Associated Genetic Biomarkers
Associated Diseases

Overview

Generic Name(s):
irinotecan
Trade Name(s):
Campto and Camptosar
NCI Definition [1]:
A semisynthetic derivative of camptothecin, a cytotoxic, quinoline-based alkaloid extracted from the Asian tree Camptotheca acuminata. Irinotecan, a prodrug, is converted to a biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38) by a carboxylesterase-converting enzyme. One thousand-fold more potent than its parent compound irinotecan, SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death. Because ongoing DNA synthesis is necessary for irinotecan to exert its cytotoxic effects, it is classified as an S-phase-specific agent.

Biomarker-Directed Therapies

Irinotecan has been investigated in 102 clinical trials, of which 88 are open and 14 are closed. Of the trials investigating irinotecan, 5 are early phase 1 (5 open), 28 are phase 1 (22 open), 14 are phase 1/phase 2 (12 open), 39 are phase 2 (33 open), 1 is phase 2/phase 3 (1 open), 14 are phase 3 (14 open), and 1 is phase 4 (1 open).

Deficient DNA Mismatch Repair (dMMR), MLH1 Deficient Expression, and MSH2 Deficient Expression are the most frequent biomarker inclusion criteria for irinotecan clinical trials.

Malignant solid tumor, colorectal carcinoma, and colorectal adenocarcinoma are the most common diseases being investigated in irinotecan clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Irinotecan
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Irinotecan
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating irinotecan and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
Campto, irinotecan, irinotecan (product), Camptosar, 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin, irinotecan (substance), irinotecan, irrinotecan, (+)-7-ethyl-10-hydroxycamptothecine 10-[1,4'-bipiperidine]-1'-carboxylate, irinotecan [chemical/ingredient], [1,4'-bipiperidine]-1'-carboxylic acid (s)-4,11-diethyl-3,4,12,14-tetrahydro-4-hydroxy-3,14-dioxo-1h-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-9-yl ester, (+)-(4s)-4,11-diethyl-4-hydroxy-9-[(4-piperidino-piperidino)carbonyloxy]-1h-pyrano[3',4':6,7]indolizino[1,2-b]quinol-3,14,(4h,12h)-dione
Drug Categories [2]:
Topoisomerase I inhibitors
Drug Target(s) [2]:
TOP1
NCIT ID [1]:
C62040
SNOMED ID [1]:
F-615C1

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.