Drug intelligence / Profile preview

PF-06873600 + fulvestrant

Development stage
Discontinued
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral (PF-06873600), Intramuscular (fulvestrant)
01

Overview

PF-06873600 + fulvestrant is an **investigational oral small molecule and hormonal therapy combination** for cancer. PF-06873600 is a first-in-class inhibitor of cyclin-dependent kinases 2, 4, and 6 (CDK2/4/6)[1][2][4][7]. Fulvestrant, a selective estrogen receptor degrader (SERD), is approved for hormone receptor positive metastatic breast cancer and acts as an estrogen receptor antagonist and degrader[7]. The combination was studied primarily in **hormone receptor positive (HR+), human epidermal growth factor receptor 2 negative (HER2-) advanced or metastatic breast cancer**, including post-CDK4/6 inhibitor and CDK4/6 inhibitor-naïve settings, and in patients with triple negative breast cancer and platinum-resistant ovarian cancer[1]. The rationale is that simultaneous inhibition of CDK2, 4, and 6 blocks cell cycle progression and overcomes resistance arising from cyclin E overexpression, while fulvestrant suppresses estrogen-driven growth[1][2][4].

Other names
PF-06873600 + Faslodex
02

Targets

CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)CDK2 (Cyclin-dependent kinase 2)

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