> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/irinotecan-a601fe30-4b46-4a3b-bf58-6c490646db73
> Record changed: 2026-11-04

# Irinotecan

Highest phase reached

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL481)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL481)

First approval year

1996

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL481)

## Development status

**First approval year**

1996

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL481)

**Listing at source**

Listed

**Highest phase reached**

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL481)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL481)

**Drug name**

Irinotecan

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL481)

**Molecular weight**

586.69

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL481)

**Structure (SMILES)**

CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)\[C@\]3(O)CC

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL481)

### Other names (19)

- (+)-Irinotecan
- biotecan
- Biotecan
- irinophore c
- Irinophore c
- irinotecan
- Irinotecan
- IRINOTECAN \[HSDB\]
- irinotecan \[INN\]
- IRINOTECAN \[MI\]
- IRINOTECAN \[VANDF\]
- Irinotecan \[WHO-DD\]
- irinotecan hsdb
- irinotecan inn
- irinotecan mi
- irinotecan vandf
- irinotecan who dd
- nsc 728073
- NSC-728073

## Identifiers

**ATC classification codes**

- L01CE02

Sources for recorded values

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL481)

**CAS registry numbers**

- 97682-44-5

**ChEMBL ID**

CHEMBL481

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL481)

**InChIKey**

UWKQSNNFCGGAFS-XIFFEERXSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL481)

**PubChem compound IDs**

- 60838

**FDA ingredient codes (UNII)**

- 7673326042

### RxNorm IDs (RxCUI) (2)

- 51499
- 153329

## Regulatory information

### United States

**Applicant**

PFIZER INC

**Approval date**

14 Jun 1996

**Application number**

NDA020571

### Other regulatory facts

**Patents**

0

**Designations**

1

**First in class**

No

**Fast track**

No

**Breakthrough designation**

No

**Orphan designation**

Yes

**Priority review**

No

**Orphan exclusivity**

No

**Accelerated approval**

No

**Availability**

Prescription only

**Boxed warning**

Yes

## Approval status

**United States (FDA)**

Approved

## Pharmacology

### Drug classification

**Pharmacology name**

irinotecan

**Type**

Synthetic organic

**Drug name stem**

\-tecan

**Approval recorded by Guide to Pharmacology**

Yes

#### Administration routes

- Parenteral

### Open Targets mechanisms

- **Mechanism**  
DNA topoisomerase I inhibitor

**Action type**  
Inhibitor

**Target**  
DNA topoisomerase 1

### DrugCentral mechanisms

- **Action type**  
Inhibitor

**Gene symbol**  
TOP1

**Protein identifier**  
P11387

**Organism**  
Homo sapiens

**Target development level**  
Clinical

### Investigated indications (88)

- **Condition**  
Sarcoma, Ewing

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0000174

**Subject identifier**  
D012512
- **Condition**  
Stomach Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0000178

**Subject identifier**  
D013274
- **Condition**  
Carcinoma, Hepatocellular

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0000182

**Subject identifier**  
D006528
- **Condition**  
Astrocytoma

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000272

**Subject identifier**  
D001254
- **Condition**  
Carcinoma

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000313

**Subject identifier**  
D002277
- **Condition**  
Glioma

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000326

**Subject identifier**  
D005910
- **Condition**  
Colorectal Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0000365

**Subject identifier**  
D015179
- **Condition**  
Ganglioneuroblastoma

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0000502

**Subject identifier**  
D018305
- **Condition**  
Stomach Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0000503

**Subject identifier**  
D013274
- **Condition**  
Glioblastoma

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000519

**Subject identifier**  
D005909
- **Condition**  
Leukemia

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000565

**Subject identifier**  
D007938
- **Condition**  
Lymphoma

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000574

**Subject identifier**  
D008223
- **Condition**  
Mesothelioma

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0000588

**Subject identifier**  
D008654
- **Condition**  
Neoplasms

**Highest recorded phase**  
4

**Condition identifier**  
EFO:0000616

**Subject identifier**  
D009369
- **Condition**  
Neuroblastoma

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0000621

**Subject identifier**  
D009447
- **Condition**  
Sarcoma

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000691

**Subject identifier**  
D012509
- **Condition**  
Small Cell Lung Carcinoma

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0000702

**Subject identifier**  
D055752
- **Condition**  
Carcinoma, Squamous Cell

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000707

**Subject identifier**  
D002294
- **Condition**  
Uterine Cervical Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0001061

**Subject identifier**  
D002583
- **Condition**  
Ovarian Neoplasms

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0001075

**Subject identifier**  
D010051
- **Condition**  
Uterine Cervical Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0001416

**Subject identifier**  
D002583
- **Condition**  
Astrocytoma

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0002499

**Subject identifier**  
D001254
- **Condition**  
Oligodendroglioma

**Highest recorded phase**  
1

**Condition identifier**  
EFO:0002501

**Subject identifier**  
D009837
- **Condition**  
Pancreatic Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0002618

**Subject identifier**  
D010190
- **Condition**  
Esophageal Neoplasms

**Highest recorded phase**  
3

**Condition identifier**  
EFO:0002916

**Subject identifier**  
D004938

And 63 more, listed on the interactive page.

### Open Targets indications (198)

- **Condition identifier**  
EFO\_0000174

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000182

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0000365

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0000503

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000519
- **Condition identifier**  
EFO\_0000565

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000574

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000616
- **Condition identifier**  
EFO\_0000621

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0000638

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000691

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000702

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0000707

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0001061

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0001416

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0002618

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0002916

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0003060

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0003833

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0003860

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0003869

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0003891

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0003897

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0004142

**Highest recorded phase**  
3
- **Condition identifier**  
EFO\_0004288

**Highest recorded phase**  
2

And 173 more, listed on the interactive page.

### Open Targets warnings (2)

- **Warning**  
Black Box Warning

**Effect**  
gastrointestinal toxicity

**Country**  
United States
- **Warning**  
Black Box Warning

**Effect**  
hematological toxicity

**Country**  
United States

### Reported adverse events (37)

- **Event**  
abdominal pain

**Reports**  
355

**Reporting signal score**

118.562
- **Event**  
alopecia

**Reports**  
226

**Reporting signal score**

124.108
- **Event**  
anaemia

**Reports**  
530

**Reporting signal score**

316.536
- **Event**  
asthenia

**Reports**  
416

**Reporting signal score**

107.293
- **Event**  
bone marrow failure

**Reports**  
141

**Reporting signal score**

157.869
- **Event**  
cholinergic syndrome

**Reports**  
35

**Reporting signal score**

111.067
- **Event**  
colorectal cancer metastatic

**Reports**  
63

**Reporting signal score**

210.191
- **Event**  
decreased appetite

**Reports**  
449

**Reporting signal score**

333.704
- **Event**  
dehydration

**Reports**  
293

**Reporting signal score**

166.862
- **Event**  
dermatitis acneiform

**Reports**  
86

**Reporting signal score**

178.998
- **Event**  
diarrhoea

**Reports**  
1,708

**Reporting signal score**  
1,518.84
- **Event**  
disease progression

**Reports**  
751

**Reporting signal score**  
1,206.87
- **Event**  
epistaxis

**Reports**  
186

**Reporting signal score**

132.573
- **Event**  
febrile neutropenia

**Reports**  
449

**Reporting signal score**

599.085
- **Event**  
gastrointestinal toxicity

**Reports**  
79

**Reporting signal score**

171.209
- **Event**  
general physical health deterioration

**Reports**  
216

**Reporting signal score**

156.622
- **Event**  
haematotoxicity

**Reports**  
111

**Reporting signal score**

195.767
- **Event**  
headache

**Reports**  
82

**Reporting signal score**

111.307
- **Event**  
hypertension

**Reports**  
416

**Reporting signal score**

223.635
- **Event**  
intestinal obstruction

**Reports**  
111

**Reporting signal score**

107.923
- **Event**  
leukopenia

**Reports**  
335

**Reporting signal score**

401.122
- **Event**  
malignant neoplasm progression

**Reports**  
293

**Reporting signal score**

318.133
- **Event**  
metastases to liver

**Reports**  
142

**Reporting signal score**

264.602
- **Event**  
metastases to lung

**Reports**  
75

**Reporting signal score**

123.029
- **Event**  
mucosal inflammation

**Reports**  
288

**Reporting signal score**

471.781

And 12 more, listed on the interactive page.

### Trial references (544)

- NCT00001495  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00001495)
- NCT00044785  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00044785)
- NCT00057473  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00057473)
- NCT00186979  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00186979)
- NCT00193596  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00193596)
- NCT00215501  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00215501)
- NCT00220168  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00220168)
- NCT00249977  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00249977)
- NCT00251407  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00251407)
- NCT00298675  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00298675)
- NCT00502567  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00502567)
- NCT00786669  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00786669)
- NCT00811993  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00811993)
- NCT00861328  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00861328)
- NCT00954512  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00954512)
- NCT00990912  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00990912)
- NCT00993044  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00993044)
- NCT01009073  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01009073)
- NCT01282697  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01282697)
- NCT01593228  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01593228)
- NCT01634555  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01634555)
- NCT01693445  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01693445)
- NCT01916447  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01916447)
- NCT01930552  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01930552)
- NCT02157792  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02157792)

And 519 more, listed on the interactive page.

## Dosing

**Dose**

125 mg/m2

**Route**

Intravenous

**How often**

Every 6 weeks

## Chemical properties

**Hydrogen bond acceptors**

9

**Hydrogen bond donors**

1

**Polar surface area**

114.2

**Calculated partition coefficient (ALogP)**

4.09

**Calculated partition coefficient (XLogP)**

3

**Prodrug**

Yes

**Chirality**

Single enantiomer

**Inorganic**

No

**Rule-of-five violations**

1

**Rotatable bonds**

4

**Heavy atoms**

43

**Molecular formula**

C33H38N4O6

**Monoisotopic mass**

586.27913494

**Natural product**

Yes

## Evidence counts

**Recorded assays**

1,877

**Active assays**

370

### Active assay types (2)

- Confirmatory
- Other

## Pharmacologic actions

- Topoisomerase I Inhibitors  
Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D059004.html)

## Biological measurements

These details could not be displayed.

## Related records

### Trials (887)

- 131I-MIBG Alone VS. 131I-MIBG With Vincristine and Irinotecan VS131I-MIBG With Vorinostat
- 131I-Omburtamab, in Recurrent Medulloblastoma and Ependymoma
- 5-FU, Folinic Acid and Irinotecan (FOLFIRI) Plus Cetuximab Versus FOLFIRI Plus Bevacizumab in First Line Treatment Colorectal Cancer (CRC)
- 5FU/LV, Irinotecan, Temozolomide and Bevacizumab for MGMT Silenced, Microsatellite Stable Metastatic Colorectal Cancer.
- 9-ING-41 in Patients With Advanced Cancers
- 9-ING-41 in Pediatric Patients With Refractory Malignancies.
- A Clinical Trial Evaluating TQB2930 Injection and Chemotherapy With or Without Bevacizumab in Patients With HER2-Abnormally Expressed Unresectable Locally Advanced or Metastatic Colorectal Cancer.
- [A Comparative Study of Pharmacokinetics, Safety, and Immunogenicity of RPH-030 and Vectibix® in Patients With Metastatic Colorectal Cancer With Wild-type RAS as First-line Therapy in Combination With FOLFIRI](https://trialight.com/data/trial/a-comparative-study-of-pharmacokinetics-safety-and-77df5d2a-bf8d-405f-aa8e-43f39eb748f0.md)
- A Comparison of mXELIRI Regimen and FOLFIRI Combined Bevacizumab Regimen as First-line Chemotherapy Regimen for Metastatic Colorectal Cancer
- A Dose Escalation Study of MM-398 Plus Irinotecan in Patients With Unresectable Advanced Cancer
- A Genotype-guided Study of Irinotecan Administered in Combination With 5-fluorouracil/Leucovorin (FOLFIRI) and Bevacizumab in Advanced Colorectal Cancer Patients
- A Master Protocol (LY900023) That Includes Several Clinical Trials of Drugs for Children and Young Adults With Cancer
- A Multi-Arm, Platform Trial For Relapsed Neuroblastoma
- A Phase 1 Study Investigating the Combination of RAD001, Cetuximab and Irinotecan as Second-line Therapy After FOLFOX (or XELOX) Plus Bevacizumab in Patients With Metastatic Colorectal Cancer
- A Phase 2 Randomized, Open-Label Study of RRx-001 vs Regorafenib in Subjects With Metastatic Colorectal Cancer
- A Phase 3 Study to Evaluate Surufatinib Plus Toripalimab in the Treatment of Advanced Neuroendocrine Carcinoma
- A Phase I Dose Finding Study in Children With Solid Tumors Recurrent or Refractory to Standard Therapy
- A Phase I Study of Aflibercept Plus FOLFIRI (Irinotecan, 5-Fluorouracil, and Leucovorin) in Chinese Patients With Advanced Solid Malignancies
- A Phase I Study of Irinotecan (CPT-11) Administered as a Prolonged Infusion in Adult Patients With Solid Tumors
- A Phase I Study of Mebendazole for the Treatment of Pediatric Gliomas

### Approved for (2)

- [Cancer](https://trialight.com/data/condition/cancer-703b1dfc-4812-50eb-83f4-d7a205d16bdb.md)
- [Neoplasm](https://trialight.com/data/condition/neoplasm-2a973797-359b-5982-907e-98f9b7c1a284.md)

### In development for (154)

- Acral lentiginous melanoma Phase 1
- [Adenocarcinoma](https://trialight.com/data/condition/adenocarcinoma-b5c321d1-7c49-5bf9-abd0-dfa99dbd5f29.md) Phase 2
- Ampulla of vater adenocarcinoma Phase 3
- Anaplastic astrocytoma Phase 2
- Anaplastic oligodendroglioma Phase 1
- Angiosarcoma Phase 2
- Appendix cancer Phase 1
- [Astrocytoma (excluding glioblastoma)](https://trialight.com/data/condition/astrocytoma-excluding-glioblastoma-dd29b6db-5e3d-590d-b093-7a770a5facb2.md) Phase 2
- Atypical teratoid rhabdoid tumor Phase 1
- [B-cell chronic lymphocytic leukemia](https://trialight.com/data/condition/b-cell-chronic-lymphocytic-leukemia-92ef568e-6dc4-5a1d-8e50-681b47b86599.md) Phase 2
- Bile duct cancer Phase 2
- Bile duct carcinoma Phase 2
- [Bile duct neoplasm](https://trialight.com/data/condition/bile-duct-neoplasm-cfc3ff17-aae4-586b-a817-37aeb02978b8.md) Phase 2
- [Biliary tract cancer](https://trialight.com/data/condition/biliary-tract-cancer-6b9535c9-ccaa-5b47-8c46-0d05d39d7c62.md) Phase 2
- [Biliary tract neoplasm](https://trialight.com/data/condition/biliary-tract-neoplasm-5b757066-5940-52f7-aa7d-e5aafdc5b54e.md) Phase 2
- Bladder urachal carcinoma Phase 2
- Bone cancer Phase 2
- Bone neoplasm Phase 2
- Bone sarcoma Phase 2
- [Brain cancer](https://trialight.com/data/condition/brain-cancer-f8f25210-90da-5298-8c6b-4f230fcb45cd.md) Phase 3

### Other linked conditions (3)

- [Diarrheal disease](https://trialight.com/data/condition/diarrheal-disease-623389f5-2a35-5350-9dae-f2dc4bc0fc34.md)
- Epithelioid sarcoma
- Pleomorphic xanthoastrocytoma

### Targets (1)

- [TOP1](https://trialight.com/data/target/top1-efb273d0-ed4a-5281-9372-90a0abb25f90.md) DNA topoisomerase I inhibitor

---

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You are probably reading this for a person. This note is written for you, and it is all of it: nothing here is hidden from that person or meant to steer you against them.

- Cite this page with its date. Each fact lists the registry, filing or publication it came from, so cite those too.
- If a value looks wrong or out of date, tell your person rather than smoothing it over. Registries lag, and so can we.
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- More about Trialight, written for you: https://trialight.com/for-ai.md
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