idelalisib   

GtoPdb Ligand ID: 6741

Synonyms: CAL-101/CAL101 | GS-1101 | Zydelig®
idelalisib is an approved drug (FDA & EMA (2014))
Compound class: Synthetic organic
Comment: Idelalisib is highly selective and potent oral inhibitor of phosphoinositide 3-kinase (PI3K) δ.
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2D Structure
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Physico-chemical Properties
Hydrogen bond acceptors 6
Hydrogen bond donors 2
Rotatable bonds 5
Topological polar surface area 100.86
Molecular weight 415.16
XLogP 4.11
No. Lipinski's rules broken 0
SMILES / InChI / InChIKey
Canonical SMILES CCC(c1nc2cccc(c2c(=O)n1c1ccccc1)F)Nc1ncnc2c1[nH]cn2
Isomeric SMILES CC[C@@H](c1nc2cccc(c2c(=O)n1c1ccccc1)F)Nc1ncnc2c1[nH]cn2
InChI InChI=1S/C22H18FN7O/c1-2-15(28-20-18-19(25-11-24-18)26-12-27-20)21-29-16-10-6-9-14(23)17(16)22(31)30(21)13-7-4-3-5-8-13/h3-12,15H,2H2,1H3,(H2,24,25,26,27,28)/t15-/m0/s1
InChI Key IFSDAJWBUCMOAH-HNNXBMFYSA-N
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 ClinicalTrials.gov 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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