Losmapimod is a promising new agent against cardiovascular diseases. This compound works by inhibiting p38 MAP kinases, which play an important role in the development of atherosclerosis and heart failure caused by ischemic conditions. Losmapimod did not cause an improvement in exercise tolerance or lung function, despite being well-tolerated in this COPD population.The p38 MAPK inhibitor losmapimod (GW856553) attenuates the pro-inflammatory response in humans by reducing PIC production.
|Animal models||Spontaneously hypertensive stroke-prone rats|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
A low-frequency variant in MAPK14 provides mechanistic evidence of a link with myeloperoxidase: a prognostic cardiovascular risk marker.
Waterworth DM, et al. J Am Heart Assoc. 2014 Aug 27;3(4). PMID: 25164947.
Losmapimod, a novel p38 mitogen-activated protein kinase inhibitor, in non-ST-segment elevation myocardial infarction: a randomised phase 2 trial.
Newby LK, et al. Lancet. 2014 Sep 27;384(9949):1187-95. PMID: 24930728.
Evaluation of antidepressant properties of the p38 MAP kinase inhibitor losmapimod (GW856553) in Major Depressive Disorder: Results from two randomised, placebo-controlled, double-blind, multicentre studies using a Bayesian approach.
Inamdar A, et al. J Psychopharmacol. 2014 Apr 2;28(6):570-581. PMID: 24699061.
Efficacy and safety of the p38 MAPK inhibitor losmapimod for patients with chronic obstructive pulmonary disease: a randomised, double-blind, placebo-controlled trial.
Watz H, et al. Lancet Respir Med. 2014 Jan;2(1):63-72. PMID: 24461903.
Losmapimod: a novel drug against cardiovascular diseases?
Dewenter M, et al. Dtsch Med Wochenschr. 2013 Jan;138(1-2):39-42. PMID: 23250695.
Safety, tolerability, pharmacokinetics and pharmacodynamics of losmapimod following a single intravenous or oral dose in healthy volunteers.
Barbour AM, et al. Br J Clin Pharmacol. 2013 Jul;76(1):99-106. PMID: 23215699.
|Related p38 MAPK Products|
SB 239063 is a potent and selective p38 MAPK inhibitor (IC50 = 44 nM for p38α). SB 239063 displays > 220-fold selectivity over ERK, JNK1 and other kinases; ~ 3-fold more selective than SB 203580.
SD-06 is a p38 MAP kinase inhibitor; inhibits p38α with an IC50 value of 170 nM and inhibits LPS-stimulated TNF-release in rats (83% inhibition at 1mg/kg, po). IC50 value: 170 nM Target: p38MAPK
SKF-86002 is a potent inhibitor of p38 MAP kinase wit IC50 of 0.5-1 uM; inhibits LPS-induced IL-1 and TNF-α production in human monocytes.
TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM. IC50 value: 20 nM. TA-02 is a novel compound with similar cardiogenic properties as SB203580 and SB202190. TA-02 especially inhibits TGFBR-2.
Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. Phase 1.
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