Drug intelligence / Profile preview

rucaparib + sacituzumab govitecan

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

Overview

**Rucaparib + sacituzumab govitecan** is an experimental drug combination comprising a PARP inhibitor (rucaparib) and an antibody-drug conjugate (sacituzumab govitecan, also known by its brand name Trodelvy). Rucaparib selectively inhibits poly(ADP-ribose) polymerase enzymes (PARP1, PARP2, PARP3), which are involved in DNA repair, exploiting the DNA repair deficiencies of certain cancer cells. Sacituzumab govitecan consists of an anti-TROP-2 monoclonal antibody linked to SN-38, a topoisomerase I inhibitor; this ADC binds to TROP-2-expressing tumor cells and delivers the cytotoxic SN-38, inhibiting DNA topoisomerase I and resulting in DNA damage and cell death. The combination is being studied in the SEASTAR phase 1b/2 trial for patients with advanced solid tumors, particularly those with triple-negative breast cancer (TNBC) and other homologous recombination repair-deficient cancers[1][3][5].

Other names
rucaparib + Trodelvyrucaparib + sacituzumab govitecan-hziy
02

Targets

PARP3 (Poly(adp-ribose) polymerase 3)TACSTD2 (Tumor-associated calcium signal transducer 2)TOP1 (DNA Topoisomerase I)PARP2 (Poly (adp-ribose) polymerase 2)

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