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Irinotecan/Tegafur
Irinotecan/Tegafur is a Topoisomerase I inhibitor + Fluoropyrimidine antimetabolite combination Small molecule drug developed by Sunshine Lake Pharma Co., Ltd.. It is currently in Phase 3 development for Colorectal cancer (phase 3 development), Gastric cancer (potential indication). Also known as: Irinotecan Hydrochloride Injection/Tegafur Gimeracil Oteracil Potassium Capsule.
Irinotecan inhibits topoisomerase I to prevent DNA unwinding during replication, while tegafur is a prodrug of fluorouracil that inhibits thymidylate synthase to disrupt nucleotide synthesis.
Irinotecan is a small molecule inhibitor of DNA topoisomerase 1, classified as an INHIBITOR. It is being studied in clinical trials for various types of cancer, including Non Small Cell Lung Cancer, Head and Neck Squamous Cell Carcinoma, Small Cell Lung Cancer, Pancreatic Ductal Adenocarcinoma, and Colorectal Cancer.
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Baseline phase 3 → approval rate
+58.3pp
Industry-wide phase 3 drugs reach approval ~58.3% of the time (BIO/Informa 2023 industry benchmark across all therapeutic areas). -
Oncology Phase 3 boost
+3.0pp
Oncology Phase 3 trials have higher approval rates (~61%) than the cross-industry average due to clearer endpoints and FDA oncology pathway.
| Regulator | Country | Likely year | Lag vs FDA |
|---|---|---|---|
| FDA | US | 2028–2030 | — |
| EMA | EU | 2029–2031 | +0.7 yr |
| MHRA | GB | 2029–2031 | +0.7 yr |
| Health Canada | CA | 2029–2032 | +0.9 yr |
| TGA | AU | 2029–2032 | +1.2 yr |
| PMDA | JP | 2029–2032 | +1.5 yr |
| NMPA | CN | 2030–2033 | +2.3 yr |
| MFDS | KR | 2029–2032 | +1.4 yr |
| CDSCO | IN | 2029–2033 | +1.8 yr |
| ANVISA | BR | 2030–2033 | +2.3 yr |
Hover any row for the lag rationale. Lag estimates are reduced when the drug has FDA Breakthrough or EMA PRIME designation (sponsors file globally in parallel).
Estimate based on the BIO/Informa industry phase transition rates plus per-drug modifiers for therapeutic area, sponsor type, FDA designations, mechanism, and trial design. Per-jurisdiction lags from Tufts CSDD international approval studies. Not investment, clinical or regulatory advice. Methodology: /methodology#likelihood.
At a glance
| Generic name | Irinotecan/Tegafur |
|---|---|
| Also known as | Irinotecan Hydrochloride Injection/Tegafur Gimeracil Oteracil Potassium Capsule |
| Sponsor | Sunshine Lake Pharma Co., Ltd. |
| Drug class | Topoisomerase I inhibitor + Fluoropyrimidine antimetabolite combination |
| Target | Topoisomerase I; Thymidylate synthase |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | Phase 3 |
Mechanism of action
This combination leverages two complementary chemotherapy mechanisms: irinotecan causes DNA damage by stabilizing topoisomerase I-DNA complexes, leading to double-strand breaks during replication, while tegafur (a 5-FU prodrug) blocks thymidylate synthase to deplete dTMP and inhibit DNA synthesis. The dual mechanism targets cancer cells through both direct DNA damage and nucleotide depletion pathways.
Approved indications
- Colorectal cancer (phase 3 development)
- Gastric cancer (potential indication)
Common side effects
- Neutropenia
- Diarrhea
- Nausea/vomiting
- Anemia
- Fatigue
- Mucositis
Key clinical trials
- 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)
- Phase III Study to Compare GFH375 and Chemotherapy in Patients With KRAS G12D-Mutant Metastatic Pancreatic Cancer (PHASE3)
- Study of Larotinib in Unresectable Advanced or Recurrent Esophageal Cancer (PHASE3)
- HR070803 in Combination With Oxaliplatin, S-1 Versus NALIRIFOX as Adjuvant Therapy for Pancreatic Cancer (PHASE2)
- Irinotecan Liposome Combined With Oxaliplatin and Tegafur as Adjuvant Therapy for Pancreatic Cancer (NA)
- A Study of KC1036 Versus Investigator's Choice of Chemotherapy in Patients With Advanced Esophageal Cancer (PHASE3)
- A Multiple Ascending Dose Study of MEDI7247 in Advanced or Metastatic Solid Tumors (PHASE1)
- S-1, Irinotecan, and Oxaliplatin in Locally-Advanced Pancreatic Cancer (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:
- Irinotecan/Tegafur CI brief — competitive landscape report
- Irinotecan/Tegafur updates RSS · CI watch RSS
- Sunshine Lake Pharma Co., Ltd. portfolio CI
Frequently asked questions about Irinotecan/Tegafur
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Related
- Drug class: All Topoisomerase I inhibitor + Fluoropyrimidine antimetabolite combination drugs
- Target: All drugs targeting Topoisomerase I; Thymidylate synthase
- Manufacturer: Sunshine Lake Pharma Co., Ltd. — full pipeline
- Therapeutic area: All drugs in Oncology
- Indication: Drugs for Colorectal cancer (phase 3 development)
- Indication: Drugs for Gastric cancer (potential indication)
- Also known as: Irinotecan Hydrochloride Injection/Tegafur Gimeracil Oteracil Potassium Capsule
Primary sources · FDA · ClinicalTrials.gov · EMA · SEC EDGAR · ChEMBL · Wikidata · full sourcing