Basic information Camptothecin anticancer drugs Uses Production methods Safety Related Supplier
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Topotecan

Basic information Camptothecin anticancer drugs Uses Production methods Safety Related Supplier
Topotecan Basic information
Topotecan Chemical Properties
  • Melting point:−114 °C(lit.)
  • Boiling point:>100 °C(lit.)
  • Density 1.2 g/mL at 25 °C(lit.)
  • vapor density 1.3 (vs air)
  • vapor pressure 613 psi ( 21.1 °C)
  • Flash point:12 °C
  • storage temp. 2-8°C
  • solubility H2O: soluble
  • pka8.92±0.40(Predicted)
  • form liquid
  • color yellow
  • CAS DataBase Reference123948-87-8(CAS DataBase Reference)
Safety Information
MSDS
Topotecan Usage And Synthesis
  • Camptothecin anticancer drugsCamptothecin anticancer drugs are alkaloids or derivatives of them after the structure transformation raised from deciduous plant Davidia involucrata Camptotheca acuminate seed or root bark. Clinical application of them mainly includes camptothecin,hydroxycamptothecin, topotecan and irinotecan.
    Topotecan is a water-soluble semi-synthetic derivative of camptothecin,it is a topoisomerase I inhibitor, inhibiting DNA single strand DNA scission reconnect to damage DNA, its cytotoxicity occurs in cancer cell division S phase, it is an s phase cell cycle specific drug . In vivo it is a two-compartment model,it can be quickly distributed to the liver, kidneys and other parts , of a single intravenous infusion 1.5mg/m2 every 30 minutes , t1/2αis 4.1 to 8.1 minutes, plasma protein binding rate is 6.6%~21.3%,it can go into the cerebrospinal fluid. Most of it is excreted by the kidneys, a small part of it is excreted by the bile, within 12 hours, 90% of it is excreted.Clearance rate of renal dysfunction decreases.it is clinically used for the treatment of small cell lung cancer (SCLC), and advanced ovarian cancer, because it can penetrate the blood-brain barrier ,it has a certain effect on the central nervous system cancer and brain metastases. Usage: every single drug dose 1.2mg/m2 intravenous infusion once a day, once every 5 days, 21 days is 1 cycle, there is the need to reduce the dose when in combination with other anticancer drugs. The main adverse events are hematologic toxicity, white blood cells, platelets and hemoglobin decrease; non-hematologic toxicity adverse events are loss of appetite, nausea, vomiting, hair loss, stomatitis, diarrhea, headache, fever, constipation, transient elevated transaminase; occasionally breathing difficulties, hematuria, andelectrocardiogram abnormalities.
    Severe bone marrow suppression are hanged. Monitor the blood and adjust the dose in accordance with changes in blood during the treatment , if necessary, granulocyte colony stimulating factor (G-CSF), and transfusion of blood components may be given .
    The above information is edited by the chemicalbook of Tian Ye.
  • UsesAnti-cancer drugs.It can be used alone for the treatment of initially or continuously ineffective chemotherapy metastatic ovarian cancer.
  • Production methodsCompound (I) with 37% formaldehyde and 40% dimethylamine,after aminomethylation in acetic acid, produces the product.
  • DescriptionTopotecan was launched in the US for the second-line treatment of ovarian cancer. It can be prepared in four steps from camptothecin and is a water soluble derivative of the natural product with decreased toxicity. Unlike its chemical relative irinotecan, topotecacan in not a prodrug and does not require bioactivation. It is an inhibitor of topoisomerase I. Specifically, it inhibits the release of topoisomerase I from DNA, where it relaxes supercoiled DNA, giving rise to single-strand breaks. When the replication fork reaches this complex, double-stand breaks can occur. This signals apoptosis and eventually gives rise to cell death. Evidence indicates hycamtin is safe for people with impaired hepatic function.
  • Chemical PropertiesOff-white Cryst
  • OriginatorSmithKline Beecham (UK)
  • Usesantineoplastic;DNA topoisomerase type 1 inhibitor
  • DefinitionChEBI: A pyranoindolizinoquinoline used as an antineoplastic agent. It is a derivative of camptothecin and works by binding to the topoisomerase I-DNA complex and preventing religation of these 328 single strand breaks.
  • brand nameHycamtin
Topotecan Preparation Products And Raw materials
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