IDELALISIB
Idelalisib is a kinase inhibitor used for patients with relapsed chronic lymphocytic leukemia (CLL). It is prescribed in combination with rituximab for individuals who have other health issues that make rituximab alone a suitable option. This medication is specifically for those whose cancer has returned and is not used as an initial therapy.
How IDELALISIB Works
This drug works by targeting PI3Kδ, a protein found in both healthy and cancerous B-cells. By blocking this kinase and other signaling pathways, it prevents cancer cells from moving to the lymph nodes and bone marrow while also triggering cell death. This process stops the tumor cells from growing, sticking together, and surviving.
Details
- Status
- Prescription
- First Approved
- 2026-02-17
- Routes
- ORAL
- Dosage Forms
- TABLET
IDELALISIB Approval History
What IDELALISIB Treats
3 indicationsIDELALISIB is approved for 3 conditions since its original approval in 2026. These indications span multiple therapeutic areas including oncology, immunology, and more.
- Chronic Lymphocytic Leukemia
- Follicular Lymphoma
- Non-Hodgkin Lymphoma
IDELALISIB Boxed Warning
FATAL AND SERIOUS TOXICITIES: HEPATIC, SEVERE DIARRHEA, COLITIS, PNEUMONITIS, INFECTIONS, and INTESTINAL PERFORATION Fatal and/or serious hepatotoxicity occurred in 16% of Zydelig-treated patients. Monitor hepatic function prior to and during treatment. Interrupt and then reduce or discontinue Zydelig as recommended [see Dosage and Administration (2.2) , Warnings and Precautions (5.1) ] . Fatal and/or serious and severe diarrhea or colitis occurred in 20% of Zydelig-treated patients. Monitor for...
WARNING: FATAL AND SERIOUS TOXICITIES: HEPATIC, SEVERE DIARRHEA, COLITIS, PNEUMONITIS, INFECTIONS, and INTESTINAL PERFORATION Fatal and/or serious hepatotoxicity occurred in 16% of Zydelig-treated patients. Monitor hepatic function prior to and during treatment. Interrupt and then reduce or discontinue Zydelig as recommended [see Dosage and Administration (2.2) , Warnings and Precautions (5.1) ] . Fatal and/or serious and severe diarrhea or colitis occurred in 20% of Zydelig-treated patients. Monitor for the development of severe diarrhea or colitis. Interrupt and then reduce or discontinue Zydelig as recommended [see Dosage and Administration (2.2) , Warnings and Precautions (5.2) ] . Fatal and/or serious pneumonitis occurred in 4% of Zydelig-treated patients. Monitor for pulmonary symptoms and bilateral interstitial infiltrates. Interrupt or discontinue Zydelig as recommended [see Dosage and Administration (2.2) , Warnings and Precautions (5.3) ] . Fatal and/or serious infections occurred in 48% of Zydelig-treated patients. Monitor for signs and symptoms of infection. Interrupt Zydelig if infection is suspected [see Dosage and Administration (2.2) , Warnings and Precautions (5.4) ]. Fatal and serious intestinal perforation can occur in Zydelig-treated patients across clinical trials. Discontinue Zydelig for intestinal perforation [see Warnings and Precautions (5.5) ] . WARNING: FATAL AND SERIOUS TOXICITIES: HEPATIC, SEVERE DIARRHEA, COLITIS, PNEUMONITIS, INFECTIONS, and INTESTINAL PERFORATION See full prescribing information for complete boxed warning. Fatal and/or serious hepatotoxicity occurred in 16% of Zydelig-treated patients. Monitor hepatic function prior to and during treatment. Interrupt and then reduce or discontinue Zydelig. ( 5.1 ) Fatal and/or serious and severe diarrhea or colitis occurred in 20% of Zydelig-treated patients. Monitor for the development of severe diarrhea or colitis. Interrupt and then reduce or discontinue Zydelig. ( 5.2 ) Fatal and/
IDELALISIB Target & Pathway
ProTarget
A family of enzymes involved in cell growth, proliferation, and survival signaling. PI3K pathway activation is common in cancer. Inhibiting specific PI3K isoforms is effective in certain blood cancers and solid tumors.
IDELALISIB Competitive Set
ProThree rings of competition based on shared molecular targets and treated indications.
Indication competitors
Same indication, different mechanism — what else might this patient receive?
Filters applied: drops same-active-ingredient (505(b)(2) reformulations), route-mismatch (topical vs systemic), and cross-therapeutic-area matches in same-indication rings.
What's emerging in IDELALISIB's indications
See all emerging drugs →Phase 3 candidates targeting molecules with no FDA-approved drug, in indications IDELALISIB treats. First-in-class if their pivotal trials read out positive.
Drugs Similar to IDELALISIB
3 of 20FDA-approved drugs for similar conditions. Compare mechanisms and indications to understand treatment alternatives.
Clinical Trial Registry
51 trials| Trial | Sponsor ID | Phase | Status | Title |
|---|---|---|---|---|
| NCT02970318 results posted | ACE-CL-309 2015-004454-17 | Ph 3 | active not recruiting | A Study of Acalabrutinib vs Investigator's Choice of Idelalisib Plus Rituximab or Bendamustine Plus Rituximab in R/R CLL |
| NCT06846671 CaDAnCe-302 | BGB-16673-302 2024-518893-15-00 | Ph 3 | recruiting | A Study of BGB-16673 Compared to Investigator's Choice in Participants With Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma Previously Exposed to Both Bruton Tyrosine Kinase (BTK) and B-cell Leukemia/Lymphoma 2 Protein (BCL2) Inhibitors |
| NCT04666038 BRUIN CLL-321 results posted | 18073 J2N-OX-JZNN, LOXO-BTK-20020 | Ph 3 | active not recruiting | Study of LOXO-305 (Pirtobrutinib) Versus Investigator's Choice (Idelalisib Plus Rituximab or Bendamustine Plus Rituximab) in Patients With Previously Treated Chronic Lymphocytic Leukemia (CLL)/Small Lymphocytic Lymphoma (SLL) |
| NCT07218341 | 27296 J2N-MC-JZ03, J2N-MC-JZNY | Ph 4 | recruiting | A Study of Pirtobrutinib (LY3527727) in Participants With Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma |
| NCT07139873 | DZ2024B0002 | Ph 3 | recruiting | A Study of DZD8586 Versus Investigator's Choice in r/r CLL/SLL (TAI-SHAN6) |
| NCT02135133 results posted | 13-309 | Ph 2 | completed | A Study of Idelalisib (GS1101, CAL101) + Ofatumumab in Previously Untreated CLL/SLL |
| NCT02787369 | 15-558 | Ph 1 | active not recruiting | ACY-1215 in Combination With BCR Pathway Inhibitors in Relapsed CLL |
| NCT02457598 results posted | GS-US-401-1757 2015-000834-30 | Ph 1 | terminated | Dose Escalation and Dose Expansion Study of Tirabrutinib in Combination With Other Targeted Anti-cancer Therapies in Adults With B-cell Malignancies |
| NCT03890289 GAUDEALIS results posted | FIL_GAUDEALIS | Ph 2 | terminated | Idelalisib+Obinutuzumab in Patients With Relapsed/Refractory Follicular Lymphoma |
| NCT06205290 | CA082-1170 | Ph 3 | withdrawn | A Study to Compare the Efficacy and Safety of Lisocabtagene Maraleucel vs Investigator's Choice Options in Adult Participants With Relapsed or Refractory Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma, Whose Disease Has Failed Treatment With Both BTKi and BCL2i Therapies |
| NCT03878524 | STUDY00015588 NCI-2020-02743, STUDY00015588 | Ph 1 | terminated | Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) PRIME Trial |
| NCT03257722 PIL results posted | GCC-16053 | Ph 1, Ph 2 | terminated | Pembrolizumab + Idelalisib for Lung Cancer Study |
| NCT02332980 results posted | MC1485 NCI-2014-02561, MC1485 | Ph 2 | completed | Pembrolizumab Alone or With Idelalisib or Ibrutinib in Treating Patients With Relapsed or Refractory Chronic Lymphocytic Leukemia or Other Low-Grade B-Cell Non-Hodgkin Lymphomas |
| NCT04699461 LOTIS-6 results posted | ADCT 402-202 2020-003695-40 | Ph 2 | terminated | Study to Evaluate the Efficacy and Safety of Loncastuximab Tesirine Versus Idelalisib in Participants With Relapsed or Refractory Follicular Lymphoma |
| NCT02962401 RemodelWM3 | RemodelWM3 | Ph 2 | completed | Efficacity of Idelalisib and Obinutuzumab in Patient With Relapsed Refractory Waldenstrom's Macroglobulinemia |
| NCT02536300 results posted | GS-US-313-1580 2015-000366-66 | Ph 3 | terminated | Dose Optimization Study of Idelalisib in Follicular Lymphoma |
| NCT05725200 EVIDENT | EVIDENT | Ph 2 | recruiting | Study to Investigate Outcome of Individualized Treatment in Patients With Metastatic Colorectal Cancer |
| NCT02968563 results posted | GS-US-401-1958 2015-003909-42, CLLRUmbrella1 | Ph 2 | completed | Study to Evaluate the Safety and Efficacy of the Combination of Tirabrutinib and Idelalisib With and Without Obinutuzumab in Adults With Relapsed or Refractory Chronic Lymphocytic Leukemia (CLL) |
| NCT02639910 COSMOS results posted | MOR208C205 | Ph 2 | completed | Study to Evaluate Safety and Preliminary Efficacy of Tafasitamab With Idelalisib or Venetoclax in R/R CLL/SLL Patients Pretreated With BTKi |
| NCT01620216 results posted | IRB00007195 NCI-2012-01084, CA180-392 | Ph 2 | terminated | Targeted Therapy in Treating Patients With Relapsed or Refractory Acute Lymphoblastic Leukemia or Acute Myelogenous Leukemia |
| NCT03576443 ILIAD | NLG-LBC-07 | Ph 2 | completed | Trial of Idelalisib in Patients With Relapsed Diffuse Large B-cell Lymphoma |
| NCT03742323 | REALIB-LLA-2017 | Ph 1, Ph 2 | terminated | REALIB-LLA-2017: Idelalisib in Patients With Acute Lymphoblastic Leukemia |
| NCT02468557 results posted | GS-US-385-1577 | Ph 1 | terminated | Study of Single Agent Idelalisib Followed by Idelalisib in Combination With Chemotherapy in Adults With Metastatic Pancreatic Ductal Adenocarcinoma |
| NCT02242045 results posted | GS-US-313-1380 | Ph 1 | completed | Study to Evaluate Safety, Tolerability, and Pharmacokinetics of Idelalisib in Japanese Participants With Relapsed or Refractory Indolent B-Cell Non-Hodgkin Lymphomas (iNHL) or Chronic Lymphocytic Leukemia (CLL) |
| NCT01088048 results posted | 101-07 | Ph 1 | completed | Study to Investigate Idelalisib in Combination With Chemotherapeutic Agents, Immunomodulatory Agents and Anti-CD20 Monoclonal Antibody (mAb) in Participants With Relapsed or Refractory Indolent B-cell Non-Hodgkin's Lymphoma, Mantle Cell Lymphoma or Chronic Lymphocytic Leukemia |
| NCT02538614 results posted | GS-US-312-1579 | Ph 1 | terminated | Study of Idelalisib in Combination With BI 836826 in Participants With Chronic Lymphocytic Leukemia |
| NCT02436135 Madison results posted | GS-US-397-1245 | Ph 1 | terminated | Study to Evaluate Safety, Tolerability, and Pharmacokinetics of Idelalisib in Adults Receiving Ruxolitinib as Therapy for Primary, Post-Polycythemia Vera, or Post-Essential Thrombocythemia Myelofibrosis With Progressive or Relapsed Disease |
| NCT01796470 results posted | GS-US-339-0103 | Ph 2 | terminated | Entospletinib in Combination With Idelalisib in Adults With Relapsed or Refractory Hematologic Malignancies |
| NCT02779283 | IRB00011766 NCI-2016-00083, IRB00011766 | Ph 1 | completed | Personalized Kinase Inhibitor Therapy Combined With Chemotherapy in Treating Patients With Newly Diagnosed Acute Myeloid Leukemia and Acute Lymphoblastic Leukemia |
| NCT01569295 Tugela results posted | GS-US-312-0115 2011-006292-20 | Ph 3 | completed | Study Evaluating the Efficacy and Safety of Idelalisib in Combination With Bendamustine and Rituximab for Previously Treated Chronic Lymphocytic Leukemia (CLL) (Tugela ) |
| NCT02739360 results posted | GS-US-313-2120 2015-005766-39 | Ph 4 | terminated | Roll Over Study to Provide Idelalisib to Participants Previously Treated With the Investigational PI3Kδ Inhibitor, GS-9820 |
| NCT02603445 | CBCL201X2102C | Ph 1 | completed | Study of Safety and Efficacy of BCL201 and Idelalisib in Patients With FL and MCL |
| NCT01090414 results posted | 101-99 | Ph 1, Ph 2 | terminated | An Extension Study for Subjects Who Are Deriving Benefit With Idelalisib (GS-1101; CAL-101) Following Completion of a Prior Idelalisib Study |
| NCT01539291 results posted | GS-US-312-0117 2011-006293-72 | Ph 3 | terminated | Extension Study of Idelalisib in Participants With Chronic Lymphocytic Leukemia (CLL) Who Participated in GS-US-312-0116 (NCT01539512) |
| NCT01659021 results posted | GS-US-312-0119 2012-001236-65 | Ph 3 | terminated | Efficacy and Safety of Idelalisib in Combination With Ofatumumab for Previously Treated Chronic Lymphocytic Leukemia |
| NCT01282424 DELTA results posted | 101-09 2010-022155-33 | Ph 2 | completed | Efficacy and Safety Study of Idelalisib in Participants With Indolent B-Cell Non-Hodgkin Lymphomas |
| NCT01539512 results posted | GS-US-312-0116 2011-005180-24 | Ph 3 | completed | A Randomized, Double-Blind, Placebo-Controlled Study of Idelalisib in Combination With Rituximab for Previously Treated Chronic Lymphocytic Leukemia (CLL) |
| NCT02258529 results posted | GS-US-313-1414 | Ph 2 | terminated | Idelalisib in Combination With Rituximab for Previously Untreated Follicular Lymphoma and Small Lymphocytic Lymphoma |
| NCT03349346 | GS-US-313-1090 2017-001468-39 | Ph 1 | withdrawn | Idelalisib With Rituximab, Ifosfamide, Carboplatin, Etoposide (RICE) in Children and Adolescents |
| NCT01306643 results posted | 101-10 | Ph 1, Ph 2 | completed | Safety and Efficacy Study of Idelalisib (GS-1101, CAL-101) in Patients With Previously Treated Low-grade Lymphoma |
| NCT02044822 results posted | GS-US-312-0133 2013-003314-41 | Ph 2 | terminated | Efficacy and Safety of Idelalisib in Combination With Rituximab in Patients With Previously Untreated Chronic Lymphocytic Leukemia With 17p Deletion |
| NCT01980888 results posted | GS-US-312-0123 2013-003313-17 | Ph 3 | terminated | Efficacy and Safety of Idelalisib in Combination With Bendamustine and Rituximab in Adults With Previously Untreated Chronic Lymphocytic Leukemia |
| NCT01980875 results posted | GS-US-312-0118 2013-004551-20 | Ph 3 | terminated | Efficacy and Safety of Idelalisib in Combination With Obinutuzumab Compared to Chlorambucil in Combination With Obinutuzumab for Previously Untreated Chronic Lymphocytic Leukemia |
| NCT01393106 results posted | 101-11 | Ph 2 | completed | Safety and Efficacy of Idelalisib in Relapsed or Refractory Hodgkin Lymphoma |
| NCT01203930 results posted | 101-08 | Ph 2 | terminated | A Study of Idelalisib and Rituximab in Elderly Patients With Untreated CLL or SLL |
| NCT01732926 Bridalveil results posted | GS-US-313-0125 2012-004034-42 | Ph 3 | terminated | Efficacy and Safety of Idelalisib (GS-1101) in Combination With Bendamustine and Rituximab for Previously Treated Indolent Non-Hodgkin Lymphomas |
| NCT01732913 Yosemite results posted | GS-US-313-0124 | Ph 3 | terminated | Efficacy and Safety of Idelalisib (GS-1101) in Combination With Rituximab for Previously Treated Indolent Non-Hodgkin Lymphomas |
| NCT01838434 | A051201 NCI-2012-01734, U10CA031946 | Ph 1 | completed | Lenalidomide With or Without Idelalisib in Treating Patients With Relapsed or Refractory Mantle Cell Lymphoma |
| NCT01644799 | A051202 CDR0000736814, NCI-2012-01988 | Ph 1 | completed | Lenalidomide and Idelalisib in Treating Patients With Recurrent Follicular Lymphoma |
| NCT02662296 | 2561.00 NCI-2015-02201, 2561.00 | Ph 2 | withdrawn | Ibrutinib or Idelalisib in Treating Patients With Persistent or Relapsed Chronic Lymphocytic Leukemia, Small Lymphocytic Lymphoma, or Non-Hodgkin Lymphoma After Donor Stem Cell Transplant |
Showing 50 of 51 trials
Active Pipeline
Ongoing clinical trials by development phase
Key Completed Trials
Completed studies with published results, ranked by significance
Trial Timeline
Full development history with FDA approval milestones
Understanding FDA Approval Types
| Count | Type | What it means |
|---|---|---|
| - | ORIG | Original approval - drug first enters market |
| - | SUPPL - Efficacy | New indication (new disease/condition approved) |
| - | SUPPL - Labeling | Label text changes (warnings, dosing updates) |
| - | SUPPL - Manufacturing | Production changes (new facility) |
| - | SUPPL - Chemistry | Formulation changes (new dosage strength) |
Green lines in the timeline show ORIG and Efficacy approvals - the clinically meaningful milestones.
IDELALISIB FDA Label Details
Indications & Usage
IDELALISIB is indicated for the treatment of Chronic Lymphocytic Leukemia; Follicular Lymphoma; Non-Hodgkin Lymphoma.
WARNING: FATAL AND SERIOUS TOXICITIES: HEPATIC, SEVERE DIARRHEA, COLITIS, PNEUMONITIS, INFECTIONS, and INTESTINAL PERFORATION Fatal and/or serious hepatotoxicity occurred in 16% of Zydelig-treated patients. Monitor hepatic function prior to and during treatment. Interrupt and then reduce or disconti...
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ZYDELIG
Full clinical data, patents, trials, and competitive landscape for idelalisib.
Data Sources
Data sourced from official FDA and NIH databases. Click links to verify on original sources.