Alpelisib
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Also known as Byl-719BYL719NVP-BYL719PiqrayVijoiceALPELISIB (BYL719)AlpesilibAlpelisib
Summary
Alpelisib (CHEMBL2396661) is an approved small molecule (ATC L01EM03) targeting PIK3CA, PIK3CB, and PIK3CD; indicated across 25 conditions including breast carcinoma and neoplasm; with CIViC clinical evidence for 20 variant-indication associations (e.g. PIK3CA C420R in breast cancer).
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01EM03
- Targets: 4 (PIK3CA, PIK3CB, PIK3CD…)
- Indications: 25 conditions
- Clinical trials: 97
- Precision-oncology evidence (CIViC): 20 variant–indication associations
- Chemistry: 441.5 Da · C19H22F3N5O2S
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL2396661 |
| Name | Alpelisib |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 56649450 |
| ATC | L01EM03 |
| Molecular formula | C19H22F3N5O2S |
| Molecular weight | 441.5 |
| InChIKey | STUWGJZDJHPWGZ-LBPRGKRZSA-N |
SMILES: CC1=C(SC(=N1)NC(=O)N2CCC[C@H]2C(=O)N)C3=CC(=NC=C3)C(C)(C)C(F)(F)F
IUPAC name: (2S)-1-N-[4-methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)-4-pyridinyl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
Also known as: Alpelisib, Byl-719, BYL719, NVP-BYL719, Piqray, Vijoice, BYL-719, ALPELISIB, VIJOICE, PIQRAY, ALPELISIB (BYL719), alpelisib
Patent coverage: 2,467 distinct patent families (6,070 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 5,778 (95%) 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 | 8.3 | 42.7% | P42336 |
| PIK3CB | phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta | Inhibition | 5.92 | 5% | P42338 |
| PIK3CD | phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta | Inhibition | 6.54 | 6% | O00329 |
| PIK3CG | phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma | Inhibition | 6.6 | 0.7% | P48736 |
Broader ChEMBL bioactivity targets: 12 (assay-derived). Sample: PI3-kinase p110-alpha/p85-alpha, PI3-kinase p110-delta/p85-alpha, cAMP-dependent protein kinase catalytic subunit gamma, 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-kinase beta, Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform.
Bioactivity
ChEMBL activities: 64 potent at pChembl ≥ 5 of 64 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| PIK3CA | 8.77 | IC50 | 1.7 | nM | CHEMBL_ACT_26030793 |
| PIK3CA | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_25715642 |
| PIK3R1 | 8.41 | IC50 | 3.9 | nM | CHEMBL_ACT_22965936 |
| PIK3CA | 8.4 | IC50 | 4 | nM | CHEMBL_ACT_29055512 |
| PIK3CA | 8.34 | IC50 | 4.6 | nM | CHEMBL_ACT_16756869 |
| PIK3CA | 8.34 | IC50 | 4.6 | nM | CHEMBL_ACT_25645332 |
| PIK3CA | 8.34 | IC50 | 4.6 | nM | CHEMBL_ACT_25715517 |
| PIK3CA | 8.32 | IC50 | 4.8 | nM | CHEMBL_ACT_25715518 |
| PIK3CA | 8.3 | IC50 | 5 | nM | CHEMBL_ACT_13350818 |
| PIK3CA | 8.3 | IC50 | 5 | nM | CHEMBL_ACT_15687183 |
| PIK3CA | 8.3 | IC50 | 5 | nM | CHEMBL_ACT_15694977 |
| PIK3CA | 8.3 | IC50 | 5 | nM | CHEMBL_ACT_18135347 |
| PIK3CA | 8.3 | IC50 | 5 | nM | CHEMBL_ACT_22899846 |
| PIK3CA | 8.3 | IC50 | 5 | nM | CHEMBL_ACT_24954273 |
| PIK3CA | 8.3 | IC50 | 5 | nM | CHEMBL_ACT_25636466 |
| PIK3CA | 8.3 | IC50 | 5 | nM | CHEMBL_ACT_29055476 |
| PIK3CA | 8.3 | IC50 | 5 | nM | CHEMBL_ACT_29057539 |
| PIK3CA | 8.21 | IC50 | 6.1 | nM | CHEMBL_ACT_25956318 |
| PIK3CA | 8.02 | IC50 | 9.5 | nM | CHEMBL_ACT_22851172 |
| PIK3CA | 7.75 | IC50 | 17.8 | nM | CHEMBL_ACT_22909027 |
| PI4KB | 7.41 | IC50 | 39 | nM | CHEMBL_ACT_29165504 |
| PIK3CD | 7.16 | IC50 | 69 | nM | CHEMBL_ACT_25636516 |
| PIK3CD | 7.14 | IC50 | 72 | nM | CHEMBL_ACT_22966019 |
| PIK3CA | 7.13 | IC50 | 74 | nM | CHEMBL_ACT_13350733 |
| PIK3CA | 7.13 | IC50 | 74 | nM | CHEMBL_ACT_15686586 |
| PIK3CA | 7.13 | IC50 | 74 | nM | CHEMBL_ACT_24953807 |
| PIK3CA | 7.06 | IC50 | 87 | nM | CHEMBL_ACT_29294706 |
| PIK3CG | 7.03 | IC50 | 94 | nM | CHEMBL_ACT_22965954 |
| PIK3CG | 6.99 | IC50 | 102 | nM | CHEMBL_ACT_25636513 |
| PIK3CG | 6.86 | IC50 | 139 | nM | CHEMBL_ACT_22851158 |
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
25 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 |
|---|---|---|---|
| breast carcinoma | 4 | MONDO:0004989 | EFO:0000305 |
| neoplasm | 4 | MONDO:0005070 | EFO:0000616 |
| breast neoplasm | 4 | MONDO:0021100 | EFO:0003869 |
| head and neck squamous cell carcinoma | 2 | MONDO:0010150 | EFO:0000181 |
| squamous cell carcinoma | 2 | MONDO:0005096 | EFO:0000707 |
| upper aerodigestive tract neoplasm | 2 | MONDO:0005398 | EFO:0004284 |
| endometrium neoplasm | 2 | MONDO:0021251 | MONDO:0011962 |
| triple-negative breast carcinoma | 2 | MONDO:0005494 | EFO:0005537 |
| ovarian carcinoma | 2 | MONDO:0005140 | EFO:0001075 |
| colorectal neoplasm | 2 | MONDO:0005335 | MONDO:0005575 |
| lymphedema | 2 | MONDO:0019297 | MONDO:0019313 |
| liver disorder | 1 | MONDO:0005154 | EFO:0001421 |
| plasma cell myeloma | 1 | MONDO:0009693 | EFO:0001378 |
| exocrine pancreatic carcinoma | 1 | MONDO:0005192 | EFO:0002618 |
| esophageal squamous cell carcinoma | 1 | MONDO:0005580 | EFO:0005922 |
| rectal cancer | 1 | MONDO:0006519 | EFO:1000657 |
| oropharynx cancer | 1 | MONDO:0004608 | EFO:1001931 |
| gastric neoplasm | 1 | MONDO:0021085 | MONDO:0001056 |
| gastrointestinal stromal tumor | 1 | MONDO:0011719 | MONDO:0011719 |
| meningioma | 1 | MONDO:0016642 | MONDO:0016642 |
| uveal melanoma | 1 | MONDO:0006486 | EFO:1000616 |
4 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 97.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 33 |
| PHASE1 | 32 |
| Not specified | 11 |
| PHASE3 | 9 |
| PHASE1/PHASE2 | 9 |
| PHASE4 | 1 |
| PHASE2/PHASE3 | 1 |
| EARLY_PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT05631795 | PHASE4 | COMPLETED | Study to Assess the Safety of Alpelisib Plus Fulvestrant, in Men and Post-menopausal Women With HR-positive, HER2-negative, Advanced Breast Cancer (aBC) With PIK3CA Mutation, Whose Disease Progressed on or After Endocrine Treatment |
| NCT04208178 | PHASE3 | ACTIVE_NOT_RECRUITING | Study of Alpelisib (BYL719) in Combination With Trastuzumab and Pertuzumab as Maintenance Therapy in Patients With HER2-positive Advanced Breast Cancer With a PIK3CA Mutation |
| NCT05038735 | PHASE3 | ACTIVE_NOT_RECRUITING | Study to Assess the Efficacy and Safety of Alpelisib Plus Fulvestrant in Participants With HR-positive (HR+), HER2-negative, Advanced Breast Cancer After Treatment With a CDK4/6 Inhibitor and an Aromatase Inhibitor. |
| NCT05063786 | PHASE3 | ACTIVE_NOT_RECRUITING | Trastuzumab + Alpelisib +/- Fulvestrant vs Trastuzumab + CT in Patients With PIK3CA Mutated Previously Treated HER2+ Advanced BrEasT Cancer (ALPHABET) |
| NCT05501886 | PHASE3 | ACTIVE_NOT_RECRUITING | Gedatolisib Plus Fulvestrant With or Without Palbociclib vs Standard-of-Care for the Treatment of Patients With Advanced or Metastatic HR+/HER2- Breast Cancer (VIKTORIA-1) |
| NCT05646862 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study Evaluating the Efficacy and Safety of Inavolisib Plus Fulvestrant Compared With Alpelisib Plus Fulvestrant in Participants With HR-Positive, HER2-Negative, PIK3CA Mutated, Locally Advanced or Metastatic Breast Cancer Post CDK4/6i and Endocrine Combination Therapy |
| NCT05948943 | PHASE2/PHASE3 | RECRUITING | Alpelisib in Pediatric and Adult Patients With Lymphatic Malformations Associated With a PIK3CA Mutation. |
| NCT02437318 | PHASE3 | COMPLETED | Study Assessing the Efficacy and Safety of Alpelisib Plus Fulvestrant in Men and Postmenopausal Women With Advanced Breast Cancer Which Progressed on or After Aromatase Inhibitor Treatment. |
| NCT03439046 | PHASE3 | COMPLETED | Study of the Molecular Features of Postmenopausal Women With HR+ HER2-negative aBC on First-line Treatment With Ribociclib and Letrozole and, in Patients With a PIK3CA Mutation, on Second-line Treatment With Alpelisib Plus Fulvestrant |
| NCT04251533 | PHASE3 | TERMINATED | Study Assessing the Efficacy and Safety of Alpelisib + Nab-paclitaxel in Subjects With Advanced TNBC Who Carry Either a PIK3CA Mutation or Have PTEN Loss |
| NCT04729387 | PHASE3 | TERMINATED | Alpelisib Plus Olaparib in Platinum-resistant/Refractory, High-grade Serous Ovarian Cancer, With no Germline BRCA Mutation Detected |
| NCT01872260 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | Study of LEE011, BYL719 and Letrozole in Advanced ER+ Breast Cancer |
| NCT02925234 | PHASE2 | RECRUITING | The Drug Rediscovery Protocol (DRUP Trial) |
| NCT04524000 | PHASE2 | ACTIVE_NOT_RECRUITING | Study Assessing the Efficacy and Safety of Treatment With Alpelisib Plus Fulvestrant in Japanese Men and Postmenopausal Women With Advanced Breast Cancer |
| NCT04544189 | PHASE2 | ACTIVE_NOT_RECRUITING | Study Assessing the Efficacy and Safety of Treatment With Alpelisib Plus Fulvestrant Versus Placebo Plus Fulvestrant in Chinese Men and Postmenopausal Women With Advanced Breast Cancer |
| NCT04589650 | PHASE2 | ACTIVE_NOT_RECRUITING | Study Assessing the Efficacy, Safety and PK of Alpelisib (BYL719) in Pediatric and Adult Patients With PIK3CA-related Overgrowth Spectrum |
| NCT04762979 | PHASE2 | ACTIVE_NOT_RECRUITING | Alpelisib (BYL719) in Combination With Continued Endocrine Therapy Following Progression on Endocrine Therapy in Hormone Receptor Positive, HER2 Negative, PIK3CA Mutant Metastatic Breast Cancer |
| NCT04980833 | PHASE2 | ACTIVE_NOT_RECRUITING | Study Assessing Long-term Safety and Efficacy of Alpelisib in Patients With PIK3CA-Related Overgrowth Spectrum (PROS) Who Previously Participated in Study CBYL719F12002 (EPIK-P1) |
| NCT05090358 | PHASE2 | ACTIVE_NOT_RECRUITING | Preventing High Blood Sugar in People Being Treated for Metastatic Breast Cancer |
| NCT05154487 | PHASE2 | ACTIVE_NOT_RECRUITING | A Study of Alpelisib and Fulvestrant to Treat Endometrial Cancer |
| NCT05230810 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | Clinical Trial of Alpelisb and Tucatinib in Patients With PIK3CA-Mutant HER2+ Metastatic Breast Cancer. |
| NCT05563220 | PHASE1/PHASE2 | RECRUITING | Open-Label Umbrella Study To Evaluate Safety And Efficacy Of Elacestrant In Various Combination In Participants With Metastatic Breast Cancer |
| NCT05564377 | PHASE2 | RECRUITING | Targeted Therapy Directed by Genetic Testing in Treating Patients With Locally Advanced or Advanced Solid Tumors, The ComboMATCH Screening Trial |
| NCT05577754 | PHASE2 | RECRUITING | Assessment of the Efficacy and Safety of Alpelisib (BYL719) in Pediatric and Adult Patients With Megalencephaly-CApillary Malformation Polymicrogyria Syndrome (MCAP) |
| NCT05625087 | PHASE2 | ACTIVE_NOT_RECRUITING | Detection of Tumor DNA in the Blood of Patients Receiving Standard Therapy for Hormone Receptor-positive (HR+) Non-HER2 Expressing (HER2-) Metastatic Breast Cancer as a Tool to Select Those Who May Benefit From the Next Course of Fulvestrant in Combination With Alpelisib or Ribociclib |
| NCT05933395 | PHASE2 | RECRUITING | Genetically-informed Therapy for ER+ Breast Cancer Post-CDK4/6 Inhibitor |
| NCT05983159 | PHASE2 | RECRUITING | A Trial of Targeted Therapies for Patients With Slow-Flow or Fast-Flow Vascular Malformations |
| NCT06145308 | PHASE2 | RECRUITING | Precision Treatment of Recurrent/Metastatic Salivary Gland Carcinoma Guided by Molecular Typing |
| NCT06739395 | PHASE2 | RECRUITING | Precision Medicine Trial Based on Molecular Matching Therapy for Patients With Standard Treatment Exhaustion |
| NCT06997588 | PHASE2 | RECRUITING | EPIK-P4: A Phase II Single-arm Study to Assess the Efficacy, Safety and Pharmacokinetics of Alpelisib (BYL719) in Pediatric and Adult Patients With PIK3CA-related Overgrowth Spectrum (PROS) |
| NCT07543822 | PHASE2 | ACTIVE_NOT_RECRUITING | 24VA022; VATCH Alpelisib for TIE2/PIK3CA Pathway VAs |
| NCT01708161 | PHASE1/PHASE2 | TERMINATED | A Phase Ib/II Study of the Combination of BYL719 Plus AMG 479 in Adult Patients With Selected Solid Tumors |
| NCT01719380 | PHASE2 | COMPLETED | Study of LGX818 and Cetuximab or LGX818, BYL719, and Cetuximab in BRAF Mutant Metastatic Colorectal Cancer |
| NCT01923168 | PHASE2 | COMPLETED | Study of Letrozole With or Without BYL719 or Buparlisib, for the Neoadjuvant Treatment of Postmenopausal Women |
| NCT02145312 | PHASE2 | UNKNOWN | An Open Label, Single Arm, Multicenter Phase II Study of BYL719 in Patients With Recurrent or Metastatic Squamous Cell Carcinoma of Head and Neck Who Failed to Respond to Platinum-based Therapy. |
| NCT02276027 | PHASE2 | COMPLETED | A Phase II, Open Label, Multiple Arm Study of AUY922, BYL719, INC280, LDK378 and MEK162 in Chinese Patients With Advanced Non-small Cell Lung Cancer |
| NCT02298595 | PHASE1/PHASE2 | WITHDRAWN | Cetuximab, Cisplatin and BYL719 for HPV-Associated Oropharyngeal Squamous Cell Carcinoma |
| NCT02379247 | PHASE1/PHASE2 | COMPLETED | BYL719 and Nab-Paclitaxel in Locally Recurrent or Metastatic HER-2 Negative Breast Cancer |
| NCT02506556 | PHASE2 | COMPLETED | Phosphatidylinositol 3-kinase (PI3K) Alpha iNhibition In Advanced Breast Cancer |
| NCT03056755 | PHASE2 | COMPLETED | Study Assessing the Efficacy and Safety of Alpelisib Plus Fulvestrant or Letrozole, Based on Prior Endocrine Therapy, in Patients With PIK3CA Mutant, HR+, HER2- Advanced Breast Cancer Who Have Progressed on or After Prior Treatments |
Clinical evidence (CIViC)
Variant × indication × effect (20 predictive associations from 21 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| PIK3CA C420R | Breast Cancer | Sensitivity/Response | Alpelisib + Fulvestrant | CIViC A | EID11275 |
| PIK3CA E542K | Breast Cancer | Sensitivity/Response | Fulvestrant + Alpelisib | CIViC A | EID7315 |
| PIK3CA E545K OR PIK3CA E545A OR PIK3CA E545G OR PIK3CA E545D | Breast Cancer | Sensitivity/Response | Fulvestrant + Alpelisib | CIViC A | EID7468 |
| PIK3CA H1047R OR PIK3CA H1047Y OR PIK3CA H1047L | Breast Cancer | Sensitivity/Response | Fulvestrant + Alpelisib | CIViC A | EID7318 |
| PIK3CA Mutation | Breast Cancer | Sensitivity/Response | Alpelisib + Fulvestrant | CIViC A | EID7313 |
| PIK3CA Q546E OR PIK3CA Q546R | Breast Cancer | Sensitivity/Response | Fulvestrant + Alpelisib | CIViC A | EID7316 |
| BRAF V600 | Colorectal Cancer | Sensitivity/Response | Cetuximab + Encorafenib + Alpelisib | CIViC B | EID6047 |
| SGK1 Overexpression | Breast Cancer | Resistance | Alpelisib | CIViC B | EID1730 +1 |
| RB1 PHOSPHORYLATION | Breast Cancer | Resistance | Alpelisib | CIViC B | EID1609 |
| PIK3CA P447_L455del | Estrogen-receptor Positive Breast Cancer | Sensitivity/Response | Letrozole + Alpelisib | CIViC C | EID9575 |
| PIK3CA Q75E | Squamous Cell Carcinoma | Sensitivity/Response | Alpelisib | CIViC C | EID12159 |
| CDK4 EXPRESSION | Estrogen-receptor Positive Breast Cancer | Sensitivity/Response | Alpelisib | CIViC D | EID264 |
| PIK3CA Amplification | Stomach Carcinoma | Sensitivity/Response | Alpelisib | CIViC D | EID1403 |
| PIK3CA H1047R | Head And Neck Cancer | Sensitivity/Response | Alpelisib | CIViC D | EID1401 |
| PIK3CA Mutation | Cancer | Sensitivity/Response | Alpelisib | CIViC D | EID1402 |
| PIK3CA N345K OR PIK3CA M1043V OR PIK3CA Q75E | Squamous Cell Carcinoma | Sensitivity/Response | Alpelisib | CIViC D | EID12160 |
| PTEN Mutation | Prostate Adenocarcinoma | Sensitivity/Response | PI3Kbeta Inhibitor AZD8186 + Enzalutamide + Alpelisib | CIViC D | EID1522 |
| SGK1 Overexpression | Breast Cancer | Sensitivity/Response | SGK1-Inh + Alpelisib | CIViC D | EID1731 |
| HRAS G12V | Head And Neck Squamous Cell Carcinoma | Resistance | Alpelisib | CIViC D | EID9087 |
| PTEN Loss | Breast Cancer | Resistance | Alpelisib | CIViC D | EID716 |
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.
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 |
| IDELALISIB | ChEMBL + PubChem | Phase 4 (approved) | PIK3CA, PIK3CB, PIK3CD, PIK3CG |
| INAVOLISIB | ChEMBL + PubChem | 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: breast carcinoma, neoplasm, breast neoplasm, colorectal carcinoma, estrogen-receptor positive breast cancer, squamous cell carcinoma, gastric carcinoma, head and neck cancer, cancer, prostate adenocarcinoma, head and neck squamous cell carcinoma
- Drugs: Crizotinib, Idelalisib, Inavolisib, Copanlisib, Duvelisib, Leniolisib, Buparlisib, Dactolisib, Gedatolisib, Lestaurtinib, Taselisib, Afatinib, Pazopanib, Selumetinib, Sunitinib, Gefitinib, Dasatinib, Fedratinib, Umbralisib, Resveratrol, Belinostat, Caffeine, Midostaurin, Romidepsin, Theophylline
- Biomarker genes: CDK4, RB1, SGK1