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
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.
