Last reviewed 2026-04-23 · How we verify

Irinotecan Injection

Irinotecan is a topoisomerase I inhibitor that prevents DNA religation during replication, leading to DNA damage and cancer cell death.

Irinotecan is a topoisomerase I inhibitor that prevents DNA religation during replication, leading to DNA damage and cancer cell death. Used for Metastatic colorectal cancer, Small cell lung cancer, Ovarian cancer.

At a glance

Mechanism of action

Irinotecan is a camptothecin derivative that inhibits topoisomerase I, an enzyme essential for DNA unwinding and replication. By stabilizing the topoisomerase I-DNA complex, it prevents the religation of DNA strands, causing irreversible DNA damage during the S phase of the cell cycle. This leads to apoptosis in rapidly dividing cancer cells.

Approved indications

• Metastatic colorectal cancer
• Small cell lung cancer
• Ovarian cancer
• Gastric cancer

Common side effects

• Neutropenia
• Diarrhea
• Nausea and vomiting
• Alopecia
• Anemia
• Abdominal pain
• Asthenia/fatigue

Key clinical trials

• Dinutuximab With Chemotherapy, Surgery and Stem Cell Transplantation for the Treatment of Children With Newly Diagnosed High Risk Neuroblastoma (PHASE3)
• Comparing the New Anti-cancer Drug Eribulin With Chemotherapy Against the Usual Chemotherapy Alone in Metastatic Urothelial Cancer (PHASE3)
• A Study Comparing the Combination of Pembrolizumab and Sacituzumab Govitecan Versus Standard of Care in the Treatment of Advanced Urothelial Cancer (PHASE3)
• Oxaliplatin Combined With Irinotecan Liposome Injection II Through Hepatic Artery Infusion (HAIC) Followed by 5-FU/LV (HAIC) or Tegorgor Oral Combination Therapy for Hepatic Metastasis of Pancreatic Cancer (PHASE2)
• A Clinical Study to Evaluate Injection TQB2102 for the Treatment of Patients With HER2 IHC3+ Advanced Colorectal Cancer Who Progressed After Treatment With Oxaliplatin, Irinotecan and Fluoropyrimidine-Based Drugs (PHASE3)
• Apatinib Combined With Liposomal Irinotecan for Refractory or Metastatic Osteosarcoma (PHASE1, PHASE2)
• A Study of Fruquintinib Plus FOLFIRI as Second-Line Treatment for Participants With Metastatic Colorectal Cancer (mCRC) (PHASE2)
• Neoadjuvant FOLFOXIRI and Chemoradiotherapy Versus Neoadjuvant CAPOX/FOLFOX and Chemoradiotherapy Followed by Surgery or a Watch-and-Wait Approach in High Risk Locally Advanced Rectal Cancer (PHASE3)

Primary sources

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