{
    "comments": "Carfilzomib is a tetrapeptide analogue of epoxomicin, an <i>Actinomycete</i> derived selective proteasome inhibitor <Reference id=24384/>.",
    "bioactivityComments": "Carfilzomib causes a dose-dependent inhibition of 20S proteasomal chymotrypsin-like activity in CD138<sup>+</sup> plasma cells purified from MM patient samples <Reference id=24385/>.  Maximum inhibition of approximately 70% is achieved with 10-25nM carfilzomib.",
    "clinicalUse": "Carfilzomib is approved to treat multiple myeloma (MM) in patients who have undergone at least two prior therapies, including treatment with <Ligand id=6391/> and an immunomodulatory therapy. As of July 2015, the approval also includes patients with relapsed MM, in whom carfilzomib is to be used in combination with <Ligand id=7331/> and <Ligand id=2768/>. Across the EU, carfilzomib has orphan drug status as a MM therapy.<br>In January 2016, the US FDA expanded carfilzomib's approval to include combination therapy (plus <Ligand id=2768/> or dexamethasone and <Ligand id=7331/>) for relapsed or refractory MM patients who have received one to three lines of therapy, and as a single agent for the treatment of patients with relapsed or refractory MM who have received one or more lines of therapy.",
    "mechanismOfAction": "This drug is a proteasome inhibitor, inhibiting the chymotrypsin-like activity of the &beta;-5 subunit of the 20S proteasome and causing an inhibition of cellular proliferation and ultimately leading to apoptosis <Reference id=24385/>.",
    "absorptionAndDistribution": "",
    "metabolism": "",
    "elimination": "",
    "populationPharmacokinetics": "",
    "organFunctionImpairment": "",
    "immuno": "",
    "gtmp": ""
}