Drug intelligence / Profile preview

FGFC1

Development stage
Preclinical
Modality
Small Molecules
Administration
Not Established
01

Overview

FGFC1 is a **natural bisindole alkaloid** derived from the deep-sea marine fungus Stachybotrys longispora FG216. It exerts multiple pharmacological activities, including **fibrinolytic, anti-inflammatory, and antitumor effects**. Its mechanism of action includes direct **inhibition of thrombin-activatable fibrinolysis inhibitor (TAFI)**, resulting in enhanced fibrinolysis and anticoagulation activity. In cancer models, FGFC1 **selectively inhibits proliferation and induces apoptosis in erlotinib-resistant non-small cell lung cancer (NSCLC) cells** harboring EGFR T790M/L858R mutations. It achieves this by binding to EGFR, **suppressing EGFR phosphorylation and inhibiting the downstream PI3K/Akt/mTOR signaling pathway**, leading to mitochondrial dysfunction and accumulation of reactive oxygen species, which triggers apoptosis. In acute myeloid leukemia (AML), specifically Ara-C-resistant cells, FGFC1 induces both apoptosis and pyroptosis via mitochondrial dysfunction and ROS generation, further inhibiting the PI3K/Akt/mTOR signaling pathway. Preclinical data suggest promising anti-thrombotic, anti-NSCLC, and anti-leukemic potential.

Other names
Fungi fibrinolytic compound 1
02

Targets

PI3K (Phosphoinositide-3-kinase regulatory subunit 6)LBS (Plasminogen lysine-binding sites)EGFR (Epidermal growth factor receptor)mTOR (Mammalian target of rapamycin kinase)AKT (RAC-alpha serine/threonine-protein kinase)

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