Drug intelligence / Profile preview

enzalutamide + trastuzumab

Development stage
Unknown
Lead developer
Astellas Pharma
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

Enzalutamide plus trastuzumab is a combination therapy that targets both androgen receptor (AR) signaling and HER2 pathways. Enzalutamide is an androgen receptor signaling inhibitor, while trastuzumab is an anti-HER2 antibody. This combination has been studied in patients with HER2-positive and androgen receptor-positive metastatic or locally advanced breast cancer. In clinical trials, the combination was well tolerated, and a subset of heavily pretreated patients experienced durable disease control. The combination works through distinct mechanisms - enzalutamide inhibits dihydrotestosterone-mediated nuclear localization of AR and attenuates the increased expression of pHER3 and total HER3 protein, while trastuzumab targets HER2 to inhibit tumor growth.

02

Targets

AR (Adrenergic receptors)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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