Drug intelligence / Profile preview

ASP9853 + docetaxel

Development stage
Discontinued
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

**ASP9853 + docetaxel** is a combination therapy investigated for advanced solid tumors. ASP9853 is a small molecule inhibitor of **inducible nitric oxide synthase (iNOS) dimerization**, leading to decreased nitric oxide (NO) production. Docetaxel is a taxane-class antineoplastic agent that inhibits microtubule depolymerization, disrupting cell division and inducing apoptosis. Preclinical studies demonstrated synergistic antitumor activity of ASP9853 with taxanes (docetaxel and paclitaxel) in xenograft cancer models. In a Phase I clinical trial, ASP9853 was administered orally daily in combination with intravenous docetaxel every three weeks in patients with advanced non-hematologic malignancies. The combination showed increased toxicity (notably neutropenia and leukopenia) compared to docetaxel alone, and did not result in improved clinical efficacy; the study was terminated early without determination of the maximum tolerated dose or recommended Phase II dose[1][3][7][9].

Other names
ASP9853 + docetaxel
02

Targets

TUBB (Tubulin (alpha and beta subunits))NOS2 (Nitric Oxide Synthase 2)

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