Drug intelligence / Profile preview

DP86

Development stage
Preclinical
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

DP86 is an experimental small molecule and an analogue of the alkylating agent temozolomide (TMZ), specifically developed to treat glioblastoma multiforme (GBM). As an imidazotetrazine derivative, DP86 is designed to overcome common mechanisms of resistance to standard TMZ therapy, such as the expression of O6-methylguanine-DNA methyltransferase (MGMT) and deficiencies in the mismatch repair (MMR) system. The drug functions by inducing DNA damage, likely through the formation of DNA interstrand cross-links, leading to cell cycle arrest and apoptosis. While DP86 has demonstrated efficacy in preclinical GBM cell lines and primary culture models, it is reported to be less potent than its related analogue, DP68. Initial pharmacokinetic studies indicate that DP86 undergoes rapid elimination from the serum.

02

Targets

DNA

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