USP35 Anticancer Anti - Tumor Drug Vincristine sulfate CAS 2068-78-2

USP35 Anticancer Anti - Tumor Drug Vincristine sulfate CAS 2068-78-2

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Vincristine Description

Vincristine Sulfate, a dimeric Vinca alkaloid, has been shown to bind to Tubulin via a protein self association reaction. This compound acts as a Tubuiln inhibitor by binding to sites at the ends of microtubules, which regulate the inhibition of Tubulin dimer addition to microtubule ends. Experiments have reported Vincristine Sulfate to demonstrate a capacity to suppress growth of proliferating cells through marked apoptosis and cell cycle arrest at G2/M. The cell death caused by this agent seems to result in a sustained accumulation of endogenous ceramide levels. Ceramide, has been proposed as a lipid second messenger with specific antiproliferative mediating responses. Vincristine Sulfate is an inhibitor of MAO. Vincristine Sulfate is also a substrate of PGP and CYP3A4.

Vincristine, also known as leurocristine and marketed under the brandname Oncovin among others, is a chemotherapy medication used to treat a number of types of cancer. This includes acute lymphocytic leukemia, acute myeloid leukemia, Hodgkin's disease, neuroblastoma, and small cell lung cancer among others.

Vincristine Sulfate​ Function

Vincristine Sulfate, USP is a white to off-white powder. It is soluble in methanol, freely soluble in water, but only slightly soluble in 95% ethanol. In 98% ethanol, Vincristine Sulfate, USP has an ultraviolet spectrum with maxima at 221 nm (ε¸+47,100).

Vincristine Sulfate Injection, USP (vincristine sulfate) is a sterile, preservative-free, single use only solution available for intravenous use in 2 mL (1 mg and 2 mg) vials. Each mL contains 1 mg Vincristine Sulfate, USP, 100 mg mannitol and Water for Injection, USP q.s. Sulfuric acid or sodium hydroxide have been added for pH control. The pH of Vincristine Sulfate Injection, USP (vincristine sulfate) ranges from 4.0 to 5.0. At the time of manufacture, the air in the containers is replaced by nitrogen.

Therapeutic indications: Vinblastine sulphate is a cytotoxic drug that arrests cell growth at the metaphase. Its actions are more pronounced on the rapidly dividing cell than on the normal cell. It appears to act, like vincristine, by binding to the microtubular proteins of the mitotic spindle, preventing polymerisation.

Vinblastine sulphate is effective as a single agent, but its therapeutic effect is enhanced when used in combination with other antineoplastic drugs. Vinblastine sulphate has been used in the treatment of Hodgkin's disease (Stages III and IV); Lymphocytic lymphoma (nodular and diffuse, poorly and well differentiated); Histiocytic lymphoma; Advanced stages of mycosis fungoides; Advanced carcinoma of the testis; Kaposi's sarcoma and Letterer-Siwe disease (histocytosis X). Vinblastine sulphate may be used in the treatment of choriocarcinoma resistant to other chemotherapeutic agents; Carcinoma of the breast, unresponsive to appropriate endocrine surgery and hormonal therapy.

Vincristine Medical uses

Vincristine is delivered via intravenous infusion for use in various types of chemotherapy regimens.[3] Its main uses are in non-Hodgkin's lymphoma as part of the chemotherapy regimen CHOP, Hodgkin's lymphoma as part of MOPP, COPP, BEACOPP, or the less popular Stanford V chemotherapy regimen in acute lymphoblastic leukemia (ALL), and in treatment for nephroblastoma.It is also used to induce remission in ALL with dexamethasone and L-Asparaginase, and in combination with prednisone to treat childhood leukemia.Vincristine is occasionally used as an immunosuppressant, for example, in treating thrombotic thrombocytopenic purpura (TTP) or chronic idiopathic thrombocytopenic purpura (ITP).

Dosage and Administration

Acute Lymphocytic Leukemia, Lymphomas, Rhabdomyosarcoma, Neuroblastoma, Wilms Tumor
Adult
IV 1.4 mg/m 2 weekly (typical dose, 2 mg).

Children weighing more than 10 kg (or body surface area at least 1 m 2 )
IV 1.4 to 2 mg/m 2 weekly for 3 to 8 wk. Do not exceed a max of 2 mg/dose.

Children weighing up to 10 kg (or body surface area less than 1 m 2 )
IV 0.05 mg/kg weekly initially. Titrate dose as tolerated, up to a max of 2 mg/dose. Continue therapy for 3 to 8 wk.

Adjustment in Hepatic Insufficiency

Adult
IV A 50% reduction in dose is recommended for patients having a direct serum bilirubin value more than 3 mg/dL.

Neuroblastoma, Combination Therapy

Children weighing more than 10 kg (or body surface area at least 1 m 2 )
IV Vincristine 1 mg/m 2 /day by continuous infusion over 24 h for 3 days (total dose of 3 mg/m 2 over a 3-day period).

General Advice

• Do not dilute vincristine for routine IV use. For continuous IV infusion, vincristine may be diluted with 0.9% Sodium Chloride or 5% Dextrose.
• Administer by IV injection or continuous IV infusion.
• Do not filter.
• Give over a 1-min period by IV push injection or IV side arm into a running infusion.
• Continuous infusions can only be administered through a central venous catheter resting in the vena cava. A peripherally-inserted central catheter, or PICC line, may also be appropriate.