Drug intelligence / Profile preview

nab-pro-beta-lapachone

Development stage
Preclinical
Lead developer
Merck
Modality
Nanoparticles → Drug Delivery Systems, Small Molecules
Administration
Intravenous
01

Overview

nab-pro-beta-lapachone is a **nanoparticle albumin-bound (nab) formulation of prodrug beta-lapachone**. Beta-lapachone is a synthetic derivative of the natural product β-lapachone, originally isolated from Tabebuia avellanedae, that possesses potent **antitumor activity** in preclinical models. The prodrug is bioactivated selectively in tumor cells overexpressing the enzyme NAD(P)H:quinone oxidoreductase 1 (NQO1), which is highly expressed in many solid tumors. Upon NQO1-mediated reduction, beta-lapachone induces reactive oxygen species (ROS), causing DNA damage, PARP1 hyperactivation, NAD^+^ and ATP depletion, and ultimately programmed necrotic or apoptotic cell death in cancer cells. The nab-pro formulation is designed to improve the pharmacokinetics and tumor delivery versus unformulated compound. beta-Lapachone is under investigation as a targeted therapy for multiple solid cancers, including pancreatic cancer, non-small cell lung cancer, triple-negative breast cancer, and bladder cancer, with its mechanism leveraging both potent direct cytotoxicity and immunomodulatory effects in the tumor microenvironment[1][2][4][5].

Brand names
nab-pro-beta-lapachone
Other names
nab-pro-beta-lapachone
02

Targets

PARP1 (Poly (adp-ribose) polymerase 1)NQO1

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