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

Details

Stereochemistry ABSOLUTE
Molecular Formula C33H38N4O6.ClH.3H2O
Molecular Weight 677.186
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of IRINOTECAN HYDROCHLORIDE

SMILES

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

InChI

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

HIDE SMILES / InChI

Molecular Formula ClH
Molecular Weight 36.4609
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

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

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

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
Characterization of CPT-11 hydrolysis by human liver carboxylesterase isoforms hCE-1 and hCE-2.
2000 Mar 1
A dose-finding study of irinotecan (CPT-11) plus a four-day continuous 5-fluorouracil infusion in advanced 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
Lung cancer: therapeutic options for stage IV and recurrent NSCLC.
2001
Chemoradiation in locally advanced non-small cell lung cancer.
2001
Irinotecan plus fluorouracil/leucovorin for metastatic colorectal cancer: a new survival standard.
2001
Irinotecan: a new agent comes of age.
2001
Gemcitabine: progress in the treatment of pancreatic 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
A phase II trial of irinotecan (CPT-11) for unresectable biliary tree carcinoma.
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
Ternary combination of irinotecan, fluorouracil-folinic acid and oxaliplatin: results on human colon cancer cell lines.
2001 Feb
Combination chemotherapy in patients with malignant pleural effusions from non-small cell lung cancer : cisplatin, ifosfamide, and irinotecan with recombinant human granulocyte colony-stimulating factor support.
2001 Feb
New state of the art in small-cell lung cancer.
2001 Jan
Irinotecan in combined-modality therapy for locally advanced non-small-cell lung cancer.
2001 Jan
Rationale and dose-finding studies of the combination of irinotecan and a taxane on a weekly schedule.
2001 Jan
Treatment of non-small-cell lung cancer in North America: the emerging role of irinotecan.
2001 Jan
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
Oral fluoropyrimidine-based combination therapy in gastrointestinal cancer.
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
Characterization of a novel mechanism accounting for the adverse cholinergic effects of the anticancer drug irinotecan.
2001 Jan
A phase II study of irinotecan in patients with advanced hepatocellular carcinoma.
2001 Jan 1
Glucagon-like peptide (GLP)-2 reduces chemotherapy-associated mortality and enhances cell survival in cells expressing a transfected GLP-2 receptor.
2001 Jan 15
Irinotecan plus fluorouracil and leucovorin for metastatic colorectal cancer.
2001 Jan 25
The changing face of chemotherapy in colorectal cancer.
2001 Jan 5
[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
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
Determinants of prognosis and response to therapy in colorectal cancer.
2001 Mar
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
Impact on survival following successful neoadjuvant chemotherapy and radical surgery for Stage IIb bulky and Stage IIIb cervical cancer.
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
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 21:02:56 UTC 2021
Edited
by admin
on Fri Jun 25 21:02:56 UTC 2021
Record UNII
042LAQ1IIS
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
IRINOTECAN HYDROCHLORIDE
MART.   ORANGE BOOK   USAN   USP   USP-RS   VANDF  
USAN  
Official Name English
IRINOTECAN HYDROCHLORIDE [MART.]
Common Name English
ONIVYDE
Brand Name English
U-101,440E
Code English
IRINOTECAN HYDROCHLORIDE [ORANGE BOOK]
Common Name English
IRINOTECAN HYDROCHLORIDE TRIHYDRATE [EP MONOGRAPH]
Common Name English
IRINOTECAN HYDROCHLORIDE [USP-RS]
Common Name English
IRINOTECAN HYDROCHLORIDE [USP MONOGRAPH]
Common Name English
IRINOTECAN HYDROCHLORIDE HYDRATE
JAN  
Common Name English
NSC-759878
Code English
XELIRI COMPONENT IRINOTECAN HYDROCHLORIDE
Common Name English
IRINOTECAN HYDROCHLORIDE [USAN]
Common Name English
(1,4'-BIPIPERIDINE)-1'-CARBOXYLIC ACID, 4,11-DIETHYL-3,4,12,14-TETRAHYDRO-4-HYDROXY-3,14-DIOXO-1H-PYRANO(3',4':6,7)INDOLIZINO(1,2-B)QUINOLIN-9-YL ESTER, MONOHYDROCHLORIDE, TRIHYDRATE, (S)-
Common Name English
CPT-11
Code English
CAMPTO
Brand Name English
IRINOTECAN HYDROCHLORIDE TRIHYDRATE
MI  
Common Name English
IRINOTECAN MONOHYDROCHLORIDE TRIHYDRATE [WHO-DD]
Common Name English
(+)-7-ETHYL-10-HYDROXYCAMPTOTHECINE 10-(1,4'-BIPIPERIDINE)-1'-CARBOXYLATE, MONOHYDROCHLORIDE, TRIHYDRATE
Common Name English
IRINOTECAN HYDROCHLORIDE TRIHYDRATE [EMA EPAR]
Common Name English
DQ-2805
Code English
IRINOTECAN HYDROCHLORIDE TRIHYDRATE [MI]
Common Name English
IRINOTECAN HYDROCHLORIDE HYDRATE [JAN]
Common Name English
CAMPTOSAR
Brand Name English
IRINOTECAN HYDROCHLORIDE [VANDF]
Common Name English
IRINOTECAN MONOHYDROCHLORIDE TRIHYDRATE
WHO-DD  
Common Name English
U-101440E
Code English
Classification Tree Code System Code
EU-Orphan Drug EU/3/11/933
Created by admin on Fri Jun 25 21:02:56 UTC 2021 , Edited by admin on Fri Jun 25 21:02:56 UTC 2021
EMA ASSESSMENT REPORTS ONIVYDE (AUTHORIZED: PANCREATIC NEOPLASMS):
Created by admin on Fri Jun 25 21:02:56 UTC 2021 , Edited by admin on Fri Jun 25 21:02:56 UTC 2021
NCI_THESAURUS C2843
Created by admin on Fri Jun 25 21:02:56 UTC 2021 , Edited by admin on Fri Jun 25 21:02:56 UTC 2021
Code System Code Type Description
PUBCHEM
60837
Created by admin on Fri Jun 25 21:02:56 UTC 2021 , Edited by admin on Fri Jun 25 21:02:56 UTC 2021
PRIMARY
EVMPD
SUB02772MIG
Created by admin on Fri Jun 25 21:02:56 UTC 2021 , Edited by admin on Fri Jun 25 21:02:56 UTC 2021
PRIMARY
RXCUI
153329
Created by admin on Fri Jun 25 21:02:56 UTC 2021 , Edited by admin on Fri Jun 25 21:02:56 UTC 2021
PRIMARY RxNorm
EVMPD
SUB45873
Created by admin on Fri Jun 25 21:02:56 UTC 2021 , Edited by admin on Fri Jun 25 21:02:56 UTC 2021
PRIMARY
USP_CATALOG
1347609
Created by admin on Fri Jun 25 21:02:56 UTC 2021 , Edited by admin on Fri Jun 25 21:02:56 UTC 2021
PRIMARY USP-RS
FDA UNII
042LAQ1IIS
Created by admin on Fri Jun 25 21:02:56 UTC 2021 , Edited by admin on Fri Jun 25 21:02:56 UTC 2021
PRIMARY
NCI_THESAURUS
C1381
Created by admin on Fri Jun 25 21:02:56 UTC 2021 , Edited by admin on Fri Jun 25 21:02:56 UTC 2021
PRIMARY
CAS
136572-09-3
Created by admin on Fri Jun 25 21:02:56 UTC 2021 , Edited by admin on Fri Jun 25 21:02:56 UTC 2021
PRIMARY
ChEMBL
CHEMBL481
Created by admin on Fri Jun 25 21:02:56 UTC 2021 , Edited by admin on Fri Jun 25 21:02:56 UTC 2021
PRIMARY
MERCK INDEX
M6405
Created by admin on Fri Jun 25 21:02:56 UTC 2021 , Edited by admin on Fri Jun 25 21:02:56 UTC 2021
PRIMARY Merck Index
DRUG BANK
DBSALT000103
Created by admin on Fri Jun 25 21:02:56 UTC 2021 , Edited by admin on Fri Jun 25 21:02:56 UTC 2021
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE
Related Record Type Details
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Related Record Type Details
ACTIVE MOIETY