Drug intelligence / Profile preview

isir-042

Development stage
Preclinical
Lead developer
Osaka University
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

ISIR-042 is a **novel fusicoccin derivative** developed as an investigational small molecule drug for the treatment of solid tumors, especially pancreatic cancer[6][4]. It displays preferential cytotoxicity to **hypoxic tumor cells**, a state known to contribute to therapy resistance and malignancy[6]. ISIR-042 acts in part by inhibiting the accumulation of **hypoxia-inducible factor 1-alpha (HIF-1α)** and **Akt phosphorylation**, key signaling pathways associated with tumor survival under hypoxia[6]. Experimental data show that ISIR-042 not only impairs cancer cell growth and colony formation but also suppresses stemness-related gene expression in pancreatic cancer cells[4][6]. Combination regimens of ISIR-042 with standard chemotherapeutics such as tamoxifen, 5-fluorouracil, or gemcitabine exhibit synergistic effects—significantly reducing the appearance of drug-resistant cells and inhibiting tumor xenograft growth without notable adverse effects[4]. ISIR-042 is distinct from related compounds like fusicoccin A and cotylenin A and is **not a biosimilar or generic** of an existing drug[6]. It is administered as a small molecule agent.

Brand names
isir-042isir042isir 042
Other names
isir-042isir042isir 042
02

Targets

AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)YWHA (14-3-3 protein family)

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