominal enlargement, colonic ulceration.
GU: ↓fertility, menstrual abnormalities.
Hemat: neutropenia, anemia, leukopenia, thrombocytopenia.
Local: injection site reactions.
Metab: weight loss.
MS: INFECTION, back pain.
Neuro: dizziness, headache, insomnia, weakness.
Resp: INTERSTITIAL LUNG DISEASE, coughing, dyspnea.
Misc: chills, fever.

Other regimens are used; careful modification required for all levels of toxicity/tolerance
Single Agent
- IV (Adults): Weekly dosage schedule 125 mg/m2 once weekly for 4 wk, followed by a 2-wk rest period. Cycle may be repeated using doses which depend on patient tolerance and degree of toxicity encountered. Once-every-3-wk schedule 350 mg/m2 once every 3 wk. Cycle may be repeated using doses which depend on patient tolerance and degree of toxicity encountered.
- IV (Geriatric Patients >70 yr): Weekly dosage schedule 125 mg/m2 once weekly for 4 wk, followed by a 2-wk rest period. Cycle may be repeated using doses which depend on patient tolerance and degree of toxicity encountered. Once-every-3-wk schedule 300 mg/m2 once every 3 wk. Cycle may be repeated using doses which depend on patient tolerance and degree of toxicity encountered.
- IV (Adults Patients with Reduced UGT1A1 Activity): Weekly dosage schedule 100 mg/m2 once weekly for 4 wk, followed by a 2-wk rest period. Cycle may be repeated using doses which depend on patient tolerance and degree of toxicity encountered. Once-every-3-wk schedule 300 mg/m2 once every 3 wk. Cycle may be repeated using doses which depend on patient tolerance and degree of toxicity encountered.
Hepatic Impairment
- IV (Adults): Bilirubin 12 mg/dL and history of prior pelvic/abdominal irradiation Weekly dosage schedule Initiate therapy at lower dose (100 mg/m2); once weekly for 4 wk, followed by a 2-wk rest period. Cycle may be repeated with dose adjusted as tolerated. Once-every-3-wk schedule 300 mg/m2 once every 3 wk. Cycle may be repeated with dose adjusted as tolerated.
As Part of Combination Therapy with Leucovorin and 5-Fluorouracil
- IV (Adults): Regimen 1 (Bolus regimen) 125 mg/m2 once weekly for 4 wk, followed by a 2-wk rest period. Cycle may be repeated using doses that depend on patient tolerance and degree of toxicity encountered; Regimen 2 (Infusional regimen) 180 mg/m2 every 2 wk for 3 doses, followed by a 3-wk rest period. Cycle may be repeated using doses that depend on patient tolerance and degree of toxicity encountered.
- IV (Adults Patients with Reduced UGT1A1 Activity): Regimen 1 (Bolus regimen) 100 mg/m2 once weekly for 4 wk, followed by a 2-wk rest period. Cycle may be repeated using doses that depend on patient tolerance and degree of toxicity encountered; Regimen 2 (Infusional regimen) 150 mg/m2 every 2 wk for 3 doses, followed by a 3-wk rest period. Cycle may be repeated using doses that depend on patient tolerance and degree of toxicity encountered.
Therapeutic Classification: antineoplastics
Pharmacologic Classification: enzyme inhibitors