Drug intelligence / Profile preview

aphidicolin

Development stage
Unknown
Lead developer
Cephalosporium aphidicola (natural product from fungus)
Modality
Small Molecules
Administration
In Vitro, Intravenous (as Aphidicolin Glycinate In Clinical Studies)
01

Overview

**Aphidicolin** is a tetracyclic diterpene antibiotic originally isolated from the fungus *Cephalosporium aphidicola* and other related fungi. It is a potent, reversible inhibitor of eukaryotic nuclear DNA replication, exerting its effects by specifically inhibiting DNA polymerase alpha and DNA polymerase delta in eukaryotic cells, as well as in some viruses (notably herpesviruses and vaccinia virus)[1][4][6]. Aphidicolin blocks the cell cycle at the early S phase, leading to inhibition of DNA synthesis and induction of apoptosis in sensitive cancer cell lines, such as neuroblastoma and myeloid leukemia cells[1][4][6]. It also exhibits antiviral properties and has been investigated as an antineoplastic agent and cell cycle synchronizing agent in research and early clinical trials with a soluble analogue, aphidicolin glycinate[3]. Its poor aqueous solubility has limited development as a pharmaceutical agent[2][6].

Other names
aphidicolin(+)-Aphidicolin(+/-)-Aphidicolinaphidocolin
02

Targets

POLD1 (DNA polymerase delta)POLE (DNA polymerase epsilon)POLA1 (DNA polymerase alpha)

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