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Oral Capecitabine with Irinotecan
Capecitabine is converted to 5-fluorouracil to inhibit thymidylate synthase and disrupt DNA synthesis, while irinotecan inhibits topoisomerase I to prevent DNA unwinding during replication, together producing synergistic cytotoxic effects against cancer cells.
Capecitabine is converted to 5-fluorouracil to inhibit thymidylate synthase and disrupt DNA synthesis, while irinotecan inhibits topoisomerase I to prevent DNA unwinding during replication, together producing synergistic cytotoxic effects against cancer cells. Used for Metastatic colorectal cancer, Metastatic gastric cancer, Metastatic breast cancer.
At a glance
| Generic name | Oral Capecitabine with Irinotecan |
|---|---|
| Sponsor | Pfizer |
| Drug class | Antimetabolite and topoisomerase I inhibitor combination |
| Target | Thymidylate synthase (via 5-FU); Topoisomerase I |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | Phase 3 |
Mechanism of action
Capecitabine is an oral prodrug that undergoes hepatic and tumor-selective conversion to 5-fluorouracil (5-FU), which inhibits thymidylate synthase and incorporates into DNA/RNA to disrupt nucleotide synthesis. Irinotecan is a topoisomerase I inhibitor that prevents religation of DNA strands, leading to double-strand breaks during replication. The combination leverages complementary mechanisms of action to enhance cytotoxicity in rapidly dividing cancer cells.
Approved indications
- Metastatic colorectal cancer
- Metastatic gastric cancer
- Metastatic breast cancer
Common side effects
- Diarrhea
- Neutropenia
- Nausea/vomiting
- Fatigue
- Hand-foot syndrome
- Anemia
- Mucositis
- Abdominal pain
Key clinical trials
- Perioperative Systemic Therapy for Isolated Resectable Colorectal Peritoneal Metastases (PHASE2, PHASE3)
- 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)
- A Study of ASP2138 Given Before Surgery, Then Chemotherapy After Surgery, in People With Pancreatic Ductal Cancer (PHASE1)
- A Study of ASP2138 Given by Itself or Given With Other Cancer Treatments in Adults With Stomach Cancer, Gastroesophageal Junction Cancer, or Pancreatic Cancer (PHASE1)
- A Clinical Study on the Treatment of Metastatic Colorectal Cancer at the Second-line or Beyond. (PHASE2)
- SMART TNT for the Conservative Management of Locally Advanced Rectal Cancer (PHASE1)
- Study Evaluating the Tailored Management of Locally-advanced Rectal Carcinoma (PHASE2, PHASE3)
- Exploiting Circulating Tumour DNA to Intensify the Postoperative Treatment Resected Colon Cancer Patients (PHASE2)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Oral Capecitabine with Irinotecan CI brief — competitive landscape report
- Oral Capecitabine with Irinotecan updates RSS · CI watch RSS
- Pfizer portfolio CI