Drug intelligence / Profile preview

aprinocarsen + docetaxel

Development stage
Unknown
Lead developer
Ionis Pharmaceuticals
Modality
Antisense Oligonucleotides (ASOs) → Long RNA Therapeutics → RNA Therapeutics → Nucleic Acid Therapeutics, Modified DNA Oligonucleotides → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics, Small Molecules, Single-strand DNA → Antisense DNA → DNA Therapeutics → Nucleic Acid Therapeutics
Administration
Intravenous
01

Overview

**Aprinocarsen + docetaxel** is an experimental combination regimen combining *aprinocarsen*, an antisense oligonucleotide targeting protein kinase C alpha (PKC-α), and *docetaxel*, a widely used taxane-class chemotherapeutic agent. - **Aprinocarsen** (ISIS 3521) works by binding to the 3′-untranslated region of PKC-α mRNA, leading to RNase H–mediated degradation and reduced expression of PKC-α, a signaling kinase involved in cell proliferation and differentiation. Aprinocarsen has shown the ability to reduce tumor growth in preclinical models, but single-agent efficacy in clinical trials has been limited[2]. - **Docetaxel** is a microtubule inhibitor (mitotic spindle poison) that interferes with cell division by stabilizing microtubules and causing G2/M phase arrest. It is a standard therapy in a variety of solid tumors including non–small cell lung cancer (NSCLC)[1]. This combination has been investigated primarily in phase I/II clinical studies for patients with advanced solid tumors, especially previously treated NSCLC, seeking to exploit potential synergy between PKC-α inhibition and cytotoxic chemotherapy. The combination does not appear to offer clear efficacy benefits over docetaxel alone but showed manageable toxicity profiles[1].

Other names
aprinocarsen + docetaxelISIS 3521 + docetaxel
02

Targets

PRKCA (Protein kinase C alpha)TUBB (Tubulin (alpha and beta subunits))

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