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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

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

8.3471041E11
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
A dose-finding study of irinotecan (CPT-11) plus a four-day continuous 5-fluorouracil infusion in advanced 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
[Irinotecan (CPT-11) therapy for advanced gastric cancer].
2001 Apr
Safe administration of irinotecan, oxaliplatin and raltitrexed in a DPD-deficient patient with metastatic colon cancer.
2001 Apr
The role of irinotecan and oxaliplatin in the treatment of advanced colorectal 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
[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
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
The current status of docetaxel for advanced non-small cell lung cancer.
2001 Feb
[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
Effect of bile acids on the uptake of irinotecan and its active metabolite, SN-38, by intestinal cells.
2001 Feb 16
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
[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
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
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 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