idelalisib
Trade name: zydelig
Small moleculeapprovedOrphan Drug FDAFast Track FDABreakthrough Therapy FDA
Approved
Jul 23, 2014
Idelalisib is a first-in-class selective inhibitor of adenosine-5'-triphosphate (ATP) binding to PI3Kdelta kinase, resulting in inhibition of the P13K signalling pathway in malignant B cells. The compound is approved for the treatment of several types of blood cancer. Idelalisib is intended to be used in combination with rituximab as second or subsequent line therapy for the treatment of chronic lymphocytic leukaemia. The drug may cause fatal and/or severe diarrhea or colitis, hepatotoxicity, pneumonitis and intestinal perforation. — NCATS
Clinical trial activity
62 trials · 43 clinical orgs · 2 marketing orgs
Phase 1
21
Phase 2
41
Phase 3
14
Phase 4
2
Earliest trial started Jun 1, 2008 (NCT00710528)
Timeline
2000s
- Jan 1, 2008
Gilead Sciences — Earliest Phase 1 Sponsor(trial)
2010s
- Jan 1, 2010
Gilead Sciences — Earliest Phase 2 Sponsor(trial)
- Jan 1, 2012
Gilead Sciences — Earliest Phase 3 Sponsor(trial)
- Sep 26, 2013
Orphan Drug Designation
- Jul 23, 2014
Gilead Sciences — Earliest FDA Approval
- Jul 23, 2014
Gilead Sciences — NDA Organization
2020s
- Feb 17, 2026
Natco Pharma — Marketing Organization
Indications
Approved for
Studied for
- Amyloidosis · Phase 2
- Anemia · Phase 1
- Breast Neoplasms · Phase 1
- Carcinoma, Non-Small-Cell Lung · Phase 1/Phase 2
- Colorectal Neoplasms · Phase 2
- Hodgkin Disease · Phase 2
- Immunoglobulin Light-chain Amyloidosis · Phase 2
- Leukemia, B-Cell · Phase 1
- Leukemia, Myelogenous, Chronic, BCR-ABL Positive · Phase 1
- Leukemia, Myeloid, Acute · Phase 1
- Leukemia, Myeloid, Chronic, Atypical, BCR-ABL Negative · Phase 1
- Leukemia, Myeloid, Chronic-Phase · Phase 1
- Leukemia, Myelomonocytic, Chronic · Phase 1
- Leukemia, Prolymphocytic · Phase 2
- Lymphoma · Phase 4
- Lymphoma, B-Cell · Phase 2
- Lymphoma, B-Cell, Marginal Zone · Phase 2
- Lymphoma, Follicular · Phase 3
- Lymphoma, Large B-Cell, Diffuse · Phase 2
- Lymphoma, Mantle-Cell · Phase 2
- Lymphoma, Primary Cutaneous Anaplastic Large Cell · Phase 2
- Lymphoma, T-Cell, Peripheral · Phase 1
- Multiple Myeloma · Phase 1
- Myelodysplastic Syndromes · Phase 1
- Myeloproliferative Disorders · Phase 1
- Neoplasm Metastasis · Phase 1/Phase 2
- Pancreatic Neoplasms · Phase 1
- Precursor B-Cell Lymphoblastic Leukemia-Lymphoma · Phase 2
- Precursor Cell Lymphoblastic Leukemia-Lymphoma · Phase 1/Phase 2
- Primary Myelofibrosis · Phase 1
- Prostatic Neoplasms, Castration-Resistant · Phase 1
- Recurrence · Phase 1/Phase 2
- Rhinitis, Allergic · Phase 1
- Squamous Intraepithelial Lesions · Phase 1
- Waldenstrom Macroglobulinemia · Phase 2
Mechanism of action
Approval history
- approvedAcceleratedFast trackBreakthroughJul 23, 2014
Chemistry & pharmacology
Loading structure…
SMILES
CC[C@H](NC1=NC=NC2=C1N=CN2)C3=NC4=C(C(=O)N3C5=CC=CC=C5)C(F)=CC=C4- Mol. weight
- 415.423 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Black box warningFirst in class
Sources
- WikipediaIdelalisib ↗
- NCATSYG57I8T5M0 ↗
- ChEMBLCHEMBL2216870 ↗
Also known as
- 5-fluoro-3-phenyl-2-[(1s)-1-(3h-purin-6-ylamino)propyl]quinazolin-4(3h)-one
- 5-fluoro-3-phenyl-2-[(1s)-1-(3h-purin-6-ylamino)propyl]quinazolin-4(3h)-one
- 5-fluoro-3-phenyl-2-((s)-1-(9h-purin-6-ylamino)-propyl)-3h-quinazolin-4-one
- 5-fluoro-3-phenyl-2-((s)-1-(9h-purin-6-ylamino)-propyl)-3h-quinazolin-4-one
- cal101
- cal 101
- cal 101
- cal 101
- cal 101
- cal 101
- cal 101
- cal-101
- cal-101
- cal-101
- cal-101
- cal-101
- gs-1101
- gs-1101
- gs-1101
- gs-1101
- gs-1101
- gs-11cal-101
- gs-11cal-101
- idelalisib
- idelalisib
- idelalisib
- idelalisib
- idelalisib
- idelalisib
- idelalisib
- idelalisib
- idelalisib
- idelalisib
- idelalisib
- idelaslisib
- zydelig
- zydelig
- zydelig
- zydelig
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07218341 | Phase 4 | Mar 31, 2026 | Eli Lilly |
| NCT07139873 | Phase 3 | Sep 8, 2025 | Dizal (Jiangsu) Pharmaceutical Co., Ltd. |
| NCT06846671 | Phase 3 | Apr 11, 2025 | BeOne Medicines |
| NCT06205290 | Phase 3 | Jan 16, 2024 | Bristol-Myers Squibb, Celgene |
| NCT05725200 | Phase 2 | Sep 27, 2022 | University of Oslo |
| NCT04699461 | Phase 2 | Nov 4, 2021 | ADC Therapeutics SARL |
| NCT04666038 | Phase 3 | Jan 31, 2021 | Loxo Oncology |
| NCT04304144 | Phase 2 | Mar 18, 2020 | Fortress Biotech |
| NCT03890289 | Phase 2 | Jun 30, 2019 | Fondazione Italiana Diabete Onlus, University of Bologna |
| NCT03878524 | Phase 1 | Mar 14, 2019 | OHSU Knight Cancer Institute, Oregon Health and Science University, Prospect Creek Foundation |
| NCT03349346 | Phase 1 | Oct 31, 2018 | Gilead Sciences |
| NCT03639324 | Phase 1 | Oct 1, 2018 | Virginia Commonwealth University |
| NCT03742323 | Phase 1/Phase 2 (Phase 2) | Jul 1, 2018 | PETHEMA Foundation |
| NCT03257722 | Phase 1/Phase 2 (Phase 2) | Sep 26, 2017 | Augusta University, Gilead Sciences, Merck |
| NCT03576443 | Phase 2 | Jul 7, 2017 | Nordic Lymphoma Group |
| NCT03133221 | Phase 2 | Jun 1, 2017 | Gilead Sciences, University of Maryland, Virginia Commonwealth University, Washington University in St. Louis |
| NCT03126019 | Phase 2 | Jun 1, 2017 | Incyte |
| NCT03151057 | Phase 1 | Apr 20, 2017 | Johns Hopkins University |
| NCT02962401 | Phase 2 | Mar 7, 2017 | French Innovative Leukemia Organisation |
| NCT02928510 | N/A | Jan 1, 2017 | Gilead Sciences, National Cancer Institute (NCI), University of California, Los Angeles |
Showing 20 of 62 trials
Page 1 / 4
Organizations
Research & Development (43)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Gilead Sciences | For profit | 38 | 30 | 5 | 2008 |
| National Cancer Institute (NCI) | Government | 5 | 2 | 3 | 2013 |
| Celgene | For profit | 3 | 0 | 3 | 2013 |
| Harvard University | Academic/Hospital | 3 | 3 | 2 | 2014 |
| German CLL Study Group | Academic/Hospital | 2 | 1 | 1 | 2015 |
| Virginia Commonwealth University | Academic/Hospital | 2 | 1 | 2 | 2017 |
| Acerta Pharma | For profit | 1 | 1 | 1 | 2016 |
| Acetylon Pharmaceuticals Incorporated | For profit | 1 | 0 | 1 | 2016 |
| ADC Therapeutics SARL | For profit | 1 | 1 | 1 | 2021 |
| Aptevo Therapeutics | For profit | 1 | 1 | 1 | 2012 |
| Augusta University | Academic/Hospital | 1 | 1 | 1 | 2017 |
| BeOne Medicines | For profit | 1 | 1 | 1 | 2025 |
| Biologics, Inc. | For profit | 1 | 0 | 1 | 2013 |
| Boehringer Ingelheim | For profit | 1 | 0 | 1 | 2015 |
| Boston University | Academic/Hospital | 1 | 1 | 1 | 2016 |
| Bristol-Myers Squibb | For profit | 1 | 1 | 1 | 2024 |
| Cornell University | Academic/Hospital | 1 | 0 | 1 | 2013 |
| Dizal (Jiangsu) Pharmaceutical Co., Ltd. | For profit | 1 | 1 | 1 | 2025 |
| Eli Lilly | For profit | 1 | 1 | 1 | 2026 |
| Fondazione Italiana Diabete Onlus | Academic/Hospital | 1 | 1 | 1 | 2019 |
43 organizations
Page 1 / 3
Marketing (2)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Gilead Sciences | For profit | NDA | Jul 23, 2014 |
| Natco Pharma | For profit | MKTG | Feb 17, 2026 |