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Bisantrene AI simulator
(@Bisantrene_simulator)
Hub AI
Bisantrene AI simulator
(@Bisantrene_simulator)
Bisantrene
Bisantrene is an anthracenyl bishydrazone with anthracycline-like antineoplastic activity and an antimetabolite. Bisantrene intercalates with and disrupts the configuration of DNA, resulting in DNA single-strand breaks, DNA-protein crosslinking, and inhibition of DNA replication. This agent is similar to doxorubicin in chemotherapeutic activity, but unlike anthracyclines like doxorubicin, it exhibits little cardiotoxicity.
In addition to its anthracycline-like activity, a July 2020 seminal article by Su, R et al. at the City of Hope Hospital in Los Angeles, California, USA first identified bisantrene to also be a potent (IC50 = 142nM) inhibitor of the Fat Mass and Obesity (FTO) associated protein, which is a m6A RNA demethylase. The same study found that bisantrene is a weak inhibitor of ALKBH5, which is the only other demethylase, i.e. bisantrene is also a selective inhibitor of FTO.
In 2021, bisantrene was demonstrated preclinically to be cardioprotective when administered together with cardiotoxic anthracyclines.
A bisantrene combination treatment is currently (as at early 2024) nearing the end of a Phase II clinical trial to assess its efficacy in treating AML in heavily pretreated patients and to assess any adverse side effects, including any cardiotoxicity of the combination. The December 2023 interim findings are given in the History section.
Clinical trials of Bisantrene in the 1980s showed efficacy in a range of leukaemias (including Acute Myeloid Leukaemia), breast cancer, and ovarian cancer.
High doses of bisantrene (above 200 mg/m2/day) cause adverse side effects typical of anthracycline chemotherapeutics. Common adverse side effects include hair loss, bone marrow suppression, vomiting, rash, and inflammation of the mouth. For a chemotherapy drug, it is considered to have relatively low toxicity.
Unlike other anthracycline chemotherapeutics, Bisantrene shows low levels of cardiotoxicity. In a Phase III metastatic breast cancer clinical, patients were exposed to cumulative doses in excess of 5440 mg/m2 without developing cardiac damage.[medical citation needed] The same study observed significantly lower rates of hair loss and nausea compared to patients given doxorubicin.
Bisantrene has three distinct mechanisms of action.
Bisantrene
Bisantrene is an anthracenyl bishydrazone with anthracycline-like antineoplastic activity and an antimetabolite. Bisantrene intercalates with and disrupts the configuration of DNA, resulting in DNA single-strand breaks, DNA-protein crosslinking, and inhibition of DNA replication. This agent is similar to doxorubicin in chemotherapeutic activity, but unlike anthracyclines like doxorubicin, it exhibits little cardiotoxicity.
In addition to its anthracycline-like activity, a July 2020 seminal article by Su, R et al. at the City of Hope Hospital in Los Angeles, California, USA first identified bisantrene to also be a potent (IC50 = 142nM) inhibitor of the Fat Mass and Obesity (FTO) associated protein, which is a m6A RNA demethylase. The same study found that bisantrene is a weak inhibitor of ALKBH5, which is the only other demethylase, i.e. bisantrene is also a selective inhibitor of FTO.
In 2021, bisantrene was demonstrated preclinically to be cardioprotective when administered together with cardiotoxic anthracyclines.
A bisantrene combination treatment is currently (as at early 2024) nearing the end of a Phase II clinical trial to assess its efficacy in treating AML in heavily pretreated patients and to assess any adverse side effects, including any cardiotoxicity of the combination. The December 2023 interim findings are given in the History section.
Clinical trials of Bisantrene in the 1980s showed efficacy in a range of leukaemias (including Acute Myeloid Leukaemia), breast cancer, and ovarian cancer.
High doses of bisantrene (above 200 mg/m2/day) cause adverse side effects typical of anthracycline chemotherapeutics. Common adverse side effects include hair loss, bone marrow suppression, vomiting, rash, and inflammation of the mouth. For a chemotherapy drug, it is considered to have relatively low toxicity.
Unlike other anthracycline chemotherapeutics, Bisantrene shows low levels of cardiotoxicity. In a Phase III metastatic breast cancer clinical, patients were exposed to cumulative doses in excess of 5440 mg/m2 without developing cardiac damage.[medical citation needed] The same study observed significantly lower rates of hair loss and nausea compared to patients given doxorubicin.
Bisantrene has three distinct mechanisms of action.
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