Drug intelligence / Profile preview

vb15010

Development stage
Phase 2
Lead developer
Shenzhen Yangli Pharmaceutical Technology
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

VB15010 is a potent and selective small molecule inhibitor of poly(ADP-ribose) polymerase 1 (PARP1), developed for the treatment of advanced solid tumors. It acts as a "durable trapper" of PARP1, inhibiting its enzymatic activity and trapping the enzyme on DNA, which leads to synthetic lethality in cancer cells with homologous recombination repair deficiencies such as BRCA mutations. Preclinical studies have demonstrated that VB15010 can induce sustained tumor regression in BRCA-mutant breast cancer models. The drug is currently being evaluated in Phase I/II clinical trials for safety, tolerability, pharmacokinetics, pharmacodynamics, and preliminary efficacy in patients with advanced solid tumors including breast cancer, ovarian cancer, biliary tract neoplasms, colorectal cancer, prostate cancer, and pancreatic cancer[1][2][3][4][5][7][9].

Other names
VB-15010VB15010VB 15010
02

Targets

PARP1 (Poly (adp-ribose) polymerase 1)

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