Drug intelligence / Profile preview

BAY 61-3606

Development stage
Preclinical
Lead developer
Bayer
Modality
Small Molecules
Administration
Oral
01

Overview

BAY 61-3606 is a potent and selective small molecule inhibitor of spleen tyrosine kinase (Syk), with a Ki of approximately 7.5 nM. It acts as an ATP‐competitive and reversible inhibitor that is highly selective for Syk over other kinases such as Lyn, Fyn, Src, Itk and BTK (with no significant inhibition up to concentrations of >4.7 µM). The compound has demonstrated anti-inflammatory activity and efficacy in preclinical models of allergy and asthma in rodents. Mechanistically it induces cell cycle arrest and apoptosis in certain cell types. There is also evidence for inhibitory activity against IKKα (I-kappa-B kinase alpha) and MAP4K2 (mitogen‐activated protein kinase kinase kinase kinase 2), but its primary target remains Syk[1][3][4][9].

Other names
2-(7-(3,4-Dimethoxyphenyl)-imidazo[1,2-c]pyrimidin-5-ylamino)-nicotinamide hydrochloride2-[[7-(3,4-dimethoxyphenyl)imidazo[1,2-c]pyrimidin-5-yl]amino]pyridine-3-carboxamide hydrochloride
02

Targets

SYK (Spleen Tyrosine Kinase)

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