Chemical Property of Idelalisib
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Chemical Property:
- PSA：101.38000
- LogP:3.82730
- XLogP3:3.7
- Hydrogen Bond Donor Count:2
- Hydrogen Bond Acceptor Count:7
- Rotatable Bond Count:5
- Exact Mass:415.15568639
- Heavy Atom Count:31
- Complexity:685
- Purity/Quality:
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97% *data from raw suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Drug Classes:Antineoplastic Agents
- Canonical SMILES:CCC(C1=NC2=C(C(=CC=C2)F)C(=O)N1C3=CC=CC=C3)NC4=NC=NC5=C4NC=N5
- Isomeric SMILES:CC[C@@H](C1=NC2=C(C(=CC=C2)F)C(=O)N1C3=CC=CC=C3)NC4=NC=NC5=C4NC=N5
- Recent ClinicalTrials:Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) PRIME Trial
- Recent EU Clinical Trials:A Phase 2 Randomized Study of Loncastuximab Tesirine Versus Idelalisib in Patients with Relapsed or Refractory Follicular Lymphoma (LOTIS 6)
- Recent NIPH Clinical Trials:A Phase 3 Study of LOXO-305 in Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma
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Description
Idelalisib is an orally available selective and potent phosphatidylinositol
3-kinase δ (PI3 Kδ) inhibitor originally developed
by Calistoga Pharmaceuticals, which was acquired by Gilead in
April 2014. In July 2014, the drug was approved in the USA for
the treatment of relapsed chronic lymphocytic leukemia as well
as several oncology orphan drug designations. Since idelalisib
specifically inhibits PI3Kd, which is expressed primarily in bloodcell
lineages, the therapeutic effect is localized, limiting interference
with PI3K isoform signaling that is critical to normal function
of healthy cells.
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Indications
Among the large groups of structural diverse lipid kinase inhibitors, especially against PI3Ks, idelalisib (Zydelig(R), Gilead Sciences) is the only inhibitor approved by FDA for the treatment of patients with relapsed chronic lymphocytic leukemia in combination with rituximab and patients with relapsed follicular B-cell non-Hodgkin lymphoma or small lymphocytic lymphoma.
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Clinical Use
Phosphatidylinositol 3-kinase p110δ (PI3Kδ) inhibitor:
Treatment of chronic lymphocytic leukaemia (CLL)
and follicular lymphoma (FL)
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Drug interactions
Potentially hazardous interactions with other drugs
Antibacterials: concentration reduced by rifampicin
- avoid.
Antidepressants: concentration possibly reduced by
St John’s wort - avoid.
Antiepileptics: concentration possibly reduced by
carbamazepine, fosphenytoin and phenytoin - avoid.
Antipsychotics: avoid with clozapine, increased
risk of agranulocytosis; avoid with pimozide and
quetiapine.
