Active ingredient description

Alpelisib is an inhibitor of phosphatidylinositol-3-kinase (PI3K) with inhibitory activity predominantly against PI3Kα. Gain-of-function mutations in the gene encoding the catalytic α-subunit of PI3K (PIK3CA) lead to activation of PI3Kα and Akt-signaling, cellular transformation and the generation of tumors in in vitro and in vivo models.

Medicine classification

This medicinal substance has been classified in the anatomical therapeutic chemical (ATC) classification according to its main therapeutic use as follows:

ATC code
Group title
L Antineoplastic and immunomodulating agents → L01 Antineoplastic agents → L01E Protein kinase inhibitors → L01EM Phosphatidylinositol-3-kinase (Pi3K) inhibitors
Discover more medicines within L01EM03

Product monographs

Competent medicine agencies globally have authorized commercialization of this active ingredient according to these medication package inserts (MPIs):

Structured Product Labeling (SPL/PLR)

Structural formula

Graphic representation of the active ingredient's molecular structure

Chemical formula: C₁₉H₂₂F₃N₅O₂S
Molecular mass: 441.47 g/mol

External identifiers

CAS Substance: 1217486-61-7
DrugBank Drug: DB12015
PubChem Compound: 56649450
RxNorm Ingredient: 2169285
SNOMED-CT Concept: 788050002
Alpelisib (substance)
UNII Identifier: 08W5N2C97Q


Alpelisib is an active ingredient of these brands:

United States (US)

Austria (AT)

Brazil (BR)

Canada (CA)

Estonia (EE)

Finland (FI)

France (FR)

Hong Kong (HK)

Ireland (IE)

Lithuania (LT)

Netherlands (NL)

New Zealand (NZ)

Poland (PL)

Romania (RO)

South Africa (ZA)

Turkey (TR)

United Kingdom (UK)

While we strive to include the brand names of medicines across all countries, our index remains incomplete. Therefore, it is possible that this medicine may also be marketed under different names in other countries.