Irinotecan

Topoisomerase Inhibitor

DB00762

Approved Indication

For the treatment of metastatic colorectal cancer (first-line therapy when administered with 5-fluorouracil and leucovorin). Also used in combination with cisplatin for the treatment of extensive small cell lung cancer. Irinotecan is currently under investigation for the treatment of metastatic or r

2 Targets

0 Resistance Mutations

4 References

3D Structure No structure available

No co-crystal structure available

Protein Targets

TOP1 P11387 ✓ TOP1MT Q969P6 ✓

Mechanism of Action

Irinotecan inhibits the action of topoisomerase I. Irinotecan prevents religation of the DNA strand by binding to topoisomerase I-DNA complex. The formation of this ternary complex interferes with the moving replication fork, which induces replication arrest and lethal double-stranded breaks in DNA. As a result, DNA damage is not efficiently repaired and apoptosis (programmed cell death) occurs.

Details

DrugBank ID DB00762 ↗

Approval Date 1996-06-14

Molecular Weight 586.678 g/mol

Drug Class Topoisomerase Inhibitor

ATC Codes L01XX19

Synonyms Biotecan, Camptothecin-11

PubChem CID: 60838 ↗

ChEMBL CHEMBL481 ↗

SMILES

CCC1=C2CN3C(=CC4=C(COC(=O)[C@]4(O)CC)C3=O)C2=NC2=C1C=C(OC(=O)N1CCC(CC1)N1CCCCC1)C=C2

ADMET Profile

Computing properties…

Drug References (DrugBank)

PMID:15007088 PMID:17008691 PMID:19852077 PMID:9342501