Drug intelligence / Profile preview

rapamycin + etoposide + cytarabine

Development stage
Unknown
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Rapamycin + etoposide + cytarabine is a combination regimen of three small molecule drugs used experimentally in the treatment of hematologic malignancies, particularly acute myeloid leukemia (AML) and relapsed/refractory aggressive lymphoid malignancies. Rapamycin is an mTOR inhibitor that blocks the mammalian target of rapamycin pathway, thereby inhibiting cell growth and proliferation. Etoposide is a topoisomerase II inhibitor that induces DNA strand breaks, leading to apoptosis in rapidly dividing cells. Cytarabine is an antimetabolite that inhibits DNA synthesis by acting as a pyrimidine nucleoside analog, primarily affecting cells in the S-phase of the cell cycle. The combination has been shown preclinically to enhance cytotoxicity against leukemic blasts compared to single-agent therapy, with rapamycin sensitizing AML cells to etoposide and cytarabine-induced apoptosis[1][2][3][4]. This regimen has been investigated in clinical trials for relapsed or refractory hematologic cancers but does not have established approval for any indication.

Other names
Rapamycin + HiVACSirolimus + Etoposide + CytarabineRapamycin in Combination With High-dose Etoposide and Cytarabine
02

Targets

Mechanistic target of rapamycin complex 1DNA polymerase familyTOP2A (DNA topoisomerase II)

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