Alpelisib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2019
- First approval year
- 2019
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Alpelisib
- Molecular weight
- 441.48
- Structure (SMILES)
- Cc1nc(NC(=O)N2CCC[C@H]2C(N)=O)sc1-c1ccnc(C(C)(C)C(F)(F)F)c1
- piqray
- Piqray
- vijoice
- Vijoice
- (S)-PYRROLIDINE-1,2-DICARBOXYLIC ACID 2-AMIDE 1-(4-METHYL-5-(2-(2,2,2-TRIFLUORO-1,1-DIMETHYLETHYL)-PYRIDIN-4-YL)THIAZOL-2-YL)AMIDE
- alpelisib
- Alpelisib
- ALPELISIB
- alpelisib (BYL719)
- Alpelisib (BYL719)
- ALPELISIB (BYL719)
- alpelisib [INN]
- ALPELISIB [JAN]
- ALPELISIB [MI]
- ALPELISIB [ORANGE BOOK]
- ALPELISIB [USAN]
- Alpelisib [WHO-DD]
- Alpelisib 300 mg
- alpelisib byl719
- alpelisib inn
- alpelisib jan
- alpelisib mi
- alpelisib orange book
- alpelisib usan
- alpelisib who dd
- byl 719
- byl 719a 1214 s n1 4 methyl 5 2 1 1 1 trifluoro 2 methylpropan 2 yl pyridin 4 yl thiazol 2 yl pyrrolidine 1 2 dicarboxamide
- Byl-719
- BYL-719
And 13 more, listed on the interactive page.
- CAS registry numbers
- 1217486-61-7
- ChEMBL ID
- CHEMBL2396661
- InChIKey
- STUWGJZDJHPWGZ-LBPRGKRZSA-N
- PubChem compound IDs
- 56649450
- RxNorm IDs (RxCUI)
- 2169285
- FDA ingredient codes (UNII)
- 08W5N2C97Q
- L01EM03
- L01XE
Sources for recorded values
- Applicant
- NOVARTIS
- Approval date
- 24 May 2019
- Application number
- NDA212526
- Status
- Authorised
- Status date
- 27 Jul 2020
- Authorisation date
- 27 Jul 2020
- Approved indications
- Piqray is indicated in combination with fulvestrant for the treatment of postmenopausal women, and men, with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, locally advanced or metastatic breast cancer with a PIK3CA mutation after disease progression following endocrine therapy as monotherapy (see section 5.1).
- Product number
- EMEA/H/C/004804
- Authorisation holder
- Novartis Europharm Limited
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- No
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Breast Neoplasms
European medicines record
- Patents
- 10
- Designations
- 5
- Earliest recorded loss of exclusivity
- 17 Feb 2037
- First in class
- No
- Fast track
- No
- Breakthrough designation
- Yes
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Pharmacology name
- alpelisib
- Type
- Synthetic organic
- Drug name stem
- -lisib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta
- Gene symbol
- PIK3CD
- Protein identifier
- O00329
- Median affinity
- 6.54
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha
- Gene symbol
- PIK3CA
- Protein identifier
- P42336
- Median affinity
- 8.3
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta
- Gene symbol
- PIK3CB
- Protein identifier
- P42338
- Median affinity
- 5.92
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma
- Gene symbol
- PIK3CG
- Protein identifier
- P48736
- Median affinity
- 6.6
- Affinity units
- pIC50
- Mechanism
- PI3-kinase p110-alpha subunit inhibitor
- Action type
- Inhibitor
- Target
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
- Protein identifier
- P42336
Open Targets mechanisms
- Mechanism
- PI3-kinase p110-alpha subunit inhibitor
- Action type
- Inhibitor
- Target
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
DrugCentral mechanisms
- Action type
- Inhibitor
- Gene symbol
- PIK3CA
- Protein identifier
- P42336
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Carcinoma, Squamous Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000181
- Subject identifier
- D002294
- Condition
- Breast Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000305
- Subject identifier
- D001943
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Carcinoma, Squamous Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000707
- Subject identifier
- D002294
- Condition
- Ovarian Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0001075
- Subject identifier
- D010051
- Condition
- Multiple Myeloma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001378
- Subject identifier
- D009101
- Condition
- Liver Diseases
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001421
- Subject identifier
- D008107
- Condition
- Pancreatic Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0002618
- Subject identifier
- D010190
- Condition
- Breast Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- EFO:0003869
- Subject identifier
- D001943
- Condition
- Head and Neck Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0004284
- Subject identifier
- D006258
- Condition
- Triple Negative Breast Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0005537
- Subject identifier
- D064726
- Condition
- Esophageal Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0005922
- Subject identifier
- D004938
- Condition
- Uveal Melanoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:1000616
- Subject identifier
- D000098943
- Condition
- Rectal Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:1000657
- Subject identifier
- D012004
- Condition
- Oropharyngeal Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:1001931
- Subject identifier
- D009959
- Condition
- Stomach Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0001056
- Subject identifier
- D013274
- Condition
- Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0004992
- Subject identifier
- D009369
- Condition
- Colorectal Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0005575
- Subject identifier
- D015179
- Condition
- Breast Neoplasms
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0007254
- Subject identifier
- D001943
- Condition
- Gastrointestinal Stromal Tumors
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0011719
- Subject identifier
- D046152
- Condition
- Endometrial Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0011962
- Subject identifier
- D016889
- Condition
- Meningioma
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0016642
- Subject identifier
- D008579
- Condition
- Lymphedema
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0019313
- Subject identifier
- D008209
- Condition
- Oropharyngeal Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0021364
- Subject identifier
- D009959
- Condition
- Squamous Cell Carcinoma of Head and Neck
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0044704
- Subject identifier
- D000077195
- Condition identifier
- EFO_0000181
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000305
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0000707
- Highest recorded phase
- 1
- Condition identifier
- EFO_0001421
- Highest recorded phase
- 1
- Condition identifier
- EFO_0003869
- Condition identifier
- EFO_0004952
- Highest recorded phase
- 2
- Condition identifier
- EFO_0009146
- Highest recorded phase
- 2
- Condition identifier
- EFO_0700100
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0000521
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0001056
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0002013
- Condition identifier
- MONDO_0002447
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0003060
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004989
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0004992
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005070
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005086
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005089
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005096
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005105
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005140
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005148
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005192
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005233
- Highest recorded phase
- 2
And 34 more, listed on the interactive page.
- Event
- blood glucose abnormal
- Reports
- 13
- Reporting signal score
- 20.7167
- Event
- blood glucose increased
- Reports
- 173
- Reporting signal score
- 364.632
- Event
- breast cancer
- Reports
- 28
- Reporting signal score
- 30.0322
- Event
- breast cancer metastatic
- Reports
- 58
- Reporting signal score
- 195.695
- Event
- decreased appetite
- Reports
- 68
- Reporting signal score
- 39.7969
- Event
- diabetes mellitus
- Reports
- 46
- Reporting signal score
- 53.906
- Event
- diabetic ketoacidosis
- Reports
- 49
- Reporting signal score
- 80.5776
- Event
- diarrhoea
- Reports
- 223
- Reporting signal score
- 130.5
- Event
- disease progression
- Reports
- 42
- Reporting signal score
- 23.8706
- Event
- drug hypersensitivity
- Reports
- 3
- Reporting signal score
- 20.3429
- Event
- drug interaction
- Reports
- 1
- Reporting signal score
- 20.0824
- Event
- hyperglycaemia
- Reports
- 497
- Reporting signal score
- 1,926.34
- Event
- hyperglycaemic hyperosmolar nonketotic syndrome
- Reports
- 26
- Reporting signal score
- 110.458
- Event
- ketoacidosis
- Reports
- 16
- Reporting signal score
- 30.9251
- Event
- malignant neoplasm progression
- Reports
- 99
- Reporting signal score
- 161.224
- Event
- metastases to bone
- Reports
- 39
- Reporting signal score
- 86.3926
- Event
- metastases to liver
- Reports
- 30
- Reporting signal score
- 59.4136
- Event
- mucosal inflammation
- Reports
- 36
- Reporting signal score
- 46.3032
- Event
- nausea
- Reports
- 158
- Reporting signal score
- 35.0927
- Event
- oral pain
- Reports
- 19
- Reporting signal score
- 24.0685
- Event
- pik3ca-activated mutation
- Reports
- 9
- Reporting signal score
- 38.3943
- Event
- rash
- Reports
- 403
- Reporting signal score
- 559.824
- Event
- skin toxicity
- Reports
- 14
- Reporting signal score
- 26.0254
- Event
- stomatitis
- Reports
- 62
- Reporting signal score
- 85.5488
- Event
- weight decreased
- Reports
- 58
- Reporting signal score
- 22.3084
- NCT01219699
- NCT01300962
- NCT01791478
- NCT01870505
- NCT01872260
- NCT01923168
- NCT02038010
- NCT02058381
- NCT02088684
- NCT02167854
- NCT02379247
- NCT02437318
- NCT02506556
- NCT02734615
- NCT03056755
- NCT03284957
- NCT03386162
- NCT03439046
- NCT04208178
- NCT04300790
- NCT04524000
- NCT04762979
- NCT04862143
- NCT04899349
- NCT05038735
And 43 more, listed on the interactive page.
- Dose
- 300 mg
- Route
- Oral
- How often
- Once daily
- Do not chew, crush or split tablets
- Swallow tablets whole
- Take with food
- Hydrogen bond acceptors
- 5
- Hydrogen bond donors
- 2
- Polar surface area
- 101.21
- Calculated partition coefficient (ALogP)
- 3.84
- Calculated partition coefficient (XLogP)
- 3.2
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 4
- Heavy atoms
- 30
- Molecular formula
- C19H22F3N5O2S
- Monoisotopic mass
- 441.14463062
- Natural product
- No
- 0078-0701
- 0078-0708
- 0078-0715
- 0078-1021
- 0078-1028
- 0078-1035
- 0078-1175
- Recorded assays
- 955
- Active assays
- 176
- Confirmatory
- Other
- Screening
These details could not be displayed.
Related records
Trials (102)
- 24VA022; VATCH Alpelisib for TIE2/PIK3CA Pathway VAs
- A Dose-finding Study of a Combination of Imatinib and BYL719 in the Treatment of 3rd Line GIST Patients
- A Phase Ib Dose De-escalation Study With BYL719 in Premenopausal Patients With Locally Advanced or Metastatic Breast Cancer
- A Phase Ib Study of MEK162 Plus BYL719 in Adult Patients With Selected Advanced Solid Tumors
- A Phase Ib/II Study of BYL719 and Cetuximab in Recurrent or Metastatic Head and Neck Squamous Cell Carcinoma
- A Phase Ib/II Study of the Combination of BYL719 Plus AMG 479 in Adult Patients With Selected Solid Tumors
- 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
- 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
- A Study of Alpelisib and Fulvestrant to Treat Endometrial Cancer
- A Study of BYL719 in Adult Patients With Advanced Solid Malignancies
- A Study of BYL719 in Adult Patients With Advanced Solid Malignancies, Whose Tumors Have an Alteration of the PIK3CA Gene
- A Study of LY3484356 in Participants With Advanced or Metastatic Breast Cancer or Endometrial Cancer
- A Study to Evaluate the Potential Benefit of the Addition of BYL719 to Paclitaxel in the Treatment of Breast Cancer and Head-and-neck Cancer
- A Study to Prevent Rash in People Starting Alpelisib for the Treatment of Breast Cancer
- A Trial of Targeted Therapies for Patients With Slow-Flow or Fast-Flow Vascular Malformations
- A Window of Opportunity Study to Assess the Modulation of Biomarkers in Head and Neck Squamous Cell Cancer (HNSCC) By Preoperative Treatment With BYL719
- Alpelisib (BYL719) in Combination With Continued Endocrine Therapy Following Progression on Endocrine Therapy in Hormone Receptor Positive, HER2 Negative, PIK3CA Mutant Metastatic Breast Cancer
- Alpelisib and Capecitabine in Patients With PIK3CA Mutant mCRC Patients
- Alpelisib and Enzalutamide in Treating Patients With Androgen Receptor and PTEN Positive Metastatic Breast Cancer
- Alpelisib and Paclitaxel in PIK3CA-altered Gastric Cancer
Approved for (5)
- Breast cancer
- Breast carcinoma
- Breast neoplasm
- Cancer
- Neoplasm
In development for (20)
- Colorectal cancer Phase 2
- Endometrial cancer Phase 2
- Esophageal squamous cell carcinoma Phase 1
- Exocrine pancreatic carcinoma Phase 1
- Gastric cancer Phase 1
- Gastrointestinal stromal tumor Phase 1
- Head and neck squamous cell carcinoma Phase 2
- Liver disorder Phase 1
- Lymphatic malformation Phase 2
- Meningioma Phase 1
- Neoplasm of oropharynx Phase 1
- Oropharynx cancer Phase 1
- Oropharynx squamous cell carcinoma Phase 2
- Ovarian carcinoma Phase 2
- Plasma cell myeloma Phase 1
- Rectal cancer Phase 1
- Squamous cell carcinoma Phase 2
- Triple-negative breast carcinoma Phase 2
- Upper aerodigestive tract neoplasm Phase 2
- Uveal melanoma Phase 1
Other linked conditions (1)
- Lymphangioma
Targets (1)
- PIK3CA PI3-kinase p110-alpha subunit inhibitor