Drug reference

alpelisib

PI3Kα inhibitor · Antineoplastic agent

PI3Kα inhibitorAntineoplastic agent

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

FDA category + note

Top interactionssee all 12 →

ApalutamideSevereDatabaseDDInter
CarbamazepineSevereDatabaseDDInter
EdoxabanSevereDatabaseDDInter
EnzalutamideSevereDatabaseDDInter

Mechanism

Alpelisib is an orally bioavailable inhibitor of PI3Kα with a greater than 50-fold selectivity relative to the other isoforms of PI3K.

Indications

hormone receptor–positive, HER2-negative, PIK3CA-mutated, advanced breast cancer (in combination with fulvestrant) following progression on or after endocrine-based therapyFor postmenopausal patients previously treated with endocrine therapy who are found to have a PIKC3A mutation (by liquid or tissue biopsy), in combination with fulvestrant

Pharmacokinetics

Half-life

8 to 9 h (elimination)

Metabolism

CYP3A

Side effects

Common

hyperglycemia (36%)rash (10%)diarrhea (7%)

Pregnancy & lactation

Pregnancy

Drug interactions

Apalutamide

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Carbamazepine

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Edoxaban

Severe

Database

Drug interaction classified as: absorption

Source: DDInter

Enzalutamide

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Fosphenytoin

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Lumacaftor

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Mitotane

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Phenobarbital

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Phenytoin

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Primidone

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Rifabutin

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Rifampicin

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Related guidelines

Breast cancer

ESMO · Oncology · 2024

Breast cancer

ICMR · Oncology · 2022

Cervical cancer screening and management

ICMR · Oncology · 2022

Tobacco-related cancer prevention

ICMR · Oncology · 2021

Lung cancer

ESMO · Oncology · 2024

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Textbook-sourced·Sources: Goodman & Gilman 14e, Harrison 22e·Updated: 2026-05-10