Drug intelligence / Profile preview

homospisulosine

Development stage
Preclinical
Modality
Small Molecules
01

Overview

Homospisulosine (KP7) is a synthetic analog of **spisulosine** (1-deoxysphinganine), a sphingoid amino alcohol originally isolated from the sea clam *Spisula polynyma*. While the parent compound spisulosine demonstrated potent antiproliferative activity against a broad spectrum of solid tumors in early clinical trials, its development was hindered by significant neurotoxicity. Homospisulosine was developed as a derivative to maintain anticancer efficacy while potentially improving the therapeutic window. Preclinical studies in cervical carcinoma (HeLa) cells have shown that homospisulosine induces apoptosis through the mitochondrial pathway, evidenced by the dissipation of mitochondrial membrane potential, activation of **caspase-3**, and cleavage of **PARP**. Additionally, it has been observed to increase the levels of the cell cycle inhibitor **p27** and modulate **Bcl-2** through phosphorylation at the Ser70 residue.

Other names
homospisulosineKP7KP-7KP 7
02

Targets

BCL-2 (BCL-2 family)CASP3 (Caspase-3)CDKN1B (Transmembrane emp24 domain-containing protein 7)PARP1 (Poly (adp-ribose) polymerase 1)

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