Drug intelligence / Profile preview

inavolisib + abemaciclib + letrozole

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination therapy of three small molecule drugs: **inavolisib**, a PI3K alpha-selective inhibitor; **abemaciclib**, a cyclin-dependent kinase 4/6 (CDK4/6) inhibitor; and **letrozole**, a nonsteroidal aromatase inhibitor. The combination is being investigated for the treatment of **hormone receptor-positive (HR+), HER2-negative advanced or metastatic breast cancer** with PIK3CA mutations. - Inavolisib targets the PI3K-AKT-mTOR pathway by selectively inhibiting the alpha isoform of phosphoinositide 3-kinase (PIK3CA), impeding proliferative and survival signals in cancer cells. - Abemaciclib inhibits CDK4 and CDK6, causing cell cycle arrest in G1 and preventing cancer cell proliferation. - Letrozole inhibits aromatase, lowering estrogen production and minimizing the growth stimulus for HR+ breast cancer cells. This combination is being studied in advanced clinical trials and is considered a novel strategy for patients with tumors harboring both hormone receptor expression and PIK3CA mutations[2][3].

Other names
inavolisib + abemaciclib + letrozole
02

Targets

CYP19A1 (Aromatase)PIK3CA (Phosphoinositide 3-kinase alpha)CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)

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