Drug intelligence / Profile preview

UNBS1450

Development stage
Unknown
Lead developer
Unibioscreen
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

**UNBS1450** is a hemi-synthetic cardenolide, a member of the cardiac steroid glycoside family, derived from 2″-oxovorusharin extracted from the plant *Calotropis procera*. It is a small molecule under investigation primarily for its **anticancer properties**, especially in hematologic malignancies such as acute myeloid leukemia (AML) and in solid tumors like non-small cell lung cancer (NSCLC) and glioblastoma. The drug induces apoptotic cell death at low nanomolar concentrations by inhibiting NF-κB transactivation and promoting degradation of the anti-apoptotic protein Mcl-1, triggering the intrinsic and extrinsic apoptotic pathways (caspases 8, 9, and 3/7 activation, downregulation of Mcl-1, recruitment of Bak and Bax). UNBS1450 is also a potent inhibitor of the Na+/K+-ATPase (ATP1A1), which disrupts ion gradients and signaling in cancer cells, displaying greater cytotoxicity in tumor cells than in normal cells. Preclinical studies indicated excellent differential toxicity and synergy with other apoptosis-inducing agents such as Bcl-2 antagonists. UNBS1450 has entered Phase 1 clinical trials in oncology[1][2][3][4][5][6][7][8][10].

02

Targets

ATP1A1 (Sodium/potassium-transporting ATPase subunit alpha-1)NF-κB

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