molecules of the month


oral CD38 inhibitor

in vivo efficacy in a murine model of cardiac I/R

from the previously disclosed inhibitor CD38i

J. Med. Chem.

Mitobridge (an Astellas Company), Cambridge, MA

MK-0159 Chemical Structure oral CD38 inhibitor - Mitobridge (an Astellas Company), Cambridge, MA
4 mins read

Context. MK-0159 (Mitobridge) is an oral CD38 inhibitor being developed for cardiovascular diseases. Due to its NADP+ depleting activity, which has implications for calcium homeostasis, the cell surface marker CD38 has attracted attention as a suitable target for developing cardiovascular disease agents. Although two monoclonal antibodies targeting CD38 (daratumumab and isatuximab) have been approved, both for cancer indications, the search for the first small molecule CD38 inhibitor is still ongoing. MK-0159 demonstrated potent activity against human CD38 enzymes (IC50 = 22 nM) while it significantly increased blood and heart NAD+ levels. Furthermore, it protected treated mice from cardiac ischemia/reperfusion injury, making the compound the first to demonstrate in vivo cardioprotective effects in a mouse cardiac ischemia/reperfusion injury model. Target. In…

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