Drugs / Idelalisib
last change Apr 2026 re-read 2 minutes ago

Idelalisib

Small molecule targets PIK3CD via inhibition

Developed for
chronic lymphocytic leukemia/small lymphocytic lymphoma · B-cell chronic lymphocytic leukemia · follicular lymphoma · mantle cell lymphoma · acute myeloid leukemia · diffuse large B-cell lymphoma · marginal zone lymphoma · Waldenstrom macroglobulinemia
+19 more · acute lymphoblastic leukemia · chronic myelomonocytic leukemia · lymphoplasmacytic lymphoma · plasma cell myeloma · amyloidosis · B-cell neoplasm · colorectal cancer · Hodgkins lymphoma · idiopathic pulmonary fibrosis · indolent B-cell non-Hodgkin lymphoma · lymphoid neoplasm · mediastinal malignant lymphoma · myelofibrosis · non-Hodgkin lymphoma · non-small cell lung carcinoma · pancreatic ductal adenocarcinoma · prolymphocytic leukemia · Richter transformation · allergic rhinitis
Investigated by
Gilead Sciences · National Cancer Institute (NCI) · Dana-Farber Cancer Institute · OHSU Knight Cancer Institute · Alliance for Clinical Trials in Oncology · Celgene Corporation
+26 more · German CLL Study Group · Oregon Health and Science University · Acetylon Pharmaceuticals Incorporated · Aptevo Therapeutics · Asha Nayak · Biologics, Inc. · Boehringer Ingelheim · Calluna Pharma AS · Eli Lilly and Company · Fondazione Italiana Linfomi - ETS · Fred Hutchinson Cancer Center · French Innovative Leukemia Organisation · GlaxoSmithKline · Hoffmann-La Roche · John Mark Sloan · Mayo Clinic · Merck Sharp & Dohme LLC · MorphoSys AG · Nordic Lymphoma Group · Novartis Pharmaceuticals · Oslo University Hospital · PETHEMA Foundation · Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins · University of Maryland, Baltimore · University of Miami Sylvester Comprehensive Cancer Center · Virginia Commonwealth University

Regulatory milestones approvals, filings & regulatory actions · 2 recorded

MilestoneJurisdictionBrandIndicationDateSentence it was read from
Approved EU (EMA) Zydelig 2014-09-18 europa.eu
Approved US (FDA) ZYDELIG 2014-07-23 fda.gov

Trials 53 · a red edge is where a trial was stopped

PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 117 trials
Phase 1 NCT03639324 Oct 2020 → Oct 2021 chronic lymphocytic leukemia/small lymphocytic lymphoma Virginia Commonwealth University Withdrawn No outcome recorded
Phase 1 NCT03878524 Apr → Dec 2020 acute myeloid leukemia, atypical chronic myeloid leukemia, BCR-ABL1 negative, blast phase chronic myelogenous leukemia, BCR-ABL1 positive, castration-resistant prostate carcinoma +14 OHSU Knight Cancer Institute Terminated No outcome recorded
Phase 1 NCT03349346 Jun 2019 → Feb 2021 diffuse large B-cell lymphoma, mediastinal malignant lymphoma Gilead Sciences Withdrawn No outcome recorded
Phase 1 NCT03151057 Jul 2018 → Jun 2022 B-cell chronic lymphocytic leukemia, diffuse large B-cell lymphoma, follicular lymphoma, mantle cell lymphoma Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins Terminated No outcome recorded
Phase 1 NCT02787369 May 2016 → Apr 2026 overdue chronic lymphocytic leukemia/small lymphocytic lymphoma Dana-Farber Cancer Institute Active not recruiting No outcome recorded
Phase 1 NCT02779283 Jan 2016 → Apr 2018 acute lymphoblastic leukemia, acute myeloid leukemia OHSU Knight Cancer Institute Completed No outcome recorded
Phase 1 NCT02538614 Dec 2015 → Jul 2017 chronic lymphocytic leukemia/small lymphocytic lymphoma Gilead Sciences Terminated No outcome recorded
Phase 1 NCT02603445 Nov 2015 → Jul 2018 mantle cell lymphoma Novartis Pharmaceuticals Completed No outcome recorded
Phase 1 NCT02468557 Jul 2015 → Apr 2016 pancreatic ductal adenocarcinoma Gilead Sciences Terminated No outcome recorded
Phase 1 NCT02457598 Jun 2015 → Sep 2024 B-cell neoplasm Gilead Sciences Terminated No outcome recorded
Phase 1/24 trials
Phase 1/2 NCT03742323 Jul 2018 → Jun 2020 acute lymphoblastic leukemia PETHEMA Foundation Terminated No outcome recorded
Phase 1/2 NCT03257722 Sep 2017 → Aug 2020 metastatic neoplasm, non-small cell lung carcinoma Asha Nayak Terminated No outcome recorded
Phase 1/2 NCT01306643 Feb 2011 → Aug 2015 chronic lymphocytic leukemia/small lymphocytic lymphoma, follicular lymphoma, marginal zone lymphoma Gilead Sciences Completed No outcome recorded
Phase 1/2 NCT01090414 Mar 2010 → Jun 2018 chronic lymphocytic leukemia/small lymphocytic lymphoma Gilead Sciences Terminated No outcome recorded
Phase 222 trials
Phase 2 NCT06736990 Jun 2025 → Nov 2026 expected idiopathic pulmonary fibrosis Calluna Pharma AS Active not recruiting No outcome recorded
Phase 2 NCT05725200 Sep 2022 → Dec 2038 expected colorectal cancer Oslo University Hospital Recruiting No outcome recorded
Phase 2 NCT03890289 Oct 2019 → Apr 2021 follicular lymphoma Fondazione Italiana Linfomi - ETS Terminated No outcome recorded
Phase 2 NCT03133221 Oct 2017 → Jun 2023 Waldenstrom macroglobulinemia, chronic lymphocytic leukemia/small lymphocytic lymphoma, follicular lymphoma, marginal zone lymphoma University of Maryland, Baltimore Completed No outcome recorded
Phase 2 NCT03576443 Jul 2017 → Sep 2021 diffuse large B-cell lymphoma Nordic Lymphoma Group Completed No outcome recorded
Phase 2 NCT02962401 Mar 2017 → Aug 2020 Waldenstrom macroglobulinemia French Innovative Leukemia Organisation Completed No outcome recorded
Phase 2 NCT02968563 Dec 2016 → Jun 2019 B-cell chronic lymphocytic leukemia Gilead Sciences Completed No outcome recorded
Phase 2 NCT02639910 Nov 2016 → Nov 2018 chronic lymphocytic leukemia/small lymphocytic lymphoma MorphoSys AG Completed No outcome recorded
Phase 2 NCT02662296 Mar 2016 → Feb 2022 chronic lymphocytic leukemia/small lymphocytic lymphoma, prolymphocytic leukemia Fred Hutchinson Cancer Center Withdrawn No outcome recorded
Phase 2 NCT02590588 Jan 2016 → Mar 2017 amyloidosis John Mark Sloan Terminated No outcome recorded
Phase 38 trials
Phase 3 NCT02536300 Jan 2016 → Sep 2022 follicular lymphoma Gilead Sciences Terminated No outcome recorded
Phase 3 NCT01980875 Apr 2015 → May 2016 B-cell chronic lymphocytic leukemia Gilead Sciences Terminated No outcome recorded
Phase 3 NCT01980888 Feb 2014 → May 2016 chronic lymphocytic leukemia/small lymphocytic lymphoma Gilead Sciences Terminated No outcome recorded
Phase 3 NCT01732913 Jan 2013 → May 2016 indolent B-cell non-Hodgkin lymphoma Gilead Sciences Terminated No outcome recorded
Phase 3 NCT01732926 Jan 2013 → May 2016 non-Hodgkin lymphoma Gilead Sciences Terminated No outcome recorded
Phase 3 NCT01659021 Dec 2012 → Aug 2018 chronic lymphocytic leukemia/small lymphocytic lymphoma Gilead Sciences Terminated No outcome recorded
Phase 3 NCT01539291 Oct 2012 → May 2018 chronic lymphocytic leukemia/small lymphocytic lymphoma Gilead Sciences Terminated No outcome recorded
Phase 3 NCT01569295 Jun 2012 → Jun 2019 chronic lymphocytic leukemia/small lymphocytic lymphoma Gilead Sciences Completed No outcome recorded
Phase 42 trials
Phase 4 NCT07218341 Mar 2026 → May 2030 expected chronic lymphocytic leukemia/small lymphocytic lymphoma Eli Lilly and Company Recruiting No outcome recorded
Phase 4 NCT02739360 May 2016 → Dec 2017 lymphoid neoplasm Gilead Sciences Terminated No outcome recorded
Also used as a comparator or background therapy in 9 trials
PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 11 trial
Phase 1 NCT00836914 Comparator Feb → Mar 2009 allergic rhinitis Gilead Sciences Completed No outcome recorded
Phase 21 trial
Phase 2 NCT04699461 Comparator Nov 2021 → Nov 2022 follicular lymphoma ADC Therapeutics S.A. Terminated No outcome recorded
Phase 36 trials
Phase 3 NCT07139873 Comparator Sep 2025 → Jan 2029 expected chronic lymphocytic leukemia/small lymphocytic lymphoma Dizal Pharmaceuticals Recruiting No outcome recorded
Phase 3 NCT06846671 Comparator Apr 2025 → May 2028 expected chronic lymphocytic leukemia/small lymphocytic lymphoma BeOne Medicines Recruiting No outcome recorded
Phase 3 NCT06205290 Comparator Jan 2024 → Oct 2031 B-cell chronic lymphocytic leukemia Juno Therapeutics, Inc., a Bristol-Myers Squibb Company Withdrawn No outcome recorded
Phase 3 NCT04666038 Comparator Mar 2021 → Aug 2023 overdue chronic lymphocytic leukemia/small lymphocytic lymphoma Loxo Oncology, Inc. Active not recruiting No outcome recorded
Phase 3 NCT02970318 Comparator Feb 2017 → Sep 2021 overdue B-cell chronic lymphocytic leukemia Acerta Pharma BV Active not recruiting No outcome recorded
Phase not stated1 trial
NCT02136511 Background B-cell chronic lymphocytic leukemia Gilead Sciences Approved for marketing No outcome recorded

Press releases naming this drug 15 releases

DateIssuerRelease
2015-12-08 Gilead Sciences Phase 3 Results for Zydelig® With Bendamustine and Rituximab for Relapsed Chronic Lymphocytic Leukemia (CLL) Presented at American Society of Hematology Annual Meeting gilead.com
2015-11-16 Gilead Sciences Gilead’s Zydelig® Combined with Bendamustine and Rituximab Shows Superior Efficacy to Bendamustine/Rituximab in Phase 3 Study of Patients with Relapsed Chronic Lymphocytic Leukemia gilead.com
2015-05-31 Gilead Sciences Zydelig® in Combination With Ofatumumab Improves Progression-Free Survival in Previously-Treated Patients With Chronic Lymphocytic Leukemia gilead.com
2014-12-08 Gilead Sciences Gilead Presents Follow-up Data from Zydelig Registrational Studies in Patients with Chronic Lymphocytic Leukemia, Follicular Lymphoma and Small Lymphocytic Lymphoma gilead.com
2014-09-19 Gilead Sciences European Commission Grants Marketing Authorization for Gilead’s Zydelig® (Idelalisib) for the Treatment of Chronic Lymphocytic Leukemia and Follicular Lymphoma gilead.com
2014-07-25 Gilead Sciences European CHMP Adopts Positive Opinion for Gilead’s Zydelig® (idelalisib) for the Treatment of Chronic Lymphocytic Leukemia and Follicular Lymphoma gilead.com
2014-07-23 Gilead Sciences U.S. Food and Drug Administration Approves Gilead’s Zydelig® (idelalisib) for Relapsed Chronic Lymphocytic Leukemia, Follicular Lymphoma and Small Lymphocytic Lymphoma gilead.com
2014-01-13 Gilead Sciences U.S. FDA Accepts New Drug Application for Gilead’s Idelalisib for the Treatment of Refractory Indolent Non-Hodgkin’s Lymphoma gilead.com
2013-12-08 Gilead Sciences Gilead Announces Pivotal Phase 2 Data for Idelalisib in Refractory Indolent Non-Hodgkin’s Lymphoma gilead.com
2013-11-18 Gilead Sciences Gilead’s Idelalisib Significantly Reduces Rate of Disease Progression or Death in Phase 3 Chronic Lymphocytic Leukemia Study gilead.com
2013-10-09 Gilead Sciences Gilead to Stop Phase 3 Study 116 of Idelalisib in Chronic Lymphocytic Leukemia Early Because of Positive Risk-Benefit gilead.com
2013-09-11 Gilead Sciences Gilead Submits New Drug Application to U.S. FDA for Idelalisib for the Treatment of Indolent Non-Hodgkin’s Lymphoma gilead.com

Evidence & citations 12 cited values

Every value below carries the sentence it was read from. 66 sources stand behind the page.

FieldValueCited text
Known as Idelalisib “This research study is evaluating a drug called idelalisib (formerly known as GS-1101 or CAL-101) as a possible treatment for Waldenstrom's Macroglobulinemia (WM).” NCT02439138
55

“100 mg QD of idelalisib + 100 mg QD of venetoclax” NCT03639324

NCT02136511

NCT01644799

NCT01732913

NCT02332980

NCT06846671

NCT01838434

NCT02135133

NCT03878524

NCT02242045

NCT01620216

NCT01644253

NCT02536300

NCT01306643

NCT03349346

NCT01090414

NCT06205290

NCT05725200

NCT02739360

NCT02787369

NCT02457598

NCT02962401

NCT01796470

NCT07218341

NCT02044822

NCT03890289

NCT02639910

NCT03576443

NCT01393106

NCT02779283

NCT01569295

NCT01732926

NCT04666038

NCT01282424

NCT02436135

NCT03257722

NCT07139873

NCT01980888

NCT03151057

NCT02468557

NCT02590588

NCT01980875

NCT02662296

NCT03742323

NCT02970318

NCT01659021

NCT01539291

NCT02258529

NCT01088048

NCT02603445

NCT01203930

NCT04699461

NCT02538614

NCT01539512

NCT02968563

Known as CAL-101 “A Study of Idelalisib (GS1101, CAL101) + Ofatumumab in Previously Untreated CLL/SLL” NCT02135133
5

“phosphatidylinositol 3-kinase delta (PI3K-delta) inhibitor GS-1101 (CAL-101)” NCT01659047

NCT06736990

NCT00710528

NCT02445131

NCT00836914

Known as CAL-101 (GS-1101) ChEMBL registry synonym — accepted as the source's own label CHEMBL2216870
Known as GS-1101 “This research study is evaluating a drug called idelalisib (formerly known as GS-1101 or CAL-101) as a possible treatment for Waldenstrom's Macroglobulinemia (WM).” NCT02439138
2

“Study of Phosphatidylinositol-3-kinase (PI3K) Inhibitor, Idelalisib (GS-1101), in IgM-Associated AL Amyloid” NCT02590588

NCT01659047

Known as GS-11CAL-101 ChEMBL registry synonym — accepted as the source's own label CHEMBL2216870
Known as IDELA “A randomized, double-blind, phase III study of idelalisib (IDELA) plus rituximab versus placebo plus rituximab in patients with relapsed chronic lymphocytic leukemia (CLL) was...” PMID 30995176 Apr 2019
1

“Cohort 1a: Idelalisib (IDELA) 100 mg orally twice daily (BID)” NCT01088048

Known as IDELALISIBCT-CAL101IDEALISIBCAL-101CAL 101GS-1101GS 1101ZYDELIGA-1138CAL101 ChEMBL registry synonym — accepted as the source's own label CHEMBL2216870
Known as Zydelig ClinicalTrials.gov intervention name — accepted as the source's own label NCT03133221
Action Inhibit “an oral inhibitor of phosphatidylinositol 3-kinase (PI3K) delta” NCT00836914
Modality Small molecule “Idelalisib is a small-molecule inhibitor of PI3Kδ” PMID 27247136 May 2016
Route Oral “administered orally” NCT00836914
Target PIK3CD “The phosphatidylinositol-3-kinase delta (PI3Kδ) inhibitor idelalisib” PMID 28327905 May 2017