RT Book, Section
A1 Hilal-Dandan, PhD, Department of Pharmacology, University of California, San Diego, Randa
A2 Brunton, Laurence L.
A2 Chabner, Bruce A.
A2 Knollmann, Björn C.
SR Print(0)
ID 1127872490
T1 Idelalisib: A First-in-Class Specific Inhibitor of PI3Kδ for the Treatment of B-cell Lymphomas
T2 Goodman & Gilman's: The Pharmacological Basis of Therapeutics, 12e
YR 2015
FD 2015
PB McGraw-Hill Education
PP New York, NY
SN 9780071624428
LK accessbiomedicalscience.mhmedical.com/content.aspx?aid=1127872490
RD 2023/12/06
AB Idelalisib  (zydelig)  is  a  first-in-class  oral  inhibitor  of  the  enzyme  phosphatidylinositol  3-kinase-δ  (PI3Kδ)  isoform  that  was  approved  by  the  FDA  in  July  2014  for  the  treatment  of  patients  with  relapsed  or  refractory  B-cell  malignancies  (eFigure  62–1.1).1  The  PI3Kδ  isoform  in  the  PI3K  signaling  pathway  is  constitutively  activated  in  many  B-cell  malignancies,  and  inhibition  of  this  pathway  promotes  apoptosis  in  these  cancerous  cells.  The  FDA  granted  idelalisib  accelerated  approval  for  treatment  of  relapsed  follicular  B-cell  non-Hodgkin  lymphoma  (FL)  and  relapsed  small  lymphocytic  lymphoma  (SLL).  Accelerated  approval  allows  a  drug  to  be  used  to  treat  a  serious  or  life-threatening  disease  based  on  a  surrogate  end  point  predictive  of  a  clinical  benefit  in  patients.  Idelalisib,  in  combination  with  rituximab,  was  also  approved  as  a  “breakthrough  therapy”  for  relapsed  chronic  lymphocytic  leukemia  (CLL).  Idelalisib,  available  in  100-mg  and  150-mg  tablets,  is  administered  orally  twice  daily.  Idelalisib  may  cause  serious  and  sometimes  fatal  side  effects,  including  liver  toxicity,  diarrhea,  colon  inflammation,  lung  inflammation,  intestinal  perforations,  and  skin  toxicity.  The  drug  carries  a  black  box  warning  to  caution  patients  and  healthcare  providers  about  these  serious  risks,  and  its  use  is  conditional  on  employing  a  risk  evaluation  and  mitigation  strategy  (REMS).2,3