Ligand id: 7420

Name: carfilzomib

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 12
Hydrogen bond donors 4
Rotatable bonds 24
Topological polar surface area 158.47
Molecular weight 719.43
XLogP 7.56
No. Lipinski's rules broken 3

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Carfilzomib is approved to treat multiple myeloma (MM) in patients who have undergone at least two prior therapies, including treatment with bortezomib 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 lenalidomide and dexamethasone. Across the EU, carfilzomib has orphan drug status as a MM therapy.
In January 2016, the US FDA expanded carfilzomib's approval to include combination therapy (plus dexamethasone or dexamethasone and lenalidomide) 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.
Mechanism Of Action and Pharmacodynamic Effects
This drug is a proteasome inhibitor, inhibiting the chymotrypsin-like activity of the β-5 subunit of the 20S proteasome and causing an inhibition of cellular proliferation and ultimately leading to apoptosis [2].
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