Drug intelligence / Profile preview

fulvestrant + pictilisib

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

Overview

Fulvestrant + pictilisib is a combination therapy that pairs fulvestrant, an estrogen receptor antagonist, with pictilisib, an oral inhibitor of multiple phosphatidylinositol 3-kinase (PI3K) isoforms. This combination was investigated as a potential approach to overcome resistance to endocrine therapy in estrogen receptor-positive breast cancer. The rationale behind this combination is that inhibition of the PI3K pathway might help address resistance mechanisms that develop after aromatase inhibitor therapy. In clinical trials, fulvestrant was typically administered as a 500 mg intramuscular injection on day 1 and day 15 of cycle 1 and day 1 of subsequent 28-day cycles, while pictilisib was given orally at doses ranging from 260-340 mg daily.

02

Targets

PI3K (Phosphoinositide-3-kinase regulatory subunit 6)ER (Estrogen receptor)

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