Drug intelligence / Profile preview

fostriecin

Development stage
Discontinued
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intravenous
01

Overview

Fostriecin is a **natural product-derived antitumor agent** that is a structurally unique phosphate monoester produced by *Streptomyces pulveraceus*. It functions as a potent and selective inhibitor of **serine/threonine protein phosphatase 2A (PP2A)** and is a comparatively weaker inhibitor of **protein phosphatase 1 (PP1)**. Additionally, fostriecin has inhibitory activity against **DNA topoisomerase II**. It was developed for use as an anticancer drug and demonstrates marked cytotoxicity against many cancer cell lines, producing cell cycle arrest in the G2-M phase, abnormal centrosome amplification, and cell death. Fostriecin’s **antitumor activity is thought to be primarily mediated via PP2A inhibition**, affecting cell cycle progression and mitosis. Early-phase clinical trials of fostriecin were conducted by the National Cancer Institute, but development was discontinued due to stability issues of the drug material.

Other names
fostriecinCI-920CI920CI 920NSC 339638NSC339638NSC-339638PD 110161PD110161PD-110161
02

Targets

PPP5C (Serine/threonine-protein phosphatase 5)TOP2A (DNA topoisomerase II)PPP4C (Serine/threonine-protein phosphatase 4 catalytic subunit)CN (Calcineurin)PP1 (Protein phosphatase 1)PP2A (Protein phosphatase 2A)

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