Ligand id: 6741

Name: idelalisib

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Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 8
Hydrogen bond donors 2
Rotatable bonds 5
Topological polar surface area 86.8
Molecular weight 415.16
XLogP 4.45
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Idelalisib is a treatmet for difficult to treat leukemia and lymphomas. The potential of this drug was highlighted by the early termination of a phase 3 clinical trial, so that all participants could be given the drug [1]. Idelalisib was approved in July 2014, for patients with relapsed chronic lymphocytic leukemia (CLL), in combination with rituximab. The FDA also granted the drug accelerated approval for the treatment of patients with relapsed follicular B-cell non-Hodgkin lymphoma (FL) and relapsed small lymphocytic lymphoma (SLL), particularly indicated for patients who have received at least two prior systemic therapies.

To view a full list of trials registered with assessing idelalisib, click here.
Mechanism Of Action and Pharmacodynamic Effects
PI3Kδ signaling is critical for the activation, proliferation, survival and trafficking of B lymphocytes and is hyperactive in many B-cell malignancies. Idelalisib inhibits this activity, ultimately leading to death of cancer cells.
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