bortezomib

Ligand id: 6391

Name: bortezomib

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 8
Hydrogen bond donors 4
Rotatable bonds 11
Topological polar surface area 124.44
Molecular weight 384.2
XLogP 3.24
No. Lipinski's rules broken 1

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
May be used to treat multiple myeloma in patients unsuccessfully treated with at least two previous therapies. Bortezomib is delivered by injection. The marketed drug Velcade, contains bortezomib as the mannitol boronic ester.
Mechanism Of Action and Pharmacodynamic Effects
Bortezomib is a reversible inhibitor of the chymotrypsin-like activity of the 26S proteasome. Inhibitors of proteasome activity are antiproliferative and pro-apoptotic in nature. Proteasome inhibition leads to an increase in intracellular pro-apoptotic proteins, which promote cell-cycle arrest and cell-death [1].
Pharmacokinetics
Biotransformation/Metabolism
Bortezomib is primarily oxidatively metabolized via cytochrome P450 enzymes, 3A4, 2D6, 2C19, 2C9, and 1A2. Deboronated metabolites are inactive as 26S proteasome inhibitors.
Elimination
The pathways of elimination of bortezomib have not been characterized in humans.
External links