Drug intelligence / Profile preview

SP141

Development stage
Preclinical
Lead developer
Texas Tech University Health Sciences Center
Modality
Small Molecules
Administration
Intraperitoneal, Oral
01

Overview

SP141 is a **novel small-molecule inhibitor of MDM2** (mouse double minute 2 homolog), a ubiquitin ligase that targets the tumor suppressor p53 for degradation. SP141 was rationally designed to bind directly to the MDM2 protein, resulting in **reduced MDM2 levels via promoted autoubiquitination and proteasomal degradation**[1][7][9]. This MDM2 inhibition leads to increased p53 protein, cell cycle arrest, and apoptosis in cancer cells, with evidence of potent anticancer activity independent of p53 status in both breast and pancreatic cancer models[1][3][7][9]. SP141 has demonstrated efficacy in inhibiting tumor growth and metastasis in various preclinical animal models by both intraperitoneal and oral routes. Enhanced oral delivery and bioavailability have also been achieved using FcRn-targeted nanoparticles[2][3]. SP141 is being explored primarily as an investigational therapy for cancer, notably **breast cancer** and **pancreatic cancer**[1][6][9]. Its selectivity, efficacy, and lack of significant toxicity underscore its potential as a clinical anticancer agent.

Other names
6-methoxy-1-(naphthalen-1-yl)-9H-pyrido[3,4-b]indole
02

Targets

MDM2 (Mouse double minute 2 homolog)

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