Drug intelligence / Profile preview

trastuzumab deruxtecan + ritonavir

Development stage
Unknown
Lead developer
Daiichi Sankyo
Modality
Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous (trastuzumab Deruxtecan), Oral (ritonavir)
01

Overview

This is a combination drug consisting of **trastuzumab deruxtecan** and **ritonavir**. Trastuzumab deruxtecan is an **antibody-drug conjugate (ADC)** targeting the human epidermal growth factor receptor 2 (**HER2**) and is used as a targeted therapy for HER2-positive cancers. It is composed of a monoclonal antibody (trastuzumab) linked to a cytotoxic topoisomerase I inhibitor (deruxtecan), enabling selective delivery of the chemotherapy agent to HER2-expressing tumor cells. Ritonavir is a **small molecule** originally developed as an HIV protease inhibitor but is now primarily used as a pharmacokinetic enhancer by inhibiting cytochrome P450 3A4 (CYP3A4), thus increasing the exposure of co-administered drugs metabolized by this enzyme. This combination may be considered for investigational boosting of trastuzumab deruxtecan’s exposure or in research, but there are no approved combination indications for these two agents and no direct pharmacological interaction between their primary therapeutic mechanisms[1][2][3][4].

Other names
trastuzumab deruxtecanDS-8201aDS8201aDS 8201aritoRTVritonavirNorvir
02

Targets

TOP1 (DNA Topoisomerase I)CYP3A4 (Cytochrome P450 3A4)PR (Progesterone receptor)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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