Dactolisib

Summary

Dactolisib (CHEMBL1879463) is a phase-3 clinical-stage small-molecule EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor targeting ATR, MTOR, and PIK3CA; indicated across 10 conditions including neoplasm and transitional cell carcinoma; with CIViC clinical evidence for 41 variant-indication associations (e.g. NRAS Q61K in colorectal cancer).

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Targets: 5 (ATR, MTOR, PIK3CA…)
• Indications: 10 conditions
• Clinical trials: 23
• Precision-oncology evidence (CIViC): 41 variant–indication associations
• Chemistry: 469.5 Da · C30H23N5O

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1879463
Name	Dactolisib
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	11977753
ChEBI	CHEBI:71952
Molecular formula	C30H23N5O
Molecular weight	469.5
InChIKey	JOGKUKXHTYWRGZ-UHFFFAOYSA-N

SMILES: CC(C)(C#N)C1=CC=C(C=C1)N2C3=C4C=C(C=CC4=NC=C3N(C2=O)C)C5=CC6=CC=CC=C6N=C5

IUPAC name: 2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-ylimidazo[4,5-c]quinolin-1-yl)phenyl]propanenitrile

ChEBI definition: An imidazoquinoline that is 3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinoline substituted at position 1 by a 4-(1-cyanoisopropyl)phenyl group and at position 8 by a quinolin-3-yl group. A dual PI3K/mTOR inhibitor used in cancer treatment.

Pharmacological roles (ChEBI): EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor, mTOR inhibitor, antineoplastic agent.

Also known as: Bez-235, BEZ-235, BEZ235, Dactolisib, NSC-751249, Nvp-bez-235, NVP-BEZ235, RTB-101, Rtb101, RTB101, SID124898663, SID103905146

Parent form; salt/anhydrous children: CHEMBL1911126, CHEMBL3039506

Patent coverage: 2,924 distinct patent families (7,988 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 7,391 (93%) 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
ATR	ATR checkpoint kinase	Inhibition	7.68		Q13535
MTOR	mechanistic target of rapamycin kinase	Inhibition	8.22	98.3% (common-essential)	P42345
PIK3CA	phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha	Inhibition	8.4	42.7%	P42336
PIK3CD	phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta	Inhibition	8.15	6%	O00329
PIK3CG	phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma	Inhibition	8.3	0.7%	P48736

Broader ChEMBL bioactivity targets: 35 (assay-derived). Sample: Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit alpha, Leucine-rich repeat serine/threonine-protein kinase 2, Phosphatidylinositol 3-kinase catalytic subunit type 3, Macrophage colony-stimulating factor 1 receptor, Protein deacetylase HDAC6, PI3-kinase p110-alpha/p85-alpha, PI3-kinase p110-delta/p85-alpha, Tyrosine-protein kinase JAK3, Aurora kinase B, Serine/threonine-protein kinase mTOR.

Bioactivity

ChEMBL activities: 180 potent at pChembl ≥ 5 of 180 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
MTOR	9.35	IC50	0.45	nM	CHEMBL_ACT_26139402
PRKDC	9.1	IC50	0.8	nM	CHEMBL_ACT_25847706
MTOR	8.85	IC50	1.43	nM	CHEMBL_ACT_19091463
PIK3CA	8.85	IC50	1.4	nM	CHEMBL_ACT_25847801
MTOR	8.72	IC50	1.9	nM	CHEMBL_ACT_24817280
MTOR	8.7	IC50	2	nM	CHEMBL_ACT_16756885
HDAC6	8.7	IC50	2	nM	CHEMBL_ACT_23168158
MTOR	8.7	IC50	2	nM	CHEMBL_ACT_25570174
PRKDC	8.7	IC50	2	nM	CHEMBL_ACT_25570180
MTOR	8.49	IC50	3.23	nM	CHEMBL_ACT_17750165
PIK3CA	8.4	IC50	4	nM	CHEMBL_ACT_14553265
PIK3R1	8.4	IC50	4	nM	CHEMBL_ACT_16801276
PIK3CA	8.4	IC50	4	nM	CHEMBL_ACT_18673657
PIK3CA	8.4	IC50	4	nM	CHEMBL_ACT_24773326
PIK3CA	8.4	IC50	4	nM	CHEMBL_ACT_24788885
PIK3CA	8.4	IC50	4	nM	CHEMBL_ACT_24978773
PIK3CA	8.4	IC50	4	nM	CHEMBL_ACT_24995793
PIK3CA	8.4	IC50	4	nM	CHEMBL_ACT_25556714
PIK3CA	8.4	IC50	4	nM	CHEMBL_ACT_25892706
PIK3CA	8.4	IC50	4	nM	CHEMBL_ACT_26224982
MTOR	8.37	IC50	4.3	nM	CHEMBL_ACT_25847896
PIK3CG	8.3	IC50	5	nM	CHEMBL_ACT_14553270
MTOR	8.3	IC50	5	nM	CHEMBL_ACT_14743595
PIK3CD	8.3	IC50	5	nM	CHEMBL_ACT_16801273
PIK3CG	8.3	IC50	5	nM	CHEMBL_ACT_18673661
PIK3CD	8.3	IC50	5	nM	CHEMBL_ACT_19207791
PIK3CG	8.3	IC50	5	nM	CHEMBL_ACT_24773351
PIK3CG	8.3	IC50	5	nM	CHEMBL_ACT_24978776
PIK3CD	8.3	IC50	5	nM	CHEMBL_ACT_24995796
PIK3CG	8.3	IC50	5	nM	CHEMBL_ACT_25556716

Target pathways

Aggregated over 5 target gene(s): ATR, MTOR, PIK3CA, PIK3CD, PIK3CG.

Top Reactome pathways

124 total, by targets touching each:

Pathway	Targets	Genes
PIP3 activates AKT signaling	4	MTOR, PIK3CA, PIK3CD, PIK3CG
CD28 dependent PI3K/Akt signaling	4	MTOR, PIK3CA, PIK3CD, PIK3CG
Synthesis of PIPs at the plasma membrane	3	PIK3CA, PIK3CD, PIK3CG
Constitutive Signaling by Aberrant PI3K in Cancer	3	PIK3CA, PIK3CD, PIK3CG
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling	3	PIK3CA, PIK3CD, PIK3CG
Erythropoietin activates Phosphoinositide-3-kinase (PI3K)	3	PIK3CA, PIK3CD, PIK3CG
High laminar flow shear stress activates signaling by PIEZO1 and PECAM1:CDH5:KDR in endothelial cells	3	MTOR, PIK3CA, PIK3CD
Co-stimulation by ICOS	3	PIK3CA, PIK3CD, PIK3CG
GPVI-mediated activation cascade	2	PIK3CA, PIK3CG
Disease	2	ATR, MTOR
Generic Transcription Pathway	2	ATR, MTOR
Cellular responses to stress	2	ATR, MTOR
Cellular response to heat stress	2	ATR, MTOR
Transcriptional Regulation by TP53	2	ATR, MTOR
VEGFA-VEGFR2 Pathway	2	MTOR, PIK3CA
Interleukin-3, Interleukin-5 and GM-CSF signaling	2	PIK3CA, PIK3CD
Regulation of TP53 Activity	2	ATR, MTOR
RNA Polymerase II Transcription	2	ATR, MTOR
Gene expression (Transcription)	2	ATR, MTOR
RET signaling	2	PIK3CA, PIK3CD
Cellular responses to stimuli	2	ATR, MTOR
Interleukin receptor SHC signaling	2	PIK3CA, PIK3CD
Regulation of signaling by CBL	2	PIK3CA, PIK3CD
Signaling by CSF1 (M-CSF) in myeloid cells	2	PIK3CA, PIK3CD
PI3K Cascade	1	PIK3CA
IRS-mediated signalling	1	PIK3CA
Meiotic synapsis	1	ATR
Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants	1	PIK3CA
PI3K events in ERBB4 signaling	1	PIK3CA
Adaptive Immune System	1	MTOR

Dominant GO biological processes

GO term	Targets
phosphatidylinositol 3-kinase/protein kinase B signal transduction	4
inflammatory response	3
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	3
cell migration	3
phosphatidylinositol-3-phosphate biosynthetic process	3
phosphatidylinositol phosphate biosynthetic process	3
phosphatidylinositol-mediated signaling	3
lipid metabolic process	3
DNA damage response	2
regulation of cellular response to heat	2
regulation of cellular response to stress	2
positive regulation of lamellipodium assembly	2
negative regulation of macroautophagy	2
T cell costimulation	2
cellular response to insulin stimulus	2

Indications & clinical

Indications

10 indications (0 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	2	MONDO:0005070	EFO:0000616
transitional cell carcinoma	2	MONDO:0006474	EFO:1000601
pancreatic neuroendocrine tumor	2	MONDO:0019954	EFO:1000045
breast neoplasm	2	MONDO:0021100	MONDO:0007254
endometrium neoplasm	2	MONDO:0021251	MONDO:0011962
severe acute respiratory syndrome	2	MONDO:0005091	MONDO:0100096
kidney cancer	1	MONDO:0002367	MONDO:0002367

3 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 23.

Phase distribution

Phase	Trials
PHASE1	10
PHASE2	8
PHASE1/PHASE2	3
PHASE3	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04139915	PHASE3	WITHDRAWN	Effect of RTB101 on Illness Associated With Respiratory Tract Infections in the Elderly
NCT04668352	PHASE3	COMPLETED	A Phase 3 Study to Determine if RTB101 Prevents Clinically Symptomatic Respiratory Illness in the Elderly
NCT03373903	PHASE2	ACTIVE_NOT_RECRUITING	Dose Finding Study to Determine if BEZ235 Alone or in Combination With RAD001 Decreases the Incidence of Respiratory Tract Infections in the Elderly
NCT04584710	PHASE2	ACTIVE_NOT_RECRUITING	A Phase 2 Study of RTB101 as COVID-19 Post-Exposure Prophylaxis in Older Adults
NCT01288092	PHASE2	WITHDRAWN	BEZ235 Trial in Patients With HER2-(Human Epidermal Growth Factor Receptor 2 Negative) /HR+ (Hormonal Receptor Positive) Metastatic Breast Cancer
NCT01290406	PHASE2	WITHDRAWN	BEZ235 Trial in Patients With Advanced Endometrial Carcinoma
NCT01453595	PHASE1/PHASE2	TERMINATED	BEZ235 in Patients With Advanced Renal Cell Carcinoma (RCC)
NCT01495247	PHASE1/PHASE2	TERMINATED	Phase Ib/II Trial of BEZ235 With Paclitaxel in Patients With HER2 Negative, Locally Advanced or Metastatic Breast Cancer
NCT01628913	PHASE2	TERMINATED	Efficacy and Safety of BEZ235 Compared to Everolimus in Patients With Advanced Pancreatic Neuroendocrine Tumors
NCT01690871	PHASE2	WITHDRAWN	A Phase II Study of Orally Administered BEZ235 Monotherapy in Patients With Metastatic or Unresectable Malignant PEComa
NCT01717898	PHASE1/PHASE2	TERMINATED	A Multicenter Phase I/II Trial of Abiraterone Acetate + BEZ235 in Metastatic, Castration-Resistant Prostate Cancer
NCT01856101	PHASE2	TERMINATED	Study of BEZ235 as Monotherapy in Patients With Transitional Cell Carcinoma After Failure of Platinum Based Chemotherapy
NCT04409327	PHASE2	TERMINATED	Phase 2 Study to Determine if RTB101 Reduces the Severity of COVID-19 in Older Adults Residing in Nursing Homes
NCT00620594	PHASE1	COMPLETED	A Phase I/II Study of BEZ235 in Patients With Advanced Solid Malignancies Enriched by Patients With Advanced Breast Cancer
NCT01195376	PHASE1	COMPLETED	A Study of BEZ235 in Adult Japanese Patients With Advanced Solid Tumors
NCT01248494	PHASE1	COMPLETED	PhIb BKM120 or BEZ235+Endocrine Treatment in Post-Menopausal Patients With Hormone Receptor + Metastatic Breast Cancer
NCT01285466	PHASE1	COMPLETED	A Trial of Oral BEZ235 and BKM120 in Combination With Paclitaxel With or Without Trastuzumab
NCT01337765	PHASE1	COMPLETED	Safety, Pharmacokinetics and Pharmacodynamics of BEZ235 Plus MEK162 in Selected Advanced Solid Tumor Patients
NCT01343498	PHASE1	COMPLETED	Study of PI3 Kinase/mTOR Inhibitor BEZ235 Twice Daily for Advanced Solid Tumors
NCT01482156	PHASE1	COMPLETED	Dose Finding Study of RAD001 (Everolimus, Afinitor®) in Combination With BEZ235 in Patients With Advanced Solid Tumors
NCT01508104	PHASE1	TERMINATED	Safety Study of BEZ235 With Everolimus in Subjects With Advanced Solid Tumors
NCT01634061	PHASE1	COMPLETED	Phase Ib of Abiraterone Acetate Plus BEZ235 or BKM120 in Castration-resistant Prostate Cancer (CRPC) Patients
NCT01756118	PHASE1	COMPLETED	A Phase I, Dose-finding Study of BEZ235 in Adult Patients With Relapsed or Refractory Acute Leukemia

Clinical evidence (CIViC)

Variant × indication × effect (41 predictive associations from 43 curated evidence items):

Variant	Indication	Effect	Therapy	Level	CIViC
NRAS Q61K	Colorectal Cancer	Sensitivity/Response	Dactolisib	CIViC B	EID2194 +1
PIK3CA H1047R	Head And Neck Cancer	Sensitivity/Response	Dactolisib	CIViC D	EID1361 +1
AR OVEREXPRESSION	Breast Cancer	Sensitivity/Response	Dactolisib	CIViC D	EID859
BRAF V600E	Melanoma	Sensitivity/Response	Dactolisib + Selumetinib	CIViC D	EID1005
BRAF V600E	Colorectal Cancer	Sensitivity/Response	Dactolisib + GDC-0879	CIViC D	EID1428
KRAS A146T	Colorectal Cancer	Sensitivity/Response	Dactolisib + Selumetinib	CIViC D	EID2206
KRAS A146V	Colorectal Cancer	Sensitivity/Response	Dactolisib + Selumetinib	CIViC D	EID2209
KRAS G12C	Colorectal Cancer	Sensitivity/Response	Dactolisib + Selumetinib	CIViC D	EID2212
KRAS G12D	Colorectal Cancer	Sensitivity/Response	Dactolisib + Selumetinib	CIViC D	EID2218
KRAS G12D	Lung Non-small Cell Carcinoma	Sensitivity/Response	Dactolisib + Selumetinib	CIViC D	EID305
KRAS G12V	Colorectal Cancer	Sensitivity/Response	Dactolisib + Selumetinib	CIViC D	EID2001
KRAS G13D	Colorectal Cancer	Sensitivity/Response	Dactolisib + Selumetinib	CIViC D	EID2183
NRAS G12D	Colorectal Cancer	Sensitivity/Response	Dactolisib	CIViC D	EID1998
NRAS G12S	Colorectal Cancer	Sensitivity/Response	Dactolisib	CIViC D	EID2215
NRAS G13C	Colorectal Cancer	Sensitivity/Response	Dactolisib	CIViC D	EID2197
NRAS G13R	Colorectal Cancer	Sensitivity/Response	Dactolisib	CIViC D	EID2203
NRAS Q61H	Colorectal Cancer	Sensitivity/Response	Dactolisib	CIViC D	EID2171
NRAS Q61K	Colorectal Cancer	Sensitivity/Response	Selumetinib + Dactolisib	CIViC D	EID2192
NRAS Q61L	Colorectal Cancer	Sensitivity/Response	Dactolisib	CIViC D	EID2177
NRAS Q61R	Colorectal Cancer	Sensitivity/Response	Dactolisib	CIViC D	EID2186
PIK3CA Amplification	Her2-receptor Positive Breast Cancer	Sensitivity/Response	Dactolisib	CIViC D	EID8269
PIK3CA Amplification	Her2-receptor Positive Breast Cancer	Sensitivity/Response	Lapatinib + Dactolisib	CIViC D	EID8271
PIK3CA Amplification	Her2-receptor Positive Breast Cancer	Sensitivity/Response	Trastuzumab + Dactolisib	CIViC D	EID8272
PIK3CA Amplification	Her2-receptor Positive Breast Cancer	Sensitivity/Response	Dactolisib + Lapatinib + Trastuzumab	CIViC D	EID8273
PIK3CA E545K	Her2-receptor Positive Breast Cancer	Sensitivity/Response	Trastuzumab + Dactolisib	CIViC D	EID8180
PIK3CA E545K	Her2-receptor Positive Breast Cancer	Sensitivity/Response	Dactolisib + Trastuzumab + Lapatinib	CIViC D	EID8181
PIK3CA H1047R	Head And Neck Cancer	Sensitivity/Response	Cetuximab + Dactolisib	CIViC D	EID1363
PIK3CA H1047R	Lung Adenocarcinoma	Sensitivity/Response	Dactolisib	CIViC D	EID1447
PIK3CA H1047R	Her2-receptor Positive Breast Cancer	Sensitivity/Response	Dactolisib + Trastuzumab	CIViC D	EID8182
PIK3CA Mutation	Head And Neck Cancer	Sensitivity/Response	Dactolisib	CIViC D	EID1360

+11 more predictive associations (showing top 30 by level).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

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.

199 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
Idelalisib	ChEMBL + PubChem	Phase 4 (approved)	ATR, MTOR, PIK3CA, PIK3CD, PIK3CG
Crizotinib	ChEMBL + PubChem	Phase 4 (approved)	MTOR, PIK3CA, PIK3CD, PIK3CG
ALPELISIB	ChEMBL	Phase 4 (approved)	MTOR, PIK3CA, PIK3CD, PIK3CG
COPANLISIB	ChEMBL	Phase 4 (approved)	MTOR, PIK3CA, PIK3CD, PIK3CG
BUPARLISIB	ChEMBL	Phase 3	MTOR, PIK3CA, PIK3CD, PIK3CG
GEDATOLISIB	ChEMBL	Phase 3	MTOR, PIK3CA, PIK3CD, PIK3CG
TASELISIB	ChEMBL	Phase 3	MTOR, PIK3CA, PIK3CD, PIK3CG
APITOLISIB	ChEMBL	Phase 2	MTOR, PIK3CA, PIK3CD, PIK3CG
AZD-6482	ChEMBL	Phase 2	MTOR, PIK3CA, PIK3CD, PIK3CG
BGT-226 FREE BASE	ChEMBL	Phase 2	MTOR, PIK3CA, PIK3CD, PIK3CG
BIMIRALISIB	ChEMBL	Phase 2	MTOR, PIK3CA, PIK3CD, PIK3CG
FIMEPINOSTAT	ChEMBL	Phase 2	MTOR, PIK3CA, PIK3CD, PIK3CG
IZORLISIB	ChEMBL	Phase 2	MTOR, PIK3CA, PIK3CD, PIK3CG
OMIPALISIB	ChEMBL	Phase 2	MTOR, PIK3CA, PIK3CD, PIK3CG
ONATASERTIB	ChEMBL	Phase 2	MTOR, PIK3CA, PIK3CD, PIK3CG
PAXALISIB	ChEMBL	Phase 2	MTOR, PIK3CA, PIK3CD, PIK3CG
PF-04691502	ChEMBL	Phase 2	MTOR, PIK3CA, PIK3CD, PIK3CG
PICTILISIB	ChEMBL	Phase 2	MTOR, PIK3CA, PIK3CD, PIK3CG
SAMOTOLISIB	ChEMBL	Phase 2	MTOR, PIK3CA, PIK3CD, PIK3CG
SAPANISERTIB	ChEMBL	Phase 2	MTOR, PIK3CA, PIK3CD, PIK3CG
SONOLISIB	ChEMBL	Phase 2	MTOR, PIK3CA, PIK3CD, PIK3CG
TG100-115	ChEMBL	Phase 2	MTOR, PIK3CA, PIK3CD, PIK3CG
VISTUSERTIB	ChEMBL	Phase 2	MTOR, PIK3CA, PIK3CD, PIK3CG
VOXTALISIB	ChEMBL	Phase 2	MTOR, PIK3CA, PIK3CD, PIK3CG
ZSTK-474	ChEMBL	Phase 2	MTOR, PIK3CA, PIK3CD, PIK3CG
Afatinib	PubChem	Approved	MTOR, PIK3CA, PIK3CD, PIK3CG
Pazopanib	PubChem	Approved	MTOR, PIK3CA, PIK3CD, PIK3CG
Selumetinib	PubChem	Approved	MTOR, PIK3CA, PIK3CD, PIK3CG
Fedratinib	ChEMBL + PubChem	Phase 4 (approved)	ATR, PIK3CA, PIK3CG
INAVOLISIB	ChEMBL + PubChem	Phase 4 (approved)	PIK3CA, PIK3CD, PIK3CG
DASATINIB	ChEMBL	Phase 4 (approved)	MTOR, PIK3CA, PIK3CD
DUVELISIB	ChEMBL	Phase 4 (approved)	PIK3CA, PIK3CD, PIK3CG
LENIOLISIB	ChEMBL	Phase 4 (approved)	PIK3CA, PIK3CD, PIK3CG
SUNITINIB	ChEMBL	Phase 4 (approved)	PIK3CA, PIK3CD, PIK3CG
LESTAURTINIB	ChEMBL	Phase 3	PIK3CA, PIK3CD, PIK3CG
AMG-319	ChEMBL	Phase 2	PIK3CA, PIK3CD, PIK3CG
BERZOSERTIB	ChEMBL	Phase 2	ATR, MTOR, PIK3CA
EGANELISIB	ChEMBL	Phase 2	PIK3CA, PIK3CD, PIK3CG
NEMIRALISIB	ChEMBL	Phase 2	PIK3CA, PIK3CD, PIK3CG
OSI-027	ChEMBL	Phase 2	MTOR, PIK3CA, PIK3CG
PILARALISIB	ChEMBL	Phase 2	PIK3CA, PIK3CD, PIK3CG
ROGINOLISIB	ChEMBL	Phase 2	PIK3CA, PIK3CD, PIK3CG
SERABELISIB	ChEMBL	Phase 2	PIK3CA, PIK3CD, PIK3CG
Gefitinib	PubChem	Approved	MTOR, PIK3CD, PIK3CG
UMBRALISIB	ChEMBL	Phase 4 (approved)	PIK3CD, PIK3CG
CERALASERTIB	ChEMBL	Phase 3	ATR, MTOR
EPIGALOCATECHIN GALLATE	ChEMBL	Phase 3	MTOR, PIK3CA
RESVERATROL	ChEMBL	Phase 3	MTOR, PIK3CA
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
CAMONSERTIB	ChEMBL	Phase 2	ATR, MTOR
CC-115	ChEMBL	Phase 2	MTOR, PIK3CA
DEZAPELISIB	ChEMBL	Phase 2	PIK3CD, PIK3CG
QUISINOSTAT	ChEMBL	Phase 2	PIK3CA, PIK3CD
RISOVALISIB	ChEMBL	Phase 2	PIK3CA, PIK3CD
SELETALISIB	ChEMBL	Phase 2	PIK3CD, PIK3CG
TENALISIB	ChEMBL	Phase 2	PIK3CD, PIK3CG
AMIODARONE	ChEMBL	Phase 4 (approved)	MTOR