Drug intelligence / Profile preview

AZD5305 + datopotamab deruxtecan

Development stage
Preclinical
Lead developer
AstraZeneca
Modality
Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Oral, Intravenous
01

Overview

**AZD5305 + datopotamab deruxtecan** is an experimental combination of two targeted anti-cancer agents. - **AZD5305** is a highly selective oral PARP1 inhibitor (Poly(ADP-ribose) polymerase 1 inhibitor), designed to exploit DNA repair deficiencies in tumor cells, particularly those with homologous recombination repair defects such as BRCA mutations, leading to synthetic lethality and cancer cell death[2][6]. - **Datopotamab deruxtecan** (also known as Dato-DXd, brand name Datroway) is an antibody-drug conjugate (ADC) comprising a monoclonal antibody against Trop-2 (trophoblast cell surface antigen 2), conjugated via a cleavable linker to a cytotoxic topoisomerase I inhibitor payload (DXd). The antibody targets Trop-2 on cancer cells, internalizes, and then releases the payload intracellularly, leading to DNA breaks, replication inhibition, and apoptosis in cancer cells[1][3][5]. This combination is being investigated for the treatment of advanced solid tumors, especially breast and ovarian cancers, but is not yet approved as a combination therapy.

Brand names
Datroway
Other names
datopotamab deruxtecan-dlnkdatopotamab deruxtecanDato-DXd
02

Targets

TACSTD2 (Tumor-associated calcium signal transducer 2)TOP1 (DNA Topoisomerase I)

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