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
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
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18784279
Curator's Comment: Irinotecan crosses the blood-brain barrier
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | CAMPTOSAR Approved UseCAMPTOSAR 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 Date1996 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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
Dose | Population | Adverse 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%) Sources: 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%) |
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) Sources: 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) |
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) Sources: 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) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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
Title | Date | PubMed |
---|---|---|
Camptothecin resistance: role of the ATP-binding cassette (ABC), mitoxantrone-resistance half-transporter (MXR), and potential for glucuronidation in MXR-expressing cells. | 1999 Dec 1 |
|
Factors affecting the pharmacokinetics of CPT-11: the body mass index, age and sex are independent predictors of pharmacokinetic parameters of CPT-11. | 2001 |
|
Treatment of extensive stage small cell lung cancer. | 2001 |
|
Gemcitabine: progress in the treatment of pancreatic cancer. | 2001 |
|
[Chemotherapy of irinotecan (CPT-11) combined with cisplatin in patients with advanced gastric cancer]. | 2001 Apr |
|
Antitumor activity of XR5944, a novel and potent topoisomerase poison. | 2001 Apr |
|
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 |
|
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 |
|
Effect of bile acids on the uptake of irinotecan and its active metabolite, SN-38, by intestinal cells. | 2001 Feb 16 |
|
Breast cancer resistance protein directly confers SN-38 resistance of lung cancer cells. | 2001 Feb 9 |
|
Irinotecan: summary and future directions. | 2001 Jan |
|
Establishment of the standard regimen for non-small-cell lung cancer in Japan. | 2001 Jan |
|
Oral fluoropyrimidine-based combination therapy in gastrointestinal cancer. | 2001 Jan |
|
In vitro synergistic interactions between the cisplatin analogue nedaplatin and the DNA topoisomerase I inhibitor irinotecan and the mechanism of this interaction. | 2001 Jan |
|
Overexpression of the ATP-binding cassette half-transporter, ABCG2 (Mxr/BCrp/ABCP1), in flavopiridol-resistant human breast cancer cells. | 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 cisplatin in advanced gastric or gastroesophageal junction carcinoma. | 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 |
|
Determinants of prognosis and response to therapy in colorectal cancer. | 2001 Mar |
|
[Chemotherapy of colonic carcinoma in the year 2001]. | 2001 Mar 22 |
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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 |
|
Advances in chemotherapy for small cell lung cancer: single-agent activity of newer agents. | 2001 May-Jun |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.drugs.com/dosage/irinotecan.html
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9033637
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.
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ACTIVE MOIETY
SUBSTANCE RECORD