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 |
---|---|---|
[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
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20696757
15 nM vinblastine inhibit CHO cell proliferation
Substance Class |
Chemical
Created
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on
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Fri Dec 15 14:59:50 GMT 2023
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N00W22YO2B
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C67422
Created by
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FDA ORPHAN DRUG |
867921
Created by
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NCI_THESAURUS |
C932
Created by
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Code System | Code | Type | Description | ||
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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. | ||
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C931
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1713004
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100000087899
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11199
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m11449
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DTXSID601017133
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49842
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5388983
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CHEMBL159
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PARENT -> SALT/SOLVATE |
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ACTIVE MOIETY |