Irinotel

Irinotecan HCl trihydrate

Monotherapy or in combination therapy for metastatic carcinoma of colon or rectum that has recurred or progressed following 5-fluorouracil (5-FU) therapy; previously untreated metastatic carcinoma of colon or rectum; NSCLC or small cell lung cancer; cervical, ovarian & esophageal cancer; malignant glioma; inoperable or recurrent gastric cancer. In combination w/ cetuximab for epidermal growth factor receptor (EGFR)-expressing metastatic CRC after failure of irinotecan-including cytotoxic therapy. In combination w/ 5-FU, folinic acid & bevacizumab as 1st-line treatment for patients w/ metastatic carcinoma of colon or rectum.

IV infusion Over 30-90 min for all doses. Premed: Antiemetic agents at least 30 min prior to administration of irinotecan. Monotherapy Wkly dosage regimen: 125 mg/m². Patients w/ prior extensive RT, performance status of 2, increased bilirubin levels, or gastric cancer Initially 100 mg/m² in repeated 6-wk cycle comprising wkly treatment for 4 wk, followed by 2-wk rest. Once-every-2-wk dosage regimen 250 mg/m² every 2 wk. Patients w/ age ≥65 yr, prior extensive RT, performance status of 2, increased bilirubin levels, or gastric cancer Initially 200 mg/m². Once-every-3-wk dosage regimen 350 mg/m². Patients w/ age ≥65 yr, prior extensive RT, performance status of 2, increased bilirubin levels, or gastric cancer Initially 300 mg/m². In combination w/ 5-FU & leucovorin for metastatic CRC Irinotecan 125 mg/m², 5-FU 500 mg/m², & leucovorin 20 mg/m². Patients w/ age ≥65 yr, prior extensive RT, performance status of 2, increased bilirubin levels, or gastric cancer Initially, irinotecan 100 mg/m² & 5-FU 400 mg/m² in repeated 6-wk cycle comprising wkly treatment for 4 wk, followed by 2-wk rest. In combination w/ bevacizumab Irinotecan 125 mg/m²/bolus, 5-FU 500 mg/m², folinic acid 20 mg/m² once wkly for 4 wk every 6 wk. In combination w/ cisplatin for NSCLC, small cell lung, cervical, gastric & esophageal cancer Irinotecan 65 mg/m² & cisplatin 30 mg/m². Patients w/ age ≥65 yr, prior extensive RT, performance status of 2, increased bilirubin levels, or gastric cancer 50 mg/m² in repeated 6-wk cycle comprising wkly treatment for 4 wk, followed by 2-wk rest.

Hypersensitivity to irinotecan, topotecan or other camptothecin analogues. Patients w/ chronic inflammatory bowel disease &/or bowel obstruction; bilirubin >3x ULN range; severe bone marrow failure; WHO performance status >2. Pregnancy & lactation.

Temporarily discontinue if neutropenic fever occurs or if ANC drops <500/mm³. Interrupt treatment if severe diarrhea occurs. Not to be administered until neutrophil count returns to >1,500 cells/mm³; in patients w/ bilirubin >3x ULN. Delay treatment in patients who experienced severe neutropenia or GI adverse events eg, diarrhea, nausea & vomiting. May induce both early (<24 hr onset after dosing) & late forms (≥24 hr onset after dosing) of diarrhea. Severe myelosuppression; history of bleeding disorders; lymphocytopenia; hyperglycemia in patients w/ history of DM or glucose intolerance; akathisia. Monitor infusion site for signs of inflammation in case of extravasation. Reduce dose if total WBC count <2,000/mm³, neutrophil count <1,000/mm³, Hb 8 g/dL & platelet count <100,000/mm³. Treat late diarrhea w/ loperamide. Give fluid & electrolyte replacement in patients w/ severe diarrhea. Previous cytotoxic or radiation (abdominal or pelvic) therapy. Live vaccines. Hepatic impairment (serum bilirubin >2 mg/dL, transaminase >3x ULN if no liver metastases or >5x ULN if w/ liver metastases). Not recommended in renal impairment. Women of childbearing potential should avoid becoming pregnant while receiving treatment. Pregnancy. Discontinue lactation. Ped. Elderly >65 yr.

Neutropenia, thrombocytopenia & anemia, eosinophilia; diarrhea; flushing; insomnia & dizziness; renal failure; elevated serum transaminases, bilirubin & liver enzymes; pneumonitis; alopecia, skin rashes & pain, symptoms resembling cholinergic syndrome, asthenia, fever & abdominal pain.

Exacerbated myelosuppresion & diarrhea w/ other antineoplastic agents having similar adverse effects. Enhanced lymphocytopenia w/ other dexamethasone. Increased risk of infections w/ live vaccines. Concomitant use w/ prochlorperazine.

Cytotoxic Chemotherapy

L01CE02 - irinotecan ; Belongs to the class of Topoisomerase 1 (TOP1) inhibitors. Used in the treatment of cancer.

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