Alpelisib

DRACPC ID  DRACPC0021

Active Ingredients   Alpelisib

Description  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.

Synonyms  BYL719; Phosphoinositide 3-kinase Inhibitor BYL719; Piqray; VIJOICE; Alpelisib

Type  Small Molecule

Disease  Breast Cancer

Classification

  

PI3K inhibitor Amino acid and derivative

Structure Information


Molecular Formula  C19H22F3N5O2S

Molecular Weight  441.5

Active Sequence  Not available

Sequence Length  Not available

Modification  Not available

Structure

 

Show IUPAC/InChI/SMILES

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

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

InChI_Key STUWGJZDJHPWGZ-LBPRGKRZSA-N

SMILES  O=C(N1[C@H](C(N)=O)CCC1)NC2=NC(C)=C(C3=CC(C(C)(C)C(F)(F)F)=NC=C3)S2

External Codes


PubChem CID  56649450

DrugBank Accession Number  DB12015

NCI Thesaurus Code  C94214  

UNII  08W5N2C97Q   GSRS

CAS  1217486-61-7



Drug approval


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.
Alpelisib is also used to treat adult and pediatric patients two years of age and older with severe manifestations of PIK3CA-Related Overgrowth Spectrum (PROS) who require systemic therapy. This indication is approved under accelerated approval based on response rate and duration of response. Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial(s).

Drug Name Strength Dosage Form/Route Company Marketing Status Drug ID Approval year
Piqray 50mg Tablet; Oral Novartis Prescription NDA: 212526 2019
Piqray 150mg Tablet; Oral Novartis Prescription NDA: 212526 2019
Piqray 200mg Tablet; Oral Novartis Prescription NDA: 212526 2019
Vijoice 50mg Tablet; Oral Novartis Prescription NDA: 215039 2022
Vijoice 125mg Tablet; Oral Novartis Prescription NDA: 215039 2022
Vijoice 200mg Tablet; Oral Novartis Prescription NDA: 215039 2022
Piqray 300 mg Tablet; Oral Novartis Europharm Limited Prescription EMEA/H/C/004804 2020
Piqray 50mg Tablet; Oral Novartis Pharmaceuticals Canada Inc Prescription DIN: 02497042 2020
Piqray 150mg Tablet; Oral Novartis Pharmaceuticals Canada Inc Prescription DIN: 02497069 2020
Piqray 200mg Tablet; Oral Novartis Pharmaceuticals Canada Inc Prescription DIN: 02497077 2020
Piqray 50mg Tablet, Kit; Oral Novartis Pharmaceuticals Canada Inc Prescription DIN: 02497085 2020

ClinicalTrials.gov Identifier Title Condition or disease Phase Purpose
NCT05143229 Phase I Trial Of Alpelisib Plus Sacituzumab Govitecan In Patients With Metastatic Or Locally Recurrent HER2-Negative Breast Cancer Breast Cancer Phase 1 Treatment
NCT02058381 A Phase Ib Dose De-escalation Study of the Combination of Tamoxifen Plus Goserelin Acetate With Alpelisib (BYL719) or Buparlisib (BKM120) in Premenopausal Patients With Hormone Receptor-positive/HER2-negative Locally Advanced or Metastatic Breast Cancer Pre-menopausal Breast Cancer; PI3K Pathway Inhibition Phase 1 Treatment
NCT04524000 A Phase II Open-label, 2-Part, Multi-center Study of BYL719 (Alpelisib) in Combination With Fulvestrant for Men and Postmenopausal Women With PIK3CA Mutation Hormone Receptor (HR) Positive, HER2-negative, Advanced Breast Cancer Which Progressed on or After Aromatase Inhibitor (AI) Treatment in Japan Advanced Breast Cancer Phase 2 Treatment
NCT04753203 A Phase lb/ll, Open Label, Single Arm Study to Assess Efficacy and Safety of Alpelisib and Capecitabine in Patients With PIK3CA Mutant Metastatic Colorectal Cancer Who Failed Two Prior Standard Chemotherapies Metastatic Colorectal Cancer; PIK3CA Gene Mutation Phase 1/2 Treatment
NCT04526470 Phase IB/II Study of Alpelisib in Combination With Paclitaxel in Patients With PIK3CA-altered Metastatic/Recurrent Gastric Cancer Solid Tumor; Stomach Cancer Phase 1/2 Treatment

    More clinical information is obtained from ClinicalTrials.gov.





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