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Two doxorubicin molecules intercalated within DNA. [1] Anthracyclines are a class of drugs used in cancer chemotherapy that are extracted from Streptomyces peucetius bacterium. [2] [3] [4] These compounds are used to treat many cancers, including leukemias, lymphomas, breast, stomach, uterine, ovarian, bladder cancer, and lung cancers.
Doxorubicin showed better activity than daunorubicin against mouse tumors, and especially solid tumors. It also showed a higher therapeutic index, yet the cardiotoxicity remained. [50] Doxorubicin and daunorubicin together can be thought of as prototype compounds for the anthracyclines. Subsequent research has led to many other anthracycline ...
Currently, there are four main anthracyclines in medical use: Doxorubicin; Daunorubicin (doxorubicin precursor) Epirubicin (a doxorubicin stereoisomer) Idarubicin (a daunorubicin derivative) [17] Idarubicin is able to pass through cell membranes easier than daunorubicin and doxorubicin because it possesses less polar subunits, making it more ...
Daunorubicin, also known as daunomycin, is a chemotherapy medication used to treat cancer. [2] Specifically it is used for acute myeloid leukemia (AML), acute lymphoblastic leukemia (ALL), chronic myelogenous leukemia (CML), and Kaposi's sarcoma. [2] It is administered by injection into a vein. [2]
Cardiotoxicity (heart damage) is especially prominent with the use of anthracycline drugs (doxorubicin, epirubicin, idarubicin, and liposomal doxorubicin). The cause of this is most likely due to the production of free radicals in the cell and subsequent DNA damage .
The total plasma clearance of epirubicin is approximately 45 to 50 L/h/m2, which is almost 2-fold higher than that of doxorubicin. [ 9 ] [ 10 ] Area under the plasma concentration versus time curve values (adjusted for dose) are 1.3 to 1.7 times higher for doxorubicin than epirubicin following single-dose intravenous administration.
[10] The United States Food and Drug Administration has also approved a dexrazoxane for use as a treatment of extravasation resulting from IV anthracycline chemotherapy . [ 11 ] [ 12 ] Extravasation is an adverse event in which chemotherapies containing anthracylines leak out of the blood vessel and necrotize the surrounding tissue.
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 (IC 50 = 142nM) inhibitor of the Fat Mass and Obesity (FTO) associated protein, which is a m 6 A RNA demethylase. The same study found that ...