alpelisib

Trade name: Piqray

Small moleculeapproved

Approved

May 24, 2019

Alpelisib (BYL719) is a PI3Kα-selective inhibitor. PI3K-AKT-mTOR pathway is frequently activated in cancer, therefore investigational PI3K inhibitor alpelisib is considered to be effective as an anticancer agent and has been in clinical development by Novartis. Alpelisib have demonstrated activity in preclinical models of solid tumors and had favorable tolerability profiles, with the most common adverse events consistent with “on-target” inhibition of PI3K in early clinical studies. There are ongoing clinical trials of alpelisib in a range of cancer types, including breast cancer, head and neck squamous cell carcinoma, non-small cell lung carcinoma, lymphoma, and glioblastoma multiforme. Combination therapy with other chemo therapeutics may be preferable. — NCATS

Clinical trial activity

96 trials · 65 clinical orgs · 1 marketing orgs

Phase 1
46
Phase 2
55
Phase 3
10
Phase 4
1

Earliest trial started Oct 5, 2010 (NCT01219699)

Timeline

2010s

  1. Jan 1, 2010

    Novartis — Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 2014

    Novartis — Earliest Phase 2 Sponsor(trial)

  3. Jan 1, 2015

    Novartis — Earliest Phase 3 Sponsor(trial)

  4. May 24, 2019

    Novartis — Earliest FDA Approval

  5. May 24, 2019

    Novartis — Marketing Organization

  6. May 24, 2019

    Novartis — NDA Organization

Indications

Studied for

Mechanism of action

Approval history

  • approvedPriority reviewMay 24, 2019

Chemistry & pharmacology

Loading structure…

SMILES

CC1=C(SC(NC(=O)N2CCC[C@H]2C(N)=O)=N1)C3=CC(=NC=C3)C(C)(C)C(F)(F)F
Mol. weight
441.47 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

Sources

Also known as

  • alpelisib
  • alpelisib
  • alpelisib
  • alpelisib
  • byl719
  • byl719
  • byl719
  • byl-719
  • byl-719
  • nvp-byl719
  • nvp-byl719
  • nvp-byl719

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT06997588Phase 2Oct 9, 2025Novartis
NCT06997887N/AMay 9, 2025National Taiwan University
NCT06545682Phase 1/Phase 2 (Phase 2)Dec 1, 2024University of Texas at Houston
NCT06739395Phase 2Nov 1, 2024Tianjin Medical University
NCT06582004N/ASep 30, 2024National Taiwan University
NCT06354088Phase 1Apr 24, 2024Columbia University, University of California, Berkeley
NCT05948943Phase 2/Phase 3 (Phase 3)Nov 24, 2023Novartis
NCT05967286Phase 2Oct 23, 2023National Cancer Institute (NCI)
NCT05933395Phase 2Oct 10, 2023Dartmouth University
NCT05983159Phase 2Sep 30, 2023Murdoch University, Peter MacCallum Cancer Centre, University of Melbourne
NCT05966584Phase 2Jul 6, 2023AstraZeneca, Memorial Sloan-Kettering Cancer Center, Novartis
NCT05826964Phase 2Jun 12, 2023University of Miami
NCT05733455Phase 1May 9, 2023Columbia University
NCT05625087Phase 2Feb 28, 2023Breast Cancer Research Foundation, Institut Gustave Roussy, Novartis, UNICANCER
NCT05646862Phase 3Jan 31, 2023Roche
NCT05563220Phase 1/Phase 2 (Phase 2)Dec 31, 2022Pipeline Therapeutics, Inc.
NCT05238831Phase 2Dec 1, 2022Genentech, OHSU Knight Cancer Institute, Oregon Health and Science University
NCT05577754Phase 2Nov 28, 2022Novartis, University of Burgundy
NCT05472220Phase 1Nov 1, 2022Novartis, University of California, San Francisco
NCT05501886Phase 3Sep 30, 2022Celcuity
Showing 20 of 96 trials
Page 1 / 5

Organizations

Research & Development (65)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
NovartisFor profit613752010
National Cancer Institute (NCI)Government6122013
Columbia UniversityAcademic/Hospital3312014
Cornell UniversityAcademic/Hospital3312013
Peter MacCallum Cancer CentreAcademic/Hospital3222015
Seoul National UniversityAcademic/Hospital3312017
University of Texas at HoustonAcademic/Hospital3322018
Array BioPharmaFor profit2212012
AstraZenecaFor profit2022012
Memorial Sloan-Kettering Cancer CenterAcademic/Hospital2212021
National Taiwan UniversityAcademic/Hospital2212024
UNICANCERAcademic/Hospital2212018
University of California, San FranciscoAcademic/Hospital2212016
University of KansasAcademic/Hospital2222015
University of TorontoAcademic/Hospital2122015
Aix-University of MarseilleAcademic/Hospital1112019
Big Ten Cancer Research ConsortiumAcademic/Hospital1112021
Borstkanker Onderzoek GroepAcademic/Hospital1112022
Breast Cancer Research FoundationAcademic/Hospital1012023
Brown UniversityAcademic/Hospital1112016
65 organizations
Page 1 / 4

Marketing (2)

OrganizationOrg typeRelationshipDate
NovartisFor profitMKTGMay 24, 2019
NovartisFor profitNDAMay 24, 2019