Drug intelligence / Profile preview

azenosertib + paclitaxel

Development stage
Phase 1
Lead developer
Zentalis Pharmaceuticals
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Azenosertib + paclitaxel is an investigational combination therapy being studied primarily for ovarian cancer, especially in patients with Cyclin E1-positive or platinum-resistant disease. **Azenosertib** is a selective, orally bioavailable small molecule WEE1 kinase inhibitor that disrupts cell cycle checkpoints, sensitizing cancer cells to DNA damage induced by chemotherapy. **Paclitaxel** is a well-established anti-microtubule agent that causes cell cycle arrest in mitosis by stabilizing microtubules and inhibiting their depolymerization. When used together, azenosertib impairs the DNA damage response and promotes premature mitotic entry, thereby enhancing the cytotoxic effects of paclitaxel. Preclinical and early clinical studies show that this combination has synergistic antitumor activity, particularly in Cyclin E1-amplified tumors, and can result in notable tumor regression and improved response rates compared to chemotherapy alone. This combination is undergoing clinical investigation and is not yet approved for general use.

02

Targets

WEE1 (WEE1 G2 checkpoint kinase)TUBB (Tubulin (alpha and beta subunits))

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