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
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
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 |
DescriptionCurator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/24404355
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24404355
Curator's Comment: 1950s
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | VINBLASTINE SULFATE Approved UseVinblastine 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 Date1987 |
|||
Primary | VINBLASTINE SULFATE Approved UseVinblastine 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 Date1987 |
|||
Primary | VINBLASTINE SULFATE Approved UseVinblastine 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 Date1987 |
|||
Primary | VINBLASTINE SULFATE Approved UseVinblastine 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 Date1987 |
|||
Primary | VINBLASTINE SULFATE Approved UseVinblastine 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 Date1987 |
|||
Primary | VINBLASTINE SULFATE Approved UseVinblastine 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 Date1987 |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
26.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7070351/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7070351/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7070351/ |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/889590/ |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
0.3% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/6873152/ |
VINBLASTINE serum | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
||
1.1% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/6873152/ |
VINBLASTINE serum | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse 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%) Sources: Page: p.4727Ileus (grade 4, 16.7%) |
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%) Sources: Page: p.4726Ileus (grade 4, 33.3%) Neutropenic fever (grade 4, 33.3%) |
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%) Sources: Page: p.4726Fatigue (grade 3, 25%) |
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%) Sources: Page: p.254Sepsis (grade 5, 16.7%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical 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] | ||||
Sources: https://pubmed.ncbi.nlm.nih.gov/31155684/ |
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
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
yes [Km 137.3 uM] | ||||
yes [Km 89.2 uM] | ||||
yes | ||||
yes | ||||
yes | ||||
yes | yes (co-administration study) Comment: Enhanced toxicity has been reported in patients receiving concomitant erythromycin |
PubMed
Title | Date | PubMed |
---|---|---|
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 |
|
[Results of organ-preserving therapy for invasive bladder cancer]. | 2002 May-Jun |
|
Metastatic renal clear cell carcinoma mimicking stage IV lung cancer. | 2003 |
|
[Diagnostic difficulties in primary mesothelioma]. | 2004 |
|
Aggresomes formed by alpha-synuclein and synphilin-1 are cytoprotective. | 2004 Feb 6 |
|
Resistance to microtubule-targeted cytotoxins in a K562 leukemia cell variant associated with altered tubulin expression and polymerization. | 2004 May |
|
Anticancer agents are potent neurotoxins in vitro and in vivo. | 2004 Sep |
|
Salvage high-dose chemotherapy for children with extragonadal germ-cell tumours. | 2005 Aug 22 |
|
Mitomycin C, vinblastine and cisplatin (MVP): an active and well-tolerated salvage regimen for advanced breast cancer. | 2005 Feb 14 |
|
Radiation-induced leiomyosarcoma of the oropharynx. | 2006 Aug 22 |
|
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 |
|
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 |
|
Primary malignant teratoma with a primitive neuroectodermal tumor component in thyroid gland: a case report. | 2007 Jun |
|
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 |
|
Subdural effusion in a CNS involvement of systemic juvenile xanthogranuloma: a case report treated with vinblastin. | 2008 Feb |
|
Kaposi's sarcoma of the hand mimicking squamous cell carcinoma in a woman with no evidence of HIV infection: a case report. | 2008 Jun 19 |
|
A review on plant-derived natural products and their analogs with anti-tumor activity. | 2008 Mar |
|
[Metastases from urethelial carcinoma: role of chemotherapy]. | 2008 Nov |
|
Anterior segment manifestations of human immunodeficiency virus/acquired immune deficiency syndrome. | 2008 Sep-Oct |
|
Valvular dysfunction and left ventricular changes in Hodgkin's lymphoma survivors. A longitudinal study. | 2009 Aug 18 |
|
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 |
|
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 |
|
Simple and reproducible HPLC-DAD-ESI-MS/MS analysis of alkaloids in Catharanthus roseus roots. | 2010 Jan 5 |
|
A screen for kinetochore-microtubule interaction inhibitors identifies novel antitubulin compounds. | 2010 Jul 15 |
|
Primary pure gastric yolk sac tumor. | 2010 Mar 31 |
|
Antinociceptive effect of vinpocetine--a comprehensive survey. | 2010 May 30 |
|
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
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20696757
15 nM vinblastine inhibit CHO cell proliferation
Substance Class |
Chemical
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C67422
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FDA ORPHAN DRUG |
867921
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NCI_THESAURUS |
C932
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VINBLASTINE SULFATE
Created by
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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. | ||
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C931
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1713004
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11199
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m11449
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DTXSID601017133
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CHEMBL159
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ACTIVE MOIETY |