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rapamycin + mitoxantrone + etoposide + cytarabine
- Development stage
- Unknown
- Lead developer
- Merck
- Modality
- Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral, Intravenous
01
Overview
This is a combination chemotherapy regimen consisting of rapamycin (also known as sirolimus), mitoxantrone, etoposide, and cytarabine. Rapamycin is an inhibitor of the mammalian target of rapamycin (mTOR), a key regulator of cell growth and proliferation. Mitoxantrone is an anthracenedione that inhibits topoisomerase II, leading to DNA damage and apoptosis. Etoposide is a topoisomerase II inhibitor that induces DNA strand breaks, while cytarabine is a nucleoside analog that inhibits DNA synthesis. This combination has been studied primarily in patients with relapsed or refractory acute myeloid leukemia (AML) to enhance the sensitivity of leukemic cells to chemotherapy by targeting mTOR signaling pathways[1][2][3]. The regimen has shown activity in clinical trials but also significant toxicity.
- Brand names
- RapamuneNone for the combination or for MEC as a regimen
- Other names
- sirolimus + mitoxantrone + etoposide + cytarabineS-MEC
02
Targets
DNA polymerase familyTOP2A (DNA topoisomerase II)Mechanistic target of rapamycin complex 1
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