Drug intelligence / Profile preview

paclitaxel + encequidar + dostarlimab + trastuzumab

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

Overview

This is a combination regimen consisting of four agents: - **Paclitaxel** is a microtubule-stabilizing chemotherapeutic agent that inhibits cell division. - **Encequidar** is an oral, minimally absorbed, gut-specific P-glycoprotein (P-gp) inhibitor that enhances the oral bioavailability of paclitaxel by inhibiting its efflux in the gastrointestinal tract[1][2][3]. - **Dostarlimab** is a humanized monoclonal antibody targeting programmed cell death protein 1 (PD-1), functioning as an immune checkpoint inhibitor to enhance anti-tumor immune responses[9]. - **Trastuzumab** is a monoclonal antibody targeting human epidermal growth factor receptor 2 (HER2), used primarily in HER2-positive cancers to inhibit proliferation of tumor cells overexpressing this receptor[7]. This specific four-drug combination does not have an established brand name or unique regulatory approval as a fixed regimen. Each component has demonstrated efficacy in various cancer types—most notably breast cancer for paclitaxel/encequidar/trastuzumab and endometrial or other solid tumors for dostarlimab—but there are no published clinical trials or regulatory approvals for this exact quadruple combination. The rationale for combining these agents would be to leverage cytotoxic chemotherapy (paclitaxel), improved oral delivery (encequidar), HER2-targeted therapy (trastuzumab), and immunotherapy via PD-1 blockade (dostarlimab).

Other names
paclitaxel and encequidar and dostarlimab and trastuzumaboPac+E+dostarlimab+trastuzumab
02

Targets

ABCB1 (P-glycoprotein)TUBB (Tubulin (alpha and beta subunits))PDCD1 (Programmed cell death protein 1 receptor)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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