Drug intelligence / Profile preview

BBIT20

Development stage
Preclinical
Lead developer
iMed.ULisboa
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intraperitoneal
01

Overview

BBIT20 is a **natural monoterpene indole alkaloid derivative** (specifically dregamine 5-bromo-pyridin-2-ylhydrazone) that serves as a **small molecule inhibitor of homologous DNA repair** in cancer cells. Its mechanism centers on **disrupting the BRCA1–BARD1 interaction**, which is essential for homologous recombination-mediated DNA repair. This results in the downregulation of DNA repair-related genes, increased DNA damage, cell cycle arrest, induction of apoptosis, and generation of reactive oxygen species. BBIT20 has shown pronounced antitumor activity in preclinical models, particularly in **triple-negative breast cancer** and **ovarian cancer** (including BRCA1-deficient and platinum-resistant models). It acts synergistically with standard chemotherapeutics like cisplatin and PARP inhibitors (such as olaparib), exhibits high selectivity for cancer cells over normal cells, and notably does **not induce acquired drug resistance** in tested cancer models. BBIT20 is currently positioned as an investigational compound with preclinical evidence of efficacy and low toxicity[1][3][4][5][6][7].

Other names
dregamine 5-bromo-pyridin-2-ylhydrazonedregamine5-bromo-pyridin-2-ylhydrazonedregamine-5-bromo-pyridin-2-ylhydrazone
02

Targets

Breast cancer type 1 susceptibility protein-BRCA1-associated RING domain protein 1 heterodimer interface

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