Idelalisib

Idelalisib, sold under the brand name Zydelig, is a medication used to treat certain blood cancers. Idelalisib acts as a phosphoinositide 3-kinase inhibitor; more specifically, it blocks P110δ, the delta isoform of the enzyme phosphoinositide 3-kinase. It was developed by Gilead Sciences. It is taken orally (swallowed by mouth).

Idelalisib
Idelalisib structure
Clinical data
Pronunciation/aɪˈdɛləlɪsɪb/
eye-DEL-ə-li-sib
Trade namesZydelig
Other namesGS-1101, CAL-101
AHFS/Drugs.comMonograph
MedlinePlusa614040
Pregnancy
category
  • AU: D
Routes of
administration		Oral
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • CA: ℞-only
  • US: WARNINGRx-only
  • EU: Rx-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Protein binding>84%
MetabolismAldehyde oxidase (~70%), CYP3A4 (~30%); UGT1A4 (minor)
MetabolitesGS-563117 (inactive in vitro)
Onset of actionTmax = 1.5 hours
Elimination half-life8.2 hours
ExcretionFeces (78%), urine (14%)
Identifiers
  • 5-Fluoro-3-phenyl-2-[(1S)-1-(7H-purin-6-ylamino)propyl]-4(3H)-quinazolinone
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.235.089
Chemical and physical data
FormulaC22H18FN7O
Molar mass415.432 g·mol−1
3D model (JSmol)
SMILES
  • CC[C@H](Nc1ncnc2nc[nH]c12)c4nc3cccc(F)c3c(=O)n4c5ccccc5
  • 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
  • Key:IFSDAJWBUCMOAH-HNNXBMFYSA-N
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