Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C46H58N4O9 |
Molecular Weight | 810.9741 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 9 / 9 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12N3CC[C@@]14C5=CC(=C(OC)C=C5N(C)[C@@]4([H])[C@](O)([C@H](OC(C)=O)[C@]2(CC)C=CC3)C(=O)OC)[C@]6(C[C@@]7([H])CN(C[C@](O)(CC)C7)CCC8=C6NC9=C8C=CC=C9)C(=O)OC
InChI
InChIKey=JXLYSJRDGCGARV-CFWMRBGOSA-N
InChI=1S/C46H58N4O9/c1-8-42(54)23-28-24-45(40(52)57-6,36-30(15-19-49(25-28)26-42)29-13-10-11-14-33(29)47-36)32-21-31-34(22-35(32)56-5)48(4)38-44(31)17-20-50-18-12-16-43(9-2,37(44)50)39(59-27(3)51)46(38,55)41(53)58-7/h10-14,16,21-22,28,37-39,47,54-55H,8-9,15,17-20,23-26H2,1-7H3/t28-,37-,38+,39+,42-,43+,44+,45-,46-/m0/s1
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 |
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 |
---|---|---|
Microtubular integrity differentially modifies the saturated and unsaturated fatty acid metabolism in cultured Hep G2 human hepatoma cells. | 2005 Oct |
|
Reversal of P-glycoprotein-dependent resistance to vinblastine by newly synthesized bisbenzylisoquinoline alkaloids in mouse leukemia P388 cells. | 2005 Oct |
|
Radiation-induced leiomyosarcoma of the oropharynx. | 2006 Aug 22 |
|
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 |
|
[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 |
|
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 |
|
[Influence of antitumor preparations on the concentration of free radicals in cells of Fusarium bulbigenum var. blasticola fungus during primary and tumour-like secondary growth]. | 2007 Mar-Apr |
|
A case of nodular sclerosis Hodgkin's lymphoma repeatedly relapsing in the context of composite plasma cell-hyaline vascular Castleman's disease: successful response to rituximab and radiotherapy. | 2007 Nov |
|
The use of vinca alkaloids in preparation for splenectomy of corticosteroid refractory chronic immune thrombocytopenic purpura patients. | 2007 Oct |
|
Intraoperative radiotherapy (IORT) is an option for patients with localized breast recurrences after previous external-beam radiotherapy. | 2007 Sep 14 |
|
Mitigation of nociception via transganglionic degenerative atrophy: possible mechanism of vinpocetine-induced blockade of retrograde axoplasmic transport. | 2008 |
|
Vinflunine in the treatment of bladder cancer. | 2008 Dec |
|
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 |
|
The effect of platelet autoantibodies on the course of the disease and clinical response of patients with idiopathic thrombocytopenic purpura. | 2008 Feb |
|
Subdural effusion in a CNS involvement of systemic juvenile xanthogranuloma: a case report treated with vinblastin. | 2008 Feb |
|
Treatment of locally advanced and metastatic bladder cancer. | 2008 Jan |
|
Wound healing in patients with cancer. | 2008 Jan 11 |
|
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 |
|
Natural and synthetic polymers as inhibitors of drug efflux pumps. | 2008 Mar |
|
[Metastases from urethelial carcinoma: role of chemotherapy]. | 2008 Nov |
|
[Squamous cell carcinoma of the renal pelvis with elevation of G-CSF in the serum: a case report]. | 2008 Nov |
|
Anterior segment manifestations of human immunodeficiency virus/acquired immune deficiency syndrome. | 2008 Sep-Oct |
|
Identifying tumor stem-like cells in mouse melanoma cell lines by analyzing the characteristics of side population cells. | 2009 Aug |
|
Valvular dysfunction and left ventricular changes in Hodgkin's lymphoma survivors. A longitudinal study. | 2009 Aug 18 |
|
rac-Methyl 4-azido-3-hydr-oxy-3-(2-nitro-phen-yl)butanoate. | 2009 Jan 28 |
|
New approaches for cancer treatment: antitumor drugs based on gene-targeted nucleic acids. | 2009 Jul |
|
Chemomodulation of human dendritic cell function by antineoplastic agents in low noncytotoxic concentrations. | 2009 Jul 10 |
|
Micropapillary bladder cancer: a review of Léon Bérard Cancer Center experience. | 2009 Jun 17 |
|
Construction of a model cell line for the assay of MDR1 (multi drug resistance gene-1) substrates/inhibitors using HeLa cells. | 2009 May |
|
Initiation of hepatitis C virus infection requires the dynamic microtubule network: role of the viral nucleocapsid protein. | 2009 May 15 |
|
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 |
|
Recent strategy for the management of advanced testicular cancer. | 2010 Feb |
|
Retrospective French nationwide survey of childhood aggressive vascular anomalies of bone, 1988-2009. | 2010 Feb 3 |
|
Hodgkin's lymphoma presenting with heart failure: a case report. | 2010 Jan 20 |
|
Simple and reproducible HPLC-DAD-ESI-MS/MS analysis of alkaloids in Catharanthus roseus roots. | 2010 Jan 5 |
|
Distinct roles for Dectin-1 and TLR4 in the pathogenesis of Aspergillus fumigatus keratitis. | 2010 Jul 1 |
|
A screen for kinetochore-microtubule interaction inhibitors identifies novel antitubulin compounds. | 2010 Jul 15 |
|
Cutaneous lesions of the nose. | 2010 Jun 4 |
|
Primary pure gastric yolk sac tumor. | 2010 Mar 31 |
|
(2E,4E)-1-(6-Chloro-2-methyl-4-phenyl-3-quinol-yl)-5-phenyl-penta-2,4-dien-1-one. | 2010 May 12 |
|
Antinociceptive effect of vinpocetine--a comprehensive survey. | 2010 May 30 |
|
Retroperitoneal lymph node dissection for residual masses after chemotherapy in nonseminomatous germ cell testicular tumor. | 2010 Nov 9 |
|
Proteomic analysis of annexin A2 phosphorylation induced by microtubule interfering agents and kinesin spindle protein inhibitors. | 2010 Sep 3 |
Patents
Sample Use Guides
It is wise to initiate therapy for adults by administering a single intravenous dose of 3.7 mg/m2 of body surface area (bsa).
Thereafter, white-blood-cell counts should be made to determine the patient’s sensitivity to vinblastine sulfate.
A simplified and conservative incremental approach to dosage at weekly intervals for adults may be outlined as follows:
First dose ........................... 3.7 mg/m2 bsa
Second dose ........................... 5.5 mg/m2 bsa
Third dose ........................... 7.4 mg/m2 bsa
Fourth dose ........................... 9.25 mg/m2 bsa
Fifth dose ........................... 11.1 mg/m2 bsa
The above-mentioned increases may be used until a maximum dose not exceeding 18.5 mg/m2 bsa for adults is reached. The dose should
not be increased after that dose which reduces the white-cell count to approximately 3000 cells/mm3
. In some adults, 3.7 mg/m2 bsa
may produce this leukopenia; other adults may require more than 11.1 mg/m2 bsa; and, very rarely, as much as 18.5 mg/m2 bsa may be
necessary. For most adult patients, however, the weekly dosage will prove to be 5.5 to 7.4 mg/m2 bsa.
When the dose of vinblastine sulfate which will produce the above degree of leukopenia has been established, a dose of 1 increment
smaller than this should be administered at weekly intervals for maintenance. Thus, the patient is receiving the maximum dose that does
not cause leukopenia. It should be emphasized that, even though 7 days have elapsed, the next dose of vinblastine sulfate should not be
given until the white-cell count has returned to at least 4000/mm3. In some cases, oncolytic activity may be encountered before leukopenic
effect. When this occurs, there is no need to increase the size of the subsequent doses
Route of Administration:
Intravenous
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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5V9KLZ54CY
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NCI_THESAURUS |
C932
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WHO-VATC |
QL01CA01
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LIVERTOX |
1029
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NDF-RT |
N0000007780
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NDF-RT |
N0000007780
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NDF-RT |
N0000175612
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WHO-ESSENTIAL MEDICINES LIST |
8.2
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WHO-ATC |
L01CA01
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EPA PESTICIDE CODE |
600072
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NCI_THESAURUS |
C67422
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D014747
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m11449
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212-734-0
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Vinblastine
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SUB00052MIG
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6851
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C930
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100000079086
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865-21-4
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11198
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PRIMARY | RxNorm | ||
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VINBLASTINE
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DTXSID8021430
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Related Record | Type | Details | ||
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TRANSPORTER -> SUBSTRATE |
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SALT/SOLVATE -> PARENT | |||
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TRANSPORTER -> SUBSTRATE | |||
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TRANSPORTER -> SUBSTRATE |
Related Record | Type | Details | ||
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PRODRUG -> METABOLITE ACTIVE |
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Related Record | Type | Details | ||
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PARENT -> IMPURITY |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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PARENT -> IMPURITY |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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Route of Elimination | PHARMACOKINETIC |
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Route of Elimination | PHARMACOKINETIC |
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