Drug intelligence / Profile preview

azd1208

Development stage
Phase 1
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

AZD1208 is a potent, highly selective, and orally available small-molecule inhibitor of the PIM family of serine/threonine kinases (PIM1, PIM2, and PIM3). It was developed primarily for oncology indications. By inhibiting all three isoforms of Pim kinases at low nanomolar concentrations, AZD1208 disrupts cell cycle progression (notably the G1/S transition), induces cell cycle arrest and apoptosis in cancer cells overexpressing these kinases[1][2][4]. The drug has demonstrated anti-tumor activity in preclinical models of acute myeloid leukemia (AML), chronic lymphocytic leukemia (CLL), gastric cancer, and other malignancies by suppressing downstream targets such as 4EBP1 and p70S6K phosphorylation[2][6][7]. In addition to its anti-cancer effects, AZD1208 has shown inhibition of adipogenesis and promotion of lipolysis in adipocyte models through modulation of key metabolic regulators[3][8]. Despite promising preclinical data, clinical development for AML, lymphoma, solid tumors and other cancers was discontinued[5].

Other names
pan-PIM kinase inhibitor AZD1208
02

Targets

PIM1 (Proviral integration site for moloney murine leukemia virus kinase 1)PIM3 (Proviral integration site for Moloney murine leukemia virus kinase 3)PIM2 (Proto-oncogene serine/threonine-protein kinase Pim2)

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