Description: |
Acumapimod (BCT197) is an orally active p38 MAP kinase inhibitor, with an IC50 of less than 1 μM for p38α. |
Target: |
IC50: less than 1 μM (p38α)[1] |
In Vivo: |
BCT197 is an oral low-molecular-weight p38 inhibitor currently in development for the treatment of several inflammatory conditions, including chronic obstructive pulmonary disease (COPD). Intermittent short-term dosing of BCT197 (75 mg on days 1 and 6) shows a marked improvement in lung function in COPD patients[2]. |
In Vitro: |
Acumapimod is an inhibitor of p38α with an IC50 value of less than 1 μM. |
References: |
[1]. Norman P, et al. Investigational p38 inhibitors for the treatment of chronic obstructive pulmonary disease. Expert Opin Investig Drugs. 2015 Mar;24(3):383-92.
[2]. De Buck S, et al. Population PK-PD Model for Tolerance Evaluation to the p38 MAP Kinase Inhibitor BCT197. CPT Pharmacometrics Syst Pharmacol. 2015 Dec;4(12):691-700. |