Idelalisib

Idelalisib
Idelalisib structure
Clinical data
Pronunciation/ˈdɛləlɪsɪb/
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
Pharmacokinetic data
Protein binding>84%[5]
MetabolismAldehyde oxidase (~70%), CYP3A4 (~30%);[6] 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 Edit this at Wikidata
Chemical and physical data
FormulaC22H18FN7O
Molar mass415.432 g·mol−1
3D model (JSmol)
  • 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

Idelalisib, sold under the brand name Zydelig, is a medication used to treat certain blood cancers.[5][4] Idelalisib acts as a phosphoinositide 3-kinase inhibitor; more specifically, it blocks P110δ, the delta isoform of the enzyme phosphoinositide 3-kinase.[7][8] It was developed by Gilead Sciences. It is taken orally (swallowed by mouth).

  1. ^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 Oct 2023.
  2. ^ "Prescription medicines: registration of new chemical entities in Australia, 2015". Therapeutic Goods Administration (TGA). 21 June 2022. Retrieved 10 April 2023.
  3. ^ "Health Canada New Drug Authorizations: 2015 Highlights". Health Canada. 4 May 2016. Retrieved 7 April 2024.
  4. ^ a b "Zydelig EPAR". European Medicines Agency (EMA). 17 September 2018. Retrieved 21 October 2020.
  5. ^ a b "Zydelig- idelalisib tablet, film coated". DailyMed. 22 October 2018. Retrieved 21 October 2020.
  6. ^ "Clinical Pharmacology and Biopharmaceutics Review: Zydelig (idelalisib)" (PDF). U.S. Food and Drug Administration. p. 6. Retrieved 15 April 2016.
  7. ^ Cite error: The named reference Spreitzer was invoked but never defined (see the help page).
  8. ^ Cite error: The named reference Wu was invoked but never defined (see the help page).

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