Drug intelligence / Profile preview

anastrozole + palbociclib

Development stage
Phase 2
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Anastrozole + palbociclib is an oral combination regimen used primarily for the treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer. Anastrozole is a non-steroidal aromatase inhibitor that reduces estrogen production by inhibiting the aromatase enzyme, thereby decreasing tumor growth in estrogen-dependent cancers. Palbociclib is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which blocks cell cycle progression from G1 to S phase by preventing phosphorylation of retinoblastoma protein, leading to reduced proliferation of cancer cells. The combination has demonstrated efficacy and safety in clinical trials as first-line therapy for postmenopausal women with HR+/HER2- advanced breast cancer, and it may also be used in other settings such as neoadjuvant therapy or in combination with additional agents for specific subtypes[1][3][5][6].

02

Targets

CYP19A1 (Aromatase)CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)

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