Drug intelligence / Profile preview

ALRN-6924 + cytarabine

Development stage
Unknown
Lead developer
Rein Therapeutics
Modality
Peptides, Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

ALRN-6924 is a novel, cell-permeating, stabilized α-helical peptide that functions as a dual inhibitor of the MDM2 and MDMX proteins. By blocking these proteins, ALRN-6924 reactivates the tumor suppressor protein p53 in cancer cells, leading to cell cycle arrest and apoptosis. Cytarabine is an antimetabolite chemotherapy agent primarily used in the treatment of various leukemias; it works by inhibiting DNA polymerase and incorporating into DNA to disrupt DNA synthesis during the S-phase of the cell cycle. The combination of ALRN-6924 with cytarabine has been investigated in early-phase clinical trials for pediatric cancers including leukemia and lymphoma, aiming to enhance anti-tumor efficacy through complementary mechanisms—p53 pathway activation (ALRN-6924) and inhibition of DNA synthesis (cytarabine)[2][3][8].

Other names
sulanemadlin
02

Targets

MDM2 (Mouse double minute 2 homolog)POLA1 (DNA polymerase alpha)MDM4 (Mouse double minute X homolog)

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