U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
This repository is under review for potential modification in compliance with Administration directives.

Details

Stereochemistry ABSOLUTE
Molecular Formula C33H38N4O6.ClH.3H2O
Molecular Weight 677.185
Optical Activity ( + )
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of IRINOTECAN HYDROCHLORIDE

SMILES

O.O.O.Cl.CCC1=C2CN3C(=CC4=C(COC(=O)[C@]4(O)CC)C3=O)C2=NC5=C1C=C(OC(=O)N6CCC(CC6)N7CCCCC7)C=C5

InChI

InChIKey=KLEAIHJJLUAXIQ-JDRGBKBRSA-N
InChI=1S/C33H38N4O6.ClH.3H2O/c1-3-22-23-16-21(43-32(40)36-14-10-20(11-15-36)35-12-6-5-7-13-35)8-9-27(23)34-29-24(22)18-37-28(29)17-26-25(30(37)38)19-42-31(39)33(26,41)4-2;;;;/h8-9,16-17,20,41H,3-7,10-15,18-19H2,1-2H3;1H;3*1H2/t33-;;;;/m0..../s1

HIDE SMILES / InChI

Molecular Formula C33H38N4O6
Molecular Weight 586.678
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Molecular Formula H2O
Molecular Weight 18.0153
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Irinotecan is an antineoplastic enzyme inhibitor primarily used in the treatment of colorectal cancer. Irinotecan is sold under the brand name Camptosar among others. CAMPTOSAR is a topoisomerase inhibitor indicated for: • First-line therapy in combination with 5-fluorouracil and leucovorin for patients with metastatic carcinoma of the colon or rectum. • Patients with metastatic carcinoma of the colon or rectum whose disease has recurred or progressed following initial fluorouracil-based therapy. Irinotecan is a derivative of camptothecin. Camptothecins interact specifically with the enzyme topoisomerase I, which relieves torsional strain in DNA by inducing reversible single-strand breaks. Irinotecan and its active metabolite SN-38 bind to the topoisomerase I-DNA complex and prevent religation of these single-strand breaks. Current research suggests that the cytotoxicity of irinotecan is due to double-strand DNA damage produced during DNA synthesis when replication enzymes interact with the ternary complex formed by topoisomerase I, DNA, and either irinotecan or SN-38. Mammalian cells cannot efficiently repair these double-strand breaks.

CNS Activity

Curator's Comment: Irinotecan crosses the blood-brain barrier

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
CAMPTOSAR

Approved Use

CAMPTOSAR is a topoisomerase inhibitor indicated for: • First-line therapy in combination with 5-fluorouracil and leucovorin for patients with metastatic carcinoma of the colon or rectum. (1) • Patients with metastatic carcinoma of the colon or rectum whose disease has recurred or progressed following initial fluorouracil-based therapy.

Launch Date

1996
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1660 ng/mL
125 mg/m² single, intravenous
dose: 125 mg/m²
route of administration: Intravenous
experiment type: SINGLE
co-administered:
IRINOTECAN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
3392 ng/mL
340 mg/m² single, intravenous
dose: 340 mg/m²
route of administration: Intravenous
experiment type: SINGLE
co-administered:
IRINOTECAN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
10200 ng × h/mL
125 mg/m² single, intravenous
dose: 125 mg/m²
route of administration: Intravenous
experiment type: SINGLE
co-administered:
IRINOTECAN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
20604 ng × h/mL
340 mg/m² single, intravenous
dose: 340 mg/m²
route of administration: Intravenous
experiment type: SINGLE
co-administered:
IRINOTECAN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
5.8 h
125 mg/m² single, intravenous
dose: 125 mg/m²
route of administration: Intravenous
experiment type: SINGLE
co-administered:
IRINOTECAN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
11.7 h
340 mg/m² single, intravenous
dose: 340 mg/m²
route of administration: Intravenous
experiment type: SINGLE
co-administered:
IRINOTECAN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
51%
125 mg/m² single, intravenous
dose: 125 mg/m²
route of administration: Intravenous
experiment type: SINGLE
co-administered:
IRINOTECAN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Other AEs: Fatigue, Weight loss...
Other AEs:
Fatigue (grade 1-2, 33.3%)
Weight loss (grade 1-2, 33.3%)
Diarrhea (grade 1-2, 50%)
Nausea (grade 1-2, 58.3%)
Vomiting (grade 1-2, 50%)
Cholinergic syndrome (grade 1-2, 33.3%)
Mucositis (grade 1-2, 33.3%)
Dyspnea (grade 1-2, 8.3%)
Fever (grade 1-2, 8.3%)
Fatigue (grade 3, 8.3%)
Diarrhea (grade 3, 8.3%)
Nausea (grade 3, 8.3%)
Vomiting (grade 3, 8.3%)
Cholinergic syndrome (grade 3, 33.3%)
Sources:
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Other AEs: Leukopenia, Leukopenia...
Other AEs:
Leukopenia (grade 2, 1 patient)
Leukopenia (grade 3, 2 patients)
Leukopenia (grade 4, 1 patient)
Neutropenia (grade 2, 2 patients)
Neutropenia (grade 3, 2 patients)
Neutropenia (grade 4, 1 patient)
Nausea (grade 1, 4 patients)
Nausea (grade 3, 1 patient)
Vomiting (grade 4, 1 patient)
Diarrhea (grade 1, 2 patients)
Diarrhea (grade 2, 3 patients)
Diarrhea (grade 4, 1 patient)
Anorexia (grade 1, 3 patients)
Anorexia (grade 2, 2 patients)
Sources:
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Other AEs: Leukopenia, Leukopenia...
Other AEs:
Leukopenia (grade 1, 4 patients)
Leukopenia (grade 2, 1 patient)
Leukopenia (grade 3, 2 patients)
Neutropenia (grade 1, 2 patients)
Neutropenia (grade 2, 2 patients)
Neutropenia (grade 4, 2 patients)
Thrombocytopenia (grade 1, 2 patients)
Nausea (grade 1, 3 patients)
Nausea (grade 2, 3 patients)
Nausea (grade 3, 2 patients)
Vomiting (grade 1, 2 patients)
Vomiting (grade 2, 2 patients)
Vomiting (grade 3, 1 patient)
Vomiting (grade 4, 1 patient)
Diarrhea (grade 1, 3 patients)
Diarrhea (grade 2, 2 patients)
Diarrhea (grade 3, 1 patient)
Diarrhea (grade 4, 1 patient)
Anorexia (grade 1, 3 patients)
Anorexia (grade 2, 2 patients)
Sources:
AEs

AEs

AESignificanceDosePopulation
Cholinergic syndrome grade 1-2, 33.3%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Fatigue grade 1-2, 33.3%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Mucositis grade 1-2, 33.3%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Weight loss grade 1-2, 33.3%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Diarrhea grade 1-2, 50%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Vomiting grade 1-2, 50%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Nausea grade 1-2, 58.3%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Dyspnea grade 1-2, 8.3%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Fever grade 1-2, 8.3%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Cholinergic syndrome grade 3, 33.3%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Diarrhea grade 3, 8.3%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Fatigue grade 3, 8.3%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Nausea grade 3, 8.3%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Vomiting grade 3, 8.3%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Diarrhea grade 1, 2 patients
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Anorexia grade 1, 3 patients
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Nausea grade 1, 4 patients
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Leukopenia grade 2, 1 patient
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Anorexia grade 2, 2 patients
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Neutropenia grade 2, 2 patients
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Diarrhea grade 2, 3 patients
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Nausea grade 3, 1 patient
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Leukopenia grade 3, 2 patients
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Neutropenia grade 3, 2 patients
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Diarrhea grade 4, 1 patient
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Leukopenia grade 4, 1 patient
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Neutropenia grade 4, 1 patient
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Vomiting grade 4, 1 patient
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Neutropenia grade 1, 2 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Thrombocytopenia grade 1, 2 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Vomiting grade 1, 2 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Anorexia grade 1, 3 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Diarrhea grade 1, 3 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Nausea grade 1, 3 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Leukopenia grade 1, 4 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Leukopenia grade 2, 1 patient
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Anorexia grade 2, 2 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Diarrhea grade 2, 2 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Neutropenia grade 2, 2 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Vomiting grade 2, 2 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Nausea grade 2, 3 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Diarrhea grade 3, 1 patient
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Vomiting grade 3, 1 patient
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Leukopenia grade 3, 2 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Nausea grade 3, 2 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Diarrhea grade 4, 1 patient
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Vomiting grade 4, 1 patient
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
Neutropenia grade 4, 2 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: M+F
Sources:
PubMed

PubMed

TitleDatePubMed
Management of chemotherapy-induced adverse effects in the treatment of colorectal cancer.
2001
Treatment of extensive stage small cell lung cancer.
2001
Lung cancer: therapeutic options for stage IV and recurrent NSCLC.
2001
Irinotecan: a new agent comes of age.
2001
[Home chemotherapy and/or outpatient chemotherapy for patient with advanced gastric cancer].
2001 Apr
[Irinotecan (CPT-11) therapy for advanced gastric cancer].
2001 Apr
[Chemotherapy of irinotecan (CPT-11) combined with cisplatin in patients with advanced gastric cancer].
2001 Apr
Safe administration of irinotecan, oxaliplatin and raltitrexed in a DPD-deficient patient with metastatic colon cancer.
2001 Apr
Human plasma carboxylesterase and butyrylcholinesterase enzyme activity: correlations with SN-38 pharmacokinetics during a prolonged infusion of irinotecan.
2001 Apr
Antitumor activity of XR5944, a novel and potent topoisomerase poison.
2001 Apr
Use of a modified ornithine decarboxylase promoter to achieve efficient c-MYC- or N-MYC-regulated protein expression.
2001 Apr 1
Subcellular localization and distribution of the breast cancer resistance protein transporter in normal human tissues.
2001 Apr 15
26S proteasome inhibition induces apoptosis and limits growth of human pancreatic cancer.
2001 Apr 2-27
The current status of docetaxel for advanced non-small cell lung cancer.
2001 Feb
[Medical treatment of pulmonary neoplasms].
2001 Feb
Combination chemotherapy in patients with malignant pleural effusions from non-small cell lung cancer : cisplatin, ifosfamide, and irinotecan with recombinant human granulocyte colony-stimulating factor support.
2001 Feb
Effect of bile acids on the uptake of irinotecan and its active metabolite, SN-38, by intestinal cells.
2001 Feb 16
Breast cancer resistance protein directly confers SN-38 resistance of lung cancer cells.
2001 Feb 9
New state of the art in small-cell lung cancer.
2001 Jan
Current status of irinotecan in lung cancer.
2001 Jan
Docetaxel followed by gemcitabine and irinotecan in solid tumors.
2001 Jan
Rationale and dose-finding studies of the combination of irinotecan and a taxane on a weekly schedule.
2001 Jan
Treatment of non-small-cell lung cancer in North America: the emerging role of irinotecan.
2001 Jan
Irinotecan in small-cell lung cancer: the US experience.
2001 Jan
Influence of cytokines, monoclonal antibodies and chemotherapeutic drugs on epithelial cell adhesion molecule (EpCAM) and LewisY antigen expression.
2001 Jan
The HER tyrosine kinase inhibitor CI1033 enhances cytotoxicity of 7-ethyl-10-hydroxycamptothecin and topotecan by inhibiting breast cancer resistance protein-mediated drug efflux.
2001 Jan 15
Repression of cyclin B1 expression after treatment with adriamycin, but not cisplatin in human lung cancer A549 cells.
2001 Jan 26
Adjuvant therapy for colon cancer: the European experience.
2001 Jan-Feb
[Molecular factors predictive of response to chemotherapy in advanced stages of colorectal cancer].
2001 Jan-Feb
[Irinotecan in colorectal cancer].
2001 Jan-Feb
[Refinement and role of the diagnosis of Gilbert disease with molecular biology].
2001 Jan-Feb
New chemotherapy approaches in colorectal cancer.
2001 Jul
Control of irinotecan-induced diarrhea by octreotide after loperamide failure.
2001 Jun
Phase I-II study of irinotecan in combination with mitomycin C in patients with advanced gastrointestinal cancer.
2001 Jun
Irinotecan plus cisplatin in advanced gastric or gastroesophageal junction carcinoma.
2001 Mar
Cisplatin and irinotecan in upper gastrointestinal malignancies.
2001 Mar
Optimizing chemoradiation therapy approaches to unresectable stage III non--small cell lung cancer.
2001 Mar
Topoisomerase I targeting agents in small-cell lung cancer.
2001 Mar
Oxaliplatin: a new agent for colorectal cancer.
2001 Mar
Determinants of prognosis and response to therapy in colorectal cancer.
2001 Mar
[Chemotherapy of colonic carcinoma in the year 2001].
2001 Mar 22
Modulation of irinotecan-induced diarrhea by cotreatment with neomycin in cancer patients.
2001 May
Integrating the oral fluoropyrimidines into the management of advanced colorectal cancer.
2001 May
Enhanced chemosensitivity to CPT-11 with proteasome inhibitor PS-341: implications for systemic nuclear factor-kappaB inhibition.
2001 May 1
Advances in chemotherapy for small cell lung cancer: single-agent activity of newer agents.
2001 May-Jun
Patents

Sample Use Guides

Usual Adult Dose for Colorectal Cancer Either as a single agent or in combination with fluorouracil and leucovorin: 125 mg/m2 intravenously over 90 minutes once a week for four doses or as a single agent: 350 mg/m2 intravenously over 90 minutes every three weeks or in combination with fluorouracil and leucovorin: 180 mg/m2 intravenously over 90 minutes every other week for three doses.
Route of Administration: Intravenous
In Vitro Use Guide
The sensitivity to CPT-11 (Irinotecan) alone, of 5 human colon-cancer cell lines, expressed as IC50 values, varied between 2.5 and 6.1uM. The anti-proliferative effectsof the active metabolite SN-38 showed IC50 values between 5.6 and 38 nM, 130 to 570 times lower than those measured for CPT-11 alone. The sensitivity to SN-38 was highest in LS174T and COLO320 cells, intermediate in SW1398 cells and lowest in COLO 205 and WiDr cells.
Substance Class Chemical
Created
by admin
on Mon Mar 31 18:00:48 GMT 2025
Edited
by admin
on Mon Mar 31 18:00:48 GMT 2025
Record UNII
042LAQ1IIS
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
IRINOTECAN HYDROCHLORIDE TRIHYDRATE
MI  
Preferred Name English
IRINOTECAN HYDROCHLORIDE
MART.   ORANGE BOOK   USAN   USP   USP-RS   VANDF  
USAN  
Official Name English
IRINOTECAN HYDROCHLORIDE [MART.]
Common Name English
ONIVYDE
Brand Name English
U-101,440E
Code English
IRINOTECAN HYDROCHLORIDE [ORANGE BOOK]
Common Name English
IRINOTECAN HYDROCHLORIDE TRIHYDRATE [EP MONOGRAPH]
Common Name English
IRINOTECAN HYDROCHLORIDE [USP-RS]
Common Name English
IRINOTECAN HYDROCHLORIDE [USP MONOGRAPH]
Common Name English
IRINOTECAN HYDROCHLORIDE HYDRATE
JAN  
Common Name English
NSC-759878
Code English
XELIRI COMPONENT IRINOTECAN HYDROCHLORIDE
Common Name English
IRINOTECAN HYDROCHLORIDE [USAN]
Common Name English
(1,4'-BIPIPERIDINE)-1'-CARBOXYLIC ACID, 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, MONOHYDROCHLORIDE, TRIHYDRATE, (S)-
Common Name English
CPT-11
Code English
CAMPTO
Brand Name English
(+)-7-ETHYL-10-HYDROXYCAMPTOTHECINE 10-(1,4'-BIPIPERIDINE)-1'-CARBOXYLATE, MONOHYDROCHLORIDE, TRIHYDRATE
Common Name English
IRINOTECAN HYDROCHLORIDE TRIHYDRATE [EMA EPAR]
Common Name English
DQ-2805
Code English
IRINOTECAN HYDROCHLORIDE TRIHYDRATE [MI]
Common Name English
IRINOTECAN HYDROCHLORIDE HYDRATE [JAN]
Common Name English
CAMPTOSAR
Brand Name English
Irinotecan hydrochloride trihydrate [WHO-DD]
Common Name English
IRINOTECAN HYDROCHLORIDE [VANDF]
Common Name English
IRINOTECAN MONOHYDROCHLORIDE TRIHYDRATE
WHO-DD  
Common Name English
U-101440E
Code English
Classification Tree Code System Code
EU-Orphan Drug EU/3/11/933
Created by admin on Mon Mar 31 18:00:48 GMT 2025 , Edited by admin on Mon Mar 31 18:00:48 GMT 2025
EMA ASSESSMENT REPORTS ONIVYDE (AUTHORIZED: PANCREATIC NEOPLASMS):
Created by admin on Mon Mar 31 18:00:48 GMT 2025 , Edited by admin on Mon Mar 31 18:00:48 GMT 2025
NCI_THESAURUS C2843
Created by admin on Mon Mar 31 18:00:48 GMT 2025 , Edited by admin on Mon Mar 31 18:00:48 GMT 2025
Code System Code Type Description
USAN
HH-3
Created by admin on Mon Mar 31 18:00:48 GMT 2025 , Edited by admin on Mon Mar 31 18:00:48 GMT 2025
PRIMARY
PUBCHEM
60837
Created by admin on Mon Mar 31 18:00:48 GMT 2025 , Edited by admin on Mon Mar 31 18:00:48 GMT 2025
PRIMARY
EPA CompTox
DTXSID60929485
Created by admin on Mon Mar 31 18:00:48 GMT 2025 , Edited by admin on Mon Mar 31 18:00:48 GMT 2025
PRIMARY
NSC
759878
Created by admin on Mon Mar 31 18:00:48 GMT 2025 , Edited by admin on Mon Mar 31 18:00:48 GMT 2025
PRIMARY
DAILYMED
042LAQ1IIS
Created by admin on Mon Mar 31 18:00:48 GMT 2025 , Edited by admin on Mon Mar 31 18:00:48 GMT 2025
PRIMARY
EVMPD
SUB02772MIG
Created by admin on Mon Mar 31 18:00:48 GMT 2025 , Edited by admin on Mon Mar 31 18:00:48 GMT 2025
PRIMARY
RXCUI
153329
Created by admin on Mon Mar 31 18:00:48 GMT 2025 , Edited by admin on Mon Mar 31 18:00:48 GMT 2025
PRIMARY RxNorm
EVMPD
SUB45873
Created by admin on Mon Mar 31 18:00:48 GMT 2025 , Edited by admin on Mon Mar 31 18:00:48 GMT 2025
PRIMARY
FDA UNII
042LAQ1IIS
Created by admin on Mon Mar 31 18:00:48 GMT 2025 , Edited by admin on Mon Mar 31 18:00:48 GMT 2025
PRIMARY
CHEBI
90881
Created by admin on Mon Mar 31 18:00:48 GMT 2025 , Edited by admin on Mon Mar 31 18:00:48 GMT 2025
PRIMARY
NCI_THESAURUS
C1381
Created by admin on Mon Mar 31 18:00:48 GMT 2025 , Edited by admin on Mon Mar 31 18:00:48 GMT 2025
PRIMARY
CAS
136572-09-3
Created by admin on Mon Mar 31 18:00:48 GMT 2025 , Edited by admin on Mon Mar 31 18:00:48 GMT 2025
PRIMARY
SMS_ID
100000131566
Created by admin on Mon Mar 31 18:00:48 GMT 2025 , Edited by admin on Mon Mar 31 18:00:48 GMT 2025
PRIMARY
RS_ITEM_NUM
1347609
Created by admin on Mon Mar 31 18:00:48 GMT 2025 , Edited by admin on Mon Mar 31 18:00:48 GMT 2025
PRIMARY
ChEMBL
CHEMBL481
Created by admin on Mon Mar 31 18:00:48 GMT 2025 , Edited by admin on Mon Mar 31 18:00:48 GMT 2025
PRIMARY
MERCK INDEX
m6405
Created by admin on Mon Mar 31 18:00:48 GMT 2025 , Edited by admin on Mon Mar 31 18:00:48 GMT 2025
PRIMARY Merck Index
DRUG BANK
DBSALT000103
Created by admin on Mon Mar 31 18:00:48 GMT 2025 , Edited by admin on Mon Mar 31 18:00:48 GMT 2025
PRIMARY
CHEBI
5971
Created by admin on Mon Mar 31 18:00:48 GMT 2025 , Edited by admin on Mon Mar 31 18:00:48 GMT 2025
PRIMARY
Related Record Type Details
ANHYDROUS->SOLVATE
PARENT -> SALT/SOLVATE
Related Record Type Details
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Related Record Type Details
ACTIVE MOIETY