U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C33H38N4O6
Molecular Weight 586.678
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of IRINOTECAN

SMILES

CCC1=C2C=C(OC(=O)N3CCC(CC3)N4CCCCC4)C=CC2=NC5=C1CN6C5=CC7=C(COC(=O)[C@]7(O)CC)C6=O

InChI

InChIKey=UWKQSNNFCGGAFS-XIFFEERXSA-N
InChI=1S/C33H38N4O6/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/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

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
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
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
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
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
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
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
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
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
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
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
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
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
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
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
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
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
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
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
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
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
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
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
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
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
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
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
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
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
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
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
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
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
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
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
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
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
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
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
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
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
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
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
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
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
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
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
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
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
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
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
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
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
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
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
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
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
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
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
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
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
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
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
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
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
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
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
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
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
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
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
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
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
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
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
Sources:
PubMed

PubMed

TitleDatePubMed
Comparison of in vitro activities of camptothecin and nitidine derivatives against fungal and cancer cells.
1999 Dec
Characterization of CPT-11 hydrolysis by human liver carboxylesterase isoforms hCE-1 and hCE-2.
2000 Mar 1
Management of chemotherapy-induced adverse effects in the treatment of colorectal cancer.
2001
Irinotecan and mitomycin C in 5-fluorouracil-refractory colorectal cancer patients. A phase I/II study of the Southern Italy Cooperative Oncology Group.
2001
Treatment of extensive stage small cell lung cancer.
2001
Lung cancer: therapeutic options for stage IV and recurrent NSCLC.
2001
Chemoradiation in locally advanced non-small cell lung cancer.
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
A phase II trial of irinotecan (CPT-11) for unresectable biliary tree carcinoma.
2001 Apr
26S proteasome inhibition induces apoptosis and limits growth of human pancreatic cancer.
2001 Apr 2-27
[Medical treatment of pulmonary neoplasms].
2001 Feb
[Weekly low dose CPT-11 for multiple lung metastases of colon cancer on an out-patient treatment: a case report].
2001 Feb
Prospective phase II trial of iriontecan, 5-fluorouracil, and leucovorin in combination as salvage therapy for advanced colorectal cancer.
2001 Feb
Irinotecan and chronomodulated infusion of 5-fluorouracil and folinic acid in the treatment of patients with advanced colorectal carcinoma: a phase I study.
2001 Feb 15
Phase II study of irinotecan as first-line chemotherapy for patients with advanced colorectal carcinoma.
2001 Feb 15
Irinotecan: summary and future directions.
2001 Jan
Establishment of the standard regimen for non-small-cell lung cancer in Japan.
2001 Jan
Irinotecan in small-cell lung cancer: the US experience.
2001 Jan
A phase I study of irinotecan in pediatric patients: a pediatric oncology group study.
2001 Jan
Overexpression of the ATP-binding cassette half-transporter, ABCG2 (Mxr/BCrp/ABCP1), in flavopiridol-resistant human breast cancer cells.
2001 Jan
[A case of small cell carcinoma of esophagus successfully treated by chemotherapy with CPT-11 and CDDP].
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
Irinotecan plus fluorouracil and leucovorin for metastatic colorectal cancer.
2001 Jan 25
Repression of cyclin B1 expression after treatment with adriamycin, but not cisplatin in human lung cancer A549 cells.
2001 Jan 26
The changing face of chemotherapy in colorectal cancer.
2001 Jan 5
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
Topoisomerase I-DNA covalent complexes in human colorectal cancer xenografts with different p53 and microsatellite instability status: relation with their sensitivity to CTP-11.
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
Active transepithelial transport of irinotecan (CPT-11) and its metabolites by human intestinal Caco-2 cells.
2001 Jun
Hepatic extraction, metabolism, and biliary excretion of irinotecan in the isolated perfused rat liver.
2001 Jun
Irinotecan plus cisplatin in advanced gastric or gastroesophageal junction carcinoma.
2001 Mar
Irinotecan/gemcitabine combination chemotherapy in pancreatic cancer.
2001 Mar
Cisplatin and irinotecan in upper gastrointestinal malignancies.
2001 Mar
Irinotecan in the treatment of colorectal cancer: clinical overview.
2001 Mar 1
Roles of NF-kappaB and 26 S proteasome in apoptotic cell death induced by topoisomerase I and II poisons in human nonsmall cell lung carcinoma.
2001 Mar 16
Preliminary study of fortnightly irinotecan hydrochloride plus cisplatin therapy in patients with advanced gastric and colorectal cancer.
2001 May
[A modified administrated schedule for combination therapy with irinotecan and cisplatin as a neoadjuvant chemotherapy in locally advanced cervical cancer--a report of 2 cases as a pilot study].
2001 May
[Platinum compounds in cancer therapy--past, present, and future].
2001 May
CPT-11 alters the circadian rhythm of dihydropyrimidine dehydrogenase mRNA in mouse liver.
2001 May
Modulation of irinotecan-induced diarrhea by cotreatment with neomycin in cancer patients.
2001 May
Phase I study of hepatic arterial infusion of floxuridine and dexamethasone with systemic irinotecan for unresectable hepatic metastases from colorectal cancer.
2001 May 15
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 Fri Dec 15 15:58:53 GMT 2023
Edited
by admin
on Fri Dec 15 15:58:53 GMT 2023
Record UNII
7673326042
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
IRINOTECAN
HSDB   INN   MI   VANDF   WHO-DD  
INN  
Official Name English
NSC-728073
Code English
irinotecan [INN]
Common Name English
IRINOTECAN [VANDF]
Common Name English
BIOTECAN
Brand Name English
Irinotecan [WHO-DD]
Common Name English
IRINOTECAN [HSDB]
Common Name English
IRINOTECAN [MI]
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 344311
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
WHO-VATC QL01XX19
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
LIVERTOX NBK548037
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
NDF-RT N0000000176
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
NDF-RT N0000175609
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
NCI_THESAURUS C2843
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
WHO-ATC L01XX19
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
FDA ORPHAN DRUG 567516
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
Code System Code Type Description
EPA CompTox
DTXSID1041051
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
PRIMARY
DRUG CENTRAL
1482
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
PRIMARY
ChEMBL
CHEMBL481
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
PRIMARY
IUPHAR
6823
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
PRIMARY
INN
6694
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
PRIMARY
DAILYMED
7673326042
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
PRIMARY
LACTMED
Irinotecan
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
PRIMARY
EVMPD
SUB08295MIG
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
PRIMARY
HSDB
7607
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
PRIMARY
MESH
C051890
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
PRIMARY
NSC
728073
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
PRIMARY
DRUG BANK
DB00762
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
PRIMARY
WIKIPEDIA
IRINOTECAN
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
PRIMARY
CAS
97682-44-5
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
PRIMARY
PUBCHEM
60838
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
PRIMARY
RXCUI
51499
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
PRIMARY RxNorm
FDA UNII
7673326042
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
PRIMARY
NCI_THESAURUS
C62040
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
PRIMARY
SMS_ID
100000083374
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
PRIMARY
CHEBI
80630
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
PRIMARY
MERCK INDEX
m6405
Created by admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
PRIMARY Merck Index
Related Record Type Details
TARGET -> INHIBITOR
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
CES1A1
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
CES2 is 64 times more efficient in metabolizing CPT-11 than CES1A1 (Humerickhouse et al., 2000).
MAJOR
BINDER->LIGAND
BINDING
TRANSPORTER -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
SALT/SOLVATE -> PARENT
METABOLIC ENZYME -> SUBSTRATE
)No tumor reduction in SQ20b cells was seen after incubation of CPT-11 with hCE-1, compared with a 60% reduction for hCE-2 .
SALT/SOLVATE -> PARENT
Related Record Type Details
METABOLITE INACTIVE -> PARENT
MAJOR
URINE
METABOLITE INACTIVE -> PARENT
METABOLITE ACTIVE -> PRODRUG
METABOLITE INACTIVE -> PARENT
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC Children and Adolescent
PHARMACOKINETIC
ADULT
PHARMACOKINETIC
Route of Elimination PHARMACOKINETIC URINE
PHARMACOKINETIC