Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C33H38N4O6 |
| Molecular Weight | 586.678 |
| Optical Activity | ( + ) |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CCC1=C2CN3C(=CC4=C(COC(=O)[C@]4(O)CC)C3=O)C2=NC5=C1C=C(OC(=O)N6CCC(CC6)N7CCCCC7)C=C5
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.
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 |
|---|---|---|---|---|
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 |
|
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 |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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 |
|
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 |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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 |
|
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 |
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 |
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 |
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 |
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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| New chemotherapy approaches in colorectal cancer. | 2001-07 |
|
| Advances in chemotherapy for small cell lung cancer: single-agent activity of newer agents. | 2001-06-23 |
|
| 26S proteasome inhibition induces apoptosis and limits growth of human pancreatic cancer. | 2001-06-16 |
|
| Control of irinotecan-induced diarrhea by octreotide after loperamide failure. | 2001-06 |
|
| Phase I-II study of irinotecan in combination with mitomycin C in patients with advanced gastrointestinal cancer. | 2001-06 |
|
| Active transepithelial transport of irinotecan (CPT-11) and its metabolites by human intestinal Caco-2 cells. | 2001-06 |
|
| Hepatic extraction, metabolism, and biliary excretion of irinotecan in the isolated perfused rat liver. | 2001-06 |
|
| Phase I study of hepatic arterial infusion of floxuridine and dexamethasone with systemic irinotecan for unresectable hepatic metastases from colorectal cancer. | 2001-05-15 |
|
| Enhanced chemosensitivity to CPT-11 with proteasome inhibitor PS-341: implications for systemic nuclear factor-kappaB inhibition. | 2001-05-01 |
|
| Preliminary study of fortnightly irinotecan hydrochloride plus cisplatin therapy in patients with advanced gastric and colorectal cancer. | 2001-05 |
|
| [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]. | 2001-05 |
|
| [Platinum compounds in cancer therapy--past, present, and future]. | 2001-05 |
|
| CPT-11 alters the circadian rhythm of dihydropyrimidine dehydrogenase mRNA in mouse liver. | 2001-05 |
|
| Modulation of irinotecan-induced diarrhea by cotreatment with neomycin in cancer patients. | 2001-05 |
|
| Impact on survival following successful neoadjuvant chemotherapy and radical surgery for Stage IIb bulky and Stage IIIb cervical cancer. | 2001-05 |
|
| Integrating the oral fluoropyrimidines into the management of advanced colorectal cancer. | 2001-05 |
|
| Potentiation of antitumor activity of irinotecan by chemically modified oligonucleotides. | 2001-05 |
|
| Subcellular localization and distribution of the breast cancer resistance protein transporter in normal human tissues. | 2001-04-15 |
|
| Prevention of irinotecan (CPT-11)-induced diarrhea by oral alkalization combined with control of defecation in cancer patients. | 2001-04-15 |
|
| Adjuvant therapy for colon cancer: the European experience. | 2001-04-13 |
|
| [Molecular factors predictive of response to chemotherapy in advanced stages of colorectal cancer]. | 2001-04-13 |
|
| [Irinotecan in colorectal cancer]. | 2001-04-13 |
|
| Topoisomerase I-DNA covalent complexes in human colorectal cancer xenografts with different p53 and microsatellite instability status: relation with their sensitivity to CTP-11. | 2001-04-13 |
|
| Perioperative radiotherapy and concurrent radiochemotherapy in rectal cancer. | 2001-04-06 |
|
| Use of a modified ornithine decarboxylase promoter to achieve efficient c-MYC- or N-MYC-regulated protein expression. | 2001-04-01 |
|
| [Home chemotherapy and/or outpatient chemotherapy for patient with advanced gastric cancer]. | 2001-04 |
|
| [Irinotecan (CPT-11) therapy for advanced gastric cancer]. | 2001-04 |
|
| [Chemotherapy of irinotecan (CPT-11) combined with cisplatin in patients with advanced gastric cancer]. | 2001-04 |
|
| Safe administration of irinotecan, oxaliplatin and raltitrexed in a DPD-deficient patient with metastatic colon cancer. | 2001-04 |
|
| A phase II trial of irinotecan (CPT-11) for unresectable biliary tree carcinoma. | 2001-04 |
|
| The role of irinotecan and oxaliplatin in the treatment of advanced colorectal cancer. | 2001-04 |
|
| Human plasma carboxylesterase and butyrylcholinesterase enzyme activity: correlations with SN-38 pharmacokinetics during a prolonged infusion of irinotecan. | 2001-04 |
|
| Antitumor activity of XR5944, a novel and potent topoisomerase poison. | 2001-04 |
|
| [Chemotherapy by combination of low-dose CPT-11 and PSK in an elderly man with liver metastasis from gastric cancer]. | 2001-04 |
|
| Pharmacogenetics of anticancer agents: lessons from amonafide and irinotecan. | 2001-04 |
|
| [Chemotherapy of colonic carcinoma in the year 2001]. | 2001-03-22 |
|
| Irinotecan plus cisplatin in advanced gastric or gastroesophageal junction carcinoma. | 2001-03 |
|
| Irinotecan/gemcitabine combination chemotherapy in pancreatic cancer. | 2001-03 |
|
| Cisplatin and irinotecan in upper gastrointestinal malignancies. | 2001-03 |
|
| [A case of AFP-producing gastric cancer responding to low-dose CPT-11 and low-dose cisplatin combination chemotherapy]. | 2001-03 |
|
| Effect of bile acids on the uptake of irinotecan and its active metabolite, SN-38, by intestinal cells. | 2001-02-16 |
|
| The current status of docetaxel for advanced non-small cell lung cancer. | 2001-02 |
|
| [Medical treatment of pulmonary neoplasms]. | 2001-02 |
|
| North Central Cancer Treatment Group--Mayo Clinic trials in colon cancer. | 2001-02 |
|
| Modulation of camptothecin analogs in the treatment of cancer: a review. | 2001-02 |
|
| Adjuvant therapy of colon cancer. | 2001-02 |
|
| 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 |
|
| Factors affecting the pharmacokinetics of CPT-11: the body mass index, age and sex are independent predictors of pharmacokinetic parameters of CPT-11. | 2001 |
|
| Irinotecan and mitomycin C in 5-fluorouracil-refractory colorectal cancer patients. A phase I/II study of the Southern Italy Cooperative Oncology Group. | 2001 |
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
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
Mon Mar 31 18:15:17 GMT 2025
by
admin
on
Mon Mar 31 18:15:17 GMT 2025
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| Record UNII |
7673326042
|
| Record Status |
Validated (UNII)
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| Record Version |
|
-
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| Classification Tree | Code System | Code | ||
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FDA ORPHAN DRUG |
344311
Created by
admin on Mon Mar 31 18:15:17 GMT 2025 , Edited by admin on Mon Mar 31 18:15:17 GMT 2025
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WHO-VATC |
QL01XX19
Created by
admin on Mon Mar 31 18:15:17 GMT 2025 , Edited by admin on Mon Mar 31 18:15:17 GMT 2025
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LIVERTOX |
NBK548037
Created by
admin on Mon Mar 31 18:15:17 GMT 2025 , Edited by admin on Mon Mar 31 18:15:17 GMT 2025
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NDF-RT |
N0000000176
Created by
admin on Mon Mar 31 18:15:17 GMT 2025 , Edited by admin on Mon Mar 31 18:15:17 GMT 2025
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NDF-RT |
N0000175609
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admin on Mon Mar 31 18:15:17 GMT 2025 , Edited by admin on Mon Mar 31 18:15:17 GMT 2025
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NCI_THESAURUS |
C2843
Created by
admin on Mon Mar 31 18:15:17 GMT 2025 , Edited by admin on Mon Mar 31 18:15:17 GMT 2025
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WHO-ATC |
L01XX19
Created by
admin on Mon Mar 31 18:15:17 GMT 2025 , Edited by admin on Mon Mar 31 18:15:17 GMT 2025
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FDA ORPHAN DRUG |
567516
Created by
admin on Mon Mar 31 18:15:17 GMT 2025 , Edited by admin on Mon Mar 31 18:15:17 GMT 2025
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DTXSID1041051
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1482
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CHEMBL481
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6823
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6694
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7673326042
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Irinotecan
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SUB08295MIG
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7607
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C051890
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728073
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DB00762
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IRINOTECAN
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97682-44-5
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60838
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51499
Created by
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PRIMARY | RxNorm | ||
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7673326042
Created by
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C62040
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100000083374
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80630
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m6405
Created by
admin on Mon Mar 31 18:15:17 GMT 2025 , Edited by admin on Mon Mar 31 18:15:17 GMT 2025
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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 ACTIVE -> PRODRUG | |||
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METABOLITE INACTIVE -> PARENT |
MAJOR
URINE
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METABOLITE INACTIVE -> PARENT |
URINE
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METABOLITE INACTIVE -> PARENT |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| Biological Half-life | PHARMACOKINETIC |
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Children and Adolescent PHARMACOKINETIC PHARMACOKINETIC |
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| Route of Elimination | PHARMACOKINETIC |
|
URINE PHARMACOKINETIC |
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