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

Details

Stereochemistry ABSOLUTE
Molecular Formula C33H38N4O6
Molecular Weight 586.6793
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of IRINOTECAN

SMILES

CCc1c2cc(ccc2nc-3c1Cn4c3cc5c(COC(=O)[C@@]5(CC)O)c4=O)OC(=O)N6CCC(CC6)N7CCCCC7

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 586.6793
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

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

834710400000
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
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
Factors affecting the pharmacokinetics of CPT-11: the body mass index, age and sex are independent predictors of pharmacokinetic parameters of CPT-11.
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
The role of irinotecan and oxaliplatin in the treatment of advanced colorectal cancer.
2001 Apr
[Chemotherapy by combination of low-dose CPT-11 and PSK in an elderly man with liver metastasis from gastric cancer].
2001 Apr
Pharmacogenetics of anticancer agents: lessons from amonafide and irinotecan.
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
Prevention of irinotecan (CPT-11)-induced diarrhea by oral alkalization combined with control of defecation in cancer patients.
2001 Apr 15
26S proteasome inhibition induces apoptosis and limits growth of human pancreatic cancer.
2001 Apr 2-27
[Medical treatment of pulmonary neoplasms].
2001 Feb
North Central Cancer Treatment Group--Mayo Clinic trials in colon cancer.
2001 Feb
Modulation of camptothecin analogs in the treatment of cancer: a review.
2001 Feb
Adjuvant therapy of colon cancer.
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
New state of the art in small-cell lung cancer.
2001 Jan
Current status of irinotecan in lung cancer.
2001 Jan
Irinotecan: summary and future directions.
2001 Jan
Docetaxel followed by gemcitabine and irinotecan in solid tumors.
2001 Jan
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
Perioperative radiotherapy and concurrent radiochemotherapy in rectal cancer.
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
Irinotecan/gemcitabine combination chemotherapy in pancreatic cancer.
2001 Mar
Cisplatin and irinotecan in upper gastrointestinal malignancies.
2001 Mar
[A case of AFP-producing gastric cancer responding to low-dose CPT-11 and low-dose cisplatin combination chemotherapy].
2001 Mar
Optimizing chemoradiation therapy approaches to unresectable stage III non--small cell lung cancer.
2001 Mar
Irinotecan in the treatment of colorectal cancer: clinical overview.
2001 Mar 1
[Chemotherapy of colonic carcinoma in the year 2001].
2001 Mar 22
[Platinum compounds in cancer therapy--past, present, and future].
2001 May
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
Potentiation of antitumor activity of irinotecan by chemically modified oligonucleotides.
2001 May
Enhanced chemosensitivity to CPT-11 with proteasome inhibitor PS-341: implications for systemic nuclear factor-kappaB inhibition.
2001 May 1
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
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 Jun 25 22:01:44 UTC 2021
Edited
by admin
on Fri Jun 25 22:01:44 UTC 2021
Record UNII
7673326042
Record Status Validated (UNII)
Record Version
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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 Jun 25 22:01:44 UTC 2021 , Edited by admin on Fri Jun 25 22:01:44 UTC 2021
WHO-VATC QL01XX19
Created by admin on Fri Jun 25 22:01:44 UTC 2021 , Edited by admin on Fri Jun 25 22:01:44 UTC 2021
LIVERTOX 516
Created by admin on Fri Jun 25 22:01:44 UTC 2021 , Edited by admin on Fri Jun 25 22:01:44 UTC 2021
NDF-RT N0000000176
Created by admin on Fri Jun 25 22:01:44 UTC 2021 , Edited by admin on Fri Jun 25 22:01:44 UTC 2021
NDF-RT N0000175609
Created by admin on Fri Jun 25 22:01:44 UTC 2021 , Edited by admin on Fri Jun 25 22:01:44 UTC 2021
NCI_THESAURUS C2843
Created by admin on Fri Jun 25 22:01:44 UTC 2021 , Edited by admin on Fri Jun 25 22:01:44 UTC 2021
WHO-ATC L01XX19
Created by admin on Fri Jun 25 22:01:44 UTC 2021 , Edited by admin on Fri Jun 25 22:01:44 UTC 2021
FDA ORPHAN DRUG 567516
Created by admin on Fri Jun 25 22:01:44 UTC 2021 , Edited by admin on Fri Jun 25 22:01:44 UTC 2021
Code System Code Type Description
EPA CompTox
97682-44-5
Created by admin on Fri Jun 25 22:01:44 UTC 2021 , Edited by admin on Fri Jun 25 22:01:44 UTC 2021
PRIMARY
DRUG CENTRAL
1482
Created by admin on Fri Jun 25 22:01:44 UTC 2021 , Edited by admin on Fri Jun 25 22:01:44 UTC 2021
PRIMARY
ChEMBL
CHEMBL481
Created by admin on Fri Jun 25 22:01:44 UTC 2021 , Edited by admin on Fri Jun 25 22:01:44 UTC 2021
PRIMARY
IUPHAR
6823
Created by admin on Fri Jun 25 22:01:44 UTC 2021 , Edited by admin on Fri Jun 25 22:01:44 UTC 2021
PRIMARY
INN
6694
Created by admin on Fri Jun 25 22:01:44 UTC 2021 , Edited by admin on Fri Jun 25 22:01:44 UTC 2021
PRIMARY
LACTMED
Irinotecan
Created by admin on Fri Jun 25 22:01:44 UTC 2021 , Edited by admin on Fri Jun 25 22:01:44 UTC 2021
PRIMARY
EVMPD
SUB08295MIG
Created by admin on Fri Jun 25 22:01:44 UTC 2021 , Edited by admin on Fri Jun 25 22:01:44 UTC 2021
PRIMARY
HSDB
7607
Created by admin on Fri Jun 25 22:01:44 UTC 2021 , Edited by admin on Fri Jun 25 22:01:44 UTC 2021
PRIMARY
MESH
C051890
Created by admin on Fri Jun 25 22:01:44 UTC 2021 , Edited by admin on Fri Jun 25 22:01:44 UTC 2021
PRIMARY
DRUG BANK
DB00762
Created by admin on Fri Jun 25 22:01:44 UTC 2021 , Edited by admin on Fri Jun 25 22:01:44 UTC 2021
PRIMARY
WIKIPEDIA
IRINOTECAN
Created by admin on Fri Jun 25 22:01:44 UTC 2021 , Edited by admin on Fri Jun 25 22:01:44 UTC 2021
PRIMARY
CAS
97682-44-5
Created by admin on Fri Jun 25 22:01:44 UTC 2021 , Edited by admin on Fri Jun 25 22:01:44 UTC 2021
PRIMARY
PUBCHEM
60838
Created by admin on Fri Jun 25 22:01:44 UTC 2021 , Edited by admin on Fri Jun 25 22:01:44 UTC 2021
PRIMARY
RXCUI
51499
Created by admin on Fri Jun 25 22:01:44 UTC 2021 , Edited by admin on Fri Jun 25 22:01:44 UTC 2021
PRIMARY RxNorm
FDA UNII
7673326042
Created by admin on Fri Jun 25 22:01:44 UTC 2021 , Edited by admin on Fri Jun 25 22:01:44 UTC 2021
PRIMARY
NCI_THESAURUS
C62040
Created by admin on Fri Jun 25 22:01:44 UTC 2021 , Edited by admin on Fri Jun 25 22:01:44 UTC 2021
PRIMARY
MERCK INDEX
M6405
Created by admin on Fri Jun 25 22:01:44 UTC 2021 , Edited by admin on Fri Jun 25 22:01:44 UTC 2021
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
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
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