NCIt definition : A calcium (Ca2 ) release-activated channel (CRAC) inhibitor, with potential antineoplastic
activity. Upon administration, RP4010 binds to and inhibits CRACs, thereby preventing
the transport of extracellular Ca2 into the cell and inhibiting the subsequent activation
of Ca2 -mediated signaling and transcription of target genes. CRACs, specialized plasma
membrane Ca2 ion channels composed of the plasma membrane based Orai channels and
the endoplasmic reticulum (ER) stromal interaction molecules (STIMs), play key roles
in calcium homeostasis and are over-activated in a number of cancer cell types. Aberrant
activation of CRACs leads to increased cancer cell proliferation.;
Semantic type(s)