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Chemistry

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Also known as: 1217486-61-7, Byl-719, Byl719, Piqray, Nvp-byl719, Vijoice
Molecular Formula
C19H22F3N5O2S
Molecular Weight
441.5  g/mol
InChI Key
STUWGJZDJHPWGZ-LBPRGKRZSA-N
FDA UNII
08W5N2C97Q

Alpelisib
Alpelisib is an orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. Alpelisib specifically inhibits PI3K in the PI3K/AKT kinase (or protein kinase B) signaling pathway, thereby inhibiting the activation of the PI3K signaling pathway. This may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis. Dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents.
1 2D Structure

Alpelisib

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
(2S)-1-N-[4-methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide
2.1.2 InChI
InChI=1S/C19H22F3N5O2S/c1-10-14(11-6-7-24-13(9-11)18(2,3)19(20,21)22)30-16(25-10)26-17(29)27-8-4-5-12(27)15(23)28/h6-7,9,12H,4-5,8H2,1-3H3,(H2,23,28)(H,25,26,29)/t12-/m0/s1
2.1.3 InChI Key
STUWGJZDJHPWGZ-LBPRGKRZSA-N
2.1.4 Canonical SMILES
CC1=C(SC(=N1)NC(=O)N2CCCC2C(=O)N)C3=CC(=NC=C3)C(C)(C)C(F)(F)F
2.1.5 Isomeric SMILES
CC1=C(SC(=N1)NC(=O)N2CCC[C@H]2C(=O)N)C3=CC(=NC=C3)C(C)(C)C(F)(F)F
2.2 Other Identifiers
2.2.1 UNII
08W5N2C97Q
2.3 Synonyms
2.3.1 MeSH Synonyms

1. Byl719

2. Nvp-byl719

3. Piqray

2.3.2 Depositor-Supplied Synonyms

1. 1217486-61-7

2. Byl-719

3. Byl719

4. Piqray

5. Nvp-byl719

6. Vijoice

7. Alpelisib (byl719)

8. (s)-n1-(4-methyl-5-(2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl)thiazol-2-yl)pyrrolidine-1,2-dicarboxamide

9. Byl 719

10. Chembl2396661

11. 08w5n2c97q

12. (2s)-n1-[4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethylethyl)-4-pyridinyl]-2-thiazolyl]-1,2-pyrrolidinedicarboxamide

13. (2s)-1-n-[4-methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl]-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide

14. (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

15. 1,2-pyrrolidinedicarboxamide, N1-(4-methyl-5-(2-(2,2,2-trifluoro-1,1-dimethylethyl)-4-pyridinyl)-2-thiazolyl)-, (2s)-

16. 1,2-pyrrolidinedicarboxamide, N1-[4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethylethyl)-4-pyridinyl]-2-thiazolyl]-, (2s)-

17. Alpelisib [inn]

18. (2s)-n~1~-{4-methyl-5-[2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl]-1,3-thiazol-2-yl}pyrrolidine-1,2-dicarboxamide

19. (s)-n1-(4-methyl-5-(2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl)thiazol-2-yl)pyrrolidine-1,2-dicarboxamide.

20. Unii-08w5n2c97q

21. 4jps

22. 1lt

23. Alpelisib [usan]

24. Piqray (tn)

25. Alpelisib [jan]

26. Alpelisib [mi]

27. Alpelisib [usan:inn]

28. Alpelisib [who-dd]

29. Alpelisib (jan/usan/inn)

30. Gtpl7955

31. Schembl1911869

32. Alpelisib [orange Book]

33. Chebi:93752

34. Dtxsid70153355

35. Ex-a405

36. Byl 719; Byl719

37. Bdbm50436459

38. Mfcd22417085

39. Nsc765974

40. Nsc800065

41. S2814

42. Zinc68198368

43. Akos022186315

44. Ccg-269139

45. Cs-0663

46. Db12015

47. Nsc-765974

48. Nsc-800065

49. Ncgc00346717-03

50. Ncgc00346717-06

51. (2s)-n1-[4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethylethyl)-4-pyridinyl]-2-thiazolyl]-1,2-pyrrolidine

52. 1217486-47-9

53. As-16349

54. Hy-15244

55. Sw220128-1

56. Cas:1217486-61-7;byl-719

57. D11011

58. A855666

59. J-004627

60. Q27074391

61. (2s)-n1-(4-methyl-5-(1-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl)-1,3-thiazol-2-yl)pyrrolidine-1,2-dicarboxamide

62. (2s)-n1-[4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethylethyl)-4-pyridinyl]-2-thiazolyl]-1,2-pyrrolidinedicarboxamide;alpelisib

2.4 Create Date
2012-03-05
3 Chemical and Physical Properties
Molecular Weight 441.5 g/mol
Molecular Formula C19H22F3N5O2S
XLogP33.2
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count8
Rotatable Bond Count4
Exact Mass441.14463062 g/mol
Monoisotopic Mass441.14463062 g/mol
Topological Polar Surface Area129 Ų
Heavy Atom Count30
Formal Charge0
Complexity663
Isotope Atom Count0
Defined Atom Stereocenter Count1
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Indication

Alpelisib is indicated in combination with fulvestrant to treat postmenopausal women, and men, with advanced or metastatic breast cancer. This cancer must be hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, and PIK3CA mutated. The cancer must be detected by an FDA-approved test following progression on or after an endocrine-based regimen.


FDA Label


Treatment of breast cancer


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).


Treatment of PIK3CA related overgrowth spectrum


Treatment of Fallopian tube carcinoma (excluding rhabdomyosarcoma and germ cell tumours), Treatment of ovarian carcinoma (excluding rhabdomyosarcoma and germ cell tumours), Treatment of peritoneal carcinoma (excluding blastomas and sarcomas)


5 Pharmacology and Biochemistry
5.1 Pharmacology

Alpelisib does not prolong the QTcF interval. Patients taking alpelisib experience a dose dependent benefit from treatment with a 51% advantage of a 200mg daily dose over a 100mg dose and a 22% advantage of 300mg once daily over 150mg twice daily. This suggests patients requiring a lower dose may benefit from twice daily dosing.


5.2 ATC Code

L01XE


L - Antineoplastic and immunomodulating agents

L01 - Antineoplastic agents

L01E - Protein kinase inhibitors

L01EM - Phosphatidylinositol-3-kinase (pi3k) inhibitors

L01EM03 - Alpelisib


5.3 Absorption, Distribution and Excretion

Absorption

Alpelisib reached a peak concentration in plasma of 1320912ng/mL after 2 hours. Alpelisib has an AUClast of 11,1003760h ng/mL and an AUCINF of 11,1003770h ng/mL. A large, high fat meal increases the AUC by 73% and Cmax by 84% while a small, low fat meal increases the AUC by 77% and Cmax by 145%.


Route of Elimination

36% of an oral dose is eliminated as unchanged drug in the feces and 32% as the primary metabolite BZG791 in the feces. 2% of an oral dose is eliminated in the urine as unchanged drug and 7.1% as the primary metabolite BZG791. In total 81% of an oral dose is eliminated in the feces and 14% is eliminated in the urine.


Volume of Distribution

The apparent volume of distribution at steady state is 114L.


Clearance

The mean apparent oral clearance was 39.0L/h. The predicted clearance is 9.2L/hr under fed conditions.


5.4 Metabolism/Metabolites

Alpelisib is metabolized by hydrolysis reactions to form the primary metabolite. It is also metabolized by CYP3A4. The full metabolism of Alpelisib has yet to be determined but a series of reactions have been proposed. The main metabolic reaction is the substitution of an amine group on alpelisib for a hydroxyl group to form a metabolite known as M4 or BZG791. Alpelisib can also be glucuronidated to form the M1 and M12 metabolites.


5.5 Biological Half-Life

The mean half life of alprelisib is 8 to 9 hours.


5.6 Mechanism of Action

Phosphatidylinositol-3-kinase- (PI3K) is responsible for cell proliferation in response to growth factor-tyrosine kinase pathway activation. In some cancers PI3K's p110 catalytic subunit is mutated making it hyperactive. Alpelisib inhibits (PI3K), with the highest specificity for PI3K.


KDMF

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26th North American ISSX
Not Confirmed
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Alpelisib

Registrant Name : Novartis Korea Co., Ltd.

Registration Date : 2021-05-12

Registration Number : Wed196-21-ND

Manufacturer Name : Novartis Pharmaceutical Manu...

Manufacturer Address : Kolodvorska Cesta 27, Menges, 1234, Slovenia

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Listed Suppliers

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Arevipharma

Germany
26th North American ISSX
Not Confirmed
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Arevipharma

Germany
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Alpelisib

About the Company : Arevipharma GmbH is a modern manufacturer of active pharmaceutical ingredients and intermediates with more than 140 years of expertise. Our customers are generic and research-based...

Arevipharma GmbH is a modern manufacturer of active pharmaceutical ingredients and intermediates with more than 140 years of expertise. Our customers are generic and research-based pharmaceutical companies on five continents. Our business partners recognise us as a competent, reliable and efficient company that is distinguished by individual service and an innovative character. The company’s 140 year history is based on the knowledge, skills, commitment and loyalty of its employees. Arevipharma also feels committed to its owners and investors. Due to the consistent expansion of new technologies,
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02

26th North American ISSX
Not Confirmed
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Alpelisib

About the Company : Beijing Mesochem Technology Co. Ltd., which is located in the national economic and technological development area of Yizhuang, China, manufactures pharmaceutical chemicals, fine c...

Beijing Mesochem Technology Co. Ltd., which is located in the national economic and technological development area of Yizhuang, China, manufactures pharmaceutical chemicals, fine chemicals and fundamental chemical materials. It has an efficient research and development team. Beijing Mesochem provides its customers customized development, craft optimization, contract customization and outsourcing services. The company has a well-established industrial base in Weinan, Shanxi Province. The production base features a 20,000 ㎡ plant with a production capacity of over 8,000 MT per year.
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03

Hetero Drugs

India
26th North American ISSX
Not Confirmed
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Hetero Drugs

India
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Alpelisib

About the Company : Hetero is a research based global pharmaceutical company focused on development, manufacturing and marketing of Active Pharmaceutical Ingredients (APIs), Intermediate Chemicals & F...

Hetero is a research based global pharmaceutical company focused on development, manufacturing and marketing of Active Pharmaceutical Ingredients (APIs), Intermediate Chemicals & Finished Dosages. Ever since its establishment in 1993, Hetero showed a tradition of excellence and deep sense of commitment in developing cost effective processes to offer wide range of affordable drugs. Hetero is building on the strengths of vertical integration in discovery research, process chemistry, API manufacturing, formulation development and commercialization.
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26th North American ISSX
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Alpelisib

About the Company : Founded in 2003, Hyderabad-based MSN Labs is one of the fastest-growing research-based pharmaceutical company in India. Boasting a diverse product portfolio, with multiple products...

Founded in 2003, Hyderabad-based MSN Labs is one of the fastest-growing research-based pharmaceutical company in India. Boasting a diverse product portfolio, with multiple products in the market and in the pipeline, MSN has 6 API (including Oncology) and one finished dosage facilities (one more for Oncology is being built) and an integrated R&D Center for Contract Research And Manufacturing Services (CRAMS) located in Hyderabad. MSN has won the trust of more than 250 customers across 65 countries around the globe covering the US, Europe, Latin America, Middle-East, Asia Pacific, Africa and CIS markets. Our product basket offers 100 APIs
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26th North American ISSX
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Alpelisib

About the Company : ScinoPharm Taiwan Ltd. is a leading process R&D and API manufacturing service provider to the global pharmaceutical industry. With cGMP production facilities, ScinoPharm offers a w...

ScinoPharm Taiwan Ltd. is a leading process R&D and API manufacturing service provider to the global pharmaceutical industry. With cGMP production facilities, ScinoPharm offers a wide portfolio of services ranging from custom synthesis for early phase pharmaceutical activities to brand companies as well as APIs for the generic industry.Combining cost-effective resources and productivity of Asia along with unmatched regulatory know-how, ScinoPharm is uniquely positioned to serve global pharmaceutical R&D and manufacturing needs at any level and for any company in this sector.
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Teva API

Israel
26th North American ISSX
Not Confirmed
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Teva API

Israel
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Alpelisib

About the Company : Teva API is a standalone business unit within Teva Pharmaceutical Industries, the world’s largest generic drug manufacturer. Employing over 4,000 professionals at 15 internationa...

Teva API is a standalone business unit within Teva Pharmaceutical Industries, the world’s largest generic drug manufacturer. Employing over 4,000 professionals at 15 international plant sites and 6 R&D centers, Teva API is a leading international supplier of active pharmaceutical ingredients (APIs) with the industry’s broadest portfolio of over 350 products. Its leadership in cutting-edge development, large-scale production capacity and global support make it an ideal API partner of choice. Over its more than 85 years of existence, Teva API has acquired and established top-rated manufacturing and development facilities around the world.
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FDA Orange Book

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NOVARTIS

Switzerland
26th North American ISSX
Not Confirmed
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NOVARTIS

Switzerland
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ALPELISIB

Brand Name : PIQRAY

Dosage Form : TABLET;ORAL

Dosage Strength : 50MG

Approval Date : 2019-05-24

Application Number : 212526

RX/OTC/DISCN : RX

RLD : Yes

TE Code :

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NOVARTIS

Switzerland
26th North American ISSX
Not Confirmed
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NOVARTIS

Switzerland
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26th North American ISSX
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ALPELISIB

Brand Name : PIQRAY

Dosage Form : TABLET;ORAL

Dosage Strength : 150MG

Approval Date : 2019-05-24

Application Number : 212526

RX/OTC/DISCN : RX

RLD : Yes

TE Code :

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NOVARTIS

Switzerland
26th North American ISSX
Not Confirmed
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NOVARTIS

Switzerland
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26th North American ISSX
Not Confirmed

ALPELISIB

Brand Name : PIQRAY

Dosage Form : TABLET;ORAL

Dosage Strength : 200MG

Approval Date : 2019-05-24

Application Number : 212526

RX/OTC/DISCN : RX

RLD : Yes

TE Code :

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NOVARTIS

Switzerland
26th North American ISSX
Not Confirmed
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NOVARTIS

Switzerland
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26th North American ISSX
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ALPELISIB

Brand Name : VIJOICE

Dosage Form : TABLET;ORAL

Dosage Strength : 50MG

Approval Date : 2022-04-05

Application Number : 215039

RX/OTC/DISCN : RX

RLD : Yes

TE Code :

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05

NOVARTIS

Switzerland
26th North American ISSX
Not Confirmed
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NOVARTIS

Switzerland
arrow
26th North American ISSX
Not Confirmed

ALPELISIB

Brand Name : VIJOICE

Dosage Form : TABLET;ORAL

Dosage Strength : 125MG

Approval Date : 2022-04-05

Application Number : 215039

RX/OTC/DISCN : RX

RLD : Yes

TE Code :

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06

NOVARTIS

Switzerland
26th North American ISSX
Not Confirmed
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NOVARTIS

Switzerland
arrow
26th North American ISSX
Not Confirmed

ALPELISIB

Brand Name : VIJOICE

Dosage Form : TABLET;ORAL

Dosage Strength : 200MG

Approval Date : 2022-04-05

Application Number : 215039

RX/OTC/DISCN : RX

RLD : Yes

TE Code :

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07

NOVARTIS

Switzerland
26th North American ISSX
Not Confirmed
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NOVARTIS

Switzerland
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26th North American ISSX
Not Confirmed

ALPELISIB

Brand Name : VIJOICE

Dosage Form : GRANULES;ORAL

Dosage Strength : 50MG/PACKET

Approval Date : 2024-04-24

Application Number : 218466

RX/OTC/DISCN : RX

RLD : Yes

TE Code :

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