Drug intelligence / Profile preview

S-8184 + paclitaxel

Development stage
Unknown
Lead developer
Sonus Pharmaceuticals
Modality
Nanoparticles → Drug Delivery Systems, Small Molecules
Administration
Intravenous
01

Overview

S-8184 + paclitaxel is a **combination formulation consisting of paclitaxel incorporated into a vitamin E-based emulsion (S-8184)**, designed to improve delivery and reduce toxicity compared to conventional paclitaxel preparations[1][3][4]. Key features include: - **Mechanism of Action:** Paclitaxel stabilizes microtubules by promoting their assembly from tubulin dimers and blocking depolymerization, thus inhibiting normal cell division and inducing apoptosis in cancer cells[2]. - **Formulation Characteristics:** The emulsion is free of Cremophor EL (CrEL), the solvent traditionally used in Taxol, thereby reducing hypersensitivity and neurotoxicity; it can be administered by rapid (15-minute) IV infusion without steroid premedication[1][3]. - **Nanoparticle Size:** 60–200 nm particles are engineered for enhanced tumor uptake[1]. - **Additional Component:** The emulsion includes a P-glycoprotein inhibitor to limit drug resistance in cancer cells[1]. - **Clinical Data:** Demonstrated **antitumor activity with lower toxicity** in early human studies, with maximum tolerated doses higher than Taxol and efficacy in taxane-resistant cancers[1][3][4]. - **Indications:** Investigated primarily for advanced/metastatic cancers (lung, ovarian, breast, colorectal, pancreatic, urothelial)[1][3][4].

Brand names
TOCOSOL Paclitaxel
Other names
S-8184 paclitaxel injectable emulsionS8184 paclitaxel injectable emulsionS 8184 paclitaxel injectable emulsionS-8184 Paclitaxel EmulsionS8184 Paclitaxel EmulsionS 8184 Paclitaxel Emulsion
02

Targets

TUBB (Tubulin (alpha and beta subunits))ABCB1 (P-glycoprotein)

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