Drug intelligence / Profile preview

A112

Development stage: Preclinical
Modality: Small Molecules
Administration: Injection

Overview

A112 is a tamibarotene dimethylaminoethyl ester, a derivative of trans retinoic acid, being investigated as a potential treatment for acute promyelocytic leukemia (APL) and acute myeloid leukemia (AML). It demonstrates potent anti-cancer activity by inhibiting leukemia cell growth, inducing differentiation of leukemic cells (evidenced by increased CD11b expression), and promoting apoptosis. Its mechanism involves the activation of CCAAT/enhancer-binding protein β (C/EBPβ) and cyclin-dependent kinase (CDK) inhibitors p21(Waf1/cip1) and p27(Kip1). Furthermore, A112 induces apoptosis through the activation of caspase-3, caspase-9, and the cleavage of poly(ADP-ribose) polymerase (PARP).

Other names: tamibarotene dimethylaminoethyl ester

Targets

RARA (Retinoic acid receptor alpha)C/EBPβ (CCAAT/enhancer-binding protein beta)CASP3 (Caspase-3)CDKN1B (Transmembrane emp24 domain-containing protein 7)CASP9 (Caspase-9)

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