Scroll

alpelisib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
phosphatidylinositol 3-kinase inhibitors, antineoplastics	5328	1217486-61-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: alpelisib piqray BYL-719 NVP-BYL-719 vijoice	Alpelisib is an inhibitor of phosphatidylinositol-3- kinase (PI3K) with inhibitory activity predominantly against PI3Kalpha. Gain-of-function mutations in the gene encoding the catalytic alpha-subunit of PI3K (PIK3CA) lead to activation of PI3Kalpha and Akt-signaling, cellular transformation and the generation of tumors in in vitro and in vivo models. Molecular weight: 441.47 Formula: C19H22F3N5O2S CLOGP: 2.47 LIPINSKI: 0 HAC: 7 HDO: 2 TPSA: 101.21 ALOGS: -4.92 ROTB: 5 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

alpelisib
piqray
BYL-719
NVP-BYL-719
vijoice

Alpelisib is an inhibitor of phosphatidylinositol-3- kinase (PI3K) with inhibitory activity predominantly against PI3Kalpha. Gain-of-function mutations in the gene encoding the catalytic alpha-subunit of PI3K (PIK3CA) lead to activation of PI3Kalpha and Akt-signaling, cellular transformation and the generation of tumors in in vitro and in vivo models.

Molecular weight: 441.47
Formula: C19H22F3N5O2S
CLOGP: 2.47
LIPINSKI: 0
HAC: 7
HDO: 2
TPSA: 101.21
ALOGS: -4.92
ROTB: 5

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.30	g	O

ADMET properties:

Show entries

Search:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ
S (Water solubility)	0.02 mg/mL	Bocci G, Oprea TI, Benet LZ

Showing 1 to 2 of 2 entries

Previous1Next

Approvals:

Date	Agency	Company	Orphan
April 24, 2019	FDA	NOVARTIS PHARMS CORP
July 27, 2020	EMA	Novartis Europharm Limited

FDA Adverse Event Reporting System (Female)

Show entries

Search:

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hyperglycaemia	2465.81	27.78	654	8152	41213	63439003
Rash	602.50	27.78	543	8263	560328	62919888
Blood glucose increased	572.72	27.78	263	8543	83493	63396723
Malignant neoplasm progression	543.07	27.78	252	8554	81869	63398347
Metastases to bone	239.37	27.78	95	8711	20924	63459292
Metastases to liver	231.95	27.78	96	8710	23543	63456673
Death	214.88	27.78	261	8545	374120	63106096
Diarrhoea	194.07	27.78	350	8456	715016	62765200
Diabetic ketoacidosis	176.85	27.78	76	8730	20429	63459787
Diabetes mellitus	119.59	27.78	82	8724	55728	63424488

Showing 1 to 10 of 41 entries

Previous1 2 3 4 5Next

FDA Adverse Event Reporting System (Male)

Show entries

Search:

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hyperglycaemia	103.00	43.35	27	182	39453	34917269

Showing 1 to 1 of 1 entries

Previous1Next

FDA Adverse Event Reporting System (Geriatric)

Show entries

Search:

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hyperglycaemia	1139.61	28.10	348	5393	69987	79668660
Malignant neoplasm progression	362.32	28.10	182	5559	135808	79602839
Blood glucose increased	354.37	28.10	170	5571	114805	79623842
Rash	269.63	28.10	264	5477	578094	79160553
Metastases to bone	212.48	28.10	76	5665	24351	79714296
Metastases to liver	197.90	28.10	75	5666	28239	79710408
Diarrhoea	134.93	28.10	232	5509	880257	78858390
Diabetic ketoacidosis	128.10	28.10	58	5683	34064	79704583
Death	109.18	28.10	166	5575	566348	79172299
Diabetes mellitus	85.37	28.10	59	5682	78331	79660316

Showing 1 to 10 of 32 entries

Previous1 2 3 4Next

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Show entries

Search:

Source	Code	Description
ATC	L01EM03	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Phosphatidylinositol-3-kinase (Pi3K) inhibitors

Showing 1 to 1 of 1 entries

Previous1Next

Drug Use | Suggest Off label Use Form| |View source of the data|

Show entries

Search:

Disease	Relation	SNOMED_ID	DOID
PIK3CA-related overgrowth spectrum (PROS)	indication	737037004
Germline BRCA-mutated, HER2-negative metastatic breast cancer	indication	767444009

Showing 1 to 2 of 2 entries

Previous1Next

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Show entries

Search:

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	4.6	acidic
pKa2	13.49	acidic
pKa3	5.2	Basic
pKa4	2.4	Basic

Showing 1 to 4 of 4 entries

Previous1Next

Orange Book patent data (new drug applications)

Show entries

Search:

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
150MG	PIQRAY	NOVARTIS	N212526	May 24, 2019	RX	TABLET	ORAL	8227462	April 29, 2033	IN COMBINATION WITH FULVESTRANT FOR TREATMENT OF POSTMENOPAUSAL WOMEN, AND MEN, WITH HR-POSITIVE, HER-2-NEGATIVE, PIK3CA-MUTATED, ADVANCED OR METASTATIC BREAST CANCER
200MG	PIQRAY	NOVARTIS	N212526	May 24, 2019	RX	TABLET	ORAL	8227462	April 29, 2033	IN COMBINATION WITH FULVESTRANT FOR TREATMENT OF POSTMENOPAUSAL WOMEN, AND MEN, WITH HR-POSITIVE, HER-2-NEGATIVE, PIK3CA-MUTATED, ADVANCED OR METASTATIC BREAST CANCER
50MG	PIQRAY	NOVARTIS	N212526	May 24, 2019	RX	TABLET	ORAL	8227462	April 29, 2033	IN COMBINATION WITH FULVESTRANT FOR TREATMENT OF POSTMENOPAUSAL WOMEN, AND MEN, WITH HR-POSITIVE, HER-2-NEGATIVE, PIK3CA-MUTATED, ADVANCED OR METASTATIC BREAST CANCER

Showing 1 to 3 of 3 entries

Previous1Next

Orange Book exclusivity data (new drug applications)

Show entries

Search:

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
125MG	VIJOICE	NOVARTIS	N215039	April 5, 2022	RX	TABLET	ORAL	May 24, 2024	NEW CHEMICAL ENTITY
125MG	VIJOICE	NOVARTIS	N215039	April 5, 2022	RX	TABLET	ORAL	April 5, 2029	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 2 YEARS OF AGE AND OLDER WITH SEVERE MANIFESTATIONS OF PIK3CA-RELATED OVERGROWTH SPECTRUM (PROS) WHO REQUIRE SYSTEMIC THERAPY
150MG	PIQRAY	NOVARTIS	N212526	May 24, 2019	RX	TABLET	ORAL	May 24, 2024	NEW CHEMICAL ENTITY
200MG	PIQRAY	NOVARTIS	N212526	May 24, 2019	RX	TABLET	ORAL	May 24, 2024	NEW CHEMICAL ENTITY
200MG	VIJOICE	NOVARTIS	N215039	April 5, 2022	RX	TABLET	ORAL	May 24, 2024	NEW CHEMICAL ENTITY
200MG	VIJOICE	NOVARTIS	N215039	April 5, 2022	RX	TABLET	ORAL	April 5, 2029	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 2 YEARS OF AGE AND OLDER WITH SEVERE MANIFESTATIONS OF PIK3CA-RELATED OVERGROWTH SPECTRUM (PROS) WHO REQUIRE SYSTEMIC THERAPY
50MG	PIQRAY	NOVARTIS	N212526	May 24, 2019	RX	TABLET	ORAL	May 24, 2024	NEW CHEMICAL ENTITY
50MG	VIJOICE	NOVARTIS	N215039	April 5, 2022	RX	TABLET	ORAL	May 24, 2024	NEW CHEMICAL ENTITY
50MG	VIJOICE	NOVARTIS	N215039	April 5, 2022	RX	TABLET	ORAL	April 5, 2029	TREATMENT OF ADULT AND PEDIATRIC PATIENTS 2 YEARS OF AGE AND OLDER WITH SEVERE MANIFESTATIONS OF PIK3CA-RELATED OVERGROWTH SPECTRUM (PROS) WHO REQUIRE SYSTEMIC THERAPY

Showing 1 to 9 of 9 entries

Previous1Next

Bioactivity Summary:

Show entries

Search:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform	Kinase	P42336	PK3CA_HUMAN	INHIBITOR	IC50	8.34	SCIENTIFIC LITERATURE	DRUG LABEL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Kinase	O00329	PK3CD_HUMAN		IC50	6.54	CHEMBL
Cyclin-G-associated kinase	Kinase	O14976	GAK_HUMAN		Kd	5.30	CHEMBL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform	Kinase	P42338	PK3CB_HUMAN		IC50	5.92	CHEMBL
Serine/threonine-protein kinase mTOR	Kinase	P42345	MTOR_HUMAN		IC50	5.52	CHEMBL
cAMP-dependent protein kinase catalytic subunit gamma	Kinase	P22612	KAPCG_HUMAN		Kd	5.70	CHEMBL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform	Kinase	P48736	PK3CG_HUMAN		IC50	6.60	CHEMBL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform	Kinase		PK3CB_RAT		IC50	5.66	CHEMBL

Showing 1 to 8 of 8 entries

Previous1Next

External reference:

Show entries

Search:

ID	Source
1LT	PDB_CHEM_ID
018005	NDDF
08W5N2C97Q	UNII
2169285	RXNORM
317932	MMSL
358240	MMSL
37038	MMSL
4038445	VANDF
56649450	PUBCHEM_CID
788050002	SNOMEDCT_US

Showing 1 to 10 of 19 entries

Previous1 2Next

Pharmaceutical products:

Show entries

Search:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
PIQRAY	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0701	TABLET	200 mg	ORAL	NDA	31 sections
PIQRAY	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0701	TABLET	200 mg	ORAL	NDA	31 sections
PIQRAY	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0701	TABLET	200 mg	ORAL	NDA	31 sections
PIQRAY	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0708	TABLET	150 mg	ORAL	NDA	31 sections
PIQRAY	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0708	TABLET	150 mg	ORAL	NDA	31 sections
PIQRAY	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0708	TABLET	150 mg	ORAL	NDA	31 sections
VIJOICE	HUMAN PRESCRIPTION DRUG LABEL	1	0078-1021	TABLET	50 mg	ORAL	NDA	30 sections
VIJOICE	HUMAN PRESCRIPTION DRUG LABEL	1	0078-1021	TABLET	50 mg	ORAL	NDA	30 sections
VIJOICE	HUMAN PRESCRIPTION DRUG LABEL	1	0078-1028	TABLET	125 mg	ORAL	NDA	30 sections
VIJOICE	HUMAN PRESCRIPTION DRUG LABEL	1	0078-1028	TABLET	125 mg	ORAL	NDA	30 sections

Showing 1 to 10 of 10 entries

Previous1Next