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

Details

Stereochemistry ABSOLUTE
Molecular Formula 4C33H38N4O6.C12H22O35S8
Molecular Weight 3329.514
Optical Activity UNSPECIFIED
Defined Stereocenters 13 / 13
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of IRINOTECAN SUCROSOFATE

SMILES

CCC1=C2C=C(OC(=O)N3CCC(CC3)N4CCCCC4)C=CC2=NC5=C1CN6C5=CC7=C(COC(=O)[C@]7(O)CC)C6=O.CCC8=C9C=C(OC(=O)N%10CCC(CC%10)N%11CCCCC%11)C=CC9=NC%12=C8CN%13C%12=CC%14=C(COC(=O)[C@]%14(O)CC)C%13=O.CCC%15=C%16C=C(OC(=O)N%17CCC(CC%17)N%18CCCCC%18)C=CC%16=NC%19=C%15CN%20C%19=CC%21=C(COC(=O)[C@]%21(O)CC)C%20=O.CCC%22=C%23C=C(OC(=O)N%24CCC(CC%24)N%25CCCCC%25)C=CC%23=NC%26=C%22CN%27C%26=CC%28=C(COC(=O)[C@]%28(O)CC)C%27=O.OS(=O)(=O)OC[C@H]%29O[C@@](COS(O)(=O)=O)(O[C@H]%30O[C@H](COS(O)(=O)=O)[C@@H](OS(O)(=O)=O)[C@H](OS(O)(=O)=O)[C@H]%30OS(O)(=O)=O)[C@@H](OS(O)(=O)=O)[C@@H]%29OS(O)(=O)=O

InChI

InChIKey=BCPSLKYBXGKPIW-RTXWKGGWSA-N
InChI=1S/4C33H38N4O6.C12H22O35S8/c4*1-3-22-23-16-21(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;13-48(14,15)37-1-4-6(43-51(22,23)24)8(45-53(28,29)30)9(46-54(31,32)33)11(40-4)42-12(3-39-50(19,20)21)10(47-55(34,35)36)7(44-52(25,26)27)5(41-12)2-38-49(16,17)18/h4*8-9,16-17,20,41H,3-7,10-15,18-19H2,1-2H3;4-11H,1-3H2,(H,13,14,15)(H,16,17,18)(H,19,20,21)(H,22,23,24)(H,25,26,27)(H,28,29,30)(H,31,32,33)(H,34,35,36)/t4*33-;4-,5-,6-,7-,8+,9-,10+,11-,12+/m00001/s1

HIDE SMILES / InChI

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

Molecular Formula C12H22O35S8
Molecular Weight 982.802
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 9 / 9
E/Z Centers 0
Optical Activity UNSPECIFIED

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

CNS Activity

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

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
CAMPTOSAR

Approved Use

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

Launch Date

1996
Cmax

Cmax

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

AUC

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

T1/2

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

Funbound

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

Doses

DosePopulationAdverse events​
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
Sources:
Other AEs: Fatigue, Weight loss...
Other AEs:
Fatigue (grade 1-2, 33.3%)
Weight loss (grade 1-2, 33.3%)
Diarrhea (grade 1-2, 50%)
Nausea (grade 1-2, 58.3%)
Vomiting (grade 1-2, 50%)
Cholinergic syndrome (grade 1-2, 33.3%)
Mucositis (grade 1-2, 33.3%)
Dyspnea (grade 1-2, 8.3%)
Fever (grade 1-2, 8.3%)
Fatigue (grade 3, 8.3%)
Diarrhea (grade 3, 8.3%)
Nausea (grade 3, 8.3%)
Vomiting (grade 3, 8.3%)
Cholinergic syndrome (grade 3, 33.3%)
Sources:
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
Sources:
Other AEs: Leukopenia, Leukopenia...
Other AEs:
Leukopenia (grade 2, 1 patient)
Leukopenia (grade 3, 2 patients)
Leukopenia (grade 4, 1 patient)
Neutropenia (grade 2, 2 patients)
Neutropenia (grade 3, 2 patients)
Neutropenia (grade 4, 1 patient)
Nausea (grade 1, 4 patients)
Nausea (grade 3, 1 patient)
Vomiting (grade 4, 1 patient)
Diarrhea (grade 1, 2 patients)
Diarrhea (grade 2, 3 patients)
Diarrhea (grade 4, 1 patient)
Anorexia (grade 1, 3 patients)
Anorexia (grade 2, 2 patients)
Sources:
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
Sources:
Other AEs: Leukopenia, Leukopenia...
Other AEs:
Leukopenia (grade 1, 4 patients)
Leukopenia (grade 2, 1 patient)
Leukopenia (grade 3, 2 patients)
Neutropenia (grade 1, 2 patients)
Neutropenia (grade 2, 2 patients)
Neutropenia (grade 4, 2 patients)
Thrombocytopenia (grade 1, 2 patients)
Nausea (grade 1, 3 patients)
Nausea (grade 2, 3 patients)
Nausea (grade 3, 2 patients)
Vomiting (grade 1, 2 patients)
Vomiting (grade 2, 2 patients)
Vomiting (grade 3, 1 patient)
Vomiting (grade 4, 1 patient)
Diarrhea (grade 1, 3 patients)
Diarrhea (grade 2, 2 patients)
Diarrhea (grade 3, 1 patient)
Diarrhea (grade 4, 1 patient)
Anorexia (grade 1, 3 patients)
Anorexia (grade 2, 2 patients)
Sources:
AEs

AEs

AESignificanceDosePopulation
Cholinergic syndrome grade 1-2, 33.3%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
Sources:
Fatigue grade 1-2, 33.3%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
Sources:
Mucositis grade 1-2, 33.3%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
Sources:
Weight loss grade 1-2, 33.3%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
Sources:
Diarrhea grade 1-2, 50%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
Sources:
Vomiting grade 1-2, 50%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
Sources:
Nausea grade 1-2, 58.3%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
Sources:
Dyspnea grade 1-2, 8.3%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
Sources:
Fever grade 1-2, 8.3%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
Sources:
Cholinergic syndrome grade 3, 33.3%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
Sources:
Diarrhea grade 3, 8.3%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
Sources:
Fatigue grade 3, 8.3%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
Sources:
Nausea grade 3, 8.3%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
Sources:
Vomiting grade 3, 8.3%
21 mg/m2 1 times / day multiple, oral
MTD
Dose: 21 mg/m2, 1 times / day
Route: oral
Route: multiple
Dose: 21 mg/m2, 1 times / day
Sources:
unhealthy, adult
n = 12
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 12
Sources:
Diarrhea grade 1, 2 patients
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
Sources:
Anorexia grade 1, 3 patients
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
Sources:
Nausea grade 1, 4 patients
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
Sources:
Leukopenia grade 2, 1 patient
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
Sources:
Anorexia grade 2, 2 patients
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
Sources:
Neutropenia grade 2, 2 patients
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
Sources:
Diarrhea grade 2, 3 patients
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
Sources:
Nausea grade 3, 1 patient
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
Sources:
Leukopenia grade 3, 2 patients
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
Sources:
Neutropenia grade 3, 2 patients
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
Sources:
Diarrhea grade 4, 1 patient
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
Sources:
Leukopenia grade 4, 1 patient
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
Sources:
Neutropenia grade 4, 1 patient
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
Sources:
Vomiting grade 4, 1 patient
290 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 290 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 290 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 7
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 7
Sources:
Neutropenia grade 1, 2 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
Sources:
Thrombocytopenia grade 1, 2 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
Sources:
Vomiting grade 1, 2 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
Sources:
Anorexia grade 1, 3 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
Sources:
Diarrhea grade 1, 3 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
Sources:
Nausea grade 1, 3 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
Sources:
Leukopenia grade 1, 4 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
Sources:
Leukopenia grade 2, 1 patient
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
Sources:
Anorexia grade 2, 2 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
Sources:
Diarrhea grade 2, 2 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
Sources:
Neutropenia grade 2, 2 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
Sources:
Vomiting grade 2, 2 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
Sources:
Nausea grade 2, 3 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
Sources:
Diarrhea grade 3, 1 patient
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
Sources:
Vomiting grade 3, 1 patient
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
Sources:
Leukopenia grade 3, 2 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
Sources:
Nausea grade 3, 2 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
Sources:
Diarrhea grade 4, 1 patient
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
Sources:
Vomiting grade 4, 1 patient
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
Sources:
Neutropenia grade 4, 2 patients
320 mg/m2 1 times / 3 weeks multiple, intravenous
MTD
Dose: 320 mg/m2, 1 times / 3 weeks
Route: intravenous
Route: multiple
Dose: 320 mg/m2, 1 times / 3 weeks
Sources:
unhealthy, adult
n = 8
Health Status: unhealthy
Condition: solid tumors
Age Group: adult
Sex: M+F
Population Size: 8
Sources:
PubMed

PubMed

TitleDatePubMed
Management of chemotherapy-induced adverse effects in the treatment of colorectal cancer.
2001
Irinotecan and mitomycin C in 5-fluorouracil-refractory colorectal cancer patients. A phase I/II study of the Southern Italy Cooperative Oncology Group.
2001
Treatment of extensive stage small cell lung cancer.
2001
Irinotecan (CPT-11): recent developments and future directions--colorectal cancer and beyond.
2001
Gemcitabine: progress in the treatment of pancreatic cancer.
2001
[Irinotecan (CPT-11) therapy for advanced 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
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
North Central Cancer Treatment Group--Mayo Clinic trials in 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
Breast cancer resistance protein directly confers SN-38 resistance of lung cancer cells.
2001 Feb 9
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
A phase I study of irinotecan in pediatric patients: a pediatric oncology group study.
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
The changing face of chemotherapy in colorectal cancer.
2001 Jan 5
Perioperative radiotherapy and concurrent radiochemotherapy in rectal cancer.
2001 Jan-Feb
[Refinement and role of the diagnosis of Gilbert disease with molecular biology].
2001 Jan-Feb
Irinotecan plus cisplatin in advanced gastric or gastroesophageal junction carcinoma.
2001 Mar
Cisplatin and irinotecan in upper gastrointestinal malignancies.
2001 Mar
Optimizing chemoradiation therapy approaches to unresectable stage III non--small cell lung cancer.
2001 Mar
Oxaliplatin: a new agent for colorectal 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
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
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 Sat Dec 16 09:58:34 GMT 2023
Edited
by admin
on Sat Dec 16 09:58:34 GMT 2023
Record UNII
OL741S3N8B
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
IRINOTECAN SUCROSOFATE
USAN   WHO-DD  
USAN  
Official Name English
IRINOTECAN SUCROSOFATE [USAN]
Common Name English
MM-398
Code English
Irinotecan sucrosofate [WHO-DD]
Common Name English
PEP-02
Code English
SULFATE OF SUCROSE (ESTER) AND OF IRINOTECAN (SALT): SUCROSE OCTAKIS(HYDROGEN SULFATE) SALT WITH (4S)-4,11-DIETHYL-4-HYDROXY-3,14-DIOXO-3,4,12,14-TETRAHYDRO-1H-PYRANO(3',4':6,7)INDOLIZINO(1,2-B)QUINOLIN-9-YL (1,4'-BIPIPERIDINE)-1'-CARBOXYLATE
Systematic Name English
Code System Code Type Description
SMS_ID
100000175102
Created by admin on Sat Dec 16 09:58:34 GMT 2023 , Edited by admin on Sat Dec 16 09:58:34 GMT 2023
PRIMARY
PUBCHEM
76964235
Created by admin on Sat Dec 16 09:58:34 GMT 2023 , Edited by admin on Sat Dec 16 09:58:34 GMT 2023
PRIMARY
ChEMBL
CHEMBL3039564
Created by admin on Sat Dec 16 09:58:34 GMT 2023 , Edited by admin on Sat Dec 16 09:58:34 GMT 2023
PRIMARY
NCI_THESAURUS
C82676
Created by admin on Sat Dec 16 09:58:34 GMT 2023 , Edited by admin on Sat Dec 16 09:58:34 GMT 2023
PRIMARY
INN
11847
Created by admin on Sat Dec 16 09:58:34 GMT 2023 , Edited by admin on Sat Dec 16 09:58:34 GMT 2023
PRIMARY
CAS
1361317-83-0
Created by admin on Sat Dec 16 09:58:34 GMT 2023 , Edited by admin on Sat Dec 16 09:58:34 GMT 2023
NON-SPECIFIC STOICHIOMETRY
DRUG BANK
DBSALT002617
Created by admin on Sat Dec 16 09:58:34 GMT 2023 , Edited by admin on Sat Dec 16 09:58:34 GMT 2023
PRIMARY
FDA UNII
OL741S3N8B
Created by admin on Sat Dec 16 09:58:34 GMT 2023 , Edited by admin on Sat Dec 16 09:58:34 GMT 2023
PRIMARY
USAN
AB-66
Created by admin on Sat Dec 16 09:58:34 GMT 2023 , Edited by admin on Sat Dec 16 09:58:34 GMT 2023
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE
Related Record Type Details
ACTIVE MOIETY