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RO5503781 + cytarabine + anthracycline
- Development stage
- Unknown
- Lead developer
- Roche
- Modality
- Small Molecules
- Administration
- Oral (RO5503781), Intravenous (cytarabine, Anthracycline)
01
Overview
RO5503781 (idasanutlin, RG7388) + cytarabine + anthracycline is an experimental combination regimen investigated as treatment for acute myeloid leukaemia (AML). **RO5503781** is a second-generation selective inhibitor of the p53–MDM2 interaction, restoring p53 pathway activity, which leads to apoptosis of cancer cells with wild-type p53. **Cytarabine** is a nucleoside analog antimetabolite that inhibits DNA synthesis, frequently used as chemotherapy for AML. **Anthracycline** class drugs (in the referenced trial, specifically idarubicin or daunorubicin) intercalate DNA and inhibit topoisomerase II, causing double-stranded DNA breaks and apoptosis. The combination aims to synergistically block cancer cell growth and division through cellular stress and apoptotic signaling pathways. RO5503781 is given orally, cytarabine and anthracycline are given intravenously[1][5][6].
- Other names
- idasanutlin + cytarabine + anthracycline
02
Targets
MDM2 (Mouse double minute 2 homolog)DNAMDM4 (Mouse double minute X homolog)TOP2A (DNA topoisomerase II)
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