Irinotecan
CAMPTOSAR
Pronunciation: ir-in-oe-TEE-kan
What it isTopoisomerase I inhibitor; colorectal and pancreatic cancer.
Why this oneIt has activity in colorectal cancer after fluoropyrimidine failure.
What limits it⚑ Early cholinergic diarrhea responds to atropine; delayed secretory diarrhea needs aggressive loperamide. UGT1A1*28 raises toxicity.
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Metastatic colorectal carcinoma — first line with 5-FU/LV (Regimen 1, bolus) | Adult | 125 mg/m² IV over 90 min days 1, 8, 15, 22 q6wk (+ LV 20 mg/m² and 5-FU 500 mg/m² bolus) | 125 mg/m²; reduce to 100 → 75 mg/m² for toxicity | 125 mg/m² per dose |
| Metastatic colorectal carcinoma — first line with 5-FU/LV (Regimen 2, infusional) | Adult | 180 mg/m² IV over 90 min days 1, 15, 29 q6wk (+ LV 200 mg/m², 5-FU 400 mg/m² bolus + 600 mg/m² over 22 h, days 1, 2, 15, 16, 29, 30) | 180 mg/m²; reduce to 150 → 120 mg/m² for toxicity | 180 mg/m² per dose |
| Metastatic colorectal carcinoma — recurred/progressed after 5-FU (single agent, weekly) | Adult | 125 mg/m² IV over 90 min days 1, 8, 15, 22, then 2-wk rest | 50–150 mg/m² (adjust in 25–50 mg/m² steps by tolerance) | 150 mg/m² weekly |
| Metastatic colorectal carcinoma — recurred/progressed after 5-FU (single agent, q3wk) | Adult (start 300 mg/m² if age ≥70) | 350 mg/m² IV over 90 min q3wk | 350 mg/m²; may reduce to 200 mg/m² in 50 mg/m² steps | 350 mg/m² q3wk |
Titration Next cycle, weekly single-agent only: ↑25 mg/m² if no toxicity (max 150 mg/m²)
Renal Not studied — use caution; not recommended on dialysis
Hepatic Caution; consider ↓ starting dose 1 level for ↑ bilirubin; no dosing recommendation for bilirubin >2 mg/dL
Consider ↓ starting dose ≥1 level for UGT1A1 *28/*28, *6/*6, *6/*28, prior pelvic/abdominal RT, PS 2, or ↑ bilirubin. Start next cycle only when granulocytes ≥1500/mm³, platelets ≥100,000/mm³ and diarrhea resolved; dose levels per Tables 2/4.
Instructions
- Dilute in D5W (preferred) or NS to 0.12–2.8 mg/mL; no other drugs in the bag
- Infuse IV over 90 min
- Use immediately or store diluted ≤24 h at 2–8 °C
- Premedicate with antiemetics ≥30 min before (e.g., dexamethasone 10 mg + 5-HT3 antagonist); atropine for cholinergic symptoms
- Avoid extravasation (if it occurs: flush with sterile water, apply ice)
- Hazardous drug — gloves; special handling/disposal
Available strengths
- inj 4.3, 20 mg/mL
Cautions
- Diarrhea and cholinergic reactions
- Myelosuppression
- Increased neutropenia risk with reduced UGT1A1 activity (*28, *6)
- Hypersensitivity incl. anaphylaxis
- Renal impairment/acute renal failure (volume depletion)
- Pulmonary toxicity (interstitial pulmonary disease)
- Toxicity of 5-day 5-FU/LV regimen — avoid combination
- Increased toxicity with performance status 2
- Embryo-fetal toxicity
- Hepatic impairment
Adverse reactions
- Diarrhea (≥30%)
- Nausea (≥30%)
- Vomiting (≥30%)
- Abdominal pain (≥30%)
- Neutropenia (≥30%)
- Leukopenia (≥30%)
- Anemia (≥30%)
- Asthenia (≥30%)
- Alopecia (≥30%)
- Anorexia (≥30%)
- Constipation (≥30%)
- Fever (≥30%)
Pregnancy Can cause fetal harm (embryofetal mortality/teratogenicity in animals below clinical exposure); females contraception 6 mo, males condoms 3 mo after last dose.
Lactation Present in human milk; do not breastfeed during treatment and for 7 days after the final dose.
Cost
| Strength | #/mo | generic $/unit | CostPlus | |
|---|---|---|---|---|
| 4.3 mg/mL | inj | per unit | not offered | |
| 20 mg/mL | inj | per unit | not offered |
⚠ BOXED WARNINGS
- Severe diarrhea
- Severe myelosuppression
Classes and tags
Clinical profile
Defining liabilityDelayed diarrhea and neutropenia