Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C33H38N4O6 |
Molecular Weight | 586.678 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
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
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
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 |
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 |
---|---|---|
Management of chemotherapy-induced adverse effects in the treatment of colorectal cancer. | 2001 |
|
A dose-finding study of irinotecan (CPT-11) plus a four-day continuous 5-fluorouracil infusion in advanced colorectal cancer. | 2001 |
|
Chemoradiation in locally advanced non-small cell lung cancer. | 2001 |
|
Prevention of irinotecan (CPT-11)-induced diarrhea by oral alkalization combined with control of defecation in cancer patients. | 2001 Apr 15 |
|
The current status of docetaxel for advanced non-small cell lung cancer. | 2001 Feb |
|
Modulation of camptothecin analogs in the treatment of cancer: a review. | 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 |
|
Treatment of non-small-cell lung cancer in North America: the emerging role of irinotecan. | 2001 Jan |
|
Overexpression of the ATP-binding cassette half-transporter, ABCG2 (Mxr/BCrp/ABCP1), in flavopiridol-resistant human breast cancer cells. | 2001 Jan |
|
Irinotecan plus fluorouracil and leucovorin for metastatic colorectal cancer. | 2001 Jan 25 |
|
Irinotecan plus fluorouracil and leucovorin for metastatic colorectal cancer. | 2001 Jan 25 |
|
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 |
|
Active transepithelial transport of irinotecan (CPT-11) and its metabolites by human intestinal Caco-2 cells. | 2001 Jun |
|
Topoisomerase I targeting agents in small-cell lung cancer. | 2001 Mar |
|
Oxaliplatin: a new agent for colorectal cancer. | 2001 Mar |
|
Determinants of prognosis and response to therapy in colorectal cancer. | 2001 Mar |
|
Irinotecan in the treatment of colorectal cancer: clinical overview. | 2001 Mar 1 |
|
Potentiation of antitumor activity of irinotecan by chemically modified oligonucleotides. | 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.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:58:53 GMT 2023
by
admin
on
Fri Dec 15 15:58:53 GMT 2023
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Record UNII |
7673326042
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Record Status |
Validated (UNII)
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Record Version |
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English |
Classification Tree | Code System | Code | ||
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FDA ORPHAN DRUG |
344311
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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WHO-VATC |
QL01XX19
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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LIVERTOX |
NBK548037
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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NDF-RT |
N0000000176
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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NDF-RT |
N0000175609
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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NCI_THESAURUS |
C2843
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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WHO-ATC |
L01XX19
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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FDA ORPHAN DRUG |
567516
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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Code System | Code | Type | Description | ||
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DTXSID1041051
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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PRIMARY | |||
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1482
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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PRIMARY | |||
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CHEMBL481
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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PRIMARY | |||
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6823
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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PRIMARY | |||
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6694
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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PRIMARY | |||
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7673326042
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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PRIMARY | |||
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Irinotecan
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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PRIMARY | |||
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SUB08295MIG
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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PRIMARY | |||
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7607
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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PRIMARY | |||
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C051890
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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PRIMARY | |||
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728073
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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PRIMARY | |||
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DB00762
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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PRIMARY | |||
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IRINOTECAN
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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PRIMARY | |||
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97682-44-5
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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PRIMARY | |||
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60838
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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PRIMARY | |||
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51499
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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PRIMARY | RxNorm | ||
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7673326042
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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PRIMARY | |||
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C62040
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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PRIMARY | |||
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100000083374
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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PRIMARY | |||
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80630
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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PRIMARY | |||
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m6405
Created by
admin on Fri Dec 15 15:58:53 GMT 2023 , Edited by admin on Fri Dec 15 15:58:53 GMT 2023
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PRIMARY | Merck Index |
Related Record | Type | Details | ||
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TARGET -> INHIBITOR | |||
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METABOLIC ENZYME -> SUBSTRATE | |||
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METABOLIC ENZYME -> SUBSTRATE |
CES1A1
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METABOLIC ENZYME -> SUBSTRATE | |||
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METABOLIC ENZYME -> SUBSTRATE |
CES2 is 64 times more efficient in metabolizing CPT-11 than CES1A1 (Humerickhouse et al., 2000).
MAJOR
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BINDER->LIGAND |
BINDING
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TRANSPORTER -> SUBSTRATE |
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METABOLIC ENZYME -> SUBSTRATE | |||
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SALT/SOLVATE -> PARENT | |||
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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 .
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SALT/SOLVATE -> PARENT |
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Related Record | Type | Details | ||
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METABOLITE INACTIVE -> PARENT |
MAJOR
URINE
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METABOLITE INACTIVE -> PARENT | |||
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METABOLITE ACTIVE -> PRODRUG |
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METABOLITE INACTIVE -> PARENT |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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Children and Adolescent PHARMACOKINETIC PHARMACOKINETIC |
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Route of Elimination | PHARMACOKINETIC |
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URINE PHARMACOKINETIC |
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