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

1987
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

1987
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

1987
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

1987
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

1987
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

1987
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
[Clinical evaluation of the efficacy of modern first, second, and third line regimes of chemotherapy in patients with disseminated cutaneous melanoma].
2001
P-Glycoprotein conformational changes detected by antibody competition.
2001 Apr
[Treatment of germ cell tumors at the threshold of the third millennium].
2001 Aug 5
Chemotherapy versus best supportive care in stage IV non-small cell lung cancer, non metastatic to the brain.
2001 Mar-Apr
[High-dose chemotherapy with peripheral blood stem cell transplantation for advanced testicular cancer].
2002 Aug
Malignant germ cell tumors: clinical characteristics, treatment, and outcome. A report from the study group for Pediatric Solid Malignant Tumors in the Kyushu Area, Japan.
2002 Dec
5-fluorouracil-Induced cardiotoxicity.
2002 Jan-Feb
[Cerebellar, pulmonary and cutaneous localizations of juvenile xanthogranuloma].
2002 Mar
[Results of organ-preserving therapy for invasive bladder cancer].
2002 May-Jun
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
[Diagnostic difficulties in primary mesothelioma].
2004
Development and characterization of an open tubular column containing immobilized P-glycoprotein for rapid on-line screening for P-glycoprotein substrates.
2004 Jan 25
Crystal structure of vinorine synthase, the first representative of the BAHD superfamily.
2005 Apr 8
Chemotherapy: the effect of oral cryotherapy on the development of mucositis.
2005 Jul
Microtubular integrity differentially modifies the saturated and unsaturated fatty acid metabolism in cultured Hep G2 human hepatoma cells.
2005 Oct
[Ten-year outcomes of lymphogranulomatosis treatment according to the protocol MOPP-ABVD+radiotherapy].
2006
CD40L induces multidrug resistance to apoptosis in breast carcinoma and lymphoma cells through caspase independent and dependent pathways.
2006 Mar 18
Cytoskeletal architecture differentially controls post-transcriptional processing of IL-6 and IL-8 mRNA in airway epithelial-like cells.
2006 May 15
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
Primary malignant teratoma with a primitive neuroectodermal tumor component in thyroid gland: a case report.
2007 Jun
A review of topotecan in combination chemotherapy for advanced cervical cancer.
2008 Feb
The effect of platelet autoantibodies on the course of the disease and clinical response of patients with idiopathic thrombocytopenic purpura.
2008 Feb
Treatment of locally advanced and metastatic bladder cancer.
2008 Jan
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
[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
rac-Methyl 4-azido-3-hydr-oxy-3-(2-nitro-phen-yl)butanoate.
2009 Jan 28
Chemomodulation of human dendritic cell function by antineoplastic agents in low noncytotoxic concentrations.
2009 Jul 10
Summary of the american college for advancement in medicine november 2007 conference on integrative medicine: advancing science and clinical practice.
2009 Sep
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
Simple and reproducible HPLC-DAD-ESI-MS/MS analysis of alkaloids in Catharanthus roseus roots.
2010 Jan 5
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 15 14:59:50 GMT 2023
Edited
by admin
on Fri Dec 15 14:59:50 GMT 2023
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 15 14:59:50 GMT 2023 , Edited by admin on Fri Dec 15 14:59:50 GMT 2023
FDA ORPHAN DRUG 867921
Created by admin on Fri Dec 15 14:59:50 GMT 2023 , Edited by admin on Fri Dec 15 14:59:50 GMT 2023
NCI_THESAURUS C932
Created by admin on Fri Dec 15 14:59:50 GMT 2023 , Edited by admin on Fri Dec 15 14:59:50 GMT 2023
Code System Code Type Description
WHO INTERNATIONAL PHARMACOPEIA
VINBLASTINE SULFATE
Created by admin on Fri Dec 15 14:59:50 GMT 2023 , Edited by admin on Fri Dec 15 14:59:50 GMT 2023
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 15 14:59:50 GMT 2023 , Edited by admin on Fri Dec 15 14:59:50 GMT 2023
PRIMARY
RS_ITEM_NUM
1713004
Created by admin on Fri Dec 15 14:59:50 GMT 2023 , Edited by admin on Fri Dec 15 14:59:50 GMT 2023
PRIMARY
SMS_ID
100000087899
Created by admin on Fri Dec 15 14:59:50 GMT 2023 , Edited by admin on Fri Dec 15 14:59:50 GMT 2023
PRIMARY
FDA UNII
N00W22YO2B
Created by admin on Fri Dec 15 14:59:50 GMT 2023 , Edited by admin on Fri Dec 15 14:59:50 GMT 2023
PRIMARY
RXCUI
11199
Created by admin on Fri Dec 15 14:59:50 GMT 2023 , Edited by admin on Fri Dec 15 14:59:50 GMT 2023
PRIMARY RxNorm
MERCK INDEX
m11449
Created by admin on Fri Dec 15 14:59:50 GMT 2023 , Edited by admin on Fri Dec 15 14:59:50 GMT 2023
PRIMARY Merck Index
EPA CompTox
DTXSID601017133
Created by admin on Fri Dec 15 14:59:50 GMT 2023 , Edited by admin on Fri Dec 15 14:59:50 GMT 2023
PRIMARY
NSC
49842
Created by admin on Fri Dec 15 14:59:50 GMT 2023 , Edited by admin on Fri Dec 15 14:59:50 GMT 2023
PRIMARY
EVMPD
SUB05098MIG
Created by admin on Fri Dec 15 14:59:50 GMT 2023 , Edited by admin on Fri Dec 15 14:59:50 GMT 2023
PRIMARY
DAILYMED
N00W22YO2B
Created by admin on Fri Dec 15 14:59:50 GMT 2023 , Edited by admin on Fri Dec 15 14:59:50 GMT 2023
PRIMARY
ECHA (EC/EINECS)
205-606-0
Created by admin on Fri Dec 15 14:59:50 GMT 2023 , Edited by admin on Fri Dec 15 14:59:50 GMT 2023
PRIMARY
DRUG BANK
DBSALT000644
Created by admin on Fri Dec 15 14:59:50 GMT 2023 , Edited by admin on Fri Dec 15 14:59:50 GMT 2023
PRIMARY
CAS
143-67-9
Created by admin on Fri Dec 15 14:59:50 GMT 2023 , Edited by admin on Fri Dec 15 14:59:50 GMT 2023
PRIMARY
CHEBI
9984
Created by admin on Fri Dec 15 14:59:50 GMT 2023 , Edited by admin on Fri Dec 15 14:59:50 GMT 2023
PRIMARY
PUBCHEM
5388983
Created by admin on Fri Dec 15 14:59:50 GMT 2023 , Edited by admin on Fri Dec 15 14:59:50 GMT 2023
PRIMARY
ChEMBL
CHEMBL159
Created by admin on Fri Dec 15 14:59:50 GMT 2023 , Edited by admin on Fri Dec 15 14:59:50 GMT 2023
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE
Related Record Type Details
ACTIVE MOIETY