Drug intelligence / Profile preview

PF-07220060 + fulvestrant

Development stage
Phase 2
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

PF-07220060 + fulvestrant is an investigational combination therapy for cancer, specifically advanced or metastatic hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) breast cancer. PF-07220060 (also known as atirmociclib) is a highly selective, next-generation oral cyclin-dependent kinase 4 (CDK4) inhibitor with significant sparing of CDK6. It works by inhibiting the CDK4/cyclin D complex, thereby blocking phosphorylation of the retinoblastoma protein and inactivating E2F-mediated transcription required for G1 cell-cycle progression. Fulvestrant is a selective estrogen receptor degrader (SERD) that binds to and accelerates degradation of the estrogen receptor, leading to inhibition of estrogen signaling in tumor cells. The combination aims to overcome resistance mechanisms seen with prior CDK4/6 inhibitor-based therapies and endocrine therapy in HR+/HER2- advanced/metastatic breast cancer[1][5][6][7][8][9].

Other names
atirmociclib + fulvestrant
02

Targets

CDK4 (Cyclin-dependent kinase 4)ESR1 (ERα)

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