Copanlisib
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Also known as Copanilisib
Summary
Copanlisib (CHEMBL3218576) is an approved small-molecule EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor (ATC L01EM02) targeting MTOR, PIK3CA, and PIK3CB; indicated across 20 conditions including neoplasm and non-hodgkin lymphoma; with CIViC clinical evidence for 2 variant-indication associations (e.g. PIK3CA Mutation in cancer).
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01EM02
- Targets: 5 (MTOR, PIK3CA, PIK3CB…)
- Indications: 20 conditions
- Clinical trials: 57
- Precision-oncology evidence (CIViC): 2 variant–indication associations
- Chemistry: 480.5 Da · C23H28N8O4
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL3218576 |
| Name | Copanlisib |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | no |
| PubChem CID | 135565596 |
| ChEBI | CHEBI:173077 |
| ATC | L01EM02 |
| Molecular formula | C23H28N8O4 |
| Molecular weight | 480.5 |
| InChIKey | MWYDSXOGIBMAET-UHFFFAOYSA-N |
SMILES: COC1=C(C=CC2=C3NCCN3C(=NC(=O)C4=CN=C(N=C4)N)N=C21)OCCCN5CCOCC5
IUPAC name: 2-amino-N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydro-1H-imidazo[1,2-c]quinazolin-5-ylidene]pyrimidine-5-carboxamide
ChEBI definition: An imidazoquinazoline that is 2,3-dihydroimidazo[1,2-c]quinazoline substituted by (2-aminopyrimidine-5-carbonyl)amino, methoxy, and 3-(morpholin-4-yl)propoxy groups at positions 5, 7 and 8, respectively. It is a intravenous pan-class I PI3K inhibitor used for the treatment of relapsed follicular lymphoma in patients who have received at least 2 prior systemic therapies.
Pharmacological roles (ChEBI): EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor, antineoplastic agent, apoptosis inducer.
Also known as: Copanlisib, COPANLISIB, copanlisib, Copanilisib
Parent form; salt/anhydrous children: CHEMBL3545068
Patent coverage: 1,789 distinct patent families (4,529 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 4,465 (99%) 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 |
|---|---|---|---|---|---|
| MTOR | mechanistic target of rapamycin kinase | Inhibition | 7.35 | 98.3% (common-essential) | P42345 |
| PIK3CA | phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha | Inhibition | 9.3 | 42.7% | P42336 |
| PIK3CB | phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta | Inhibition | 8.43 | 5% | P42338 |
| PIK3CD | phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta | Inhibition | 9.15 | 6% | O00329 |
| PIK3CG | phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma | Inhibition | 8.19 | 0.7% | P48736 |
Broader ChEMBL bioactivity targets: 10 (assay-derived). Sample: Muscarinic acetylcholine receptor M2, PI3-kinase p110-alpha/p85-alpha, PI3-kinase p110-delta/p85-alpha, Serine/threonine-protein kinase mTOR, PI3K p110 beta/p85 alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, Ras-related protein Rab-27A.
Bioactivity
ChEMBL activities: 37 potent at pChembl ≥ 5 of 37 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| PIK3R1 | 9.96 | IC50 | 0.11 | nM | CHEMBL_ACT_19060780 |
| PIK3CA | 9.96 | IC50 | 0.11 | nM | CHEMBL_ACT_25593613 |
| PIK3CD | 9.74 | IC50 | 0.18 | nM | CHEMBL_ACT_19060853 |
| PIK3CD | 9.74 | IC50 | 0.18 | nM | CHEMBL_ACT_25593650 |
| PIK3CA | 9.3 | IC50 | 0.5 | nM | CHEMBL_ACT_16801263 |
| PIK3CA | 9.3 | IC50 | 0.5 | nM | CHEMBL_ACT_19139825 |
| PIK3CA | 9.3 | IC50 | 0.5 | nM | CHEMBL_ACT_19214491 |
| PIK3CA | 9.3 | IC50 | 0.5 | nM | CHEMBL_ACT_25556607 |
| PIK3CA | 9.3 | IC50 | 0.5 | nM | CHEMBL_ACT_29092034 |
| PIK3CD | 9.15 | IC50 | 0.7 | nM | CHEMBL_ACT_16801260 |
| PIK3CG | 9.15 | IC50 | 0.7 | nM | CHEMBL_ACT_19139830 |
| PIK3CG | 9.15 | IC50 | 0.7 | nM | CHEMBL_ACT_25556626 |
| PIK3CG | 9.15 | IC50 | 0.7 | nM | CHEMBL_ACT_29092037 |
| PIK3CA | 8.85 | IC50 | 1.42 | nM | CHEMBL_ACT_25892641 |
| PIK3CG | 8.78 | IC50 | 1.68 | nM | CHEMBL_ACT_19060851 |
| PIK3CG | 8.78 | IC50 | 1.68 | nM | CHEMBL_ACT_25593647 |
| PIK3CD | 8.76 | IC50 | 1.72 | nM | CHEMBL_ACT_25892657 |
| PIK3CB | 8.43 | IC50 | 3.7 | nM | CHEMBL_ACT_16801262 |
| PIK3CB | 8.43 | IC50 | 3.7 | nM | CHEMBL_ACT_19139824 |
| PIK3CB | 8.43 | IC50 | 3.7 | nM | CHEMBL_ACT_19214493 |
| PIK3CB | 8.43 | IC50 | 3.7 | nM | CHEMBL_ACT_25556617 |
| PIK3CB | 8.43 | IC50 | 3.7 | nM | CHEMBL_ACT_29092035 |
| PIK3R1 | 8.34 | IC50 | 4.57 | nM | CHEMBL_ACT_19060849 |
| PIK3CB | 8.34 | IC50 | 4.57 | nM | CHEMBL_ACT_25593644 |
| PIK3CG | 8.19 | IC50 | 6.4 | nM | CHEMBL_ACT_16801261 |
| PIK3CD | 8.19 | IC50 | 6.4 | nM | CHEMBL_ACT_19139820 |
| PIK3CG | 8.19 | IC50 | 6.4 | nM | CHEMBL_ACT_19214494 |
| PIK3CD | 8.19 | IC50 | 6.4 | nM | CHEMBL_ACT_25556641 |
| PIK3CD | 8.19 | IC50 | 6.4 | nM | CHEMBL_ACT_29092036 |
| PIK3CB | 8.04 | IC50 | 9.12 | nM | CHEMBL_ACT_25892645 |
Target pathways
Aggregated over 5 target gene(s): MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG.
Top Reactome pathways
99 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| PIP3 activates AKT signaling | 5 | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| CD28 dependent PI3K/Akt signaling | 5 | MTOR, 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 |
| PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling | 4 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| Erythropoietin activates Phosphoinositide-3-kinase (PI3K) | 4 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| High laminar flow shear stress activates signaling by PIEZO1 and PECAM1:CDH5:KDR in endothelial cells | 4 | MTOR, PIK3CA, PIK3CB, PIK3CD |
| Co-stimulation by ICOS | 4 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| GPVI-mediated activation cascade | 3 | PIK3CA, PIK3CB, PIK3CG |
| VEGFA-VEGFR2 Pathway | 3 | MTOR, PIK3CA, PIK3CB |
| 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 |
| 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 |
| 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 |
|---|---|
| phosphatidylinositol 3-kinase/protein kinase B signal transduction | 5 |
| cell migration | 4 |
| phosphatidylinositol-3-phosphate biosynthetic process | 4 |
| phosphatidylinositol phosphate biosynthetic process | 4 |
| phosphatidylinositol-mediated signaling | 4 |
| lipid metabolic process | 4 |
| inflammatory response | 3 |
| positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | 3 |
| chemotaxis | 3 |
| positive regulation of endothelial cell migration | 3 |
| innate immune response | 3 |
| positive regulation of lamellipodium assembly | 2 |
| negative regulation of macroautophagy | 2 |
| T cell costimulation | 2 |
| cellular response to insulin stimulus | 2 |
Indications & clinical
Indications
20 indications (1 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 |
|---|---|---|---|
| neoplasm | 4 | MONDO:0005070 | EFO:0000616 |
| non-Hodgkin lymphoma | 3 | MONDO:0018908 | EFO:0005952 |
| mantle cell lymphoma | 2 | MONDO:0018876 | EFO:1001469 |
| diffuse large B-cell lymphoma | 2 | MONDO:0018905 | EFO:0000403 |
| breast carcinoma | 2 | MONDO:0004989 | EFO:0000305 |
| gallbladder neoplasm | 2 | MONDO:0021253 | EFO:0004606 |
| cholangiocarcinoma | 2 | MONDO:0019087 | EFO:0005221 |
| B-cell chronic lymphocytic leukemia | 2 | MONDO:0004948 | EFO:0000095 |
| breast neoplasm | 2 | MONDO:0021100 | MONDO:0007254 |
| follicular lymphoma | 2 | MONDO:0018906 | MONDO:0018906 |
| uterine corpus cancer | 2 | MONDO:0006003 | EFO:0007532 |
| marginal zone lymphoma | 2 | MONDO:0017604 | EFO:1000630 |
| lymphoma | 1 | MONDO:0005062 | EFO:0000574 |
| squamous cell carcinoma | 1 | MONDO:0005096 | EFO:0000707 |
| colonic neoplasm | 1 | MONDO:0005401 | MONDO:0021063 |
| non-small cell lung carcinoma | 1 | MONDO:0005233 | EFO:0003060 |
| kidney failure | 1 | MONDO:0001106 | HP:0000083 |
| urothelial carcinoma | 1 | MONDO:0040679 | EFO:0008528 |
| acute lymphoblastic leukemia | 0 | MONDO:0004967 | EFO:0000220 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 57.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE1 | 24 |
| PHASE2 | 16 |
| PHASE1/PHASE2 | 14 |
| PHASE3 | 1 |
| EARLY_PHASE1 | 1 |
| Not specified | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT02626455 | PHASE3 | TERMINATED | Study of Copanlisib in Combination With Standard Immunochemotherapy in Relapsed Indolent Non-Hodgkin’s Lymphoma (iNHL) |
| NCT02465060 | PHASE2 | ACTIVE_NOT_RECRUITING | Targeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial) |
| NCT03474744 | PHASE2 | ACTIVE_NOT_RECRUITING | Copanlisib and Rituximab in Marginal Zone Lymphoma Patients |
| NCT03789240 | PHASE2 | ACTIVE_NOT_RECRUITING | Response-Adapted Therapy With Copanlisib and Rituximab in Untreated Follicular Lymphoma |
| NCT04253262 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | A Study of Copanlisib Combined With Rucaparib in Patients With Metastatic Castration-resistant Prostate Cancer |
| NCT04572763 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | Copanlisib Plus Venetoclax in R/R DLBCL |
| NCT06360588 | PHASE2 | ACTIVE_NOT_RECRUITING | Testing Copanlisib as Potentially Targeting Treatment in Cancers With PTEN Loss (MATCH - Subprotocol Z1G) |
| NCT06400238 | PHASE2 | ACTIVE_NOT_RECRUITING | Testing Copanlisib as Potentially Targeting Treatment in Cancers With PTEN Expression (MATCH - Subprotocol Z1H) |
| NCT02342665 | PHASE1/PHASE2 | COMPLETED | Japanese Phase Ib/II Copanlisib in Relapsed, Indolent B-cell NHL |
| NCT02455297 | PHASE2 | TERMINATED | Phase IIa Study of Copanlisib in Relapsed or Refractory Mantle Cell Lymphoma (MCL) |
| NCT02535247 | PHASE1/PHASE2 | TERMINATED | Study of MK-3475 Alone or in Combination With Copanlisib in Relapsed or Refractory NK and T-cell Non-Hodgkin Lymphoma |
| NCT02631590 | PHASE2 | COMPLETED | Copanlisib (BAY 80-6946) in Combination With Gemcitabine and Cisplatin in Advanced Cholangiocarcinoma |
| NCT02728258 | PHASE2 | COMPLETED | Copanlisib in Treating Patients With Persistent or Recurrent Endometrial Cancer |
| NCT02822482 | PHASE1/PHASE2 | TERMINATED | Copanlisib in Association With Cetuximab in Patients With Recurrent and/or Metastatic Head and Neck Squamous Cell Carcinomas Harboring a PI3KCA Mutation/Amplification and/or a PTEN Loss |
| NCT03052933 | PHASE1/PHASE2 | COMPLETED | Copanlisib and Gemcitabine in Relapsed/Refractory PTCL |
| NCT03377101 | PHASE2 | WITHDRAWN | Fulvestrant and Palbociclib With or Without Copanlisib in Treating Patients With Hormone Receptor Positive, HER2 Negative, Stage IV Breast Cancer |
| NCT03458728 | PHASE1/PHASE2 | TERMINATED | Safety, Tolerability, Efficacy and Pharmacokinetics of Copanlisib in Pediatric Patients |
| NCT03581942 | PHASE1/PHASE2 | COMPLETED | Copanlisib With Ibrutinib for Patients With Recurrent/ Refractory Primary Central Nervous System Lymphoma (PCNSL) |
| NCT03711058 | PHASE1/PHASE2 | COMPLETED | Study of PI3Kinase Inhibition (Copanlisib) and Anti-PD-1 Antibody Nivolumab in Relapsed/Refractory Solid Tumors With Expansions in Mismatch-repair Proficient (MSS) Colorectal Cancer |
| NCT03803761 | PHASE1/PHASE2 | WITHDRAWN | A Study of a New Drug Combination, Copanlisib and Fulvestrant, in Advanced Breast Cancer |
| NCT03877055 | PHASE1/PHASE2 | COMPLETED | A Study of Copanlisib and Ibrutinib in Mantle Cell Lymphoma |
| NCT04108858 | PHASE1/PHASE2 | TERMINATED | Testing the Addition of an Anti-cancer Drug, Copanlisib, to the Usual Maintenance Treatment (Trastuzumab and Pertuzumab) After Initial Chemotherapy in a Phase Ib/II Trial for Advanced HER2 Positive Breast Cancer |
| NCT04155840 | PHASE2 | TERMINATED | Bendamustine and Rituximab in Combination With Copanlisib for the Treatment of Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma |
| NCT04263584 | PHASE2 | UNKNOWN | Copanlisib in Combination With Rituximab and CHOP Chemotherapy in Patients With Previously Untreated DLBCL |
| NCT04433182 | PHASE2 | TERMINATED | Copanlisib With Rituximab-Bendamustine in Patients With Relapsed-Refractory Diffuse Large B-cell Lymphoma |
| NCT04685915 | PHASE2 | WITHDRAWN | Copanlisib Plus Ibrutinib or Acalabrutinib in R/R CLL |
| NCT04750941 | PHASE2 | TERMINATED | Study of Copanlisib and Ketogenic Diet |
| NCT05082025 | PHASE2 | TERMINATED | Phase 2 Study of PI3K Inhibitor Copanlisib in Combination With Fulvestrant in Selected ER+ and/or PR+ Cancers With PI3K (PIK3CA, PIK3R1) and/or PTEN Alterations |
| NCT05387616 | PHASE2 | UNKNOWN | A Prospective Multicenter Phase 2 Study of the Chemotherapy-Free Combination of the Intravenous Phosphatidylinositol-3-Kinase (PI3K) Inhibitor Copanlisib in Combination With Obinutuzumab in Patients With Previously Untreated Follicular Lymphoma (FL) and a High Tumor Burden |
| NCT05687721 | PHASE1/PHASE2 | WITHDRAWN | Copanlisib and Avelumab as a Maintenance Therapy for Advanced Bladder Cancer |
| NCT06218667 | PHASE1/PHASE2 | WITHDRAWN | A Study of Copanlisib in Combination with Degarelix in People with Prostate Cancer |
| NCT03502733 | PHASE1 | ACTIVE_NOT_RECRUITING | Testing the Combination of Copanlisib, Nivolumab and Ipilimumab in Patients With Advanced Cancer and Lymphoma |
| NCT03586661 | PHASE1 | ACTIVE_NOT_RECRUITING | Niraparib and Copanlisib in Treating Patients With Recurrent Endometrial, Ovarian, Primary Peritoneal, or Fallopian Tube Cancer |
| NCT03884998 | PHASE1 | ACTIVE_NOT_RECRUITING | Copanlisib and Nivolumab in Treating Patients With Richter’s Transformation or Transformed Indolent Non-Hodgkin Lymphoma |
| NCT01392521 | PHASE1 | COMPLETED | Phase Ib Study of PI3(Phosphoinositol 3)-Kinase Inhibitor Copanlisib With MEK (Mitogen-activated Protein Kinase) Inhibitor Refametinib (BAY86-9766) in Patients With Advanced Cancer |
| NCT01404390 | PHASE1 | COMPLETED | Japanese BAY80-6946 Monotherapy Phase I Study |
| NCT01411410 | PHASE1 | COMPLETED | Phase I Study of PI3(Phosphoinositol 3)-Kinase Inhibitor BAY80-6946 With Paclitaxel in Patients With Advanced Cancer |
| NCT01460537 | PHASE1 | COMPLETED | Phase 1 Study of PI3 (Phosphatidylinositol-3)-Kinase Inhibitor Copanlisib With Gemcitabine or Cisplatin Plus Gemcitabine in Patients With Advanced Cancer |
| NCT02119221 | PHASE1 | COMPLETED | Copanlisib Mass Balance Study |
| NCT02155582 | PHASE1 | COMPLETED | Copanlisib Pharmacodynamic Study |
Clinical evidence (CIViC)
Variant × indication × effect (2 predictive associations from 2 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| PIK3CA Mutation | Cancer | Sensitivity/Response | Copanlisib | CIViC B | EID11678 |
| AURKB Overexpression | Head And Neck Squamous Cell Carcinoma | Sensitivity/Response | Alisertib + Barasertib + Copanlisib | CIViC D | EID10836 |
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.
195 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| Crizotinib | ChEMBL + PubChem | Phase 4 (approved) | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| Idelalisib | ChEMBL + PubChem | Phase 4 (approved) | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| ALPELISIB | ChEMBL | Phase 4 (approved) | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| BUPARLISIB | ChEMBL | Phase 3 | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| DACTOLISIB | ChEMBL | Phase 3 | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| GEDATOLISIB | ChEMBL | Phase 3 | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| TASELISIB | ChEMBL | Phase 3 | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| APITOLISIB | ChEMBL | Phase 2 | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| AZD-6482 | ChEMBL | Phase 2 | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| BGT-226 FREE BASE | ChEMBL | Phase 2 | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| BIMIRALISIB | ChEMBL | Phase 2 | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| FIMEPINOSTAT | ChEMBL | Phase 2 | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| IZORLISIB | ChEMBL | Phase 2 | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| OMIPALISIB | ChEMBL | Phase 2 | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| ONATASERTIB | ChEMBL | Phase 2 | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| PAXALISIB | ChEMBL | Phase 2 | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| PF-04691502 | ChEMBL | Phase 2 | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| PICTILISIB | ChEMBL | Phase 2 | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| SAMOTOLISIB | ChEMBL | Phase 2 | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| SAPANISERTIB | ChEMBL | Phase 2 | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| TG100-115 | ChEMBL | Phase 2 | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| VISTUSERTIB | ChEMBL | Phase 2 | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| VOXTALISIB | ChEMBL | Phase 2 | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| ZSTK-474 | ChEMBL | Phase 2 | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| Afatinib | PubChem | Approved | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| Pazopanib | PubChem | Approved | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| Selumetinib | PubChem | Approved | MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| INAVOLISIB | ChEMBL + PubChem | 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 |
| LESTAURTINIB | ChEMBL | Phase 3 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| AMG-319 | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| EGANELISIB | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| NEMIRALISIB | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| PILARALISIB | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| ROGINOLISIB | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| SERABELISIB | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| SONOLISIB | ChEMBL | Phase 2 | MTOR, PIK3CA, PIK3CD, PIK3CG |
| Gefitinib | PubChem | Approved | MTOR, PIK3CB, PIK3CD, PIK3CG |
| DASATINIB | ChEMBL | Phase 4 (approved) | MTOR, PIK3CA, PIK3CD |
| SUNITINIB | ChEMBL | Phase 4 (approved) | PIK3CA, PIK3CD, PIK3CG |
| RESVERATROL | ChEMBL | Phase 3 | MTOR, PIK3CA, PIK3CB |
| DEZAPELISIB | ChEMBL | Phase 2 | PIK3CB, PIK3CD, PIK3CG |
| OSI-027 | ChEMBL | Phase 2 | MTOR, PIK3CA, PIK3CG |
| QUISINOSTAT | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD |
| RISOVALISIB | ChEMBL | Phase 2 | PIK3CA, PIK3CB, PIK3CD |
| FEDRATINIB | ChEMBL | Phase 4 (approved) | PIK3CA, PIK3CG |
| UMBRALISIB | ChEMBL | Phase 4 (approved) | PIK3CD, PIK3CG |
| EPIGALOCATECHIN GALLATE | ChEMBL | Phase 3 | MTOR, PIK3CA |
| ACALISIB | ChEMBL | Phase 2 | PIK3CD, PIK3CG |
| AMDIZALISIB | ChEMBL | Phase 2 | PIK3CD, PIK3CG |
| AZD-8154 | ChEMBL | Phase 2 | PIK3CA, PIK3CD |
| BERZOSERTIB | ChEMBL | Phase 2 | MTOR, PIK3CA |
| BI-2536 | ChEMBL | Phase 2 | PIK3CA, PIK3CD |
| CC-115 | ChEMBL | Phase 2 | MTOR, PIK3CA |
| GSK-2636771 | ChEMBL | Phase 2 | PIK3CB, PIK3CD |
| SELETALISIB | ChEMBL | Phase 2 | PIK3CD, PIK3CG |
| TENALISIB | ChEMBL | Phase 2 | PIK3CD, PIK3CG |
| AMIODARONE | ChEMBL | Phase 4 (approved) | MTOR |
| AMITRIPTYLINE | ChEMBL | Phase 4 (approved) | MTOR |
Related Atlas pages
- Genes: MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
- Diseases: neoplasm, non-Hodgkin lymphoma, cancer, head and neck squamous cell carcinoma
- Drugs: Crizotinib, Idelalisib, Alpelisib, Buparlisib, Dactolisib, Gedatolisib, Taselisib, Afatinib, Pazopanib, Selumetinib, Inavolisib, Duvelisib, Leniolisib, Lestaurtinib, Gefitinib, Dasatinib, Sunitinib, Resveratrol, Fedratinib, Umbralisib, Epigalocatechin Gallate, Amiodarone, Amitriptyline