Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C45H54N4O8 |
Molecular Weight | 778.9323 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 8 / 8 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12N3CC[C@@]14C5=CC(=C(OC)C=C5N(C)[C@@]4([H])[C@](O)([C@H](OC(C)=O)[C@]2(CC)C=CC3)C(=O)OC)[C@]6(C[C@H]7CN(CC(CC)=C7)CC8=C6NC9=C8C=CC=C9)C(=O)OC
InChI
InChIKey=GBABOYUKABKIAF-IELIFDKJSA-N
InChI=1S/C45H54N4O8/c1-8-27-19-28-22-44(40(51)55-6,36-30(25-48(23-27)24-28)29-13-10-11-14-33(29)46-36)32-20-31-34(21-35(32)54-5)47(4)38-43(31)16-18-49-17-12-15-42(9-2,37(43)49)39(57-26(3)50)45(38,53)41(52)56-7/h10-15,19-21,28,37-39,46,53H,8-9,16-18,22-25H2,1-7H3/t28-,37-,38+,39+,42+,43+,44-,45-/m0/s1
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/10864196Curator's Comment: Description was created based on several sources, including http://www.fda.gov/ohrms/dockets/ac/04/briefing/4021B1_10_Vinorelbine%20label.pdf | https://www.medicines.org.uk/emc/medicine/1604 | http://adisinsight.springer.com/drugs/800004195
Sources: https://www.ncbi.nlm.nih.gov/pubmed/10864196
Curator's Comment: Description was created based on several sources, including http://www.fda.gov/ohrms/dockets/ac/04/briefing/4021B1_10_Vinorelbine%20label.pdf | https://www.medicines.org.uk/emc/medicine/1604 | http://adisinsight.springer.com/drugs/800004195
Vinorelbine (trade name Navelbine) is a semi-synthetic vinca-alkaloid with a broad spectrum
of anti-tumour activity. Vinorelbine is a mitotic spindle poison that impairs chromosomal segregation during mitosis. It blocks cells at G2/M. Microtubules (derived from polymers of tubulin) are the principal target of vinorelbine. Vinorelbine was developed by Pierre Fabre under licence from the CNRS in France. NAVELBINE (vinorelbine tartrate) as a single agent or in combination is indicated for the first line treatment of non small cell lung cancer and advanced breast cancer.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2095182 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10864196 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | NAVELBINE Approved UseNAVELBINE (vinorelbine tartrate) is indicated as a single agent or in combination with cisplatin for the first-line treatment of ambulatory patients with unresectable, advanced nonsmall cell lung cancer (NSCLC). In patients with Stage IV NSCLC, NAVELBINE is indicated as a single agent or in combination with cisplatin. In Stage III NSCLC, NAVELBINE is indicated in combination with cisplatin. Launch Date1994 |
|||
Primary | NAVELBINE Approved UseOral NAVELBINE (vinorelbine tartrate) as a single agent or in combination for the first line treatment of stage 3 or 4 non small cell lung cancer, and treatment of advanced breast cancer stage 3 and 4 relapsing after or refractory to an anthracycline containing regimen. Launch Date1994 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
761.8 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/11822766 |
25 mg/m² single, intravenous dose: 25 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
VINORELBINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
133.4 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/11822766 |
80 mg/m² single, oral dose: 80 mg/m² route of administration: Oral experiment type: SINGLE co-administered: |
VINORELBINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1042 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/11822766 |
25 mg/m² single, intravenous dose: 25 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
VINORELBINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1299 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/11822766 |
80 mg/m² single, oral dose: 80 mg/m² route of administration: Oral experiment type: SINGLE co-administered: |
VINORELBINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
37.9 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/11822766 |
25 mg/m² single, intravenous dose: 25 mg/m² route of administration: Intravenous experiment type: SINGLE co-administered: |
VINORELBINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
29.4 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/11822766 |
80 mg/m² single, oral dose: 80 mg/m² route of administration: Oral experiment type: SINGLE co-administered: |
VINORELBINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
14.6% |
VINORELBINE plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
30 mg/m2 1 times / week multiple, intravenous Recommended Dose: 30 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 61 years (range: 32-79 years) n = 143 Health Status: unhealthy Condition: metastatic NSCLC Age Group: 61 years (range: 32-79 years) Sex: M+F Population Size: 143 Sources: |
DLT: Neutropenia, Neutropenia... Other AEs: Leukopenia, Leukopenia... Dose limiting toxicities: Neutropenia (grade 1, 80%) Other AEs:Neutropenia (grade 4, 29%) Leukopenia (grade 1, 81%) Sources: Leukopenia (grade 4, 12%) Thrombocytopenia (grade 1, 4%) Anemia (grade 1, 77%) Anemia (grade 3, 1%) AST increased (grade 3-4, 3%) Bilirubin increased (grade 3-4, 5%) Nausea (grade 3-4, 1%) Asthenia (grade 3-4, 5%) Constipation (grade 3-4, 2%) Injection site reaction (grade 3-4, 5%) Injection site pain (grade 3-4, 1%) Neuropathy peripheral (grade 3-4, 1%) Vomiting (grade 3-4, 1%) Diarrhea (grade 3-4, 1%) Alopecia (grade 3-4, 1%) Phlebitis (grade 3-4, 1%) Dyspnea (grade 3-4, 2%) |
100 mg/m2 1 times / week multiple, oral MTD Dose: 100 mg/m2, 1 times / week Route: oral Route: multiple Dose: 100 mg/m2, 1 times / week Sources: |
unhealthy, adult n = 6 Health Status: unhealthy Condition: advanced breast cancer Age Group: adult Sex: F Population Size: 6 Sources: |
DLT: Neutropenia... Other AEs: Leukopenia, Vomiting... Dose limiting toxicities: Neutropenia (grade 3-4, 3 patients) Other AEs:Leukopenia (grade 3-4, 2 patients) Sources: Vomiting (grade 3-4, 2 patients) Diarrhoea (grade 1, 3 patients) Stomatitis (grade 3-4, 1 patient) Constipation (grade 3-4, 3 patients) Alopecia (grade 1-2, 2 patients) |
80 mg/m2 1 times / week multiple, oral RP2D Dose: 80 mg/m2, 1 times / week Route: oral Route: multiple Dose: 80 mg/m2, 1 times / week Sources: |
unhealthy, adult n = 13 Health Status: unhealthy Condition: advanced breast cancer Age Group: adult Sex: F Population Size: 13 Sources: |
DLT: Neutropenia, Neutropenia... Other AEs: Leukopenia, Vomiting... Dose limiting toxicities: Neutropenia (grade 3-4, 10 patients) Other AEs:Neutropenia (all grades, 11 patient) Leukopenia (grade 3-4, 7 patients) Sources: Vomiting (grade 3-4, 2 patients) Constipation (grade 3-4, 1 patient) Alopecia (grade 3-4, 1 patient) Anaemia (all grades, 9 patients) Leukopenia (all grades, 12 patients) Thrombocytopenia (all grades, 1 patient) Nausea (all grades, 13 patients) Vomiting (all grades, 11 patient) Diarrhoea (all grades, 9 patients) Stomatitis (all grades, 2 patients) Constipation (all grades, 8 patients) Alopecia (all grades, 9 patients) |
25 mg/m2 1 times / week multiple, intravenous Recommended Dose: 25 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 25 mg/m2, 1 times / week Co-administed with:: cisplatin(100 mg/m^2; 1/month) Sources: |
unhealthy n = 212 Health Status: unhealthy Condition: NSCLC Population Size: 212 Sources: |
DLT: Neutropenia... Other AEs: Anemia, Leukopenia... Dose limiting toxicities: Neutropenia (grade 3-4, 82%) Other AEs:Anemia (grade 3-4, 24%) Sources: Leukopenia (grade 3-4, 58%) Thrombocytopenia (grade 3-4, 5%) Febrile neutropenia (grade 3-4, 11%) Blood creatinine increased (grade 3-4, 4%) Malaise and fatigue (grade 3-4, 12%) Vomiting (grade 3-4, 13%) Nausea (grade 3-4, 14%) Constipation (grade 3-4, 3%) Weight decreased (grade 3-4, 1%) Fever (grade 3-4, 2%) Hearing impaired (grade 3-4, 4%) Injection site reaction (grade 3-4, <1%) Diarrhea (grade 3-4, <3%) Paraesthesia (grade 3-4, <1%) Numbness (grade 3-4, 2%) Arthralgia (grade 3-4, <1%) Embolism and thrombosis (grade 3-4, 3%) Weakness (grade 3-4, <3%) Infection (grade 3-4, <6%) Respiratory tract infection (grade 3-4, <5%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Thrombocytopenia | grade 1, 4% | 30 mg/m2 1 times / week multiple, intravenous Recommended Dose: 30 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 61 years (range: 32-79 years) n = 143 Health Status: unhealthy Condition: metastatic NSCLC Age Group: 61 years (range: 32-79 years) Sex: M+F Population Size: 143 Sources: |
Anemia | grade 1, 77% | 30 mg/m2 1 times / week multiple, intravenous Recommended Dose: 30 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 61 years (range: 32-79 years) n = 143 Health Status: unhealthy Condition: metastatic NSCLC Age Group: 61 years (range: 32-79 years) Sex: M+F Population Size: 143 Sources: |
Neutropenia | grade 1, 80% DLT |
30 mg/m2 1 times / week multiple, intravenous Recommended Dose: 30 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 61 years (range: 32-79 years) n = 143 Health Status: unhealthy Condition: metastatic NSCLC Age Group: 61 years (range: 32-79 years) Sex: M+F Population Size: 143 Sources: |
Leukopenia | grade 1, 81% | 30 mg/m2 1 times / week multiple, intravenous Recommended Dose: 30 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 61 years (range: 32-79 years) n = 143 Health Status: unhealthy Condition: metastatic NSCLC Age Group: 61 years (range: 32-79 years) Sex: M+F Population Size: 143 Sources: |
Anemia | grade 3, 1% | 30 mg/m2 1 times / week multiple, intravenous Recommended Dose: 30 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 61 years (range: 32-79 years) n = 143 Health Status: unhealthy Condition: metastatic NSCLC Age Group: 61 years (range: 32-79 years) Sex: M+F Population Size: 143 Sources: |
Alopecia | grade 3-4, 1% | 30 mg/m2 1 times / week multiple, intravenous Recommended Dose: 30 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 61 years (range: 32-79 years) n = 143 Health Status: unhealthy Condition: metastatic NSCLC Age Group: 61 years (range: 32-79 years) Sex: M+F Population Size: 143 Sources: |
Diarrhea | grade 3-4, 1% | 30 mg/m2 1 times / week multiple, intravenous Recommended Dose: 30 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 61 years (range: 32-79 years) n = 143 Health Status: unhealthy Condition: metastatic NSCLC Age Group: 61 years (range: 32-79 years) Sex: M+F Population Size: 143 Sources: |
Injection site pain | grade 3-4, 1% | 30 mg/m2 1 times / week multiple, intravenous Recommended Dose: 30 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 61 years (range: 32-79 years) n = 143 Health Status: unhealthy Condition: metastatic NSCLC Age Group: 61 years (range: 32-79 years) Sex: M+F Population Size: 143 Sources: |
Nausea | grade 3-4, 1% | 30 mg/m2 1 times / week multiple, intravenous Recommended Dose: 30 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 61 years (range: 32-79 years) n = 143 Health Status: unhealthy Condition: metastatic NSCLC Age Group: 61 years (range: 32-79 years) Sex: M+F Population Size: 143 Sources: |
Neuropathy peripheral | grade 3-4, 1% | 30 mg/m2 1 times / week multiple, intravenous Recommended Dose: 30 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 61 years (range: 32-79 years) n = 143 Health Status: unhealthy Condition: metastatic NSCLC Age Group: 61 years (range: 32-79 years) Sex: M+F Population Size: 143 Sources: |
Phlebitis | grade 3-4, 1% | 30 mg/m2 1 times / week multiple, intravenous Recommended Dose: 30 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 61 years (range: 32-79 years) n = 143 Health Status: unhealthy Condition: metastatic NSCLC Age Group: 61 years (range: 32-79 years) Sex: M+F Population Size: 143 Sources: |
Vomiting | grade 3-4, 1% | 30 mg/m2 1 times / week multiple, intravenous Recommended Dose: 30 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 61 years (range: 32-79 years) n = 143 Health Status: unhealthy Condition: metastatic NSCLC Age Group: 61 years (range: 32-79 years) Sex: M+F Population Size: 143 Sources: |
Constipation | grade 3-4, 2% | 30 mg/m2 1 times / week multiple, intravenous Recommended Dose: 30 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 61 years (range: 32-79 years) n = 143 Health Status: unhealthy Condition: metastatic NSCLC Age Group: 61 years (range: 32-79 years) Sex: M+F Population Size: 143 Sources: |
Dyspnea | grade 3-4, 2% | 30 mg/m2 1 times / week multiple, intravenous Recommended Dose: 30 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 61 years (range: 32-79 years) n = 143 Health Status: unhealthy Condition: metastatic NSCLC Age Group: 61 years (range: 32-79 years) Sex: M+F Population Size: 143 Sources: |
AST increased | grade 3-4, 3% | 30 mg/m2 1 times / week multiple, intravenous Recommended Dose: 30 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 61 years (range: 32-79 years) n = 143 Health Status: unhealthy Condition: metastatic NSCLC Age Group: 61 years (range: 32-79 years) Sex: M+F Population Size: 143 Sources: |
Asthenia | grade 3-4, 5% | 30 mg/m2 1 times / week multiple, intravenous Recommended Dose: 30 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 61 years (range: 32-79 years) n = 143 Health Status: unhealthy Condition: metastatic NSCLC Age Group: 61 years (range: 32-79 years) Sex: M+F Population Size: 143 Sources: |
Bilirubin increased | grade 3-4, 5% | 30 mg/m2 1 times / week multiple, intravenous Recommended Dose: 30 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 61 years (range: 32-79 years) n = 143 Health Status: unhealthy Condition: metastatic NSCLC Age Group: 61 years (range: 32-79 years) Sex: M+F Population Size: 143 Sources: |
Injection site reaction | grade 3-4, 5% | 30 mg/m2 1 times / week multiple, intravenous Recommended Dose: 30 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 61 years (range: 32-79 years) n = 143 Health Status: unhealthy Condition: metastatic NSCLC Age Group: 61 years (range: 32-79 years) Sex: M+F Population Size: 143 Sources: |
Leukopenia | grade 4, 12% | 30 mg/m2 1 times / week multiple, intravenous Recommended Dose: 30 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 61 years (range: 32-79 years) n = 143 Health Status: unhealthy Condition: metastatic NSCLC Age Group: 61 years (range: 32-79 years) Sex: M+F Population Size: 143 Sources: |
Neutropenia | grade 4, 29% DLT |
30 mg/m2 1 times / week multiple, intravenous Recommended Dose: 30 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 30 mg/m2, 1 times / week Sources: |
unhealthy, 61 years (range: 32-79 years) n = 143 Health Status: unhealthy Condition: metastatic NSCLC Age Group: 61 years (range: 32-79 years) Sex: M+F Population Size: 143 Sources: |
Diarrhoea | grade 1, 3 patients | 100 mg/m2 1 times / week multiple, oral MTD Dose: 100 mg/m2, 1 times / week Route: oral Route: multiple Dose: 100 mg/m2, 1 times / week Sources: |
unhealthy, adult n = 6 Health Status: unhealthy Condition: advanced breast cancer Age Group: adult Sex: F Population Size: 6 Sources: |
Alopecia | grade 1-2, 2 patients | 100 mg/m2 1 times / week multiple, oral MTD Dose: 100 mg/m2, 1 times / week Route: oral Route: multiple Dose: 100 mg/m2, 1 times / week Sources: |
unhealthy, adult n = 6 Health Status: unhealthy Condition: advanced breast cancer Age Group: adult Sex: F Population Size: 6 Sources: |
Stomatitis | grade 3-4, 1 patient | 100 mg/m2 1 times / week multiple, oral MTD Dose: 100 mg/m2, 1 times / week Route: oral Route: multiple Dose: 100 mg/m2, 1 times / week Sources: |
unhealthy, adult n = 6 Health Status: unhealthy Condition: advanced breast cancer Age Group: adult Sex: F Population Size: 6 Sources: |
Leukopenia | grade 3-4, 2 patients | 100 mg/m2 1 times / week multiple, oral MTD Dose: 100 mg/m2, 1 times / week Route: oral Route: multiple Dose: 100 mg/m2, 1 times / week Sources: |
unhealthy, adult n = 6 Health Status: unhealthy Condition: advanced breast cancer Age Group: adult Sex: F Population Size: 6 Sources: |
Vomiting | grade 3-4, 2 patients | 100 mg/m2 1 times / week multiple, oral MTD Dose: 100 mg/m2, 1 times / week Route: oral Route: multiple Dose: 100 mg/m2, 1 times / week Sources: |
unhealthy, adult n = 6 Health Status: unhealthy Condition: advanced breast cancer Age Group: adult Sex: F Population Size: 6 Sources: |
Constipation | grade 3-4, 3 patients | 100 mg/m2 1 times / week multiple, oral MTD Dose: 100 mg/m2, 1 times / week Route: oral Route: multiple Dose: 100 mg/m2, 1 times / week Sources: |
unhealthy, adult n = 6 Health Status: unhealthy Condition: advanced breast cancer Age Group: adult Sex: F Population Size: 6 Sources: |
Neutropenia | grade 3-4, 3 patients DLT |
100 mg/m2 1 times / week multiple, oral MTD Dose: 100 mg/m2, 1 times / week Route: oral Route: multiple Dose: 100 mg/m2, 1 times / week Sources: |
unhealthy, adult n = 6 Health Status: unhealthy Condition: advanced breast cancer Age Group: adult Sex: F Population Size: 6 Sources: |
Thrombocytopenia | all grades, 1 patient | 80 mg/m2 1 times / week multiple, oral RP2D Dose: 80 mg/m2, 1 times / week Route: oral Route: multiple Dose: 80 mg/m2, 1 times / week Sources: |
unhealthy, adult n = 13 Health Status: unhealthy Condition: advanced breast cancer Age Group: adult Sex: F Population Size: 13 Sources: |
Vomiting | all grades, 11 patient | 80 mg/m2 1 times / week multiple, oral RP2D Dose: 80 mg/m2, 1 times / week Route: oral Route: multiple Dose: 80 mg/m2, 1 times / week Sources: |
unhealthy, adult n = 13 Health Status: unhealthy Condition: advanced breast cancer Age Group: adult Sex: F Population Size: 13 Sources: |
Neutropenia | all grades, 11 patient DLT |
80 mg/m2 1 times / week multiple, oral RP2D Dose: 80 mg/m2, 1 times / week Route: oral Route: multiple Dose: 80 mg/m2, 1 times / week Sources: |
unhealthy, adult n = 13 Health Status: unhealthy Condition: advanced breast cancer Age Group: adult Sex: F Population Size: 13 Sources: |
Leukopenia | all grades, 12 patients | 80 mg/m2 1 times / week multiple, oral RP2D Dose: 80 mg/m2, 1 times / week Route: oral Route: multiple Dose: 80 mg/m2, 1 times / week Sources: |
unhealthy, adult n = 13 Health Status: unhealthy Condition: advanced breast cancer Age Group: adult Sex: F Population Size: 13 Sources: |
Nausea | all grades, 13 patients | 80 mg/m2 1 times / week multiple, oral RP2D Dose: 80 mg/m2, 1 times / week Route: oral Route: multiple Dose: 80 mg/m2, 1 times / week Sources: |
unhealthy, adult n = 13 Health Status: unhealthy Condition: advanced breast cancer Age Group: adult Sex: F Population Size: 13 Sources: |
Stomatitis | all grades, 2 patients | 80 mg/m2 1 times / week multiple, oral RP2D Dose: 80 mg/m2, 1 times / week Route: oral Route: multiple Dose: 80 mg/m2, 1 times / week Sources: |
unhealthy, adult n = 13 Health Status: unhealthy Condition: advanced breast cancer Age Group: adult Sex: F Population Size: 13 Sources: |
Constipation | all grades, 8 patients | 80 mg/m2 1 times / week multiple, oral RP2D Dose: 80 mg/m2, 1 times / week Route: oral Route: multiple Dose: 80 mg/m2, 1 times / week Sources: |
unhealthy, adult n = 13 Health Status: unhealthy Condition: advanced breast cancer Age Group: adult Sex: F Population Size: 13 Sources: |
Alopecia | all grades, 9 patients | 80 mg/m2 1 times / week multiple, oral RP2D Dose: 80 mg/m2, 1 times / week Route: oral Route: multiple Dose: 80 mg/m2, 1 times / week Sources: |
unhealthy, adult n = 13 Health Status: unhealthy Condition: advanced breast cancer Age Group: adult Sex: F Population Size: 13 Sources: |
Anaemia | all grades, 9 patients | 80 mg/m2 1 times / week multiple, oral RP2D Dose: 80 mg/m2, 1 times / week Route: oral Route: multiple Dose: 80 mg/m2, 1 times / week Sources: |
unhealthy, adult n = 13 Health Status: unhealthy Condition: advanced breast cancer Age Group: adult Sex: F Population Size: 13 Sources: |
Diarrhoea | all grades, 9 patients | 80 mg/m2 1 times / week multiple, oral RP2D Dose: 80 mg/m2, 1 times / week Route: oral Route: multiple Dose: 80 mg/m2, 1 times / week Sources: |
unhealthy, adult n = 13 Health Status: unhealthy Condition: advanced breast cancer Age Group: adult Sex: F Population Size: 13 Sources: |
Alopecia | grade 3-4, 1 patient | 80 mg/m2 1 times / week multiple, oral RP2D Dose: 80 mg/m2, 1 times / week Route: oral Route: multiple Dose: 80 mg/m2, 1 times / week Sources: |
unhealthy, adult n = 13 Health Status: unhealthy Condition: advanced breast cancer Age Group: adult Sex: F Population Size: 13 Sources: |
Constipation | grade 3-4, 1 patient | 80 mg/m2 1 times / week multiple, oral RP2D Dose: 80 mg/m2, 1 times / week Route: oral Route: multiple Dose: 80 mg/m2, 1 times / week Sources: |
unhealthy, adult n = 13 Health Status: unhealthy Condition: advanced breast cancer Age Group: adult Sex: F Population Size: 13 Sources: |
Neutropenia | grade 3-4, 10 patients DLT |
80 mg/m2 1 times / week multiple, oral RP2D Dose: 80 mg/m2, 1 times / week Route: oral Route: multiple Dose: 80 mg/m2, 1 times / week Sources: |
unhealthy, adult n = 13 Health Status: unhealthy Condition: advanced breast cancer Age Group: adult Sex: F Population Size: 13 Sources: |
Vomiting | grade 3-4, 2 patients | 80 mg/m2 1 times / week multiple, oral RP2D Dose: 80 mg/m2, 1 times / week Route: oral Route: multiple Dose: 80 mg/m2, 1 times / week Sources: |
unhealthy, adult n = 13 Health Status: unhealthy Condition: advanced breast cancer Age Group: adult Sex: F Population Size: 13 Sources: |
Leukopenia | grade 3-4, 7 patients | 80 mg/m2 1 times / week multiple, oral RP2D Dose: 80 mg/m2, 1 times / week Route: oral Route: multiple Dose: 80 mg/m2, 1 times / week Sources: |
unhealthy, adult n = 13 Health Status: unhealthy Condition: advanced breast cancer Age Group: adult Sex: F Population Size: 13 Sources: |
Weight decreased | grade 3-4, 1% | 25 mg/m2 1 times / week multiple, intravenous Recommended Dose: 25 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 25 mg/m2, 1 times / week Co-administed with:: cisplatin(100 mg/m^2; 1/month) Sources: |
unhealthy n = 212 Health Status: unhealthy Condition: NSCLC Population Size: 212 Sources: |
Febrile neutropenia | grade 3-4, 11% | 25 mg/m2 1 times / week multiple, intravenous Recommended Dose: 25 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 25 mg/m2, 1 times / week Co-administed with:: cisplatin(100 mg/m^2; 1/month) Sources: |
unhealthy n = 212 Health Status: unhealthy Condition: NSCLC Population Size: 212 Sources: |
Malaise and fatigue | grade 3-4, 12% | 25 mg/m2 1 times / week multiple, intravenous Recommended Dose: 25 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 25 mg/m2, 1 times / week Co-administed with:: cisplatin(100 mg/m^2; 1/month) Sources: |
unhealthy n = 212 Health Status: unhealthy Condition: NSCLC Population Size: 212 Sources: |
Vomiting | grade 3-4, 13% | 25 mg/m2 1 times / week multiple, intravenous Recommended Dose: 25 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 25 mg/m2, 1 times / week Co-administed with:: cisplatin(100 mg/m^2; 1/month) Sources: |
unhealthy n = 212 Health Status: unhealthy Condition: NSCLC Population Size: 212 Sources: |
Nausea | grade 3-4, 14% | 25 mg/m2 1 times / week multiple, intravenous Recommended Dose: 25 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 25 mg/m2, 1 times / week Co-administed with:: cisplatin(100 mg/m^2; 1/month) Sources: |
unhealthy n = 212 Health Status: unhealthy Condition: NSCLC Population Size: 212 Sources: |
Fever | grade 3-4, 2% | 25 mg/m2 1 times / week multiple, intravenous Recommended Dose: 25 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 25 mg/m2, 1 times / week Co-administed with:: cisplatin(100 mg/m^2; 1/month) Sources: |
unhealthy n = 212 Health Status: unhealthy Condition: NSCLC Population Size: 212 Sources: |
Numbness | grade 3-4, 2% | 25 mg/m2 1 times / week multiple, intravenous Recommended Dose: 25 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 25 mg/m2, 1 times / week Co-administed with:: cisplatin(100 mg/m^2; 1/month) Sources: |
unhealthy n = 212 Health Status: unhealthy Condition: NSCLC Population Size: 212 Sources: |
Anemia | grade 3-4, 24% | 25 mg/m2 1 times / week multiple, intravenous Recommended Dose: 25 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 25 mg/m2, 1 times / week Co-administed with:: cisplatin(100 mg/m^2; 1/month) Sources: |
unhealthy n = 212 Health Status: unhealthy Condition: NSCLC Population Size: 212 Sources: |
Constipation | grade 3-4, 3% | 25 mg/m2 1 times / week multiple, intravenous Recommended Dose: 25 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 25 mg/m2, 1 times / week Co-administed with:: cisplatin(100 mg/m^2; 1/month) Sources: |
unhealthy n = 212 Health Status: unhealthy Condition: NSCLC Population Size: 212 Sources: |
Embolism and thrombosis | grade 3-4, 3% | 25 mg/m2 1 times / week multiple, intravenous Recommended Dose: 25 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 25 mg/m2, 1 times / week Co-administed with:: cisplatin(100 mg/m^2; 1/month) Sources: |
unhealthy n = 212 Health Status: unhealthy Condition: NSCLC Population Size: 212 Sources: |
Blood creatinine increased | grade 3-4, 4% | 25 mg/m2 1 times / week multiple, intravenous Recommended Dose: 25 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 25 mg/m2, 1 times / week Co-administed with:: cisplatin(100 mg/m^2; 1/month) Sources: |
unhealthy n = 212 Health Status: unhealthy Condition: NSCLC Population Size: 212 Sources: |
Hearing impaired | grade 3-4, 4% | 25 mg/m2 1 times / week multiple, intravenous Recommended Dose: 25 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 25 mg/m2, 1 times / week Co-administed with:: cisplatin(100 mg/m^2; 1/month) Sources: |
unhealthy n = 212 Health Status: unhealthy Condition: NSCLC Population Size: 212 Sources: |
Thrombocytopenia | grade 3-4, 5% | 25 mg/m2 1 times / week multiple, intravenous Recommended Dose: 25 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 25 mg/m2, 1 times / week Co-administed with:: cisplatin(100 mg/m^2; 1/month) Sources: |
unhealthy n = 212 Health Status: unhealthy Condition: NSCLC Population Size: 212 Sources: |
Leukopenia | grade 3-4, 58% | 25 mg/m2 1 times / week multiple, intravenous Recommended Dose: 25 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 25 mg/m2, 1 times / week Co-administed with:: cisplatin(100 mg/m^2; 1/month) Sources: |
unhealthy n = 212 Health Status: unhealthy Condition: NSCLC Population Size: 212 Sources: |
Neutropenia | grade 3-4, 82% DLT |
25 mg/m2 1 times / week multiple, intravenous Recommended Dose: 25 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 25 mg/m2, 1 times / week Co-administed with:: cisplatin(100 mg/m^2; 1/month) Sources: |
unhealthy n = 212 Health Status: unhealthy Condition: NSCLC Population Size: 212 Sources: |
Arthralgia | grade 3-4, <1% | 25 mg/m2 1 times / week multiple, intravenous Recommended Dose: 25 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 25 mg/m2, 1 times / week Co-administed with:: cisplatin(100 mg/m^2; 1/month) Sources: |
unhealthy n = 212 Health Status: unhealthy Condition: NSCLC Population Size: 212 Sources: |
Injection site reaction | grade 3-4, <1% | 25 mg/m2 1 times / week multiple, intravenous Recommended Dose: 25 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 25 mg/m2, 1 times / week Co-administed with:: cisplatin(100 mg/m^2; 1/month) Sources: |
unhealthy n = 212 Health Status: unhealthy Condition: NSCLC Population Size: 212 Sources: |
Paraesthesia | grade 3-4, <1% | 25 mg/m2 1 times / week multiple, intravenous Recommended Dose: 25 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 25 mg/m2, 1 times / week Co-administed with:: cisplatin(100 mg/m^2; 1/month) Sources: |
unhealthy n = 212 Health Status: unhealthy Condition: NSCLC Population Size: 212 Sources: |
Diarrhea | grade 3-4, <3% | 25 mg/m2 1 times / week multiple, intravenous Recommended Dose: 25 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 25 mg/m2, 1 times / week Co-administed with:: cisplatin(100 mg/m^2; 1/month) Sources: |
unhealthy n = 212 Health Status: unhealthy Condition: NSCLC Population Size: 212 Sources: |
Weakness | grade 3-4, <3% | 25 mg/m2 1 times / week multiple, intravenous Recommended Dose: 25 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 25 mg/m2, 1 times / week Co-administed with:: cisplatin(100 mg/m^2; 1/month) Sources: |
unhealthy n = 212 Health Status: unhealthy Condition: NSCLC Population Size: 212 Sources: |
Respiratory tract infection | grade 3-4, <5% | 25 mg/m2 1 times / week multiple, intravenous Recommended Dose: 25 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 25 mg/m2, 1 times / week Co-administed with:: cisplatin(100 mg/m^2; 1/month) Sources: |
unhealthy n = 212 Health Status: unhealthy Condition: NSCLC Population Size: 212 Sources: |
Infection | grade 3-4, <6% | 25 mg/m2 1 times / week multiple, intravenous Recommended Dose: 25 mg/m2, 1 times / week Route: intravenous Route: multiple Dose: 25 mg/m2, 1 times / week Co-administed with:: cisplatin(100 mg/m^2; 1/month) Sources: |
unhealthy n = 212 Health Status: unhealthy Condition: NSCLC Population Size: 212 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
likely | ||||
likely | ||||
likely | ||||
no [IC50 >10 uM] | ||||
no [IC50 >10 uM] | ||||
no [IC50 >10 uM] | ||||
no | ||||
Page: (PMDA) 7 |
yes [IC50 10.6 uM] | unlikely (co-administration study) Comment: Coadministration of Vinorelbine significantly did not affect the exposure of Cyclophosphamide. Page: (PMDA) 7 |
||
yes [Ki 22 uM] | ||||
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
Page: (PMDA drug information) 23 |
yes [Km 2.63 uM] | |||
yes [Km 3.64 uM] | ||||
yes | ||||
Page: 14.0 |
yes | |||
yes | ||||
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
Ongoing trials with trastuzumab in metastatic breast cancer. | 2001 |
|
Phase I-II vinorelbine (Navelbine) by continuous infusion in patients with metastatic breast cancer: cumulative toxicities limit dose escalation. | 2001 |
|
Activity and safety of vinorelbine combined with doxorubicin or fluorouracil as first-line therapy in advanced breast cancer: a stratified phase II study. | 2001 |
|
Vinorelbine-based regimens as salvage treatment in patients with advanced non-small cell lung cancer: two parallel multicenter phase II trials. | 2001 |
|
A phase II trial of fractionated vinorelbine/doxorubicin as first-line therapy for advanced breast cancer. | 2001 |
|
Chemoradiation in locally advanced non-small cell lung cancer. | 2001 |
|
The ELVIS trial: a phase III study of single-agent vinorelbine as first-line treatment in elderly patients with advanced non-small cell lung cancer. Elderly Lung Cancer Vinorelbine Italian Study. | 2001 |
|
Treatment of patients with metastatic germ cell tumors relapsing after high-dose chemotherapy. | 2001 Apr |
|
Phase III trial of cisplatin/gemcitabine with or without vinorelbine or paclitaxel in advanced non-small cell lung cancer. | 2001 Apr |
|
Phase II study of vinorelbine in the treatment of platinum-resistant ovarian carcinoma. | 2001 Apr |
|
Acute respiratory failure caused by vinorelbine tartrate in a patient with non-small cell lung cancer. | 2001 Aug |
|
The current status of docetaxel for advanced non-small cell lung cancer. | 2001 Feb |
|
Challenging the platinum combinations: docetaxel (Taxotere) combined with gemcitabine or vinorelbine in non-small cell lung cancer. | 2001 Feb |
|
Vinorelbine, cisplatin and continuous infusion of 5-fluorouracil (ViFuP) in metastatic breast cancer patients: a phase II study. | 2001 Jan |
|
Anti-vascular effects of vinflunine in the MAC 15A transplantable adenocarcinoma model. | 2001 Jan |
|
Phase I dose-finding and pharmacokinetic study of docetaxel and vinorelbine as first-line chemotherapy for metastatic breast cancer. | 2001 Jul |
|
Recent advances in the chemotherapy of non-small cell lung cancer. | 2001 Jul |
|
Rationale for non-platinum chemotherapy in advanced NSCLC. | 2001 Jul |
|
Linear immunoglobulin A bullous dermatosis induced by gemcitabine. | 2001 Jul-Aug |
|
Sequential docetaxel and vinorelbine for patients with advanced breast cancer previously treated with anthracyclines: a phase II study. | 2001 Jul-Aug |
|
Cisplatin and vinorelbine in advanced and/or metastatic adenocarcinoma of the endometrium: a new highly active chemotherapeutic regimen. | 2001 Jun |
|
In vitro activity of vinorelbine on human leukemia cells. | 2001 Jun |
|
Non-platinum based combination chemotherapy: phase I and II trials of docetaxel plus gemcitabine, vinorelbine, or irinotecan. | 2001 Jun |
|
Results of a phase III prospective, randomised trial, comparing mitoxantrone and vinorelbine (MV) in combination with standard FAC/FEC in front-line therapy of metastatic breast cancer. | 2001 Jun |
|
Importance of surgery as salvage treatment after high dose chemotherapy failure in germ cell tumors. | 2001 Jun |
|
Heterogeneity of proteinkinase C activity and PKC-zeta expression in clinical breast carcinomas. | 2001 Mar |
|
[Cisplatin and vinorelbine therapy of previously treated advanced breast cancer (preliminary studies)]. | 2001 Mar |
|
Regional plus systemic chemotherapy: an effective treatment in recurrent non-small cell lung cancer. | 2001 Mar |
|
[A case of recurrent lung cancer successfully treated with vinorelbine and cisplatin]. | 2001 Mar |
|
Efficacy of vinorelbine, epirubicin and prednisone combination regimen in pretreated elderly patients with aggressive non-Hodgkin's lymphoma. | 2001 Mar |
|
Low dose carboplatin (AUC 4.5) combined with vinorelbine in the treatment of advanced non-small cell lung cancer: a single institution phase II study. | 2001 Mar-Apr |
|
[Non-small cell lung cancer with liver metastasis responsive to gemcitabine--a case report]. | 2001 May |
|
Gemcitabine and vinorelbine as second-line therapy in non-small-cell lung cancer after prior treatment with taxane+platinum-based regimens. | 2001 May |
|
Carboplatin and vinorelbine in untreated locally advanced and metastatic non-small cell lung cancer. | 2001 May |
Sample Use Guides
NAVELBINE (vinorelbine tartrate) for intravenous injections is indicated for the treatment of non-small cell lung cancer. Single-Agent NAVELBINE (vinorelbine tartrate): The usual initial dose of single-agent NAVELBINE is 30 mg/m2 administered weekly.
Oral NAVELBINE is indicated for the treatment of non-small cell lung cancer and advanced breast cancer. As a single agent, the recommended regimen is: First three administrations
60mg/m² of body surface area, administered once weekly. Subsequent administrations
Beyond the third administration, it is recommended to increase the dose of Navelbine to 80mg/m² once weekly except in those patients for whom the neutrophil count dropped once below 500/mm3 or more than once between 500 and 1000/mm3 during the first three administrations at 60mg/m².
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11408618
IC(50) values for inhibition of HeLa cell proliferation for vinorelbine was 1.25 nM, similar to the concentrations that induced mitotic block at the metaphase/anaphase transition (3.8 nM).
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Classification Tree | Code System | Code | ||
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NDF-RT |
N0000007780
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NCI_THESAURUS |
C67422
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NCI_THESAURUS |
C932
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NDF-RT |
N0000007780
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NDF-RT |
N0000175612
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FDA ORPHAN DRUG |
540716
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WHO-ATC |
L01CA04
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FDA ORPHAN DRUG |
588417
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LIVERTOX |
1031
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WHO-VATC |
QL01CA04
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Code System | Code | Type | Description | ||
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71486-22-1
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DTXSID8040640
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100000079114
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m11457
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CHEMBL553025
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Q6C979R91Y
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39541
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DB00361
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SUB00069MIG
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5311497
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2827
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7105
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Q6C979R91Y
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6054
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C1275
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VINORELBINE
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480999
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C030852
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Vinorelbine
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7665
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760087
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ACTIVE MOIETY
METABOLITE (PARENT)
SALT/SOLVATE (PARENT)