Last reviewed 2026-04-23 · How we verify

CPT-11 based regimens

CPT-11 is a topoisomerase I inhibitor that works by stabilizing the cleavage complex of DNA and RNA, thereby inhibiting DNA replication and transcription.

CPT-11 is a topoisomerase I inhibitor that works by stabilizing the cleavage complex of DNA and RNA, thereby inhibiting DNA replication and transcription. Used for Metastatic colorectal cancer, Metastatic non-small cell lung cancer.

At a glance

Mechanism of action

This leads to DNA damage and apoptosis in rapidly dividing cancer cells. CPT-11 is a prodrug that is converted to its active metabolite SN-38, which is responsible for its therapeutic effects.

Approved indications

• Metastatic colorectal cancer
• Metastatic non-small cell lung cancer

Common side effects

• Diarrhea
• Fatigue
• Nausea
• Vomiting
• Neutropenia

Key clinical trials

• Risk-Based Therapy in Treating Younger Patients With Newly Diagnosed Liver Cancer (PHASE3)
• Irinotecan Hydrochloride, Temozolomide, and Dinutuximab With or Without Eflornithine in Treating Patients With Relapsed or Refractory Neuroblastoma (PHASE2)
• Study of ctDNA Guided Change in Tx for Refractory Minimal Residual Disease in Colon Adenocarcinomas (PHASE1)
• Gemcitabine Hydrochloride, and Radiation Therapy in Patients With Borderline Resectable Pancreatic Cancer (PHASE2)
• Bevacizumab and Oxaliplatin Combined With Irinotecan or Leucovorin and Fluorouracil in Treating Patients With Metastatic or Recurrent Colorectal Cancer (PHASE2)
• SALIRI Based Regimen as First-line Treatment for Advanced Metastatic Colorectal Cancer (PHASE2)
• Phase I Study of Biweekly SIRB Regimen for Metastatic Colorectal Cancer (PHASE1)
• S1201: Combination Chemo for Patients W/Advanced or Metastatic Esophageal, Gastric, or Gastroesophageal Junction Cancer (PHASE2)

Primary sources

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