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Association details:
| Biomarker: | ER underexpression |
|---|---|
| Cancer: | Breast Cancer |
| Drug: | vepdegestrant (ARV-471) (Ubiquitin pathway modulator, Estrogen receptor alpha degrader) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
44 - The discovery of ARV-471, an orally bioavailable estrogen receptor degrading PROTAC®for the treatment of patients with breast cancer
Published date:
03/10/2021
Excerpt:
Daily, oral-administration of single agent ARV-471 (3, 10, and 30 mpk) leads to significant anti-tumor activity of estradiol-dependent MCF7 xenografts and concomitant tumor ER protein reductions of >90% at study termination....Moreover, when a CDK4/6 inhibitor is combined with ARV-471 in the MCF7 model, even more pronounced tumor growth inhibition is observed (131% TGI), accompanied by significant reductions in ER protein levels.
Secondary therapy:
CDK4 inhibitor + CDK6 inhibitor
