Drug intelligence / Profile preview

ridaforolimus + trastuzumab

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

Overview

Ridaforolimus + trastuzumab is a combination therapy consisting of ridaforolimus, an oral mTOR (mechanistic target of rapamycin) inhibitor (a non-prodrug rapalog), and trastuzumab, a monoclonal antibody targeting the HER2/neu receptor. This combination has been investigated primarily for patients with HER2-positive cancers—especially metastatic breast cancer and uterine serous carcinoma—that are resistant to standard anti-HER2 therapies. Ridaforolimus inhibits mTOR signaling pathways involved in cell growth and proliferation, while trastuzumab blocks HER2-mediated signaling. The rationale for this combination is that dual inhibition of mTOR and HER2 can overcome resistance mechanisms in tumors with concurrent HER2 overexpression and PI3K pathway activation (such as PIK3CA mutations). Clinical studies have shown that this regimen is generally well tolerated and demonstrates antitumor activity in heavily pretreated populations[1][3][4][5].

Other names
oral deforolimus + trastuzumab
02

Targets

Mechanistic target of rapamycin complex 1ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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