U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C46H58N4O9.H2O4S
Molecular Weight 909.053
Optical Activity UNSPECIFIED
Defined Stereocenters 9 / 9
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of VINBLASTINE SULFATE

SMILES

OS(O)(=O)=O.[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(C[C@](O)(CC)C7)CCC8=C6NC9=C8C=CC=C9)C(=O)OC

InChI

InChIKey=KDQAABAKXDWYSZ-PNYVAJAMSA-N
InChI=1S/C46H58N4O9.H2O4S/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;1-5(2,3)4/h10-14,16,21-22,28,37-39,47,54-55H,8-9,15,17-20,23-26H2,1-7H3;(H2,1,2,3,4)/t28-,37-,38+,39+,42-,43+,44+,45-,46-;/m0./s1

HIDE SMILES / InChI

Molecular Formula C46H58N4O9
Molecular Weight 810.9741
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 8 / 9
E/Z Centers 0
Optical Activity UNSPECIFIED

Molecular Formula H2O4S
Molecular Weight 98.078
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

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
[High-dose chemotherapy with peripheral blood stem cell transplantation for advanced testicular cancer].
2002 Aug
5-fluorouracil-Induced cardiotoxicity.
2002 Jan-Feb
The role of combined method in organ-sparing treatment of muscle-invasive bladder cancer recurrences.
2002 Jun
[Results of organ-preserving therapy for invasive bladder cancer].
2002 May-Jun
Metastatic renal clear cell carcinoma mimicking stage IV lung cancer.
2003
NOVP chemotherapy for Hodgkin's disease transiently induces sperm aneuploidies associated with the major clinical aneuploidy syndromes involving chromosomes X, Y, 18, and 21.
2003 Jan 1
Chemotherapy for malignant pleural mesothelioma: past results and recent developments.
2003 Jan 27
Improved survival in HIV-related Hodgkin's lymphoma since the introduction of highly active antiretroviral therapy.
2003 Jan 3
Hepatic reticuloendothelial system dysfunction after ischemia-reperfusion: role of P-selectin-mediated neutrophil accumulation.
2003 Sep
[Clinical study of Hodgkin's disease after 25 years].
2004
Cisplatin-induced apoptosis in human malignant testicular germ cell lines depends on MEK/ERK activation.
2004 Aug 2
The use of vinca alkaloids in adult patients with refractory chronic idiopathic thrombocytopenia.
2004 Dec
Dynamic targeting of microtubules by TPPP/p25 affects cell survival.
2004 Dec 1
Aggresomes formed by alpha-synuclein and synphilin-1 are cytoprotective.
2004 Feb 6
Development and characterization of an open tubular column containing immobilized P-glycoprotein for rapid on-line screening for P-glycoprotein substrates.
2004 Jan 25
Resistance to microtubule-targeted cytotoxins in a K562 leukemia cell variant associated with altered tubulin expression and polymerization.
2004 May
Tissue-specificity of apoptosis in hepatoma-derived cell lines.
2004 May
Anticancer agents are potent neurotoxins in vitro and in vivo.
2004 Sep
Development and characterization of an immobilized human organic cation transporter based liquid chromatographic stationary phase.
2005 Apr 25
Crystal structure of vinorine synthase, the first representative of the BAHD superfamily.
2005 Apr 8
Mitomycin C, vinblastine and cisplatin (MVP): an active and well-tolerated salvage regimen for advanced breast cancer.
2005 Feb 14
[A case of an asynchronic triple tumorous disorder: a rectal adenocarcinoma, a carcinoma of the kidney and a prostatic adenocarcinoma--case report].
2005 Jan
[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
[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
In silico prediction of pregnane X receptor activators by machine learning approaches.
2007 Jan
Primary malignant teratoma with a primitive neuroectodermal tumor component in thyroid gland: a case report.
2007 Jun
HIV-1 integrase inhibitors are substrates for the multidrug transporter MDR1-P-glycoprotein.
2007 Mar 7
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
A review of topotecan in combination chemotherapy for advanced cervical cancer.
2008 Feb
Efficiency of propolis extract against mitochondrial stress induced by antineoplasic agents (doxorubicin and vinblastin) in rats.
2008 Feb
Subdural effusion in a CNS involvement of systemic juvenile xanthogranuloma: a case report treated with vinblastin.
2008 Feb
Wound healing in patients with cancer.
2008 Jan 11
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
[Squamous cell carcinoma of the renal pelvis with elevation of G-CSF in the serum: a case report].
2008 Nov
Valvular dysfunction and left ventricular changes in Hodgkin's lymphoma survivors. A longitudinal study.
2009 Aug 18
New approaches for cancer treatment: antitumor drugs based on gene-targeted nucleic acids.
2009 Jul
Initiation of hepatitis C virus infection requires the dynamic microtubule network: role of the viral nucleocapsid protein.
2009 May 15
Summary of the american college for advancement in medicine november 2007 conference on integrative medicine: advancing science and clinical practice.
2009 Sep
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
A screen for kinetochore-microtubule interaction inhibitors identifies novel antitubulin compounds.
2010 Jul 15
Cutaneous lesions of the nose.
2010 Jun 4
(2E,4E)-1-(6-Chloro-2-methyl-4-phenyl-3-quinol-yl)-5-phenyl-penta-2,4-dien-1-one.
2010 May 12
Factors influencing overall survival rates for patients with pineocytoma.
2010 Nov
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 Fri Dec 16 15:52:34 UTC 2022
Edited
by admin
on Fri Dec 16 15:52:34 UTC 2022
Record UNII
N00W22YO2B
Record Status Validated (UNII)
Record Version
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Name Type Language
VINBLASTINE SULFATE
EP   MART.   MI   ORANGE BOOK   USAN   USP   USP-RS   VANDF   WHO-DD   WHO-IP  
USAN  
Official Name English
NSC-49842
Code English
VINBLASTINE SULFATE [USP-RS]
Common Name English
29060LE
Code English
VINBLASTINE SULFATE [MART.]
Common Name English
ALKABAN-AQ
Common Name English
VLB MONOSULFATE
Common Name English
VINBLASTINE SULFATE [IARC]
Common Name English
29060-LE
Code English
VINBLASTINE SULPHATE
Common Name English
VINBLASTINE SULFATE [USP MONOGRAPH]
Common Name English
VINCALEUKOBLASTINE, SULFATE (1:1) (SALT)
Common Name English
VINBLASTINE SULFATE [WHO-IP]
Common Name English
VINBLASTINE SULFATE [ORANGE BOOK]
Common Name English
Vinblastine sulfate [WHO-DD]
Common Name English
VINBLASTINE SULFATE [MI]
Common Name English
VELBAN
Brand Name English
VINBLASTINI SULFAS [WHO-IP LATIN]
Common Name English
VINCALEUKOBLASTINE SULFATE
Common Name English
VINBLASTINE SULFATE [EP MONOGRAPH]
Common Name English
VINBLASTINE SULFATE [USAN]
Common Name English
VINBLASTINE SULFATE [JAN]
Common Name English
VINBLASTINE SULFATE [VANDF]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C67422
Created by admin on Fri Dec 16 15:52:34 UTC 2022 , Edited by admin on Fri Dec 16 15:52:34 UTC 2022
FDA ORPHAN DRUG 867921
Created by admin on Fri Dec 16 15:52:34 UTC 2022 , Edited by admin on Fri Dec 16 15:52:34 UTC 2022
NCI_THESAURUS C932
Created by admin on Fri Dec 16 15:52:34 UTC 2022 , Edited by admin on Fri Dec 16 15:52:34 UTC 2022
Code System Code Type Description
WHO INTERNATIONAL PHARMACOPEIA
VINBLASTINE SULFATE
Created by admin on Fri Dec 16 15:52:34 UTC 2022 , Edited by admin on Fri Dec 16 15:52:34 UTC 2022
PRIMARY Description: A white to slightly yellow, amorphous or crystalline powder. Solubility: Freely soluble in water; very slightly soluble in ethanol (~750 g/l) TS; practically insoluble in ether R. Category: Cytotoxic drug. Storage: Vinblastine sulfate should be kept in a tightly closed container, protected from light, and stored at a temperature between 2 and 8 ?C. Additional information: CAUTION: Vinblastine sulfate must be handled with care, avoiding contact with the skin and inhalation of airborne particles. It is very hygroscopic and unstable. Before the bottle is opened, it should be allowed to come to room temperature in a desiccator. Requirement: Vinblastine sulfate contains not less than 96.0% and not more than the equivalent of 101.0% of C46H58N4O9,H2SO4, calculated with reference to the dried substance.
NCI_THESAURUS
C931
Created by admin on Fri Dec 16 15:52:34 UTC 2022 , Edited by admin on Fri Dec 16 15:52:34 UTC 2022
PRIMARY
RS_ITEM_NUM
1713004
Created by admin on Fri Dec 16 15:52:34 UTC 2022 , Edited by admin on Fri Dec 16 15:52:34 UTC 2022
PRIMARY
FDA UNII
N00W22YO2B
Created by admin on Fri Dec 16 15:52:34 UTC 2022 , Edited by admin on Fri Dec 16 15:52:34 UTC 2022
PRIMARY
RXCUI
11199
Created by admin on Fri Dec 16 15:52:34 UTC 2022 , Edited by admin on Fri Dec 16 15:52:34 UTC 2022
PRIMARY RxNorm
MERCK INDEX
M11449
Created by admin on Fri Dec 16 15:52:34 UTC 2022 , Edited by admin on Fri Dec 16 15:52:34 UTC 2022
PRIMARY Merck Index
EPA CompTox
DTXSID601017133
Created by admin on Fri Dec 16 15:52:34 UTC 2022 , Edited by admin on Fri Dec 16 15:52:34 UTC 2022
PRIMARY
NSC
49842
Created by admin on Fri Dec 16 15:52:34 UTC 2022 , Edited by admin on Fri Dec 16 15:52:34 UTC 2022
PRIMARY
EVMPD
SUB05098MIG
Created by admin on Fri Dec 16 15:52:34 UTC 2022 , Edited by admin on Fri Dec 16 15:52:34 UTC 2022
PRIMARY
DAILYMED
N00W22YO2B
Created by admin on Fri Dec 16 15:52:34 UTC 2022 , Edited by admin on Fri Dec 16 15:52:34 UTC 2022
PRIMARY
ECHA (EC/EINECS)
205-606-0
Created by admin on Fri Dec 16 15:52:34 UTC 2022 , Edited by admin on Fri Dec 16 15:52:34 UTC 2022
PRIMARY
DRUG BANK
DBSALT000644
Created by admin on Fri Dec 16 15:52:34 UTC 2022 , Edited by admin on Fri Dec 16 15:52:34 UTC 2022
PRIMARY
CAS
143-67-9
Created by admin on Fri Dec 16 15:52:34 UTC 2022 , Edited by admin on Fri Dec 16 15:52:34 UTC 2022
PRIMARY
CHEBI
9984
Created by admin on Fri Dec 16 15:52:34 UTC 2022 , Edited by admin on Fri Dec 16 15:52:34 UTC 2022
PRIMARY
PUBCHEM
5388983
Created by admin on Fri Dec 16 15:52:34 UTC 2022 , Edited by admin on Fri Dec 16 15:52:34 UTC 2022
PRIMARY
ChEMBL
CHEMBL159
Created by admin on Fri Dec 16 15:52:34 UTC 2022 , Edited by admin on Fri Dec 16 15:52:34 UTC 2022
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE
Related Record Type Details
ACTIVE MOIETY