Drug intelligence / Profile preview

PSTA-5204

Development stage
Unknown
Lead developer
Prospect Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

**PSTA-5204** is an investigational oral small molecule inhibitor specifically targeting the active "ON" state of the KRAS G12D mutant protein, a common oncogenic driver in cancers such as pancreatic ductal adenocarcinoma (PDAC), non-small cell lung cancer (NSCLC), and colorectal cancer. Developed by Prosite (Shanghai) Biotechnology Co., Ltd., it demonstrates potent in vitro and in vivo antitumor efficacy, with near-complete tumor regression observed in preclinical models at low doses (e.g., 7.5-15 mg/kg), favorable pharmacokinetics, and a clean safety profile lacking hERG inhibition. It remains in preclinical development as a promising candidate for KRAS G12D-driven solid tumors.[1][5][9]

02

Targets

KRASG12D (Kirsten rat sarcoma viral oncogene homolog (KRAS) G12D mutant)BRAF (B-Raf proto-oncogene, serine/threonine kinase)PPIA (Peptidyl-prolyl cis-trans isomerase A)

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