Idelalisib
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Also known as CAL-101GS-1101Gs-11cal-101ZydeligCAL-101 (GS-1101)CAL 101IdelalisibIdelalisibÊIdelalisibÂCal101
Summary
Idelalisib (CHEMBL2216870) is an approved small-molecule antineoplastic agent (ATC L01EM01) targeting PIK3CA, PIK3CB, and PIK3CD; indicated across 19 conditions including b-cell chronic lymphocytic leukemia and neoplasm; with CIViC clinical evidence for 1 variant-indication association (e.g. PIK3CA P471L in merkel cell carcinoma).
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01EM01
- Targets: 4 (PIK3CA, PIK3CB, PIK3CD…)
- Indications: 19 conditions
- Clinical trials: 64
- Precision-oncology evidence (CIViC): 1 variant–indication association
- Chemistry: 415.4 Da · C22H18FN7O
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL2216870 |
| Name | Idelalisib |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 11625818 |
| ChEBI | CHEBI:82701 |
| ATC | L01EM01 |
| Molecular formula | C22H18FN7O |
| Molecular weight | 415.4 |
| InChIKey | IFSDAJWBUCMOAH-HNNXBMFYSA-N |
SMILES: CC[C@@H](C1=NC2=C(C(=CC=C2)F)C(=O)N1C3=CC=CC=C3)NC4=NC=NC5=C4NC=N5
IUPAC name: 5-fluoro-3-phenyl-2-[(1S)-1-(7H-purin-6-ylamino)propyl]quinazolin-4-one
ChEBI definition: A member of the class of quinazolines that is 5-fluoro-3-phenylquinazolin-4-one in which the hydrogen at position 2 is replaced by a (1S)-1-(3H-purin-6-ylamino)propyl group. used for for the treatment of refractory indolent non-Hodgkin’s lymphoma and relapsed chronic lymphocytic leukemia.
Pharmacological roles (ChEBI): antineoplastic agent, apoptosis inducer, EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor.
Also known as: CAL-101, GS-1101, Gs-11cal-101, Idelalisib, Zydelig, IDELALISIB, GS-11CAL-101, CAL-101 (GS-1101), CAL 101, ZYDELIG, idelalisib, Idelalisib; Zydelig
Patent coverage: 4,003 distinct patent families (10,163 SureChEMBL compound mentions), from 5 matched compound structure(s). One matched structure accounts for 9,090 (89%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| PIK3CA | phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha | Inhibition | 6.09 | 42.7% | P42336 |
| PIK3CB | phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta | Inhibition | 6.25 | 5% | P42338 |
| PIK3CD | phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta | Inhibition | 8.6 | 6% | O00329 |
| PIK3CG | phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma | Inhibition | 7.05 | 0.7% | P48736 |
Broader ChEMBL bioactivity targets: 18 (assay-derived). Sample: Phosphatidylinositol 3-kinase catalytic subunit type 3, PI3-kinase p110-alpha/p85-alpha, PI3-kinase p110-delta/p85-alpha, 5-hydroxytryptamine receptor 1A, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, Prostaglandin G/H synthase 1, Mu-type opioid receptor, Sodium-dependent dopamine transporter, cGMP-inhibited 3’,5’-cyclic phosphodiesterase 3A, 3’,5’-cyclic-AMP phosphodiesterase 4D.
Bioactivity
ChEMBL activities: 168 potent at pChembl ≥ 5 of 172 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| PIK3CD | 9 | IC50 | 1 | nM | CHEMBL_ACT_25038380 |
| PIK3CD | 8.97 | IC50 | 1.08 | nM | CHEMBL_ACT_23279989 |
| PIK3CD | 8.92 | IC50 | 1.2 | nM | CHEMBL_ACT_19242051 |
| PIK3CD | 8.8 | IC50 | 1.6 | nM | CHEMBL_ACT_18658752 |
| PIK3CD | 8.8 | Ki | 1.58 | nM | CHEMBL_ACT_29215579 |
| PIK3CD | 8.74 | IC50 | 1.8 | nM | CHEMBL_ACT_19174499 |
| PIK3CD | 8.7 | IC50 | 2 | nM | CHEMBL_ACT_16673471 |
| PIK3CD | 8.7 | IC50 | 2 | nM | CHEMBL_ACT_18077974 |
| PIK3CD | 8.7 | IC50 | 2 | nM | CHEMBL_ACT_18113972 |
| PIK3CD | 8.7 | IC50 | 2 | nM | CHEMBL_ACT_18952539 |
| PIK3CD | 8.7 | IC50 | 2 | nM | CHEMBL_ACT_19041449 |
| PIK3CD | 8.7 | IC50 | 2 | nM | CHEMBL_ACT_23296114 |
| PIK3CD | 8.68 | IC50 | 2.1 | nM | CHEMBL_ACT_19207806 |
| PIK3CD | 8.6 | IC50 | 2.5 | nM | CHEMBL_ACT_12645772 |
| PIK3CD | 8.6 | IC50 | 2.5 | nM | CHEMBL_ACT_14553166 |
| PIK3CD | 8.6 | IC50 | 2.5 | nM | CHEMBL_ACT_18197122 |
| PIK3CD | 8.6 | IC50 | 2.5 | nM | CHEMBL_ACT_18573179 |
| PIK3CD | 8.6 | IC50 | 2.5 | nM | CHEMBL_ACT_18578195 |
| PIK3CD | 8.6 | IC50 | 2.5 | nM | CHEMBL_ACT_19036837 |
| PIK3CD | 8.6 | IC50 | 2.5 | nM | CHEMBL_ACT_22885893 |
| PIK3CD | 8.6 | IC50 | 2.5 | nM | CHEMBL_ACT_23127306 |
| PIK3CD | 8.6 | IC50 | 2.5 | nM | CHEMBL_ACT_23258676 |
| PIK3CD | 8.6 | IC50 | 2.5 | nM | CHEMBL_ACT_24862055 |
| PIK3CD | 8.6 | IC50 | 2.5 | nM | CHEMBL_ACT_25892698 |
| PIK3CD | 8.59 | IC50 | 2.56 | nM | CHEMBL_ACT_29244756 |
| PIK3CD | 8.57 | IC50 | 2.7 | nM | CHEMBL_ACT_15166421 |
| PIK3CD | 8.57 | IC50 | 2.7 | nM | CHEMBL_ACT_18234615 |
| PIK3CD | 8.57 | IC50 | 2.7 | nM | CHEMBL_ACT_18578193 |
| PIK3CD | 8.54 | IC50 | 2.9 | nM | CHEMBL_ACT_25634111 |
| PIK3CD | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_16490965 |
Target pathways
Aggregated over 4 target gene(s): PIK3CA, PIK3CB, PIK3CD, PIK3CG.
Top Reactome pathways
62 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| PIP3 activates AKT signaling | 4 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| Synthesis of PIPs at the plasma membrane | 4 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| Constitutive Signaling by Aberrant PI3K in Cancer | 4 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| CD28 dependent PI3K/Akt signaling | 4 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling | 4 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| Erythropoietin activates Phosphoinositide-3-kinase (PI3K) | 4 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| Co-stimulation by ICOS | 4 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| GPVI-mediated activation cascade | 3 | PIK3CA, PIK3CB, PIK3CG |
| Interleukin-3, Interleukin-5 and GM-CSF signaling | 3 | PIK3CA, PIK3CB, PIK3CD |
| RET signaling | 3 | PIK3CA, PIK3CB, PIK3CD |
| Interleukin receptor SHC signaling | 3 | PIK3CA, PIK3CB, PIK3CD |
| Regulation of signaling by CBL | 3 | PIK3CA, PIK3CB, PIK3CD |
| Signaling by CSF1 (M-CSF) in myeloid cells | 3 | PIK3CA, PIK3CB, PIK3CD |
| High laminar flow shear stress activates signaling by PIEZO1 and PECAM1:CDH5:KDR in endothelial cells | 3 | PIK3CA, PIK3CB, PIK3CD |
| PI3K Cascade | 2 | PIK3CA, PIK3CB |
| IRS-mediated signalling | 2 | PIK3CA, PIK3CB |
| Downstream signal transduction | 2 | PIK3CA, PIK3CB |
| PI3K/AKT activation | 2 | PIK3CA, PIK3CB |
| Signaling by ALK | 2 | PIK3CA, PIK3CB |
| Downstream TCR signaling | 2 | PIK3CA, PIK3CB |
| Role of phospholipids in phagocytosis | 2 | PIK3CA, PIK3CB |
| Tie2 Signaling | 2 | PIK3CA, PIK3CB |
| DAP12 signaling | 2 | PIK3CA, PIK3CB |
| Role of LAT2/NTAL/LAB on calcium mobilization | 2 | PIK3CA, PIK3CB |
| Nephrin family interactions | 2 | PIK3CA, PIK3CB |
| VEGFA-VEGFR2 Pathway | 2 | PIK3CA, PIK3CB |
| RAF/MAP kinase cascade | 2 | PIK3CA, PIK3CB |
| Signaling by PDGFRA transmembrane, juxtamembrane and kinase domain mutants | 2 | PIK3CA, PIK3CB |
| Signaling by PDGFRA extracellular domain mutants | 2 | PIK3CA, PIK3CB |
| Signaling by ALK fusions and activated point mutants | 2 | PIK3CA, PIK3CB |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| cell migration | 4 |
| phosphatidylinositol-3-phosphate biosynthetic process | 4 |
| phosphatidylinositol 3-kinase/protein kinase B signal transduction | 4 |
| phosphatidylinositol phosphate biosynthetic process | 4 |
| phosphatidylinositol-mediated signaling | 4 |
| lipid metabolic process | 4 |
| chemotaxis | 3 |
| positive regulation of endothelial cell migration | 3 |
| innate immune response | 3 |
| angiogenesis | 2 |
| platelet activation | 2 |
| vascular endothelial growth factor signaling pathway | 2 |
| T cell receptor signaling pathway | 2 |
| positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | 2 |
| negative regulation of fibroblast apoptotic process | 2 |
Indications & clinical
Indications
19 indications (5 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| B-cell chronic lymphocytic leukemia | 4 | MONDO:0004948 | EFO:0000095 |
| neoplasm | 4 | MONDO:0005070 | EFO:0000616 |
| neoplasm of mature B-cells | 4 | MONDO:0004949 | EFO:0000096 |
| non-Hodgkin lymphoma | 4 | MONDO:0018908 | EFO:0005952 |
| lymphoma | 3 | MONDO:0005062 | EFO:0000574 |
| follicular lymphoma | 3 | MONDO:0018906 | MONDO:0018906 |
| Hodgkins lymphoma | 2 | MONDO:0004952 | EFO:0000183 |
| mantle cell lymphoma | 2 | MONDO:0018876 | EFO:1001469 |
| diffuse large B-cell lymphoma | 2 | MONDO:0018905 | EFO:0000403 |
| amyloidosis | 2 | MONDO:0019065 | EFO:1001875 |
| Waldenstrom macroglobulinemia | 2 | MONDO:0100280 | EFO:0009441 |
| allergic rhinitis | 1 | MONDO:0011786 | EFO:0005854 |
| acute myeloid leukemia | 1 | MONDO:0018874 | EFO:0000222 |
| plasma cell myeloma | 1 | MONDO:0009693 | EFO:0001378 |
| acute lymphoblastic leukemia | 1 | MONDO:0004967 | EFO:0000220 |
| primary myelofibrosis | 1 | MONDO:0009692 | MONDO:0044903 |
| pancreatic ductal adenocarcinoma | 1 | MONDO:0005184 | MONDO:0005184 |
2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 64.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 23 |
| PHASE1 | 16 |
| PHASE3 | 14 |
| Not specified | 5 |
| PHASE1/PHASE2 | 4 |
| PHASE4 | 2 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT07218341 | PHASE4 | RECRUITING | A Study of Pirtobrutinib (LY3527727) in Participants With Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma |
| NCT02739360 | PHASE4 | TERMINATED | Roll Over Study to Provide Idelalisib to Participants Previously Treated With the Investigational PI3Kδ Inhibitor, GS-9820 |
| NCT02970318 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study of Acalabrutinib vs Investigator’s Choice of Idelalisib Plus Rituximab or Bendamustine Plus Rituximab in R/R CLL |
| NCT04666038 | PHASE3 | 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) |
| NCT06846671 | PHASE3 | 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 |
| NCT07139873 | PHASE3 | RECRUITING | A Study of DZD8586 Versus Investigator’s Choice in r/r CLL/SLL (TAI-SHAN6) |
| NCT01539291 | PHASE3 | TERMINATED | Extension Study of Idelalisib in Participants With Chronic Lymphocytic Leukemia (CLL) Who Participated in GS-US-312-0116 (NCT01539512) |
| NCT01539512 | PHASE3 | COMPLETED | A Randomized, Double-Blind, Placebo-Controlled Study of Idelalisib in Combination With Rituximab for Previously Treated Chronic Lymphocytic Leukemia (CLL) |
| NCT01569295 | PHASE3 | COMPLETED | Study Evaluating the Efficacy and Safety of Idelalisib in Combination With Bendamustine and Rituximab for Previously Treated Chronic Lymphocytic Leukemia (CLL) (Tugela ) |
| NCT01659021 | PHASE3 | TERMINATED | Efficacy and Safety of Idelalisib in Combination With Ofatumumab for Previously Treated Chronic Lymphocytic Leukemia |
| NCT01732913 | PHASE3 | TERMINATED | Efficacy and Safety of Idelalisib (GS-1101) in Combination With Rituximab for Previously Treated Indolent Non-Hodgkin Lymphomas |
| NCT01732926 | PHASE3 | TERMINATED | Efficacy and Safety of Idelalisib (GS-1101) in Combination With Bendamustine and Rituximab for Previously Treated Indolent Non-Hodgkin Lymphomas |
| NCT01980875 | PHASE3 | TERMINATED | Efficacy and Safety of Idelalisib in Combination With Obinutuzumab Compared to Chlorambucil in Combination With Obinutuzumab for Previously Untreated Chronic Lymphocytic Leukemia |
| NCT01980888 | PHASE3 | TERMINATED | Efficacy and Safety of Idelalisib in Combination With Bendamustine and Rituximab in Adults With Previously Untreated Chronic Lymphocytic Leukemia |
| NCT02536300 | PHASE3 | TERMINATED | Dose Optimization Study of Idelalisib in Follicular Lymphoma |
| NCT06205290 | PHASE3 | 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 |
| NCT05725200 | PHASE2 | RECRUITING | Study to Investigate Outcome of Individualized Treatment in Patients With Metastatic Colorectal Cancer |
| NCT06736990 | PHASE2 | ACTIVE_NOT_RECRUITING | A Phase 2 Study of CAL101 in Patients With Idiopathic Pulmonary Fibrosis |
| NCT01090414 | PHASE1/PHASE2 | TERMINATED | An Extension Study for Subjects Who Are Deriving Benefit With Idelalisib (GS-1101; CAL-101) Following Completion of a Prior Idelalisib Study |
| NCT01203930 | PHASE2 | TERMINATED | A Study of Idelalisib and Rituximab in Elderly Patients With Untreated CLL or SLL |
| NCT01282424 | PHASE2 | COMPLETED | Efficacy and Safety Study of Idelalisib in Participants With Indolent B-Cell Non-Hodgkin Lymphomas |
| NCT01306643 | PHASE1/PHASE2 | COMPLETED | Safety and Efficacy Study of Idelalisib (GS-1101, CAL-101) in Patients With Previously Treated Low-grade Lymphoma |
| NCT01393106 | PHASE2 | COMPLETED | Safety and Efficacy of Idelalisib in Relapsed or Refractory Hodgkin Lymphoma |
| NCT01620216 | PHASE2 | TERMINATED | Targeted Therapy in Treating Patients With Relapsed or Refractory Acute Lymphoblastic Leukemia or Acute Myelogenous Leukemia |
| NCT01659047 | PHASE2 | WITHDRAWN | A Phase 2, Single-Arm, Open-Label Study Evaluating the Efficacy and Safety of Single Agent GS 1101 (CAL 101) as Therapy for Previously Treated Chronic Lymphocytic Leukemia |
| NCT01796470 | PHASE2 | TERMINATED | Entospletinib in Combination With Idelalisib in Adults With Relapsed or Refractory Hematologic Malignancies |
| NCT02044822 | PHASE2 | TERMINATED | Efficacy and Safety of Idelalisib in Combination With Rituximab in Patients With Previously Untreated Chronic Lymphocytic Leukemia With 17p Deletion |
| NCT02135133 | PHASE2 | COMPLETED | A Study of Idelalisib (GS1101, CAL101) + Ofatumumab in Previously Untreated CLL/SLL |
| NCT02258529 | PHASE2 | TERMINATED | Idelalisib in Combination With Rituximab for Previously Untreated Follicular Lymphoma and Small Lymphocytic Lymphoma |
| NCT02332980 | PHASE2 | 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 |
| NCT02439138 | PHASE2 | TERMINATED | Study of Phosphatidylinositol-3-kinase (PI3K) Inhibitor Idelalisib (GS-1101) in Waldenström Macroglobulinemia |
| NCT02445131 | PHASE2 | COMPLETED | Sequential Regimen of Bendamustine-Debulking Followed by CAL-101 and GA101-Induction and -Maintenance in CLL (CLL2-BCG) |
| NCT02590588 | PHASE2 | TERMINATED | Idelalisib for Immunoglobulin M (IgM)-Associated Primary (AL) Amyloidosis |
| NCT02639910 | PHASE2 | COMPLETED | Study to Evaluate Safety and Preliminary Efficacy of Tafasitamab With Idelalisib or Venetoclax in R/R CLL/SLL Patients Pretreated With BTKi |
| NCT02662296 | PHASE2 | 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 |
| NCT02962401 | PHASE2 | COMPLETED | Efficacity of Idelalisib and Obinutuzumab in Patient With Relapsed Refractory Waldenstrom’s Macroglobulinemia |
| NCT02968563 | PHASE2 | 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) |
| NCT03133221 | PHASE2 | COMPLETED | 1630GCC: Zydelig Maintenance in B-Cell Non-Hodgkin’s Lymphoma After Autologous Stem Cell Transplantation |
| NCT03257722 | PHASE1/PHASE2 | TERMINATED | Pembrolizumab + Idelalisib for Lung Cancer Study |
| NCT03576443 | PHASE2 | COMPLETED | Trial of Idelalisib in Patients With Relapsed Diffuse Large B-cell Lymphoma |
Clinical evidence (CIViC)
Variant × indication × effect (1 predictive associations from 1 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| PIK3CA P471L | Merkel Cell Carcinoma | Sensitivity/Response | Idelalisib | CIViC C | EID739 |
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
72 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| CRIZOTINIB | ChEMBL + PubChem | Phase 4 (approved) | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| INAVOLISIB | ChEMBL + PubChem | Phase 4 (approved) | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| ALPELISIB | ChEMBL | Phase 4 (approved) | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| COPANLISIB | ChEMBL | Phase 4 (approved) | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| DUVELISIB | ChEMBL | Phase 4 (approved) | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| LENIOLISIB | ChEMBL | Phase 4 (approved) | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| BUPARLISIB | ChEMBL | Phase 3 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| DACTOLISIB | ChEMBL | Phase 3 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| GEDATOLISIB | ChEMBL | Phase 3 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| LESTAURTINIB | ChEMBL | Phase 3 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| TASELISIB | ChEMBL | Phase 3 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| AMG-319 | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| APITOLISIB | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| AZD-6482 | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| BGT-226 FREE BASE | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| BIMIRALISIB | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| EGANELISIB | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| FIMEPINOSTAT | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| IZORLISIB | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| NEMIRALISIB | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| OMIPALISIB | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| ONATASERTIB | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| PAXALISIB | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| PF-04691502 | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| PICTILISIB | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| PILARALISIB | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| ROGINOLISIB | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| SAMOTOLISIB | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| SAPANISERTIB | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| SERABELISIB | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| TG100-115 | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| VISTUSERTIB | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| VOXTALISIB | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| ZSTK-474 | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| Afatinib | PubChem | Approved | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| Pazopanib | PubChem | Approved | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| Selumetinib | PubChem | Approved | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| SUNITINIB | ChEMBL | Phase 4 (approved) | PIK3CA, PIK3CD, PIK3CG |
| DEZAPELISIB | ChEMBL | Phase 2 | PIK3CB, PIK3CD, PIK3CG |
| QUISINOSTAT | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD |
| RISOVALISIB | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD |
| SONOLISIB | ChEMBL | Phase 2 | PIK3CA, PIK3CD, PIK3CG |
| Gefitinib | PubChem | Approved | PIK3CB, PIK3CD, PIK3CG |
| DASATINIB | ChEMBL | Phase 4 (approved) | PIK3CA, PIK3CD |
| FEDRATINIB | ChEMBL | Phase 4 (approved) | PIK3CA, PIK3CG |
| UMBRALISIB | ChEMBL | Phase 4 (approved) | PIK3CD, PIK3CG |
| RESVERATROL | ChEMBL | Phase 3 | PIK3CA, PIK3CB |
| ACALISIB | ChEMBL | Phase 2 | PIK3CD, PIK3CG |
| AMDIZALISIB | ChEMBL | Phase 2 | PIK3CD, PIK3CG |
| AZD-8154 | ChEMBL | Phase 2 | PIK3CA, PIK3CD |
| BI-2536 | ChEMBL | Phase 2 | PIK3CA, PIK3CD |
| GSK-2636771 | ChEMBL | Phase 2 | PIK3CB, PIK3CD |
| OSI-027 | ChEMBL | Phase 2 | PIK3CA, PIK3CG |
| SELETALISIB | ChEMBL | Phase 2 | PIK3CD, PIK3CG |
| TENALISIB | ChEMBL | Phase 2 | PIK3CD, PIK3CG |
| BELINOSTAT | ChEMBL | Phase 4 (approved) | PIK3CA |
| CAFFEINE | ChEMBL | Phase 4 (approved) | PIK3CD |
| MIDOSTAURIN | ChEMBL | Phase 4 (approved) | PIK3CA |
| ROMIDEPSIN | ChEMBL | Phase 4 (approved) | PIK3CA |
| THEOPHYLLINE | ChEMBL | Phase 4 (approved) | PIK3CD |
Related Atlas pages
- Genes: PIK3CA, PIK3CB, PIK3CD, PIK3CG
- Diseases: B-cell chronic lymphocytic leukemia, neoplasm, neoplasm of mature B-cells, non-Hodgkin lymphoma, lymphoma, follicular lymphoma, cutaneous neuroendocrine carcinoma
- Drugs: Crizotinib, Inavolisib, Alpelisib, Copanlisib, Duvelisib, Leniolisib, Buparlisib, Dactolisib, Gedatolisib, Lestaurtinib, Taselisib, Afatinib, Pazopanib, Selumetinib, Sunitinib, Gefitinib, Dasatinib, Fedratinib, Umbralisib, Resveratrol, Belinostat, Caffeine, Midostaurin, Romidepsin, Theophylline