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Details

Stereochemistry ABSOLUTE
Molecular Formula C46H58N4O9
Molecular Weight 810.9759
Optical Activity UNSPECIFIED
Defined Stereocenters 9 / 9
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of VINBLASTINE

SMILES

CC[C@@]1(C[C@@]2([H])C[C@](c3cc4c(cc3OC)N(C)[C@]5([H])[C@@]64CCN7CC=C[C@](CC)([C@@]67[H])[C@]([H])([C@@]5(C(=O)OC)O)OC(=O)C)(c8c(CCN(C2)C1)c9ccccc9[nH]8)C(=O)OC)O

InChI

InChIKey=JXLYSJRDGCGARV-CFWMRBGOSA-N
InChI=1S/C46H58N4O9/c1-8-42(54)23-28-24-45(40(52)57-6,36-30(15-19-49(25-28)26-42)29-13-10-11-14-33(29)47-36)32-21-31-34(22-35(32)56-5)48(4)38-44(31)17-20-50-18-12-16-43(9-2,37(44)50)39(59-27(3)51)46(38,55)41(53)58-7/h10-14,16,21-22,28,37-39,47,54-55H,8-9,15,17-20,23-26H2,1-7H3/t28-,37-,38+,39+,42-,43+,44+,45-,46-/m0/s1

HIDE SMILES / InChI

Molecular Formula C46H58N4O9
Molecular Weight 810.9759
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 8 / 9
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment:: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/24404355

Vinblastine is a Vinca alkaloid obtained from the Madagascar periwinkle plant. Vinca alkaloids were found out in the 1950's by Canadian scientists, Robert Noble and Charles Beer for the first time. Medicinal applications of this plant lead to the monitoring of these compounds for their hypoglycemic activity, which is of little importance compared to their cytotoxic effects. They have been used to treat diabetes, high blood pressure and the drugs have even been used as disinfectants. Nevertheless, the vinca alkaloids are so important for being cancer fighters. The mechanism of action of vinblastine sulfate has been related to the inhibition of microtubule formation in the mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. Vinblastine is an antineoplastic agent used to treat Hodgkin's disease, non-Hodgkin's lymphomas, mycosis fungoides, cancer of the testis, Kaposi's sarcoma, Letterer-Siwe disease, as well as other cancers.

Originator

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
VINBLASTINE SULFATE

Approved Use

Vinblastine Sulfate Injection is indicated in the palliative treatment of the following: I. Frequently Responsive Malignancies Generalized Hodgkin’s disease (Stages III and IV, Ann Arbor modification of Rye staging system) Lymphocytic lymphoma (nodular and diffuse, poorly and well differentiated) Histiocytic lymphoma Mycosis fungoides (advanced stages) Advanced carcinoma of the testis Kaposi’s sarcoma Letterer-Siwe disease (histiocytosis X) II. Less Frequently Responsive Malignancies Choriocarcinoma resistant to other chemotherapeutic agents Carcinoma of the breast, unresponsive to appropriate endocrine surgery and hormonal therapy Current principles of chemotherapy for many types of cancer include the concurrent administration of several antineoplastic agents. For enhanced therapeutic effect without additive toxicity, agents with different dose-limiting clinical toxicities and different mechanisms of action are generally selected. Therefore, although vinblastine sulfate is effective as a single agent in the aforementioned indications, it is usually administered in combination with other antineoplastic drugs. Such combination therapy produces a greater percentage of response than does a single-agent regimen. These principles have been applied, for example, in the chemotherapy of Hodgkin’s disease. Hodgkin's Disease Vinblastine sulfate has been shown to be one of the most effective single agents for the treatment of Hodgkin’s disease. Advanced Hodgkin’s disease has also been successfully treated with several multiple-drug regimens that included vinblastine sulfate. Patients who had relapses after treatment with the MOPP program— mechlorethamine hydrochloride (nitrogen mustard), vincristine sulfate, prednisone and procarbazine—have likewise responded to combination-drug therapy that included vinblastine sulfate. A protocol using cyclophosphamide in place of nitrogen mustard and vinblastine sulfate instead of vincristine sulfate is an alternative therapy for previously untreated patients with advanced Hodgkin’s disease. Advanced testicular germinal-cell cancers (embryonal carcinoma, teratocarcinoma and choriocarcinoma) are sensitive to vinblastine sulfate alone, but better clinical results are achieved when vinblastine sulfate is administered concomitantly with other antineoplastic agents. The effect of bleomycin is significantly enhanced if vinblastine sulfate is administered six to eight hours prior to the administration of bleomycin; this schedule permits more cells to be arrested during metaphase, the stage of the cell cycle in which bleomycin is active., Hodgkin's Disease Vinblastine sulfate has been shown to be one of the most effective single agents for the treatment of Hodgkin’s disease. Advanced Hodgkin’s disease has also been successfully treated with several multiple-drug regimens that included vinblastine sulfate. Patients who had relapses after treatment with the MOPP program— mechlorethamine hydrochloride (nitrogen mustard), vincristine sulfate, prednisone and procarbazine—have likewise responded to combination-drug therapy that included vinblastine sulfate. A protocol using cyclophosphamide in place of nitrogen mustard and vinblastine sulfate instead of vincristine sulfate is an alternative therapy for previously untreated patients with advanced Hodgkin’s disease. Advanced testicular germinal-cell cancers (embryonal carcinoma, teratocarcinoma and choriocarcinoma) are sensitive to vinblastine sulfate alone, but better clinical results are achieved when vinblastine sulfate is administered concomitantly with other antineoplastic agents. The effect of bleomycin is significantly enhanced if vinblastine sulfate is administered six to eight hours prior to the administration of bleomycin; this schedule permits more cells to be arrested during metaphase, the stage of the cell cycle in which bleomycin is active.

Launch Date

5.46652815E11
Primary
VINBLASTINE SULFATE

Approved Use

Vinblastine Sulfate Injection is indicated in the palliative treatment of the following: I. Frequently Responsive Malignancies Generalized Hodgkin’s disease (Stages III and IV, Ann Arbor modification of Rye staging system) Lymphocytic lymphoma (nodular and diffuse, poorly and well differentiated) Histiocytic lymphoma Mycosis fungoides (advanced stages) Advanced carcinoma of the testis Kaposi’s sarcoma Letterer-Siwe disease (histiocytosis X) II. Less Frequently Responsive Malignancies Choriocarcinoma resistant to other chemotherapeutic agents Carcinoma of the breast, unresponsive to appropriate endocrine surgery and hormonal therapy Current principles of chemotherapy for many types of cancer include the concurrent administration of several antineoplastic agents. For enhanced therapeutic effect without additive toxicity, agents with different dose-limiting clinical toxicities and different mechanisms of action are generally selected. Therefore, although vinblastine sulfate is effective as a single agent in the aforementioned indications, it is usually administered in combination with other antineoplastic drugs. Such combination therapy produces a greater percentage of response than does a single-agent regimen. These principles have been applied, for example, in the chemotherapy of Hodgkin’s disease. Hodgkin's Disease Vinblastine sulfate has been shown to be one of the most effective single agents for the treatment of Hodgkin’s disease. Advanced Hodgkin’s disease has also been successfully treated with several multiple-drug regimens that included vinblastine sulfate. Patients who had relapses after treatment with the MOPP program— mechlorethamine hydrochloride (nitrogen mustard), vincristine sulfate, prednisone and procarbazine—have likewise responded to combination-drug therapy that included vinblastine sulfate. A protocol using cyclophosphamide in place of nitrogen mustard and vinblastine sulfate instead of vincristine sulfate is an alternative therapy for previously untreated patients with advanced Hodgkin’s disease. Advanced testicular germinal-cell cancers (embryonal carcinoma, teratocarcinoma and choriocarcinoma) are sensitive to vinblastine sulfate alone, but better clinical results are achieved when vinblastine sulfate is administered concomitantly with other antineoplastic agents. The effect of bleomycin is significantly enhanced if vinblastine sulfate is administered six to eight hours prior to the administration of bleomycin; this schedule permits more cells to be arrested during metaphase, the stage of the cell cycle in which bleomycin is active., Hodgkin's Disease Vinblastine sulfate has been shown to be one of the most effective single agents for the treatment of Hodgkin’s disease. Advanced Hodgkin’s disease has also been successfully treated with several multiple-drug regimens that included vinblastine sulfate. Patients who had relapses after treatment with the MOPP program— mechlorethamine hydrochloride (nitrogen mustard), vincristine sulfate, prednisone and procarbazine—have likewise responded to combination-drug therapy that included vinblastine sulfate. A protocol using cyclophosphamide in place of nitrogen mustard and vinblastine sulfate instead of vincristine sulfate is an alternative therapy for previously untreated patients with advanced Hodgkin’s disease. Advanced testicular germinal-cell cancers (embryonal carcinoma, teratocarcinoma and choriocarcinoma) are sensitive to vinblastine sulfate alone, but better clinical results are achieved when vinblastine sulfate is administered concomitantly with other antineoplastic agents. The effect of bleomycin is significantly enhanced if vinblastine sulfate is administered six to eight hours prior to the administration of bleomycin; this schedule permits more cells to be arrested during metaphase, the stage of the cell cycle in which bleomycin is active.

Launch Date

5.46566406E11
Primary
VINBLASTINE SULFATE

Approved Use

Vinblastine Sulfate Injection is indicated in the palliative treatment of the following: I. Frequently Responsive Malignancies Generalized Hodgkin’s disease (Stages III and IV, Ann Arbor modification of Rye staging system) Lymphocytic lymphoma (nodular and diffuse, poorly and well differentiated) Histiocytic lymphoma Mycosis fungoides (advanced stages) Advanced carcinoma of the testis Kaposi’s sarcoma Letterer-Siwe disease (histiocytosis X) II. Less Frequently Responsive Malignancies Choriocarcinoma resistant to other chemotherapeutic agents Carcinoma of the breast, unresponsive to appropriate endocrine surgery and hormonal therapy Current principles of chemotherapy for many types of cancer include the concurrent administration of several antineoplastic agents. For enhanced therapeutic effect without additive toxicity, agents with different dose-limiting clinical toxicities and different mechanisms of action are generally selected. Therefore, although vinblastine sulfate is effective as a single agent in the aforementioned indications, it is usually administered in combination with other antineoplastic drugs. Such combination therapy produces a greater percentage of response than does a single-agent regimen. These principles have been applied, for example, in the chemotherapy of Hodgkin’s disease. Hodgkin's Disease Vinblastine sulfate has been shown to be one of the most effective single agents for the treatment of Hodgkin’s disease. Advanced Hodgkin’s disease has also been successfully treated with several multiple-drug regimens that included vinblastine sulfate. Patients who had relapses after treatment with the MOPP program— mechlorethamine hydrochloride (nitrogen mustard), vincristine sulfate, prednisone and procarbazine—have likewise responded to combination-drug therapy that included vinblastine sulfate. A protocol using cyclophosphamide in place of nitrogen mustard and vinblastine sulfate instead of vincristine sulfate is an alternative therapy for previously untreated patients with advanced Hodgkin’s disease. Advanced testicular germinal-cell cancers (embryonal carcinoma, teratocarcinoma and choriocarcinoma) are sensitive to vinblastine sulfate alone, but better clinical results are achieved when vinblastine sulfate is administered concomitantly with other antineoplastic agents. The effect of bleomycin is significantly enhanced if vinblastine sulfate is administered six to eight hours prior to the administration of bleomycin; this schedule permits more cells to be arrested during metaphase, the stage of the cell cycle in which bleomycin is active., Hodgkin's Disease Vinblastine sulfate has been shown to be one of the most effective single agents for the treatment of Hodgkin’s disease. Advanced Hodgkin’s disease has also been successfully treated with several multiple-drug regimens that included vinblastine sulfate. Patients who had relapses after treatment with the MOPP program— mechlorethamine hydrochloride (nitrogen mustard), vincristine sulfate, prednisone and procarbazine—have likewise responded to combination-drug therapy that included vinblastine sulfate. A protocol using cyclophosphamide in place of nitrogen mustard and vinblastine sulfate instead of vincristine sulfate is an alternative therapy for previously untreated patients with advanced Hodgkin’s disease. Advanced testicular germinal-cell cancers (embryonal carcinoma, teratocarcinoma and choriocarcinoma) are sensitive to vinblastine sulfate alone, but better clinical results are achieved when vinblastine sulfate is administered concomitantly with other antineoplastic agents. The effect of bleomycin is significantly enhanced if vinblastine sulfate is administered six to eight hours prior to the administration of bleomycin; this schedule permits more cells to be arrested during metaphase, the stage of the cell cycle in which bleomycin is active.

Launch Date

5.46652815E11
Primary
VINBLASTINE SULFATE

Approved Use

Vinblastine Sulfate Injection is indicated in the palliative treatment of the following: I. Frequently Responsive Malignancies Generalized Hodgkin’s disease (Stages III and IV, Ann Arbor modification of Rye staging system) Lymphocytic lymphoma (nodular and diffuse, poorly and well differentiated) Histiocytic lymphoma Mycosis fungoides (advanced stages) Advanced carcinoma of the testis Kaposi’s sarcoma Letterer-Siwe disease (histiocytosis X) II. Less Frequently Responsive Malignancies Choriocarcinoma resistant to other chemotherapeutic agents Carcinoma of the breast, unresponsive to appropriate endocrine surgery and hormonal therapy Current principles of chemotherapy for many types of cancer include the concurrent administration of several antineoplastic agents. For enhanced therapeutic effect without additive toxicity, agents with different dose-limiting clinical toxicities and different mechanisms of action are generally selected. Therefore, although vinblastine sulfate is effective as a single agent in the aforementioned indications, it is usually administered in combination with other antineoplastic drugs. Such combination therapy produces a greater percentage of response than does a single-agent regimen. These principles have been applied, for example, in the chemotherapy of Hodgkin’s disease. Hodgkin's Disease Vinblastine sulfate has been shown to be one of the most effective single agents for the treatment of Hodgkin’s disease. Advanced Hodgkin’s disease has also been successfully treated with several multiple-drug regimens that included vinblastine sulfate. Patients who had relapses after treatment with the MOPP program— mechlorethamine hydrochloride (nitrogen mustard), vincristine sulfate, prednisone and procarbazine—have likewise responded to combination-drug therapy that included vinblastine sulfate. A protocol using cyclophosphamide in place of nitrogen mustard and vinblastine sulfate instead of vincristine sulfate is an alternative therapy for previously untreated patients with advanced Hodgkin’s disease. Advanced testicular germinal-cell cancers (embryonal carcinoma, teratocarcinoma and choriocarcinoma) are sensitive to vinblastine sulfate alone, but better clinical results are achieved when vinblastine sulfate is administered concomitantly with other antineoplastic agents. The effect of bleomycin is significantly enhanced if vinblastine sulfate is administered six to eight hours prior to the administration of bleomycin; this schedule permits more cells to be arrested during metaphase, the stage of the cell cycle in which bleomycin is active., Hodgkin's Disease Vinblastine sulfate has been shown to be one of the most effective single agents for the treatment of Hodgkin’s disease. Advanced Hodgkin’s disease has also been successfully treated with several multiple-drug regimens that included vinblastine sulfate. Patients who had relapses after treatment with the MOPP program— mechlorethamine hydrochloride (nitrogen mustard), vincristine sulfate, prednisone and procarbazine—have likewise responded to combination-drug therapy that included vinblastine sulfate. A protocol using cyclophosphamide in place of nitrogen mustard and vinblastine sulfate instead of vincristine sulfate is an alternative therapy for previously untreated patients with advanced Hodgkin’s disease. Advanced testicular germinal-cell cancers (embryonal carcinoma, teratocarcinoma and choriocarcinoma) are sensitive to vinblastine sulfate alone, but better clinical results are achieved when vinblastine sulfate is administered concomitantly with other antineoplastic agents. The effect of bleomycin is significantly enhanced if vinblastine sulfate is administered six to eight hours prior to the administration of bleomycin; this schedule permits more cells to be arrested during metaphase, the stage of the cell cycle in which bleomycin is active.

Launch Date

5.46652815E11
Primary
VINBLASTINE SULFATE

Approved Use

Vinblastine Sulfate Injection is indicated in the palliative treatment of the following: I. Frequently Responsive Malignancies Generalized Hodgkin’s disease (Stages III and IV, Ann Arbor modification of Rye staging system) Lymphocytic lymphoma (nodular and diffuse, poorly and well differentiated) Histiocytic lymphoma Mycosis fungoides (advanced stages) Advanced carcinoma of the testis Kaposi’s sarcoma Letterer-Siwe disease (histiocytosis X) II. Less Frequently Responsive Malignancies Choriocarcinoma resistant to other chemotherapeutic agents Carcinoma of the breast, unresponsive to appropriate endocrine surgery and hormonal therapy Current principles of chemotherapy for many types of cancer include the concurrent administration of several antineoplastic agents. For enhanced therapeutic effect without additive toxicity, agents with different dose-limiting clinical toxicities and different mechanisms of action are generally selected. Therefore, although vinblastine sulfate is effective as a single agent in the aforementioned indications, it is usually administered in combination with other antineoplastic drugs. Such combination therapy produces a greater percentage of response than does a single-agent regimen. These principles have been applied, for example, in the chemotherapy of Hodgkin’s disease. Hodgkin's Disease Vinblastine sulfate has been shown to be one of the most effective single agents for the treatment of Hodgkin’s disease. Advanced Hodgkin’s disease has also been successfully treated with several multiple-drug regimens that included vinblastine sulfate. Patients who had relapses after treatment with the MOPP program— mechlorethamine hydrochloride (nitrogen mustard), vincristine sulfate, prednisone and procarbazine—have likewise responded to combination-drug therapy that included vinblastine sulfate. A protocol using cyclophosphamide in place of nitrogen mustard and vinblastine sulfate instead of vincristine sulfate is an alternative therapy for previously untreated patients with advanced Hodgkin’s disease. Advanced testicular germinal-cell cancers (embryonal carcinoma, teratocarcinoma and choriocarcinoma) are sensitive to vinblastine sulfate alone, but better clinical results are achieved when vinblastine sulfate is administered concomitantly with other antineoplastic agents. The effect of bleomycin is significantly enhanced if vinblastine sulfate is administered six to eight hours prior to the administration of bleomycin; this schedule permits more cells to be arrested during metaphase, the stage of the cell cycle in which bleomycin is active., Hodgkin's Disease Vinblastine sulfate has been shown to be one of the most effective single agents for the treatment of Hodgkin’s disease. Advanced Hodgkin’s disease has also been successfully treated with several multiple-drug regimens that included vinblastine sulfate. Patients who had relapses after treatment with the MOPP program— mechlorethamine hydrochloride (nitrogen mustard), vincristine sulfate, prednisone and procarbazine—have likewise responded to combination-drug therapy that included vinblastine sulfate. A protocol using cyclophosphamide in place of nitrogen mustard and vinblastine sulfate instead of vincristine sulfate is an alternative therapy for previously untreated patients with advanced Hodgkin’s disease. Advanced testicular germinal-cell cancers (embryonal carcinoma, teratocarcinoma and choriocarcinoma) are sensitive to vinblastine sulfate alone, but better clinical results are achieved when vinblastine sulfate is administered concomitantly with other antineoplastic agents. The effect of bleomycin is significantly enhanced if vinblastine sulfate is administered six to eight hours prior to the administration of bleomycin; this schedule permits more cells to be arrested during metaphase, the stage of the cell cycle in which bleomycin is active.

Launch Date

5.46652815E11
Primary
VINBLASTINE SULFATE

Approved Use

Vinblastine Sulfate Injection is indicated in the palliative treatment of the following: I. Frequently Responsive Malignancies Generalized Hodgkin’s disease (Stages III and IV, Ann Arbor modification of Rye staging system) Lymphocytic lymphoma (nodular and diffuse, poorly and well differentiated) Histiocytic lymphoma Mycosis fungoides (advanced stages) Advanced carcinoma of the testis Kaposi’s sarcoma Letterer-Siwe disease (histiocytosis X) II. Less Frequently Responsive Malignancies Choriocarcinoma resistant to other chemotherapeutic agents Carcinoma of the breast, unresponsive to appropriate endocrine surgery and hormonal therapy Current principles of chemotherapy for many types of cancer include the concurrent administration of several antineoplastic agents. For enhanced therapeutic effect without additive toxicity, agents with different dose-limiting clinical toxicities and different mechanisms of action are generally selected. Therefore, although vinblastine sulfate is effective as a single agent in the aforementioned indications, it is usually administered in combination with other antineoplastic drugs. Such combination therapy produces a greater percentage of response than does a single-agent regimen. These principles have been applied, for example, in the chemotherapy of Hodgkin’s disease. Hodgkin's Disease Vinblastine sulfate has been shown to be one of the most effective single agents for the treatment of Hodgkin’s disease. Advanced Hodgkin’s disease has also been successfully treated with several multiple-drug regimens that included vinblastine sulfate. Patients who had relapses after treatment with the MOPP program— mechlorethamine hydrochloride (nitrogen mustard), vincristine sulfate, prednisone and procarbazine—have likewise responded to combination-drug therapy that included vinblastine sulfate. A protocol using cyclophosphamide in place of nitrogen mustard and vinblastine sulfate instead of vincristine sulfate is an alternative therapy for previously untreated patients with advanced Hodgkin’s disease. Advanced testicular germinal-cell cancers (embryonal carcinoma, teratocarcinoma and choriocarcinoma) are sensitive to vinblastine sulfate alone, but better clinical results are achieved when vinblastine sulfate is administered concomitantly with other antineoplastic agents. The effect of bleomycin is significantly enhanced if vinblastine sulfate is administered six to eight hours prior to the administration of bleomycin; this schedule permits more cells to be arrested during metaphase, the stage of the cell cycle in which bleomycin is active., Hodgkin's Disease Vinblastine sulfate has been shown to be one of the most effective single agents for the treatment of Hodgkin’s disease. Advanced Hodgkin’s disease has also been successfully treated with several multiple-drug regimens that included vinblastine sulfate. Patients who had relapses after treatment with the MOPP program— mechlorethamine hydrochloride (nitrogen mustard), vincristine sulfate, prednisone and procarbazine—have likewise responded to combination-drug therapy that included vinblastine sulfate. A protocol using cyclophosphamide in place of nitrogen mustard and vinblastine sulfate instead of vincristine sulfate is an alternative therapy for previously untreated patients with advanced Hodgkin’s disease. Advanced testicular germinal-cell cancers (embryonal carcinoma, teratocarcinoma and choriocarcinoma) are sensitive to vinblastine sulfate alone, but better clinical results are achieved when vinblastine sulfate is administered concomitantly with other antineoplastic agents. The effect of bleomycin is significantly enhanced if vinblastine sulfate is administered six to eight hours prior to the administration of bleomycin; this schedule permits more cells to be arrested during metaphase, the stage of the cell cycle in which bleomycin is active.

Launch Date

5.46652815E11
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
26.2 h
10 mg single, intravenous
dose: 10 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
VINBLASTINE serum
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
16.7 h
14 mg single, intravenous
dose: 14 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
VINBLASTINE serum
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
31.4 h
7 mg single, intravenous
dose: 7 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
VINBLASTINE serum
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
1173 min
0.2 mg/kg single, intravenous
dose: 0.2 mg/kg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
VINBLASTINE serum
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
0.3%
VINBLASTINE serum
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
1.1%
VINBLASTINE serum
Homo sapiens
population: UNHEALTHY
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
1.3 mg/m2 1 times / day multiple, intravenous
MTD
Dose: 1.3 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 1.3 mg/m2, 1 times / day
Co-administed with::
valspodar, i.v(10 mg/kg/d)
Sources: Page: p.4727
unhealthy, 18-73
n = 6
Health Status: unhealthy
Condition: Renal Cell Carcinoma
Age Group: 18-73
Sex: M+F
Population Size: 6
Sources: Page: p.4727
DLT: Neutropenia, Ileus...
Dose limiting toxicities:
Neutropenia (grade 4, 16.7%)
Ileus (grade 4, 16.7%)
Sources: Page: p.4727
2.6 mg/m2 1 times / day multiple, intravenous
Studied dose
Dose: 2.6 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 2.6 mg/m2, 1 times / day
Co-administed with::
valspodar, i.v(5 mg/kg/d)
Sources: Page: p.4726
unhealthy, 18-73
n = 3
Health Status: unhealthy
Condition: Renal Cell Carcinoma
Age Group: 18-73
Sex: M+F
Population Size: 3
Sources: Page: p.4726
DLT: Neutropenia, Ileus...
Dose limiting toxicities:
Neutropenia (grade 4, 33.3%)
Ileus (grade 4, 33.3%)
Neutropenic fever (grade 4, 33.3%)
Sources: Page: p.4726
2.6 mg/m2 1 times / day multiple, intravenous
Studied dose
Dose: 2.6 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 2.6 mg/m2, 1 times / day
Co-administed with::
valspodar, i.v(4 mg/kg/d)
Sources: Page: p.4726
unhealthy, 18-73
n = 4
Health Status: unhealthy
Condition: Renal Cell Carcinoma
Age Group: 18-73
Sex: M+F
Population Size: 4
Sources: Page: p.4726
DLT: Neutropenia, Fatigue...
Dose limiting toxicities:
Neutropenia (grade 4, 50%)
Fatigue (grade 3, 25%)
Sources: Page: p.4726
10 mg/m2 1 times / month multiple, intravenous
MTD
Dose: 10 mg/m2, 1 times / month
Route: intravenous
Route: multiple
Dose: 10 mg/m2, 1 times / month
Co-administed with::
cyclosporine, p.o(17 mg/kg/d)
Sources: Page: p.254
unhealthy, 31-70
n = 3
Health Status: unhealthy
Condition: Renal Cell Carcinoma
Age Group: 31-70
Sex: M+F
Population Size: 3
Sources: Page: p.254
DLT: Neutropenia, Sepsis...
Dose limiting toxicities:
Neutropenia (grade 4, 66.7%)
Sepsis (grade 5, 16.7%)
Sources: Page: p.254
AEs

AEs

AESignificanceDosePopulation
Ileus grade 4, 16.7%
DLT
1.3 mg/m2 1 times / day multiple, intravenous
MTD
Dose: 1.3 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 1.3 mg/m2, 1 times / day
Co-administed with::
valspodar, i.v(10 mg/kg/d)
Sources: Page: p.4727
unhealthy, 18-73
n = 6
Health Status: unhealthy
Condition: Renal Cell Carcinoma
Age Group: 18-73
Sex: M+F
Population Size: 6
Sources: Page: p.4727
Neutropenia grade 4, 16.7%
DLT
1.3 mg/m2 1 times / day multiple, intravenous
MTD
Dose: 1.3 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 1.3 mg/m2, 1 times / day
Co-administed with::
valspodar, i.v(10 mg/kg/d)
Sources: Page: p.4727
unhealthy, 18-73
n = 6
Health Status: unhealthy
Condition: Renal Cell Carcinoma
Age Group: 18-73
Sex: M+F
Population Size: 6
Sources: Page: p.4727
Ileus grade 4, 33.3%
DLT
2.6 mg/m2 1 times / day multiple, intravenous
Studied dose
Dose: 2.6 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 2.6 mg/m2, 1 times / day
Co-administed with::
valspodar, i.v(5 mg/kg/d)
Sources: Page: p.4726
unhealthy, 18-73
n = 3
Health Status: unhealthy
Condition: Renal Cell Carcinoma
Age Group: 18-73
Sex: M+F
Population Size: 3
Sources: Page: p.4726
Neutropenia grade 4, 33.3%
DLT
2.6 mg/m2 1 times / day multiple, intravenous
Studied dose
Dose: 2.6 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 2.6 mg/m2, 1 times / day
Co-administed with::
valspodar, i.v(5 mg/kg/d)
Sources: Page: p.4726
unhealthy, 18-73
n = 3
Health Status: unhealthy
Condition: Renal Cell Carcinoma
Age Group: 18-73
Sex: M+F
Population Size: 3
Sources: Page: p.4726
Neutropenic fever grade 4, 33.3%
DLT
2.6 mg/m2 1 times / day multiple, intravenous
Studied dose
Dose: 2.6 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 2.6 mg/m2, 1 times / day
Co-administed with::
valspodar, i.v(5 mg/kg/d)
Sources: Page: p.4726
unhealthy, 18-73
n = 3
Health Status: unhealthy
Condition: Renal Cell Carcinoma
Age Group: 18-73
Sex: M+F
Population Size: 3
Sources: Page: p.4726
Fatigue grade 3, 25%
DLT
2.6 mg/m2 1 times / day multiple, intravenous
Studied dose
Dose: 2.6 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 2.6 mg/m2, 1 times / day
Co-administed with::
valspodar, i.v(4 mg/kg/d)
Sources: Page: p.4726
unhealthy, 18-73
n = 4
Health Status: unhealthy
Condition: Renal Cell Carcinoma
Age Group: 18-73
Sex: M+F
Population Size: 4
Sources: Page: p.4726
Neutropenia grade 4, 50%
DLT
2.6 mg/m2 1 times / day multiple, intravenous
Studied dose
Dose: 2.6 mg/m2, 1 times / day
Route: intravenous
Route: multiple
Dose: 2.6 mg/m2, 1 times / day
Co-administed with::
valspodar, i.v(4 mg/kg/d)
Sources: Page: p.4726
unhealthy, 18-73
n = 4
Health Status: unhealthy
Condition: Renal Cell Carcinoma
Age Group: 18-73
Sex: M+F
Population Size: 4
Sources: Page: p.4726
Neutropenia grade 4, 66.7%
DLT
10 mg/m2 1 times / month multiple, intravenous
MTD
Dose: 10 mg/m2, 1 times / month
Route: intravenous
Route: multiple
Dose: 10 mg/m2, 1 times / month
Co-administed with::
cyclosporine, p.o(17 mg/kg/d)
Sources: Page: p.254
unhealthy, 31-70
n = 3
Health Status: unhealthy
Condition: Renal Cell Carcinoma
Age Group: 31-70
Sex: M+F
Population Size: 3
Sources: Page: p.254
Sepsis grade 5, 16.7%
DLT, Disc. AE
10 mg/m2 1 times / month multiple, intravenous
MTD
Dose: 10 mg/m2, 1 times / month
Route: intravenous
Route: multiple
Dose: 10 mg/m2, 1 times / month
Co-administed with::
cyclosporine, p.o(17 mg/kg/d)
Sources: Page: p.254
unhealthy, 31-70
n = 3
Health Status: unhealthy
Condition: Renal Cell Carcinoma
Age Group: 31-70
Sex: M+F
Population Size: 3
Sources: Page: p.254
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >133 uM]
no
no
no
no
weak [IC50 100 uM]
yes [IC50 21 uM]
yes [IC50 30 uM]
yes [IC50 32 uM]
yes [IC50 35.1 uM]
yes [IC50 43.5 uM]
yes [IC50 46.8 uM]
yes [IC50 62 uM]
yes [Ki 42 uM]
yes
yes
yes
yes
yes
yes (co-administration study)
Comment: Vinblastine increased the median (95% CI) clearance of the CYP3A4 phenotyping probe midazolam from 21.7 L/h (12.6 to 28.1) to 32.3 L/h (17.3 to 53.9) (p = 0.0156, Wilcoxon signed-rank test).
Drug as victim
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Salvage high-dose chemotherapy for children with extragonadal germ-cell tumours.
2005 Aug 22
Chemotherapy: the effect of oral cryotherapy on the development of mucositis.
2005 Jul
Postoperative adjuvant chemotherapy for stage I non-small cell lung cancer.
2005 Jun
Microtubular integrity differentially modifies the saturated and unsaturated fatty acid metabolism in cultured Hep G2 human hepatoma cells.
2005 Oct
Current trends in the management of extra-abdominal desmoid tumours.
2006 Apr 3
[Comparison of TK gene mutation assay in TK6 and TK6-E6 cell induced by vinblastin and colcemid].
2006 Jul
Cytoskeletal architecture differentially controls post-transcriptional processing of IL-6 and IL-8 mRNA in airway epithelial-like cells.
2006 May 15
A novel copper complex induces ROS generation in doxorubicin resistant Ehrlich ascitis carcinoma cells and increases activity of antioxidant enzymes in vital organs in vivo.
2006 Nov 15
[Chemotherapy of advanced non small cell lung cancer: effect on survival and symptoms affecting quality of life].
2007
Will BEACOPP be the standard for high risk Hodgkin lymphoma patients in advanced stages?
2007 Aug
Multi-disciplinary treatment of a rare pelvic cavity ependymoma.
2007 Aug 31
Impact of staging with 18F-FDG-PET on outcome of patients with stage III non-small cell lung cancer: PET identifies potential survivors.
2007 Jan
HIV-1 integrase inhibitors are substrates for the multidrug transporter MDR1-P-glycoprotein.
2007 Mar 7
A case of nodular sclerosis Hodgkin's lymphoma repeatedly relapsing in the context of composite plasma cell-hyaline vascular Castleman's disease: successful response to rituximab and radiotherapy.
2007 Nov
The use of vinca alkaloids in preparation for splenectomy of corticosteroid refractory chronic immune thrombocytopenic purpura patients.
2007 Oct
Intraoperative radiotherapy (IORT) is an option for patients with localized breast recurrences after previous external-beam radiotherapy.
2007 Sep 14
Mitigation of nociception via transganglionic degenerative atrophy: possible mechanism of vinpocetine-induced blockade of retrograde axoplasmic transport.
2008
Vinflunine in the treatment of bladder cancer.
2008 Dec
Efficiency of propolis extract against mitochondrial stress induced by antineoplasic agents (doxorubicin and vinblastin) in rats.
2008 Feb
The effect of platelet autoantibodies on the course of the disease and clinical response of patients with idiopathic thrombocytopenic purpura.
2008 Feb
Subdural effusion in a CNS involvement of systemic juvenile xanthogranuloma: a case report treated with vinblastin.
2008 Feb
Treatment of locally advanced and metastatic bladder cancer.
2008 Jan
A review on plant-derived natural products and their analogs with anti-tumor activity.
2008 Mar
Natural and synthetic polymers as inhibitors of drug efflux pumps.
2008 Mar
[Metastases from urethelial carcinoma: role of chemotherapy].
2008 Nov
[Squamous cell carcinoma of the renal pelvis with elevation of G-CSF in the serum: a case report].
2008 Nov
Anterior segment manifestations of human immunodeficiency virus/acquired immune deficiency syndrome.
2008 Sep-Oct
Identifying tumor stem-like cells in mouse melanoma cell lines by analyzing the characteristics of side population cells.
2009 Aug
Valvular dysfunction and left ventricular changes in Hodgkin's lymphoma survivors. A longitudinal study.
2009 Aug 18
rac-Methyl 4-azido-3-hydr-oxy-3-(2-nitro-phen-yl)butanoate.
2009 Jan 28
New approaches for cancer treatment: antitumor drugs based on gene-targeted nucleic acids.
2009 Jul
Chemomodulation of human dendritic cell function by antineoplastic agents in low noncytotoxic concentrations.
2009 Jul 10
Micropapillary bladder cancer: a review of Léon Bérard Cancer Center experience.
2009 Jun 17
Construction of a model cell line for the assay of MDR1 (multi drug resistance gene-1) substrates/inhibitors using HeLa cells.
2009 May
Initiation of hepatitis C virus infection requires the dynamic microtubule network: role of the viral nucleocapsid protein.
2009 May 15
Reciprocal competition between lipid nanocapsules and P-gp for paclitaxel transport across Caco-2 cells.
2010 Aug 11
Long term outcome of adolescent and adult patients with pineal parenchymal tumors treated with fractionated radiotherapy between 1982 and 2003--a single institution's experience.
2010 Dec 26
Recent strategy for the management of advanced testicular cancer.
2010 Feb
Retrospective French nationwide survey of childhood aggressive vascular anomalies of bone, 1988-2009.
2010 Feb 3
Hodgkin's lymphoma presenting with heart failure: a case report.
2010 Jan 20
Simple and reproducible HPLC-DAD-ESI-MS/MS analysis of alkaloids in Catharanthus roseus roots.
2010 Jan 5
Distinct roles for Dectin-1 and TLR4 in the pathogenesis of Aspergillus fumigatus keratitis.
2010 Jul 1
A screen for kinetochore-microtubule interaction inhibitors identifies novel antitubulin compounds.
2010 Jul 15
Cutaneous lesions of the nose.
2010 Jun 4
Primary pure gastric yolk sac tumor.
2010 Mar 31
(2E,4E)-1-(6-Chloro-2-methyl-4-phenyl-3-quinol-yl)-5-phenyl-penta-2,4-dien-1-one.
2010 May 12
Antinociceptive effect of vinpocetine--a comprehensive survey.
2010 May 30
Factors influencing overall survival rates for patients with pineocytoma.
2010 Nov
Retroperitoneal lymph node dissection for residual masses after chemotherapy in nonseminomatous germ cell testicular tumor.
2010 Nov 9
Proteomic analysis of annexin A2 phosphorylation induced by microtubule interfering agents and kinesin spindle protein inhibitors.
2010 Sep 3
Patents

Sample Use Guides

It is wise to initiate therapy for adults by administering a single intravenous dose of 3.7 mg/m2 of body surface area (bsa). Thereafter, white-blood-cell counts should be made to determine the patient’s sensitivity to vinblastine sulfate. A simplified and conservative incremental approach to dosage at weekly intervals for adults may be outlined as follows: First dose ........................... 3.7 mg/m2 bsa Second dose ........................... 5.5 mg/m2 bsa Third dose ........................... 7.4 mg/m2 bsa Fourth dose ........................... 9.25 mg/m2 bsa Fifth dose ........................... 11.1 mg/m2 bsa The above-mentioned increases may be used until a maximum dose not exceeding 18.5 mg/m2 bsa for adults is reached. The dose should not be increased after that dose which reduces the white-cell count to approximately 3000 cells/mm3 . In some adults, 3.7 mg/m2 bsa may produce this leukopenia; other adults may require more than 11.1 mg/m2 bsa; and, very rarely, as much as 18.5 mg/m2 bsa may be necessary. For most adult patients, however, the weekly dosage will prove to be 5.5 to 7.4 mg/m2 bsa. When the dose of vinblastine sulfate which will produce the above degree of leukopenia has been established, a dose of 1 increment smaller than this should be administered at weekly intervals for maintenance. Thus, the patient is receiving the maximum dose that does not cause leukopenia. It should be emphasized that, even though 7 days have elapsed, the next dose of vinblastine sulfate should not be given until the white-cell count has returned to at least 4000/mm3. In some cases, oncolytic activity may be encountered before leukopenic effect. When this occurs, there is no need to increase the size of the subsequent doses
Route of Administration: Intravenous
15 nM vinblastine inhibit CHO cell proliferation
Substance Class Chemical
Created
by admin
on Sat Jun 26 10:00:19 UTC 2021
Edited
by admin
on Sat Jun 26 10:00:19 UTC 2021
Record UNII
5V9KLZ54CY
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
VINBLASTINE
HSDB   INN   MI   VANDF   WHO-DD  
INN  
Official Name English
VINBLASTINE [WHO-DD]
Common Name English
VINBLASTINE [VANDF]
Common Name English
VINBLASTINE [INN]
Common Name English
VINBLASTINA
Brand Name English
NSC-47842
Code English
VINBLASTINE [HSDB]
Common Name English
VINCRISTINE SULFATE IMPURITY H [EP]
Common Name English
VINDESINE SULFATE IMPURITY B [EP]
Common Name English
VINBLASTINE [MI]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C932
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
WHO-VATC QL01CA01
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
LIVERTOX 1029
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
NDF-RT N0000007780
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
NDF-RT N0000007780
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
NDF-RT N0000175612
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
WHO-ESSENTIAL MEDICINES LIST 8.2
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
WHO-ATC L01CA01
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
EPA PESTICIDE CODE 600072
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
NCI_THESAURUS C67422
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
Code System Code Type Description
ChEMBL
CHEMBL159
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
PRIMARY
FDA UNII
5V9KLZ54CY
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
PRIMARY
DRUG CENTRAL
2823
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
PRIMARY
DRUG BANK
DB00570
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
PRIMARY
PUBCHEM
13342
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
PRIMARY
HSDB
3263
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
PRIMARY
MESH
D014747
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
PRIMARY
MERCK INDEX
M11449
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
PRIMARY Merck Index
ECHA (EC/EINECS)
212-734-0
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
PRIMARY
LACTMED
Vinblastine
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
PRIMARY
EVMPD
SUB00052MIG
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
PRIMARY
IUPHAR
6851
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
PRIMARY
NCI_THESAURUS
C930
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
PRIMARY
CAS
865-21-4
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
PRIMARY
RXCUI
11198
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
PRIMARY RxNorm
WIKIPEDIA
VINBLASTINE
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
PRIMARY
EPA CompTox
865-21-4
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
PRIMARY
INN
1101
Created by admin on Sat Jun 26 10:00:19 UTC 2021 , Edited by admin on Sat Jun 26 10:00:19 UTC 2021
PRIMARY
Related Record Type Details
TRANSPORTER -> SUBSTRATE
SALT/SOLVATE -> PARENT
TRANSPORTER -> SUBSTRATE
Related Record Type Details
PARENT -> IMPURITY
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
PARENT -> IMPURITY
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Route of Elimination PHARMACOKINETIC
Route of Elimination PHARMACOKINETIC